This document provides an overview of oral modified release multiple-unit particulate systems (MUPS). It discusses the introduction and advantages of MUPS, challenges in formulating MUPS, and how those challenges can be overcome. Some key challenges include maintaining the drug release profile after compaction into tablets and preventing damage to pellet coatings during compression. Factors that influence the challenges such as pellet properties, polymer coatings, extragranular materials, and processing are described. Extrusion and spheronization are introduced as methods for producing pellets or granules for use in MUPS.
Detailed description of types of plasticizers, mode of selection, types of effects produced on polymers and optimization of plasticizers in aqueous/organic coating based systems.
Microencapsulation may be defined as the packaging technology of solids, liquid or gaseous material with thin polymeric coatings, forming small particles called microcapsules .
Microencapsulation involves coating tiny liquid or solid particles with a polymeric film. It has advantages like increasing bioavailability, altering drug release, and improving compliance. Common techniques include coacervation, solvent evaporation, spray drying, and polymerization. Microencapsulation can protect ingredients, mask tastes, and provide targeted delivery for applications like food, pharma, and agriculture.
Prediction of coating process parameters on scaleup/scale downSatishPuttachari
This ppt discuss about the CPP impacting the coating process parameters & optimisation. U can find validated excel sheet which calculates the CPP for the scale up/down or changing the equipment.
The document discusses 11 different techniques to determine granulation end point in pharmaceutical manufacturing processes. Visual observation is the conventional but subjective method, while techniques like power consumption, impeller torque, conductivity, and acoustic emission aim to provide more objective and reproducible measurements of changes in granule properties online. Additional offline methods like rheometry, effusivity, and spectroscopy also characterize granulation but can be more expensive.
Polymers Used In Pharmaceutical dosage delivery systemsHeenaParveen23
This document discusses characteristics and types of polymers used in drug delivery. It describes ideal polymer characteristics as being chemically inert, mechanically strong, non-toxic, and easily sterilized. The document then covers various polymer classifications including biodegradability, polymerization method (addition, condensation), structure (natural, synthetic), and environmental responsiveness to stimuli like pH, temperature, light. Specific polymer examples are provided for each classification like poly(lactic-co-glycolic acid) for biodegradable and polyvinylpyrrolidone for soluble. Mechanisms of drug release from polymers include diffusion, degradation, swelling, and erosion.
This internship report summarizes work done on the Blister Quick Servo packaging machine. The report includes specifications of the machine such as its layout, performance details, standard features, and descriptions of its major functional groups. It provides an overview of the machine's capabilities for forming, sealing, and packaging blister packs at high speeds of up to 40 cycles per minute. The report was authored by an intern as part of their mechanical engineering degree program.
Detailed description of types of plasticizers, mode of selection, types of effects produced on polymers and optimization of plasticizers in aqueous/organic coating based systems.
Microencapsulation may be defined as the packaging technology of solids, liquid or gaseous material with thin polymeric coatings, forming small particles called microcapsules .
Microencapsulation involves coating tiny liquid or solid particles with a polymeric film. It has advantages like increasing bioavailability, altering drug release, and improving compliance. Common techniques include coacervation, solvent evaporation, spray drying, and polymerization. Microencapsulation can protect ingredients, mask tastes, and provide targeted delivery for applications like food, pharma, and agriculture.
Prediction of coating process parameters on scaleup/scale downSatishPuttachari
This ppt discuss about the CPP impacting the coating process parameters & optimisation. U can find validated excel sheet which calculates the CPP for the scale up/down or changing the equipment.
The document discusses 11 different techniques to determine granulation end point in pharmaceutical manufacturing processes. Visual observation is the conventional but subjective method, while techniques like power consumption, impeller torque, conductivity, and acoustic emission aim to provide more objective and reproducible measurements of changes in granule properties online. Additional offline methods like rheometry, effusivity, and spectroscopy also characterize granulation but can be more expensive.
Polymers Used In Pharmaceutical dosage delivery systemsHeenaParveen23
This document discusses characteristics and types of polymers used in drug delivery. It describes ideal polymer characteristics as being chemically inert, mechanically strong, non-toxic, and easily sterilized. The document then covers various polymer classifications including biodegradability, polymerization method (addition, condensation), structure (natural, synthetic), and environmental responsiveness to stimuli like pH, temperature, light. Specific polymer examples are provided for each classification like poly(lactic-co-glycolic acid) for biodegradable and polyvinylpyrrolidone for soluble. Mechanisms of drug release from polymers include diffusion, degradation, swelling, and erosion.
This internship report summarizes work done on the Blister Quick Servo packaging machine. The report includes specifications of the machine such as its layout, performance details, standard features, and descriptions of its major functional groups. It provides an overview of the machine's capabilities for forming, sealing, and packaging blister packs at high speeds of up to 40 cycles per minute. The report was authored by an intern as part of their mechanical engineering degree program.
Thin film drug delivery (Oral dissolve film )Chouthri D
to know about oral dissolving films, ,thin film dds ,oral dissolve films ,oral dispersal film ,api ,advantage for oral thin film ,ingredient using in thin film ,colouring agent used in thin film ,semisolid casting method ,thin film manufacturing mathods ,solvent casting method ,hot melt extrusion ,roiling method ,plasticizer ,water soluble polymers ,comparing between odt and odf ,solid dispersion extrusion ,application of oral dissolving film ,composition of fds,surfactant,saliva stimulating agent,flavouring agent,thi film manufacturing video
This document provides an overview of orally disintegrating tablets (ODTs), including:
1. The definition and ideal properties of ODTs according to regulatory agencies.
2. The large market potential and growth of ODTs globally, especially for drugs treating central nervous system and gastrointestinal conditions.
3. Important patented technologies for developing ODTs, such as Zydis® technology which uses a lyophilization process to create a porous structure for rapid disintegration.
4. Common excipients and formulation methods used in ODTs, including lyophilization, molding, and mass extrusion.
1. Film formation is the process by which a liquid coating is converted into a solid film after application. There are two main mechanisms for this - solvent evaporation and chemical crosslinking reactions.
2. For thermoplastic coatings, film formation occurs as the solvent evaporates, causing an increase in the glass transition temperature (Tg) of the coating to match or exceed the ambient temperature. For crosslinking coatings, particles soften and coalesce during heating, then chemical reactions cause molecular weight and viscosity to increase until the surface sets.
3. Both types of coatings aim to overcome issues like solvent retention, shrinkage stresses, and environmental pollution, though crosslinking systems are more thermally and chemically
1. The document describes the formulation of ethosomes for transdermal drug delivery.
2. Ethosomes are soft lipid vesicles made of phospholipids, ethanol and water that can entrap both hydrophilic and lipophilic drug molecules and enhance skin permeation for transdermal delivery.
3. The student prepared ethosomes using lecithin, ethanol and water, and measured the particle size using dynamic light scattering which was found to be 762 nm.
The document describes the workings of a Rapid Mixer Granulator machine. It achieves excellent mixing and consistent granules at lower operating costs through high-speed agitation and shearing forces from an impeller and chopper. This leads to better mixing and control of granule size, allowing for faster tableting speeds and improved quality with fewer rejections. The machine uses a vertical shaft impeller that rotates at 5-15 m/s and a chopper that rotates much faster at 1500-4000 rpm to cut materials into smaller fragments and aid mixing.
Tablet coating is done to improve the quality, taste, and performance of tablets. The basic principle is applying a coating to tablets in a rotating bed with heated air to evaporate solvent. Objectives include protecting ingredients from environment, masking unpleasant tastes, making tablets easier to swallow, and adding functional properties like controlled release. Common coating types are film, sugar, enteric, controlled release, and specialized coatings. Process parameters must be optimized to produce an even, intact coating and avoid defects.
The document discusses tablet coating technology and processes. It begins by outlining the objectives of tablet coating, such as masking taste or odor, providing physical protection, and controlling drug release. It then describes various coating equipment like standard coating pans, perforated coating pans, and fluidized bed systems. The coating processes of sugar coating, film coating, and enteric coating are explained. Finally, potential film defects in tablet coating like sticking, roughness, capping, and cracking are reviewed along with methods to prevent or correct them.
The document describes the processes for making several fruit-based food products including squashes, RTS beverages, pickles, jams, plum pulp, fruit juice concentrates, and fruit juice. For each product, the key steps in the production process are outlined, including preparation of the fruit, addition of other ingredients like sugar and acid, boiling, cooling, packaging, and storage. Quality control tests are also listed including tests for pectin, starch, acidity, total soluble solids, and SO2 levels. In the presentation, it is noted that the fruit processing plant produces various products on a daily basis and that all the fruit beverages produced are highly nutritious and thirst-quenching.
The document discusses different methods of microencapsulation including air suspension, coacervation, multiorifice centrifugal process, spray drying, and pan coating. It provides details on the working mechanisms and variables that affect each process. Microencapsulation can be used to encapsulate solids, liquids, or gases to properties such as shelf life, taste, and controlled release profiles.
This document provides an overview of fast dissolving oral thin films (FDOTF). It begins with an introduction describing FDOTFs as thin polymeric strips that dissolve quickly in the mouth without water. The document then covers special features of FDOTFs, compares them to fast dissolving tablets, and describes their mechanism of action, classifications, properties, advantages, disadvantages, formulations, manufacturing methods, evaluation, and concludes with references.
Preformulation studies characterize the physical and chemical properties of drug molecules to develop safe, effective, and stable dosage forms. The goals are to develop formulations that are stable, safe, and effective. Major areas of study include physical characterization of properties like crystallinity and polymorphism, hygroscopicity, particle size, and powder flow. Solubility is analyzed through measurements of ionization, partition coefficient, aqueous solubility, and pH-solubility profiles. Stability is analyzed through studies of photolytic stability, stability to oxidation, and drug-excipient compatibility.
Tablet production process by ranjeet singhRanjeet Singh
Tablets are solid dosage forms consisting of active ingredients and excipients that may vary in size, shape, hardness, and other properties. Tablets are classified as compressed or molded according to the manufacturing method. Tablets offer benefits for production, packaging, stability, and ease of use compared to other dosage forms. However, some drugs are not suitable for tableting due to properties like bitterness, odor, or sensitivity to heat or moisture.
This document summarizes a seminar on biodegradable and non-biodegradable polymers. It introduces polymers and describes biodegradable polymers as those that can degrade in biological fluids over time, releasing dissolved drugs. It outlines some advantages of biodegradable polymers like sustained drug delivery and disadvantages like burst release. The document classifies polymers as biodegradable or non-biodegradable and describes factors that affect biodegradation rates. Examples of synthetic and natural biodegradable polymers are provided, such as polyglycolic acid, collagen, starch and chitosan.
This document provides an introduction to fluidized bed processing, which involves coating, granulation, and drying of particulate materials. It describes the different types of spray processes in fluidized beds, including top spray, bottom spray, and tangential spray. Bottom spray processing, developed by Dr. Dale Wurster, is commonly used in pharmaceutical applications for coating uniformity. The document outlines the key components of a fluidized bed coater and discusses important process parameters like inlet temperature, spray rate, and batch size that can impact performance. Formulation factors like coating solution strength and batch size are also reviewed. Fluidized bed processing is used to improve drug properties like taste, appearance, and release characteristics.
This document presents a study on using the liquisolid technique to enhance the dissolution profile of the poorly water soluble drug lornoxicam. The objectives were to formulate liquisolid compacts of lornoxicam using different vehicles, carrier ratios, and coating materials to improve its solubility and dissolution rate compared to conventional tablets. Various tests were performed to characterize the liquisolid formulations and determine optimal formulation parameters. The results demonstrated that liquisolid compacts with certain vehicles and powder substrate ratios achieved complete drug release within 10 minutes, representing a significant enhancement over conventional tablets.
Microencapsulation is a process where core materials are surrounded by a coating to form microparticles or microcapsules between 3-800μm in size. There are various techniques to produce microcapsules including air suspension, solvent evaporation, spray drying, pan coating, and polymerization. Microencapsulation can be used to increase bioavailability, alter drug release profiles, improve patient compliance, produce targeted drug delivery, and protect core materials. Some example applications are improving stability, reducing volatility, avoiding incompatibilities, and masking tastes.
Tablet coating is the application of a coating material to the exterior of a tablet to confer benefits over uncoated tablets. Common purposes are to mask taste/odor, protect drugs from environmental factors or gastric acid, and control drug release. Major types are sugar coating, film coating, enteric coating, and press coating. Film coating involves spraying a polymer solution onto tablets while sugar coating is a multistage process including sealing, subcoating, smoothing, coloring and polishing. Standard pans and perforated pans are commonly used coating equipment.
The document discusses the design and formulation of capsules. It describes capsules as solid dosage forms where the drug is enclosed in a soluble shell, usually made of gelatin. The two main types of capsules are hard gelatin capsules and soft gelatin capsules. Hard gelatin capsules have two pieces (body and cap) and are filled with powders, granules or pellets. Soft gelatin capsules have a more flexible, plasticized shell and can contain liquid or semi-solid fillings. The document outlines the ingredients, manufacturing process, advantages and disadvantages of both hard and soft gelatin capsules.
This document discusses different types of tablet coatings used in pharmaceutical manufacturing. The three main types are film coating, sugar coating, and compression coating. Film coating involves spraying a thin polymer film onto tablets, while sugar coating builds up sucrose layers and compression coating compacts powder around tablets. Most new tablets are film coated rather than sugar coated. The document outlines ideal characteristics for film coaters and enteric coatings, which are resistant to stomach acid but dissolve in the intestine. It provides examples of polymers used for different coating purposes.
pellets can be defined as multi particulate system or multiunit system
They are spherical particulates manufactured by agglomeration of the powder granules containing drug substance and excipients.
Pellets can be prepared by a special technique called Pelletization.
This technique is referred to an agglomeration process that convert fine powder or granules of bulk drug or excipient in to small , free flowing , spherical or semi spherical pellets .
Multi particular drug delivery system especially suitable for achieving controlled delay released oral formulation with low risk of dose dumping, flexibility of blending to attain different release patterns as well as reproducible and short gastric residence time.
Multi particulate drug delivery system are mainly oral dosage form consisting of a multiplicity of small discrete units each exhibiting some desire characteristics.
This document discusses pellets, which are small spherical units used to deliver drugs. It covers pellet formulation requirements, manufacturing processes like extrusion-spheronization, and characterization methods. Pellets offer benefits like uniform dosing and controlled release. They are made by agglomerating powders using water or other liquids to form nuclei that grow in size. Key processes include granulation, extrusion, spheronization, and coating layers onto seeds or cores. Pellets are characterized based on size, shape, porosity, and dissolution profile. Controlling these properties allows pellets to improve drug delivery.
Thin film drug delivery (Oral dissolve film )Chouthri D
to know about oral dissolving films, ,thin film dds ,oral dissolve films ,oral dispersal film ,api ,advantage for oral thin film ,ingredient using in thin film ,colouring agent used in thin film ,semisolid casting method ,thin film manufacturing mathods ,solvent casting method ,hot melt extrusion ,roiling method ,plasticizer ,water soluble polymers ,comparing between odt and odf ,solid dispersion extrusion ,application of oral dissolving film ,composition of fds,surfactant,saliva stimulating agent,flavouring agent,thi film manufacturing video
This document provides an overview of orally disintegrating tablets (ODTs), including:
1. The definition and ideal properties of ODTs according to regulatory agencies.
2. The large market potential and growth of ODTs globally, especially for drugs treating central nervous system and gastrointestinal conditions.
3. Important patented technologies for developing ODTs, such as Zydis® technology which uses a lyophilization process to create a porous structure for rapid disintegration.
4. Common excipients and formulation methods used in ODTs, including lyophilization, molding, and mass extrusion.
1. Film formation is the process by which a liquid coating is converted into a solid film after application. There are two main mechanisms for this - solvent evaporation and chemical crosslinking reactions.
2. For thermoplastic coatings, film formation occurs as the solvent evaporates, causing an increase in the glass transition temperature (Tg) of the coating to match or exceed the ambient temperature. For crosslinking coatings, particles soften and coalesce during heating, then chemical reactions cause molecular weight and viscosity to increase until the surface sets.
3. Both types of coatings aim to overcome issues like solvent retention, shrinkage stresses, and environmental pollution, though crosslinking systems are more thermally and chemically
1. The document describes the formulation of ethosomes for transdermal drug delivery.
2. Ethosomes are soft lipid vesicles made of phospholipids, ethanol and water that can entrap both hydrophilic and lipophilic drug molecules and enhance skin permeation for transdermal delivery.
3. The student prepared ethosomes using lecithin, ethanol and water, and measured the particle size using dynamic light scattering which was found to be 762 nm.
The document describes the workings of a Rapid Mixer Granulator machine. It achieves excellent mixing and consistent granules at lower operating costs through high-speed agitation and shearing forces from an impeller and chopper. This leads to better mixing and control of granule size, allowing for faster tableting speeds and improved quality with fewer rejections. The machine uses a vertical shaft impeller that rotates at 5-15 m/s and a chopper that rotates much faster at 1500-4000 rpm to cut materials into smaller fragments and aid mixing.
Tablet coating is done to improve the quality, taste, and performance of tablets. The basic principle is applying a coating to tablets in a rotating bed with heated air to evaporate solvent. Objectives include protecting ingredients from environment, masking unpleasant tastes, making tablets easier to swallow, and adding functional properties like controlled release. Common coating types are film, sugar, enteric, controlled release, and specialized coatings. Process parameters must be optimized to produce an even, intact coating and avoid defects.
The document discusses tablet coating technology and processes. It begins by outlining the objectives of tablet coating, such as masking taste or odor, providing physical protection, and controlling drug release. It then describes various coating equipment like standard coating pans, perforated coating pans, and fluidized bed systems. The coating processes of sugar coating, film coating, and enteric coating are explained. Finally, potential film defects in tablet coating like sticking, roughness, capping, and cracking are reviewed along with methods to prevent or correct them.
The document describes the processes for making several fruit-based food products including squashes, RTS beverages, pickles, jams, plum pulp, fruit juice concentrates, and fruit juice. For each product, the key steps in the production process are outlined, including preparation of the fruit, addition of other ingredients like sugar and acid, boiling, cooling, packaging, and storage. Quality control tests are also listed including tests for pectin, starch, acidity, total soluble solids, and SO2 levels. In the presentation, it is noted that the fruit processing plant produces various products on a daily basis and that all the fruit beverages produced are highly nutritious and thirst-quenching.
The document discusses different methods of microencapsulation including air suspension, coacervation, multiorifice centrifugal process, spray drying, and pan coating. It provides details on the working mechanisms and variables that affect each process. Microencapsulation can be used to encapsulate solids, liquids, or gases to properties such as shelf life, taste, and controlled release profiles.
This document provides an overview of fast dissolving oral thin films (FDOTF). It begins with an introduction describing FDOTFs as thin polymeric strips that dissolve quickly in the mouth without water. The document then covers special features of FDOTFs, compares them to fast dissolving tablets, and describes their mechanism of action, classifications, properties, advantages, disadvantages, formulations, manufacturing methods, evaluation, and concludes with references.
Preformulation studies characterize the physical and chemical properties of drug molecules to develop safe, effective, and stable dosage forms. The goals are to develop formulations that are stable, safe, and effective. Major areas of study include physical characterization of properties like crystallinity and polymorphism, hygroscopicity, particle size, and powder flow. Solubility is analyzed through measurements of ionization, partition coefficient, aqueous solubility, and pH-solubility profiles. Stability is analyzed through studies of photolytic stability, stability to oxidation, and drug-excipient compatibility.
Tablet production process by ranjeet singhRanjeet Singh
Tablets are solid dosage forms consisting of active ingredients and excipients that may vary in size, shape, hardness, and other properties. Tablets are classified as compressed or molded according to the manufacturing method. Tablets offer benefits for production, packaging, stability, and ease of use compared to other dosage forms. However, some drugs are not suitable for tableting due to properties like bitterness, odor, or sensitivity to heat or moisture.
This document summarizes a seminar on biodegradable and non-biodegradable polymers. It introduces polymers and describes biodegradable polymers as those that can degrade in biological fluids over time, releasing dissolved drugs. It outlines some advantages of biodegradable polymers like sustained drug delivery and disadvantages like burst release. The document classifies polymers as biodegradable or non-biodegradable and describes factors that affect biodegradation rates. Examples of synthetic and natural biodegradable polymers are provided, such as polyglycolic acid, collagen, starch and chitosan.
This document provides an introduction to fluidized bed processing, which involves coating, granulation, and drying of particulate materials. It describes the different types of spray processes in fluidized beds, including top spray, bottom spray, and tangential spray. Bottom spray processing, developed by Dr. Dale Wurster, is commonly used in pharmaceutical applications for coating uniformity. The document outlines the key components of a fluidized bed coater and discusses important process parameters like inlet temperature, spray rate, and batch size that can impact performance. Formulation factors like coating solution strength and batch size are also reviewed. Fluidized bed processing is used to improve drug properties like taste, appearance, and release characteristics.
This document presents a study on using the liquisolid technique to enhance the dissolution profile of the poorly water soluble drug lornoxicam. The objectives were to formulate liquisolid compacts of lornoxicam using different vehicles, carrier ratios, and coating materials to improve its solubility and dissolution rate compared to conventional tablets. Various tests were performed to characterize the liquisolid formulations and determine optimal formulation parameters. The results demonstrated that liquisolid compacts with certain vehicles and powder substrate ratios achieved complete drug release within 10 minutes, representing a significant enhancement over conventional tablets.
Microencapsulation is a process where core materials are surrounded by a coating to form microparticles or microcapsules between 3-800μm in size. There are various techniques to produce microcapsules including air suspension, solvent evaporation, spray drying, pan coating, and polymerization. Microencapsulation can be used to increase bioavailability, alter drug release profiles, improve patient compliance, produce targeted drug delivery, and protect core materials. Some example applications are improving stability, reducing volatility, avoiding incompatibilities, and masking tastes.
Tablet coating is the application of a coating material to the exterior of a tablet to confer benefits over uncoated tablets. Common purposes are to mask taste/odor, protect drugs from environmental factors or gastric acid, and control drug release. Major types are sugar coating, film coating, enteric coating, and press coating. Film coating involves spraying a polymer solution onto tablets while sugar coating is a multistage process including sealing, subcoating, smoothing, coloring and polishing. Standard pans and perforated pans are commonly used coating equipment.
The document discusses the design and formulation of capsules. It describes capsules as solid dosage forms where the drug is enclosed in a soluble shell, usually made of gelatin. The two main types of capsules are hard gelatin capsules and soft gelatin capsules. Hard gelatin capsules have two pieces (body and cap) and are filled with powders, granules or pellets. Soft gelatin capsules have a more flexible, plasticized shell and can contain liquid or semi-solid fillings. The document outlines the ingredients, manufacturing process, advantages and disadvantages of both hard and soft gelatin capsules.
This document discusses different types of tablet coatings used in pharmaceutical manufacturing. The three main types are film coating, sugar coating, and compression coating. Film coating involves spraying a thin polymer film onto tablets, while sugar coating builds up sucrose layers and compression coating compacts powder around tablets. Most new tablets are film coated rather than sugar coated. The document outlines ideal characteristics for film coaters and enteric coatings, which are resistant to stomach acid but dissolve in the intestine. It provides examples of polymers used for different coating purposes.
pellets can be defined as multi particulate system or multiunit system
They are spherical particulates manufactured by agglomeration of the powder granules containing drug substance and excipients.
Pellets can be prepared by a special technique called Pelletization.
This technique is referred to an agglomeration process that convert fine powder or granules of bulk drug or excipient in to small , free flowing , spherical or semi spherical pellets .
Multi particular drug delivery system especially suitable for achieving controlled delay released oral formulation with low risk of dose dumping, flexibility of blending to attain different release patterns as well as reproducible and short gastric residence time.
Multi particulate drug delivery system are mainly oral dosage form consisting of a multiplicity of small discrete units each exhibiting some desire characteristics.
This document discusses pellets, which are small spherical units used to deliver drugs. It covers pellet formulation requirements, manufacturing processes like extrusion-spheronization, and characterization methods. Pellets offer benefits like uniform dosing and controlled release. They are made by agglomerating powders using water or other liquids to form nuclei that grow in size. Key processes include granulation, extrusion, spheronization, and coating layers onto seeds or cores. Pellets are characterized based on size, shape, porosity, and dissolution profile. Controlling these properties allows pellets to improve drug delivery.
This document discusses multiple unit pellet systems (MUPS). It defines pelletization as a size enlargement process that converts powders into spherical pellets between 0.5-2.0 mm in size with low porosity. Pellets provide benefits over single unit dosage forms like reduced variability in gastric emptying. The document outlines various pelletization techniques including extrusion, spheronization, layering, and compression. It also discusses types of MUPS formulations and provides examples of commercial MUPS drug products. MUPS provide flexible drug release, stability, patient compliance and economic benefits for pharmaceutical companies.
This document discusses factors that can affect drug absorption from pharmaceutical formulations. It begins by defining drug absorption and noting that solubility and permeability are important for a drug to enter blood circulation. Manufacturing variables like granulation method and compression force can impact absorption rate. The type of dosage form also influences absorption, with solutions showing faster rates than solid forms like tablets or capsules. Pharmaceutical ingredients and excipients and product storage conditions are additional formulation factors that can impact a drug's absorption and bioavailability.
This document discusses tablet compression physics and testing. It covers the following key points:
1) Tablet compression physics includes factors like force transmission during compression, distribution of forces in tablets, and the effect of applied pressure on relative powder volume.
2) The main criteria for tablet formulations are to form tablets without defects and with acceptable mechanical properties, meeting regulatory standards.
3) Tablet testing controls starting materials, in-process products, and finished products to ensure quality, stability, hardness, disintegration time, and more. Dissolution testing aids in formulation development.
This presentation gives brief information on pelletization, significance of pelletization. Information also cover on formulation aspects of pellets and different existing methods of production of pellets.
A Review on TABLET COATING & A DETAILED STUDY OF ENTERIC COATING OF TABLETVishal Shelke
This document discusses tablet coating and enteric coating of tablets. It provides an overview of tablet coating, including the history and types of coating techniques. Sugar coating, film coating, and enteric coating are described in detail. The key steps and components involved in enteric coating of tablets are explained. Enteric coatings are described as necessary to protect active ingredients from stomach acid and ensure drug release in the small intestine. Evaluation methods for coated tablets are also mentioned.
Tablets are a solid dosage form made by compressing or compacting powders into a solid dose. They contain active ingredients and excipients like binders, coatings, and flavors. Tablets offer advantages like low cost, stability, and ease of production and packaging. They can be coated to control drug release or improve stability and appearance. Tablet design considerations for coating include hardness, shape, friability, porosity, and ingredients. Coating is done in pans or fluidized beds using heated air to dry the applied coating and mix the tablets. Equipment like conventional pans, perforated pans, and fluidized beds efficiently coat and dry tablets on an industrial scale.
This document provides information about pharmaceutical tablets, including their manufacturing process, types, components, quality standards, and testing methods. Tablets are solid oral dosage forms made using compression. The manufacturing process involves mixing and granulating powders, then compressing them into tablets using punches and dies. Tablets can have various coatings, release mechanisms, and purposes. Quality is ensured through testing weight variation, disintegration, dissolution, and other physical properties. Proper manufacturing and testing helps ensure tablets safely and effectively deliver medication.
Tablets are the most commonly used oral solid dosage form due to their ease of production, stability, and precise dosing. The document defines tablets and lists their advantages and disadvantages. It describes the key ingredients used in tablets, various tablet production processes like direct compression, wet granulation, and coating. Common tablet defects and evaluation tests are also discussed. The processing, formulation, and manufacturing of tablets allows for flexible drug delivery and reproducible dosing of medications.
This document discusses various pharmaceutical manufacturing processes including granulation, wet and dry granulation methods, tablet coating, capsule filling, and milling. Granulation involves agglomerating fine particles to form larger granules and can be done via wet or dry processes. Wet granulation uses a liquid to form granules while dry granulation compacts powders under pressure without moisture. Tablet coating and capsule filling are used to enclose pharmaceutical ingredients. Milling processes like ball milling and cutting milling are used to reduce particle sizes. Quality processes like auditing ensure proper manufacturing standards are followed.
Mini tablets are solid dosage forms with a diameter ≤ 3 mm and separated into subunits of conventional
tablets. Production methods are similar to standard tablets, but the only difference is the use of multiple
punches. They have advantageous for use in patients suffering from swallowing difficulty and receiving multiple drug treatment.
The document discusses microencapsulation technology. Microencapsulation is the process of coating solid or liquid particles with a polymeric film, producing microcapsules in the micrometer to millimeter range. It can protect active materials, stabilize them, and control their release. Many biodegradable polymers have been used for microencapsulation in drug delivery due to their biocompatibility and ability to achieve targeted and on-demand release. Continuous research is needed to design optimal drug delivery systems using microencapsulation and address issues with techniques and material selection.
This document discusses tablet coating defects and their remedies. It begins by describing 11 common coating defects: blistering, chipping, cratering, picking, pitting, blooming, blushing, color variation, infilling, orange peel, and cracking. For each defect, it provides the causes and recommended remedies. The document was written by Suryam.G, an Assistant Professor with an M.Pharm and CPC certification, to educate readers about tablet coating issues and how to address them.
The document discusses bi-layer tablets, which contain two layers - an immediate release layer and extended release layer. This allows drugs to be delivered in both an initial and sustained dose. The key properties of bi-layer tablets are that they must maintain integrity without separating, have sufficient strength, and reliably release drugs in a predictable manner. Challenges in manufacturing include preventing delamination, cross-contamination between layers, and lower yields than single layer tablets. Various technologies have been developed to produce bi-layer tablets, including those that use push-pull and osmotic mechanisms to control drug release over time. Recent developments continue to improve bi-layer tablets for delivering multiple or incompatible drugs.
Pellets are small spherical or semi-spherical agglomerates of drug and excipients that offer flexibility in dosage form design. They can be immediate or extended release and allow incompatible drugs to be delivered to different sites in the GI tract. Pellets are produced through various methods like extrusion-spheronization, spray drying, cryopelletization, and coating can provide properties like taste masking, extended release. Characterization of pellets involves tests of particle size, shape, surface morphology and drug release.
The document discusses pellets, which are small spherical or semi-spherical units used to deliver pharmaceutical ingredients. Pellets offer advantages over other dosage forms like tablets, including flexibility in dosing, the ability to deliver incompatible drugs simultaneously, and different release profiles. The document describes various pelletization techniques like direct pelletizing, powder layering, extrusion-spheronization, and spray drying. It also discusses methods of assessing pellet properties and performance, such as drug content, size distribution, shape, friability, porosity, and in vitro dissolution studies. Pellets can provide controlled release of drugs and offer benefits for dosage form development, drug delivery, and manufacturing.
Pharmaceutical film coating is considered a key part in the production of solid pharmaceutical dosage forms since it gives superior organoleptic properties products. In addition, it can improve the physical and chemical stability of dosage forms, and modify the release characteristics of the drug. Several troubleshooting problems such as twinning mottling, chipping, etc., may arise during or after or even during the shelf life of the film coated dosage forms. These troubleshooting problems may be due to tablet core faults, coating formulation faults and/or coating process faults. These problems must be overcome to avoid unnecessary product problems. Film coating as well as other parts of the pharmaceutical technology is subjecting to continuous innovation. The innovation may be at different levels including pharmaceutical excipients, processes, software, guidelines and equipment. In fact, of particular note is the growing interest in process analytical technology, quality by design, continuous coating processing and the inclusion of new ready for use coating formulations. In this review, we tried to explore and discuss the status of pharmaceutical film coating, the challenges that face this manufacturing process and the latest technological advances in this important manufacturing process.
IOSR Journal of Pharmacy (IOSRPHR), www.iosrphr.org, call for paper, research...iosrphr_editor
This document provides a review of recent advances in enteric coating technology. It begins with an introduction to tablet coating processes and equipment. The main focus is on enteric coatings, which are designed to resist stomach acid and release the drug in the small intestine. The ideal properties, materials used, and mechanisms of enteric coatings are described. These include polymers like cellulose acetate phthalate that are insoluble at low pH but dissolve at higher pH. The document discusses criteria for selecting drugs for enteric coatings and methods for manufacturing enteric coated tablets using spray coating techniques. In summary, the document reviews enteric coatings for oral drug delivery and controlling drug release locations in the gastrointestinal tract.
This document provides a review of recent advances in enteric coating technology. It begins with an introduction to tablet coating processes and equipment. The main topics covered include:
- The ideal properties, benefits, and limitations of enteric coatings. Commonly used enteric coating polymers like cellulose acetate phthalate are described.
- Criteria for selecting drugs suitable for enteric coated drug delivery systems. These include drugs that degrade in the stomach or undergo extensive first-pass metabolism.
- The mechanism of enteric coated timed-release tablets, which use a layered design to prevent drug release in the stomach and provide controlled release in the intestines.
- Methods for manufacturing enteric coated tablets via
The key factors affecting drug absorption from oral formulations are drug solubility and dissolution rate. The two critical rate-determining steps are the rate of drug dissolution and the rate of permeation through the gastrointestinal membrane. Drug solubility and permeability classify drugs into four Biopharmaceutics Classification System classes. In vitro drug dissolution tests aim to maintain sink conditions to obtain a good correlation with in vivo absorption, such as by increasing fluid volume, partitioning dissolved drug, or adding solvents or adsorbents. Dissolution models account for changing surface area as particles dissolve over time.
This document provides an overview of dissolution theory, interpretation of dissolution data, and dissolution testing methods. It discusses the diffusion layer model of dissolution, factors that influence dissolution rates, commonly used mathematical models to describe dissolution profiles, and classifications of dissolution testing apparatuses. The key aspects covered include the Noyes-Whitney and Nernst-Brunner equations, sink versus non-sink conditions, the rotating basket and paddle apparatuses, and criteria for comparing dissolution profiles.
The document discusses several drug delivery technologies developed by EUDRATEC, including EUDRATEC MOD for pulsed drug release, EUDRATEC COL for controlled release, and EUDRATEC DuoCoat for protecting drugs from degradation. It provides details on the design and mechanisms of these technologies, as well as in vitro and in vivo results demonstrating things like drug stability and proof of concept in humans. The document also discusses EUDRATEC PEP as a platform technology and EUDRATEC's capabilities in areas like particle manufacturing, analytics, and dissolution testing to support drug formulation development and screening.
This document provides an overview of chemical kinetics and reaction rates. It introduces key concepts such as activation energy, the Arrhenius equation, reaction order, and factors that affect reaction rates such as temperature, concentration, and surface area. It also describes the collision theory of chemical reactions and how an increase in temperature results in more molecules possessing sufficient kinetic energy to overcome the activation energy barrier.
The document discusses preformulation studies for new chemical entities. It defines preformulation studies and outlines their objectives. The major areas covered in preformulation research are physical description and bulk characterization, solubility analysis, and stability analysis. Key aspects studied include identification, purity, polymorphism, hygroscopicity, and thermal effects. Analytical methods are described for characterizing solid forms, solubility, and stability.
The key factors affecting drug absorption from oral formulations are drug solubility and dissolution rate. The two critical rate-determining steps are the rate of drug dissolution and the rate of permeation through the gastrointestinal membrane. Drug solubility and permeability classify drugs into four Biopharmaceutics Classification System classes. In vitro drug dissolution tests aim to maintain sink conditions to obtain a good correlation with in vivo absorption, such as by increasing fluid volume, partitioning dissolved drug, or adding solvents or adsorbents. Dissolution models account for changing surface area as particles dissolve over time.
This document provides an overview of Eudragit polymers, which are poly(meth)acrylate copolymers used for drug delivery applications such as enteric coatings and sustained release formulations. It discusses the Eudragit polymer portfolio and various grades. It also covers topics like enteric formulations, sustained release formulations, protective coatings, regulatory status and quality, and manufacturing of Eudragit polymers. Specific examples are provided of formulations using Eudragit polymers for applications like enteric coating of tablets. Calculations for determining drug coating amounts based on surface area are also presented.
The document discusses dissolution theory and methods. It introduces dissolution testing and provides an overview of the theory of dissolution, including the diffusion layer model. Key equations for describing dissolution rates are presented, such as the Noyes-Whitney and Nernst-Brunner equations. Factors that influence dissolution rates are also examined, including drug solubility, viscosity, diffusion layer thickness, sink conditions, pH, particle size, crystalline structure and more.
This document provides an overview of solid dispersion systems and melt extrusion technology for drug delivery. It discusses classification and preparation methods of solid dispersions, including melting, solvent evaporation and melting solvent techniques. Characterization techniques and commercial products using solid dispersions are also mentioned. For melt extrusion, the document outlines the process, equipment options, advantages and challenges. Marketed products developed using these technologies are listed as well.
The document provides information on several cutting-edge nasal spray products, including:
- Hutera, a nasal spray for hair loss containing dutasteride that penetrates hair follicles efficiently with few side effects.
- The iLet Bionic Pancreas, an automated insulin delivery device cleared by the FDA to help manage type 1 diabetes. It was developed over 20 years to reduce nighttime blood sugar checks.
- Tyrvaya nasal spray, approved to treat dry eye disease by activating tear film production without use of artificial tears.
- Several other nasal spray products are mentioned briefly, including Narcan for opioid overdose, Zomig for migraines, and PecGent for cancer pain.
The document discusses various drug delivery platform technologies, including Geomatrix, SODAS, IPDAS, CODAS, PRODAS, and MXDAS. It provides details on these technologies, how they work, benefits they provide, and examples of marketed products that use each technology. In particular, it focuses on describing Ampyra, a drug developed using Elan's MXDAS technology to provide extended release of dalfampridine for improving walking ability in multiple sclerosis patients.
This document discusses several marketed controlled release drug delivery products developed by United Pharm. It describes Cilostan CR, a double controlled release cilostazol product. It also describes Romincop syrup, which uses ion exchange resin technology to mask the bitter taste of its active ingredients. Artmac Combi Gel is discussed next, which uses a novel technology to develop a liquid-solid complex product. Clavacin Duo Capsule is then covered, which uses a double controlled release system to optimize patient treatment effects. Levobtics CR tablet is also summarized, which uses a bilayered drug absorption system to provide both rapid effect onset and sustained effects. Lastly, Gastiin CR tablet is mentioned
NURSING MANAGEMENT OF PATIENT WITH EMPHYSEMA .PPTblessyjannu21
Prepared by Prof. BLESSY THOMAS, VICE PRINCIPAL, FNCON, SPN.
Emphysema is a disease condition of respiratory system.
Emphysema is an abnormal permanent enlargement of the air spaces distal to terminal bronchioles, accompanied by destruction of their walls and without obvious fibrosis.
Emphysema of lung is defined as hyper inflation of the lung ais spaces due to obstruction of non respiratory bronchioles as due to loss of elasticity of alveoli.
It is a type of chronic obstructive
pulmonary disease.
It is a progressive disease of lungs.
TEST BANK FOR Health Assessment in Nursing 7th Edition by Weber Chapters 1 - ...rightmanforbloodline
TEST BANK FOR Health Assessment in Nursing 7th Edition by Weber Chapters 1 - 34.
TEST BANK FOR Health Assessment in Nursing 7th Edition by Weber Chapters 1 - 34.
TEST BANK FOR Health Assessment in Nursing 7th Edition by Weber Chapters 1 - 34.
The facial nerve, also known as cranial nerve VII, is one of the 12 cranial nerves originating from the brain. It's a mixed nerve, meaning it contains both sensory and motor fibres, and it plays a crucial role in controlling various facial muscles, as well as conveying sensory information from the taste buds on the anterior two-thirds of the tongue.
This particular slides consist of- what is Pneumothorax,what are it's causes and it's effect on body, risk factors, symptoms,complications, diagnosis and role of physiotherapy in it.
This slide is very helpful for physiotherapy students and also for other medical and healthcare students.
Here is a summary of Pneumothorax:
Pneumothorax, also known as a collapsed lung, is a condition that occurs when air leaks into the space between the lung and chest wall. This air buildup puts pressure on the lung, preventing it from expanding fully when you breathe. A pneumothorax can cause a complete or partial collapse of the lung.
Mental Health and well-being Presentation. Exploring innovative approaches and strategies for enhancing mental well-being. Discover cutting-edge research, effective strategies, and practical methods for fostering mental well-being.
As Mumbai's premier kidney transplant and donation center, L H Hiranandani Hospital Powai is not just a medical facility; it's a beacon of hope where cutting-edge science meets compassionate care, transforming lives and redefining the standards of kidney health in India.
The Importance of Black Women Understanding the Chemicals in Their Personal C...bkling
Certain chemicals, such as phthalates and parabens, can disrupt the body's hormones and have significant effects on health. According to data, hormone-related health issues such as uterine fibroids, infertility, early puberty and more aggressive forms of breast and endometrial cancers disproportionately affect Black women. Our guest speaker, Jasmine A. McDonald, PhD, an Assistant Professor in the Department of Epidemiology at Columbia University in New York City, discusses the scientific reasons why Black women should pay attention to specific chemicals in their personal care products, like hair care, and ways to minimize their exposure.
Sectional dentures for microstomia patients.pptxSatvikaPrasad
Microstomia, characterized by an abnormally small oral aperture, presents significant challenges in prosthodontic treatment, including limited access for examination, difficulties in impression making, and challenges with prosthesis insertion and removal. To manage these issues, customized impression techniques using sectional trays and elastomeric materials are employed. Prostheses may be designed in segments or with flexible materials to facilitate handling. Minimally invasive procedures and the use of digital technologies can enhance patient comfort. Education and training for patients on prosthesis care and maintenance are crucial for compliance. Regular follow-up and a multidisciplinary approach, involving collaboration with other specialists, ensure comprehensive care and improved quality of life for microstomia patients.
1. Oral Modified Release Multiple-Unit
Particulate Systems
( Version 7.0)
Introduction of MUPS
Challenges in Formulating MUPS
Marketed Products of MUPS
Extrusion & SPHERONIZATION
5 Appendix
Prepared by
Changbaek Lim
3. 3
A design principle of increasing importance for sustained, controlled, delayed, site specific or
pulsatile release preparations is the compaction of coated particles into disintegrating multiple
unit tablets
One challenge in the production of disintegrating multiple unit tablets is maintaining the
modified drug release after compaction, as the application of the compaction pressure can
lead to deformation of film coating and, consequently, altered drug release
To protect the coating from such changes, excipients with so-called cushioning or protective
properties are usually incorporated in the tablet formulation in addition to fillers
The compression-induced changes in the structure of a film coating may depend on
physical factors of pellets such as the size, shape, density, porosity and formulation factors
such as type and amount of coating, the properties and structure of the substrate pellets and
the incorporation of excipient particles
The demand for MUPS tablets has been increasing due to its greater advantage over
other dosage forms
Introduction
4. 4
Multi particulates are filled into hard-shell gelatin capsules, compressed into tablets, suspended in
liquids or packed in sachets
Compaction of single units results in disintegrating tablets
; becoming more and more important on the pharmaceutical market, as they provide several
advantages compared to single-unit dosage forms and pellet-filled capsules
COMPRESSION OF PELLETS TO TABLETS (MUPS)
5. 5
1. The compression of multiparticulates into tablets, unlike the hard gelatin capsule, is a
tamper-proof dosage form and has greater physicochemical and microbiological stability of
pellets as they are embedment in the inert matrix
2. Tablets have less difficulty in oesophageal transport than capsules
3. Tablets containing coated subunits can be prepared at a lower cost than these subunits filled
into hard gelatin capsules because of higher production rate of the tablet press
4. The expensive control of capsule integrity after filling is also eliminated
5. In addition, tablets containing multiparticulates without losing the controlled-release properties
could be scored, which allow a more flexible dosage regimen
ADVANTAGES of MUPS
6. Composing the tablet with equal or different kinds of particles can be combined and so that
very specific release profiles can be generated
7. Once the coated subunits have been developed different dose strengths can be prepared just by
varying the tablet size keeping the same composition – no additional development efforts
need to be taken
8. Another option for dose strength variation is the development of dividable multi-unit tablets
Since the release characteristics are related to the single subunits, dividing the tablet does not
affect the release characteristics as it is true for monolithic tablets
9. Rapid and uniform transit of subunits contained in tablets from the stomach into small intestine
owing to their small size, drug release is more uniform and possibility of dose dumping is
avoided with minimized tendency for intersubject variations
6. 6
RATIONALE OF FORMULATING MUPS
The rationale in formulating MUPS is to design chased on the release rates such as designing
controlled release, sustained release, delayed release and colon targeted drug delivery system
; oral disintegrating taste-masked dosage form
; combining drugs with different release characteristics in the same dosage form
The drug dose administered in modified release form can be increased as compared to that
possible with capsules and enhance the stability of dosage form as compared to its capsule
counterpart
It also helps in obviating the need for specialized packaging such as that required for
capsules making it a more cost effective dosage form
7. 7
IDEAL CHARACTERISTICS OF MUPS
1. Should maintain all the tablet properties
2. Pellets should not show any interaction like developing electrostatic charges; during
compression
3. The pellets should not show any deviation in its release even after compression
4. The coated pellets during the process of compression should not fuse into a nondisintegrating
matrix and should not lose its coating integrity either by breaking or cracking or rupturing
the coating layer(s) or pinholes and other imperfections
5. Like tablets, MUPS should have ease to withstand physical parameters, stability, packing
storage and transportation
6. The dosage form must disintegrate rapidly into individual pellets in gastrointestinal fluids.
9. 9
1. To ensure uniformity of content and weight
2. To compress the coated subunits to tablets with sufficient hardness and low friability
without damaging the film coatings
CHALLENGES IN FORMULATING MUPS
How to overcome of challenges ?
10. 10
Pellet shape
The shape of the pellets should be spherical or nearly spherical for good rhombohedral
packing
A more deviation in spherical shape does not result in compacts of characteristic release due
to flaws and cracks during compression
Pellet size
The size of the coated pellets can be maximum up to 2 mm to withstand compression pressure
Large sized pellets cause rupture to the coating of pellets due to segregation with tabletting
excipients and there by direct exposure of the transmitted force by the upper punch to lower
punch
Pellet Density
Pellets of density about 1.5 g/cm3 shows faster gastric emptying than pellets with higher
density of > 2 g/cm3
Pellets with < 2 mm in diameter and < 2 g/cm3 density can pass through pyloric sphincter both
in fasted and fed state which is similar to liquids in terms of gastric emptying
OVERCOME OF CHALLENGES I
In order to ensure undamaged film coatings and thus reproducible drug release after tablet
compression, various impact factors need to be considered:
11. 11
Pellet core and Core material
Pellets should have low surface to volume ratio; which might result in a decreased area of
contact between the particles as they consolidate
In favor of this, pellet core should have some degree of plasticity to have deformation in shape
during compression without any damage to the coated film
An extensive study was carried out on microcrystalline cellulose (MCC) by many researchers
both as powdered and granulated forms, and revealed that MCC shows plastic deformation
during compression and offers better protection to the coated particles as powder and
granules
Studies done with different concentrations of MCC and starch 155 confirmed that starch
strong compacts were formed by increasing concentrations of MCC while compaction with
MCC and starch 1500 results in decreased strength of compacts
Core material should not be too hard
※ DCP pellets, which obstructs the flow of pellets
In such case, compression force shows impact on the surface and results in deformation of
the surface and alters the release characteristics
OVERCOME OF CHALLENGES II
12. 12
Porosity
Porosity of pellets plays a major role in compression thereby relates to deformation
A study conducted by Nicklsson on compression of pellets with low, medium and high porosity
with extragranular materials MCC, PEG and dicalcium phosphate, the deformation of pellets
was much in favor of medium and high porous pellets
The fact found was that structures with high porous nature become denser due to the applied
compression force and forms as deformed coherent units due to the non interfering excipients
In case of compaction of reservoir pellets with high porous nature, compression force indicates
more densification and deformation with no marked difference in the drug release profiles
Conversely compaction of less porous pellets results in significant increase in the release rates of
the drug which is due to comparatively low densification and deformation
During compaction of porous pellets the entrapped air escapes out due to the compaction
pressure applied and surrounds the densifying pellets
☞ Pellets are subjected structural deformation to greater extent due to the rearrangement of
bonds; can be visualized by SEM analysis, and form coherent tablets
The formation of coherent units is attributed by the polymer coating used and the extragranular
material
The excipients used should not interfere with the pellets which alter the drug release profile
The extragranular material must form closest packing with the deformed pellets
OVERCOME OF CHALLENGES III
13. 13
Polymer coating and Film flexibility
Polymers widely used in attaining specific release profiles are cellulose derivatives and polyacryls
Cellulose and its derivatives like HPMC, HPMCP has elongation < 5% forms hard and brittle
films that fractures during compression whereas polyacryls and copolymers of acrylics form
flexible film deforms easily on compression
Plasticizers like triethyl citrate (TEC), triacetin and PEG also helps in the formation of flexible
films
Among them TEC was found efficient
During compression a highly flexible film ensures elastic properties and prevents cracking of
coating
Polymers like Eudragit along with plasticizers triethyl citrate provide greater flexibility to the
film in sufficient/required quantity
Retardation characteristics occur at higher percentages
OVERCOME OF CHALLENGES IV
14. 14
Mechanical resistance
Film flexibility provides mechanical stability to pellets during compaction
During compression, high mechanical resistance support film integrity by preventing deformation
of pellets
High mechanical stability is given by a dense structure like that provided by mini-tablets,
extrusion pellets or roller compaction granules
Furthermore, a bigger particle size supports mechanical stability and in addition leads to less
interparticle contacts which also support less film damages
OVERCOME OF CHALLENGES V
Coating thickness
The thickness of coating layer is related to mechanical resistance of pellets during compaction
Greater thicknesses support elastic properties, whereas below a certain thickness even highly
flexible films will break
The manner in which deformation of the coated pellets occurs during compaction alters the
thickness of the coating layer which has an impact on the release profile of the drug
If the deformation of the substrate pellet may stretch out the coating, making it thinner or more
permeable, faster drug release was observed
Whereas the densification of the substrate pellet may compress the coating, making it thicker or
less permeable, and consequently results in prolonged drug release
15. 15
Extra-granular material and cushioning agents
Film stability is influenced by extra-granular material during compression
Sharp-edged and abrasive crystalline materials may damage the coating as compression force
increases
his alters the drug release characteristics after compaction into tablets
Type and amount of the coating agent, selection of additives like plasticizers, use of cushioning
excipients and rate of pressure applied must be monitored carefully to maintain the drug release
properties of the sub units helps in the protection of the film
Soft materials or conventional powder excipients with plastic or elastic behavior like micro
crystalline cellulose or lactose can be used to protect film coating
The quantity of extagranular to be compressed along with pellets is 30-70% w/w
A threshold of atleast 30% (w/w) of extra-granular material should be added as it provides
support and cushioning
; hence the coated subunits embed freely in the matrix without segregation and form a coherent
tablet
With use of higher amount of pellets of at least 50%w/w
; variation may reduce, but the tendency for damage to coating increases
OVERCOME OF CHALLENGES VI
16. 16
Extra-granular material and cushioning agents
Generally suggested fillers are combination of different grades of fillers with different particle
size like Avicel PH 200 and Avicel PH 101
Cushioning agents are waxy in nature take up the pressures of compaction by re-arranging
themselves within the tablet structure or by preferentially getting deformed and/or fractured
thereby provides protection to the coated pellets
They also enhance deformation of pellets when used as extra-granular material in addition to
diluents
The best choice of cushioning agent is PEG preferably PEG 6000
Cushioning pellets are normally more porous and soft compared to coated drug pellets and
normally made of excipients which are used
The drug pellets-to-cushioning excipient(s) ratio is very critical in preventing coating film damage
– a ratio of 1:3 or 1:4 is considered most suitable
OVERCOME OF CHALLENGES VI
17. 17
Electrostatic Charges
Development of an electrostatic charge on the pellet surfaces can interfere with their flow during
tablet compression cycle
This problem is usually solved by adding talc, which acts as a glident. During development of
multiparticulate tablets comparative dissolution tests should be conducted to identify the possible
differences between the release rates of the uncompressed tabletting mixture versus the tablets
In order to ensure reproducible drug releases the difference between the two dissolution profiles
should not exceed 10%
OVERCOME OF CHALLENGES VII
18. 18
Tablet press designed MUPS have a modification in the hopper, feed frame and forced feeders
compared to normal tablet press
The hopper for feed consists of a butterfly valve to modulate the flow of blend to feed frame
The feed frame designed is continuous to ensure uniform clearance from the turret and prevent
attrition/ segregation of pellets from extra-granular material and also crushing of coated pellets
throughout the compression process, which is not possible with the regular rotary tablet press
The forced feeder used is gravity feeder, designed to prevent abrasion or grinding of pellets
TABLET PRESS FOR PREPARING MUPS
19. 19
MUPS Compression force
To a greater extent leads to damage of polymeric functional coating and alters dissolution profile
based of the designed type of formulation
In case of delayed release formulation rupture of polymer coat leads to release of drug in
acidic media and thereby, degradation of the drug
Compression speed
Probably be optimum for the formulation
High speed may cause improper die fill
Capping and lamination can be prevented by increasing the contact between punch heads and
compression rollers
PROCESS VARIABLES IN FORMULATING
21. 21
Spheronization is the process where extrudates (the output from an
extruder) are shaped into small rounded or spherical granules
In practice these usually vary in size from 0.4 to about 3.0 mm
The use of these spheroids can be relevant for a wide variety of industries
WHAT IS SPHERONIZATION?
2023-07-10
22. 22
The products produced from this process can be useful in several ways:
Product performance and functionality can be improved or changed to
meet a wide range of requirements
Plant procedures can be simplified, to reduce costs or enhance security of
operation
The process is well known and widely used in the pharmaceutical,
neutraceutical, catalyst, petrochemical, materials science and other
industries
Its use is becoming increasingly recognized in other areas of industrial
material handling
WHY CONSIDER SPHERONIZATION?
2023-07-10
23. 23
The main uses and advantages of
spheronization ( I )
Possibility Potential benefit...
Agglomerates of
material with a
uniform and controlled
size
Spheronization provides an efficient method of producing uniform
discrete particles of various sizes (size can be controlled, according
to user needs between a wide range of diameters)
As an example, where spheres would allow a better dispersion of
ingredients is especially useful in the pharmaceutical, biotechnology
(such as bone filler and regeneration) and nutraceutical industries
Producing small
particles with a high
surface area to volume
ratio
This can offer advantages in catalyst applications where
maximization of surface area can be useful
In other industries this allows for the most optimum product
for coating where this is required or desirable
The optimization of
flow characteristics
The excellent flow properties of spheres is well known
This allows the use of automated processes or use where exact
dosing is required such as tableting, mold filling, capsule filling and
other forms of packaging
2023-07-10
24. 24
The main uses and advantages of
spheronization ( II )
Possibility Potential benefit...
Producing the
optimum shape for
coating
Granules and spheres can require coating for a variety of reasons such as
the stabilization of the active ingredients or the controlled release of the
active ingredients
The most widespread use of coated spheroids is the controlled
release of medicine in the pharmaceutical industry
The easiest and most economical shape to coat is a small sphere, as no
additional material is required to coat or fill irregularities in the surface of
the particles
To facilitate the
mixing of non-
compatible Products
Filling of two incompatible active products into capsules can be easily and
cheaply done using spheronized products.
To improve
appearance of
powder or granulated
materials
Having spheres of a uniform and controlled size can significantly improve
the physical appearance of products
In markets where product differentiation is necessary to assist marketing
success, spheronization is a rapid and inexpensive way of separating your
products from the competition
2023-07-10
25. 25
The main uses and advantages of
spheronization ( III )
Possibility Potential benefit...
To improve the ability
to reproduce the same
physical properties of
packing beds
In several industrial applications columns or porous beds are used as
chemical reactors
The use of small spheres rather than irregular granules allow for easier
calculations, predictions and reproducibility.
To improve the
hardness and friability
of granules
The hardness of any tablet or sphere depends partly upon the internal
cohesive forces and partly on the surface characteristics of the product.
Spheronization increases the hardness and reduces the friability of the
materials being treated
This will reduce the amount of fines or dust during transportation or
subsequent handling
To increase the density
of granules
With spheronization both the true and the bulk density of the products
are increased
The amount of the increase depends upon the formulations being
processed
This gives the opportunity to improve both the processing and
packaging of products
2023-07-10
26. 26
The main uses and advantages of
spheronization ( IV )
Possibility Potential benefit...
To improve
accuracy in dosage
control
Improved flow characteristics facilitate accurate dosing
control
To improve the high
speed handling of
materials
Spheres have excellent flow properties. This allows the
increased ease of automated processes
To remove dust
hazard
Operations involving powders can produce dust. This
unwanted aspect of production can be a hazard to personal
safety and to the purity of the end product
The management of this is important in many industries
Spheronization will minimize the amount of dust thereby
reducing risk,keeping processes clean and preventing cross
contamination of processes and products during exposed
operations
2023-07-10
27. 27
The main uses and advantages of
spheronization ( V )
Possibility Potential benefit...
To simplify the
handling of difficult
material
Materials that are difficult to handle such as hygroscopic
materials, flavors, dyestuffs etc. can benefit from
spheronization
Once spheronized they can increase in stability and be less
affected by surrounding conditions
To simplify and
increase speed of
processing
Products that have been spheronized and dried have “fast flow”
characteristics
Problems due to blockage in transfer or valve mechanisms, or
bridging when the material is in hoppers, and losses due to
handling are reduced to a minimum
2023-07-10
29. 29
WHAT IS THE BASIC EQUIPMENT FOR
THE PROCESS OF SPHERONIZATION?
The process of spheronization consists of four key steps:
Mixing or granulation - a mixer or granulator is required
Extrusion - an extruder is required
Spheronization - a spheronizer is required
Drying and possibly coating - a coater and drier may be required
All of these steps are important and all can have a considerable influence
on the final product performance
2023-07-10
30. 30
The influence of different mixing/granulating parameters should not be
underestimated
It is true that in many cases mixing can have little or no effect on the
process or final product performance but this should never be assumed
When doing development work, it is important to keep the mixing
/granulation parameters constant (to remove a potential source of
variation) or to make systematic trials and demonstrate the effect (or lack
of effect) of changes in the mixing parameters
Mixing and/or Granulation:
2023-07-10
31. 31
The extrusion of the materials is a required step prior to spheronization
The final size of the pellets is principally determined by the diameter of
the extrudate used for the spheronization process
For example in order to obtain spheres with a diameter of about 1 mm, a 1
mm diameter hole is used on the extruder die or screen, although
dies and screens with slighter larger hole diameters will sometimes be
used to allow for shrinkage on drying
In a spheronizer, it is possible to obtain spheres with a diameter ranging
from about 0.4 mm to about 8 mm
Extrusion
2023-07-10
32. 32
A Twin Screw Variable Density production
extruder from Caleva
2023-07-10
33. 33
Modern spheronizers have several additions and adaptations depending
upon the needs of the particular product and process
The design principle of the spheronizer is relatively simple but the detailed
development of auxiliary equipment and the specifics of the design have
widened the range of applications and greatly improved the flexibility of
the machines
In principle the basic machine consists of a round disc with rotating drive
shaft, spinning at high speed at the bottom of a stationary cylindrical bowl
The spinning friction plate has a carefully designed groove pattern to the
base
This is most often cross-hatched, but several sizes and other types are
available
These discs are designed to increase the friction with the product
Spheronization I
2023-07-10
35. 35
Extrudates are added to the spheronizer and they fall onto the spinning
plate
During the early contacts of the cylindrical granules with the friction plate,
the extrudates are cut into segments with a length ranging from 1 to 1.2
times their diameter
These segments then collide with the bowl wall and they are thrown back
to the inside of the friction plate. Centrifugal force sends the material to
the outside of the disc
The action of the material being moved causes the extrudate to be
broken down into pieces of approximately equal length relative to the
diameter of the extrudate
Spheronization II
2023-07-10
36. 36
These cylindrical segments are gradually rounded by the collisions with the
bowl wall, the plate and each other
The ongoing action of particles colliding with the wall and being thrown
back to the inside of the plate creates a “rope movement” of product along
the bowl wall
The continuous collision of the particles with the wall and with the friction
plate will gradually turn the cylindrical segments into spheres, provided
that the granules are pliable enough to allow the deformation without
being destroyed
It is essential that this rope movement is present for an optimal
spheronization
Spheronization III
2023-07-10
39. 39
These cylindrical segments are gradually rounded by the collisions with the
bowl wall, the plate and each other
The ongoing action of particles colliding with the wall and being thrown
back to the inside of the plate creates a “rope movement” of product along
the bowl wall
The continuous collision of the particles with the wall and with the friction
plate will gradually turn the cylindrical segments into spheres, provided
that the granules are pliable enough to allow the deformation without
being destroyed
It is essential that this rope movement is present for an optimal
spheronization
Spheronization III
2023-07-10
40. 40
As processing continues, the shape of the pieces gradually changes as
shown below
Spheronization III
2023-07-10
41. 41
When the particles have reached the desired shape (usually in about 2 to 10
minutes) then the spheroids can be removed
When the particles have obtained the desired spherical shape, the discharge
valve of the spheronization chamber is opened and the granules are
discharged by the centrifugal force
Spheronization IV
2023-07-10
45. 45
Friction plate pattern
The most common groove pattern used for spheronizer discs is the “waffle-
iron” design, where the friction plate is like a chessboard of chopped-off
pyramids
The choice of which plate to use is not always clear
As a guideline extrudates up to 0.8 mm in diameter are normally processed
on a 2 mm pitch plate
A 3 mm pitch plate is used for extrudates up to 3 mm in diameter
Discs with a radial design are also used, as these are considered gentler on
the material being spheronized
2023-07-10
48. 48
Friction plate speed
The typical rotation speed of a production size (700 mm diameter) disc
ranges from 200 to 450 rpm
The higher the speed, the more energy is put into the particle during a
collision
The optimum speed depends on the characteristics of the product being
used and the particle size
The smaller the diameter of the disc the higher the speed required
The important parameter is the speed at the outer edge of the disc
In practice the optimum speed can be determined with a little experience
For some products it may be recommended to start at a high speed and to
lower the speed in the final stage of the process
This can be determined by simple practical tests
The process allows a high degree of flexibility for good formulations
2023-07-10
49. 49
Retention time (The length of time the product is
spheronized in the spheronizer)
Typical spheronization retention times to obtain spheres range from 3 to 8
minutes
This is relatively easy to determine and best obtained by simple trials with
specific products
For some products, the strong cohesive forces in the extrudates prevent
the extrudates from breaking up into smaller pieces
If the objective is to reduce dust and not necessarily obtain perfect spheres
then the short contact with the friction plate is sufficient to break the long
extrudates into small segments and round the edges
The edges of cylindrical granules are the most fragile part and they will
generate dust during handling and transportation
Spheronization with a short retention time can help to reduce the amount
of dust significantly.
2023-07-10
50. 50
The charge volume or weight (The quantity of
product loaded into the spheronizer)
The optimum level depends upon the machine size and the product
characteristics;
there is an optimum quantity of product to be charged per batch into the
spheronizer chamber that will produce the most narrow particle
distribution and the best spheres
A typical charge volume for a machine with a 380 mm diameter disc is 4
kg depending upon the density of the material
Increasing the load per batch increases the hardness of the spheres and
smooths the granule surface
With the larger 700 spheronizer a load of from 2 kg to about 12 kg is
normal
2023-07-10
52. 52
Rheology I
The rheology of the product can be changed by using binders or
lubricants, or by changing the mixing time and by altering the liquid
content of the mix
Although the examination of the rheology of the product seems complex
and potentially time consuming to perfect, with a Caleva Mixer Torque
Rheometer (MTR) the ideal formulation can be determined very quickly
and easily
2023-07-10
53. 53
Rheology II
Binders can be used to increase the strength of the granules and reduce the
amount of fine dust generated during spheronization
If too much binder is added and the granules become too hard, it will be
difficult to obtain good spheres
Lubricants will increase the plasticity but may also increase the amount of
fine dust generated during spheronization
Water can also be used as a lubricant
If too much water is used, sticking can occur on the friction plate and bowl
wall
It can also happen that the granules will stick together, forming big lumps
If the extrudates are too dry, a high amount of fine dust will be generated
The optimum moisture content for spheronization is slightly less than for
extrusion only
2023-07-10
54. 54
Mixer Torque Rheometer can be used to optimize rheology of your formulation
Rheology III
2023-07-10
56. 56
Drum Heating/Cooling Jacket
Heating or cooling water can be introduced in a jacket around the
spheronizer bowl
Warm water can be particularly useful on the chamber wall to drive off
moisture that would cause product to stick to the wall
Cooling the wall will avoid temperature rises in heat sensitive products,
although the average temperature rise in a spheronizer is generally rather
small (approximately 2 to 3 °C)
Air introduction (Fines air)
A slight flow of air can be introduced in the chamber from under the
friction plate
This not only prevents dust from getting between the rotating plate and
the wall of the chamber but also can help to remove moisture from the
granule’s surface, improving the friction forces and process efficiency
Auxiliary beneficial options for
spheronizer configuration I
2023-07-10
57. 57
Automatic timer
It is useful but not essential to have an automatic timer on a spheronizer
Spheronization is a batch process and not a continuous process
Proper timing of the spheronization run time for each batch will help to
maintain standard operating procedures and enhance performance
standardization and product quality
Non-Stick Coatings
For some products, the chamber wall and the plate can be coated with
non-stick materials if this is necessary for ease of use with sticky
materials or cleaning
Auxiliary beneficial options for
spheronizer configuration II
2023-07-10
60. 60
Twin Dome Granulator
Twin Dome Granulator
Applicable to the fine-granule with a pilot scale production and the low-
volume high-mix production
GMP design
Dome Die and Screw Case are easily disassembled so that the powder-
contacting parts can be cleaned by a water.
Particle diameter: 0.3 mm to 2 mm in diameter
Product shape: Cylindrical
Application examples
Pharmaceutical products
Seasonings
Granulated sugar
Health food products
Agrochemical products
Fish Feed
2023-07-10
62. 62
Extruder Twin Screw type EXD
(Radial Extrusion)
Extruder Twin Screw type EXD (Radial Extrusion)
The pioneer of wet extrusion granulator in the world.
All powder-contact parts to the product can be easily disassembled and
re-assembled.
Available in Heating/ Cooling Jacket
GMP design is available
Particle diameter: 0.5 mm to 3.0 mm in diameter
Product shape: Cylindrical
Application examples
Pharmaceutical products
Seasonings
Granulated sugar
Health food products
Agrochemical products
Fish Feed
2023-07-10
64. 64
Spheronizer/ Marumerizer
Converting the cylindrical shaped granule into the spherical shaped
granule by the friction force, the driving force and the centrifugal force.
Also different length of cylindrical granules are converted into uniform
length in a short operation time
Spherical granules can be produced with narrow/sharp particle size
distribution with high yield
All powder-contact parts to the product can be easily disassembled and re-
assembled.
GMP design is available
Particle diameter: 0.4 mm to 10 mm in diameter
Product shape: Spherical granule
Application examples
Pharmaceutical products (Coating for the Drug Delivery System of
pharmacy)
Agrochemical products (Coating for the sustained release of WDG)
2023-07-10
66. 66
Combined Granulation System
Multiple devices are combined from the product feeding to spheronization
By reducing the human intervention in the process, it contributes to the
stable product quality and the labor cost reduction
Each device is redesigned so that its structure is suitable for integration
Granulator can be chosen to meet the desired capacity, granule size
2023-07-10
76. 왜 에스라졸은 넥시움과 용출패턴이 달라야 하나
76
1.넥시움은 장용성코팅을 한 소형 pellet1000개를 압축하여 정제로 만든 제형
(외부는 일반 코팅)
→ 정제는 위에서 붕해되지만 장용pellet은 소장에서 개별적으로 붕해되고 약물용출
2.에스라졸은 정제내부에 알카리화제와 안정화제를 홉한한후 나정을 장용코팅한 코팅정
→ 정제는 위에서 붕해되지 않고 소장에서 정제가 붕해되고 약물이 용출
☞ 위에서 붕해된 넥시움이 소장 상부에서 흡수가 되는 방면 에스라졸은 소장에서 정제가
붕해되고 용출되므로 넥시움에 비해 상대적으로 천천히 흡수된다
☞ 흡수의 시간 차이를 극복하기 위해 에스라졸이 넥시움 보다 용출이 빨라야 흡수차이를
상쇄할수 있음
80. 80
TOPROL-XL uses a patented extended-release technology
TOPROL-XL (metoprolol succinate) is available in extended-release tablets
with oral administration, providing 24-hour hypertension treatment with 1 dose daily
TOPROL-XL
81. 81
Mean steady-state plasma concentrations
TOPROL-XL maintained consistent plasma levels vs immediate-release metoprolol
and immediate-release atenolol over 24 hours
TOPROL-XL
83. 태평약 제약 자체 기술 독사조신 서방성 제제
MSCR (multi-stage controlled release )기술
OROS 특허 회피 전략으로 매트릭스 시스템으로 서방성 제제 개발
한미약품 H-matrix 기술 회피 전략으로 3중 방출 제어 모델 설정
프조신 XL
2023-07-10 83
121. Elan사의 대표적인 서방성 제제기술
입상백당(Nonparel) 같은 불활성 core에 약물을 코팅한 후 방출조절이 가능한
폴리머를 적절한 비율로 코팅한 미세한 구형입자
(spherical bead, 직경 1∼2 mm )
적용하는 폴리머의 조성변경 -> 다양한 방출 양상을 나타내는 제제 개발 가능
SODAS (Spheroid oral drug absorption system)
SODAS : Technology overview
2023-07-10 121
122. Sodas® multilayer tablet technology is a multilayer drug delivery system
which focuses on the production of controlled release beads
The Sodas® technology is characterized by its inherent flexibility that
enables the production of customized dosage forms that respond directly
to individual needs such as pain and blood pressure
The technology essentially leads a pursatile drug release where the drug is
released in pulses that are separated by defined time intervals
Examples of this technology include Ritalin® LA and Focalin® XR
They are both used to treat Attention Deficit Hyperativity Disorder
(ADHD)
They provide a once-daily pulsed profile that offers the patient
efficacy throughout the day negating the need for taking the dose during
working hours unlike the twice-daily dosing of the conventional
immediate release tablet
A schematic representation of Sodas®
multilayer tablet technology
2023-07-10 122
123. Benefits offered by the SODAS® technology include
Controlled absorption with resultant reduction in peak to trough ratios,
targeted release of the drug to specific areas within the gastrointestinal
tract, absorption independent of the feeding state, suitability for use with
one or more active drug candidate, facility to produce combination dosage
forms, “sprinkle dosing” by administrating the capsule contents with soft
food, once or twice daily dose resembling multiple daily dose profiles
A schematic representation of Sodas®
multilayer tablet technology
2023-07-10 123
126. SODAS : Technology overview
The SODAS® delivery system continues to be an accepted and approved system by regulatory
authorities with five products approved and launched in the U.S. since 2002 including once daily
oral dosage forms of Avinza®, Ritalin® LA, Focalin® XR and Luvox® CR
2023-07-10 126
127. SODAS continues to be an accepted and approved system by regulatory authorities with the
most recent regulatory approvals for a SODAS based system occurring since US in 2002 with
the launch of once daily oral dosage forms of Avinza®, Ritalin® LA and Focalin® XR
A number of other compounds are in late stage development utilizing Elan’s SODAS technology
Avinza : Morphine Sulfate Extended release capsule[Norvatis]
Ritalin LA : Methylphenidate HCl , Extended release capsule[Ligand]
Focalin XR : Dexmethylphenidate (Norvatis)
SODAS : 시판제품
2023-07-10 127
142. Verelan® PM represents a commercialized product using the CODAS technology
The Verelan PM formulation was designed to begin releasing Verapamil approximately four
to five hours post ingestion
This delay in release is introduced by the level of release controlling polymer applied to the
drug loaded beads
The release controlling polymer is a combination of water soluble and water insoluble
polymers
As water from the gastrointestinal tract comes in contact with the polymer coat beads, the
water soluble polymer slowly dissolves and the drug diffuses through the resulting pores in
the coating
The water insoluble polymer continues to act as a barrier, maintaining controlled release of
the drug
When taken at bedtime, this controlled onset extended release delivery system enables a
maximum plasma concentration of Verapamil in the morning hours, when blood pressure
normally rises from its overnight low
CODAS : Technology overview
2023-07-10 142
146. PRODAS involves direct compression of an immediate release granulate to
produce individual minitablets.
These minitablets are subsequently packaged into hard gelatin capsules,
which represent the final dosage form
A more beneficial use of the technology, however, is in the production of
controlled release formulations.
In this case the incorporation of various polymer combinations within the
granulate delays the release rate of drug from each of the individual
minitablets.
These minitablets may subsequently be coated with controlled release
polymer solutions to provide additional delayed release properties
PRODAS : Technology overview
2023-07-10 146
158. 2023-07-10 158
보유기술 III
( TaPe Capsule Technology )
복합제 제조시 주성분간의 물리화학적 상호작용을 극복 복합제
내부 : 고형정제 및 펠렛을 함유하는 캡슐형 제형
안정성 및 물리화학적 상호작용문제로 단일제제화 하기 어려운 다수의 성분 복합
내부에 포함된 정제 및 펠렛 : 장용코팅, 서방화 등 다양한 제제특성
159. 2023-07-10 159
보유기술 IV
( Double SODAS Technology )
시판제품 (클라빅신듀오 캡슐)
2010년 유럽에서 발매된 사노피-아벤티스사와 BMS사가 공동으로 개발한 복합제
DuoPlavin’(DuoCover)‘과 비교해 장기복용에 따른 아스피린의 위점막 자극 등의 부작용 최소화
성분 간의 약물상호작용을 방지
→ 안정성을 높일 수 있도록 double SODAS (spheroidal oral drug absorption) 제제기술을 적용
→ 장용성펠렛(enteric coating pellet)
Double SODAS
클로피도그렐(속방성 펠렛) + 아스피린(장용성 펠렛)
→캡슐에 충진해 주성분 간의 물리적 접촉을 차단함으로써 안정성 강화
단일제 병용투여와의 비교임상시험
→클로피도그렐, 아스피린 뿐만 아니라 각각의 활성대사체에 대해서도 동등한 약물동태학적 특성
169. 169
대원 '업타파' 약 20억 독주체제 시동…동광·한림도 10억원 돌파
피타바스타틴 + 페노피브레이트 복합제 시장: 1년만에 두 배 가량 확대
피타바스타틴의 오리지널 의약품 : JW중외제약(리바로정)
한림제약 등 8개 제약사
-파타바스타틴 + 페노피브레이트 복합제국내 허가→2019.07 시판
특장점
-피파바스타틴 : LDL 콜레스테롤 감소
-페노피브레이트 : 중성지방 감소 / HDL 콜레스테롤 증가
적응증
-관상동맥심질환(CHD) 고위험이 있는 성인환자에서 피타바스타틴 2mg 단일치료
요법시 LDL-콜레스테롤 수치는 적절히 조절되지만 트리글리세라이드 수치는 높고
HDL-콜레스테롤 수치는 낮은 복합형 이상지질혈증의 치료
복합제 특장점
174. 174
에소메졸 DR
청구항 1
에스오메프라졸(esomeprazole)염을 함유하는
; 코어, 상기 코어 상에 형성된 내피 코팅층
; 상기 내피 코팅층 상에 형성된 제 1 장용성 코팅층을 포함하는 제1용출부
; 상기 내피 코팅층 상에 형성된 제 2 장용성 코팅층을 포함하는 제2용출부
; 복합 캡슐
; 상기 제1장용성 코팅층은 코팅기제로서 메타크릴산 코폴리머 LD를 내피 코팅층이 형성된
코어의 5 내지 50%(w/w)로 포함
; 상기 제2장용성 코팅층은 코팅기제로서 메타크릴산 코폴리머 S및 메타크릴산 코폴리머 L의
1.5:1 내지 3.5:1(w/w) 혼합물을 내피 코팅층이 형성된 코어의 15 내지 40 %(w/w)로 포함
; 제1용출부 및 제2용출부의 코어는 모두 미니정제인 복합 캡슐제
182. Introduction
General administration methods for the sprinkle drug products in various dosage forms including
tablets, powder, granules, immediate-release (IR) capsules, extended-release (ER) capsules, delayed-
release (DR) capsules, and multiarticulate drug delivery system (MDDS).
2023-07-10 182
183. Pentasa
The number of approved New Drug Applications (NDAs) for sprinkle drug products since 1941
A total of sixty-five original sprinkle products are available on the US pharmaceutical market
2023-07-10 183
206. 206
Diclofenac sodium 75 mg biphasic-release capsules comprising
DR pellets (magenta beads) and XR pellets (yellow beads)
Concepts of MUPS
207. 207
SEM micrographs of cross-sections of diclofenac sodium DR and XR pellets ( 500×) and Raman maps of XR pellets (spatial
resolution of 10 µm and high resolution of 3 µm)
Rocation of diclofenac sodium marked with red color, core material with different shades of blue, hypromellose—green to
yellow, and polymethacrylate-based coating—pink
Concepts of MUPS
217. 217
Pellets prepared by conventional and innovative technologies III
Schematic illustration of drug layering process of the active substance
from solution/suspension and polymer coating
218. 218
Pellets prepared by conventional and innovative technologies IV
Schematic illustration of dry powder layering of starter core and polymer coating
234. LEADING THE WORLD IN EXCIPIENTS JRS PHARMA
Capsule Filling with
JRS Pharma‘s
NON-PAREIL SEEDS
Sacchari spheri Ph.Eur.,
Sugar Spheres USP / NF
235. LEADING THE WORLD IN EXCIPIENTS JRS PHARMA
4 names for one dosage form:
Globuli
Pellets
Spheres
Non-Pareils
JRS Pharma‘s
NON-PAREIL SEEDS
Sacchari spheri Ph.Eur.,
Sugar Spheres USP / NF
236. LEADING THE WORLD IN EXCIPIENTS JRS PHARMA
Capsule Filling
With Powder With Non-Pareils
Functions as carrier for
controlled or sustained
release drug delivery
technologies
No active function
Sugar based
MCC based
Lets talk about this!
237. LEADING THE WORLD IN EXCIPIENTS JRS PHARMA
Tablets are cheap – why to use capsules filled
with spheres?
High Content Uniformity
Consistent and controlled drug release
Multiple drug can be combined in one unit
High drug stability
Many different ways to coat the active
Easy Manufacturing Process
Risk of drug dumping is reduced
238. LEADING THE WORLD IN EXCIPIENTS JRS PHARMA
Easy Manufacturing Process:
Active + (...) + Solvent:
1. Coating of NON-PAREIL SEEDS with an Active Solution
2. Drying of the pellets
For Sustained Release Formulations:
1. Coating of the Active-Spheres with coating material, e.g.
HPMC Solution, in different thickness
2. Drying of the pellets
Single Units Cores in different sizes
Active in the same concentration
Film in different thickness
239. LEADING THE WORLD IN EXCIPIENTS JRS PHARMA
Multiple Units
core
active
film
Single Units
Body
Disintegration with
different
release profiles
Easy Manufacturing Process:
240. LEADING THE WORLD IN EXCIPIENTS JRS PHARMA
Sustained Release Systems
Film coating systems: Limits
Working with spheres
(multiple dosage):
No problem !
Working with tablets
(single unit):
High risk !
241. LEADING THE WORLD IN EXCIPIENTS JRS PHARMA
Benefits of sustained release formulations?
Homogenous blood concentration levels due to
their consistent distribution in the GI-tract
Improved patient compliance by reducing
dose frequency
Therefore reduced side effects
Resistance of API to stomach acid
242. LEADING THE WORLD IN EXCIPIENTS JRS PHARMA
Characteristics of NON-PAREIL SEEDS?
specially designed spherical particles
of uniform diameter within different grades
white, uniform granules
Remainder is chiefly starch
243. LEADING THE WORLD IN EXCIPIENTS JRS PHARMA
Important properties of NON-PAREIL SEEDS
Sweet taste
Practically inert and odorless
Not sensitive against heat (up to 30°C)
High breaking hardness – uniform surface
Nearly no abrasion –
no dust development – therefore
easy to coat
High surface area for the active coating
244. LEADING THE WORLD IN EXCIPIENTS JRS PHARMA
Monograph Specifications: Sugar Spheres NF
1. Appearance White, hard, brittle, free-flowing, spherical masses
2. Identification The insoluble portion of a slurry gives a reddish-violet
to deep blue color with iodine
3. Specific rotation + 41° - + 61°
4. Loss on drying not more than 4.0 %
5. Sucrose 62.5 – 91.5 % on dried basis
6. Residue on ignition not more than 0.25 %
7. Particle size (by RoTap)
not less than 90.0 % passes the coarser sieve
sieze stated in the labelling; 100 % passes the
next coarser sieve size listed in the labelling.
Not more than 10.0 % passes the finer sieve
size stated in the labeling.