This document discusses key considerations for dosage form design and formulation. It explains that pharmaceutical formulation involves selecting excipients to solubilize, thicken, stabilize, flavor, and otherwise modify drug substances for patient delivery. Proper dosage form design requires considering the physical and chemical properties of drug substances and ensuring compatibility with excipients. Preformulation studies characterize the drug's properties including solubility, dissolution rate, and stability. Understanding these properties helps determine the appropriate dosage form and formulation to provide stable, effective delivery of the active drug to patients.
Leak tests in parenteral preparations s majzoob-20-july2015Sayeh Majzoob
The document discusses container-closure integrity testing (CCIT) for parenteral preparations. It aims to provide an overview of CCIT, including why leaks are important to avoid, different leak testing methods, criteria for choosing a suitable method, calibration and validation requirements, and regulatory aspects. The document covers visual inspection, bubble tests, dye tests, microbial ingress tests, vacuum decay methods, pressure decay methods, and high voltage leak detection. It discusses deterministic versus probabilistic methods and FDA regulatory requirements for CCIT and particulate matter.
The document discusses parenteral dosage forms. Parenterals are sterile solutions or suspensions of drugs administered directly into veins, muscles, or under the skin. They do not utilize the alimentary canal and must meet general requirements including stability, sterility, isotonicity, and being free of pyrogens, toxins, and foreign particles. Evaluation tests for parenterals include sterility, pyrogen, clarity, and leakage tests.
This document discusses various types of pharmaceutical excipients used in drug formulations. It defines excipients as pharmacologically inactive substances formulated alongside active pharmaceutical ingredients. Excipients provide bulk, facilitate drug absorption and stability, aid manufacturing, and improve handling. Common excipients include fillers, binders, disintegrants, coatings, preservatives, antioxidants, and solvents. Each excipient type has distinct functions and ideal properties. Proper excipient selection is important to ensure drug efficacy, stability, safety, and to avoid complications.
The document discusses the manufacturing process of parenteral preparations. It describes parenterals as sterile liquids or solids for injection or implantation. The manufacturing process involves planning, material management, production, quality control testing, filling, and packaging. Production areas are divided into strict zones based on cleanliness. Environmental controls and facility design aim to prevent contamination, with areas for filling, weighing, storage, and administration. Personnel flow and utility locations are also considered for efficiency.
the all u need to know about syrup is here its a verified information.and will help u to incerease your knowledge about liquid dosage forms especially Syrup
Equipments used for semi solid dosage formAli Hamza
This document discusses equipment used for manufacturing semi-solid dosage forms such as ointments, pastes, gels and jellies. It describes mills such as fluidized energy mills and roller mills that are used to mill ingredients. It also mentions mixers that are used for mixing, emulsification and deaeration in the production of ointments and creams. The document provides details on the manufacturing process and requirements for packaging and labeling of semi-solid dosage forms.
Leak tests in parenteral preparations s majzoob-20-july2015Sayeh Majzoob
The document discusses container-closure integrity testing (CCIT) for parenteral preparations. It aims to provide an overview of CCIT, including why leaks are important to avoid, different leak testing methods, criteria for choosing a suitable method, calibration and validation requirements, and regulatory aspects. The document covers visual inspection, bubble tests, dye tests, microbial ingress tests, vacuum decay methods, pressure decay methods, and high voltage leak detection. It discusses deterministic versus probabilistic methods and FDA regulatory requirements for CCIT and particulate matter.
The document discusses parenteral dosage forms. Parenterals are sterile solutions or suspensions of drugs administered directly into veins, muscles, or under the skin. They do not utilize the alimentary canal and must meet general requirements including stability, sterility, isotonicity, and being free of pyrogens, toxins, and foreign particles. Evaluation tests for parenterals include sterility, pyrogen, clarity, and leakage tests.
This document discusses various types of pharmaceutical excipients used in drug formulations. It defines excipients as pharmacologically inactive substances formulated alongside active pharmaceutical ingredients. Excipients provide bulk, facilitate drug absorption and stability, aid manufacturing, and improve handling. Common excipients include fillers, binders, disintegrants, coatings, preservatives, antioxidants, and solvents. Each excipient type has distinct functions and ideal properties. Proper excipient selection is important to ensure drug efficacy, stability, safety, and to avoid complications.
The document discusses the manufacturing process of parenteral preparations. It describes parenterals as sterile liquids or solids for injection or implantation. The manufacturing process involves planning, material management, production, quality control testing, filling, and packaging. Production areas are divided into strict zones based on cleanliness. Environmental controls and facility design aim to prevent contamination, with areas for filling, weighing, storage, and administration. Personnel flow and utility locations are also considered for efficiency.
the all u need to know about syrup is here its a verified information.and will help u to incerease your knowledge about liquid dosage forms especially Syrup
Equipments used for semi solid dosage formAli Hamza
This document discusses equipment used for manufacturing semi-solid dosage forms such as ointments, pastes, gels and jellies. It describes mills such as fluidized energy mills and roller mills that are used to mill ingredients. It also mentions mixers that are used for mixing, emulsification and deaeration in the production of ointments and creams. The document provides details on the manufacturing process and requirements for packaging and labeling of semi-solid dosage forms.
The document discusses various quality control tests that are performed on tablets during manufacturing, including tests for general appearance, hardness, friability, weight variation, content uniformity, disintegration and dissolution. It provides details on procedures and limits for these tests according to pharmacopoeial standards like the British Pharmacopoeia, Indian Pharmacopoeia and United States Pharmacopoeia. The tests are important to ensure tablets meet requirements for reproducibility, stability and accurate dosing of the active drug.
This document discusses tablet tooling and the tablet compression process. It describes the main types of tablet tooling, including 'B', 'D', 'BB', and 'DB' tooling, and provides their dimensions and specifications. It also outlines the basic components of a tablet press, including the hopper, dies, punches, cam tracks, and feeding mechanism. Finally, it explains the three main steps of the tablet compression process: filling and dosing the dies, compressing the tablets, and ejecting and exiting the tablets from the press.
This document discusses various types of solid dosage forms, with a focus on tablets and capsules. Tablets can be film coated, enteric coated, effervescent, sublingual, buccal, troches, chewable, or modified/slow release. Capsules can be hard or soft shell and contain solids or oils. Powders can be simplex, complex, indivisi or divisi. The document provides examples and describes how to write prescriptions for different solid dosage forms.
This document discusses common tablet processing problems and their remedies. It describes visual defects like capping, lamination, cracking, chipping, sticking, picking, and binding that can occur during tablet manufacturing. The causes of each defect are explained in terms of formulation issues like moisture content, binder amount, granule size, and machine issues like die wear, concavity, and speed. Solutions provided include optimizing the formulation through proper drying, lubrication, and binder selection, as well as adjusting machine settings like tapered dies, lubricated punches, and reduced speed or pressure. Overall, the document aims to help industrial pharmacists address problems in tablet manufacturing.
The document discusses sterile formulations and parenteral products. It covers key topics like routes of parenteral administration, pre-formulation of sterile products, physicochemical properties, general requirements, and sterility testing. The different routes discussed are subcutaneous, intramuscular, intravenous, and others. Ideal properties of sterile dosage forms include sterility, isotonicity, being pyrogen-free and particle-free. The document also differentiates between small volume parenterals and large volume parenterals.
1. The document discusses quality control tests for tablets, including tests for tablet characteristics before and after compression. It describes tests for properties like hardness, friability, thickness, weight variation, drug content uniformity, and dissolution.
2. Official tests discussed include weight variation, disintegration, dissolution, and drug content/assay. Non-official tests include hardness and friability. Test conditions and acceptance criteria are provided for many of the tests.
3. The purpose of the quality control tests is to ensure tablets include the correct dose of drug, the drug is released in a controlled and reproducible manner, and the tablets have sufficient mechanical strength.
Selection and evaluation of pharmaceutical packaging materials, containers an...NRx Hemant Rathod
This document discusses pharmaceutical packaging materials and their characteristics. It describes the role of packaging in protecting pharmaceuticals and presenting information. The main packaging materials discussed are glass, plastic, metal, and paper. The ideal requirements for containers include being neutral and protecting the product from various environmental factors. Common container types include well-closed, single dose, and multi dose containers. The document also examines closures and their role in preventing contamination or loss of materials. Closures discussed include screw caps, lug caps and pilfer proof closures. The characteristics and uses of different packaging materials are summarized.
IPQC Tests for capsules As per IP, BP & USPPramod Ramane
IPQC- In Process Quality Control Tests for Capsules are
1. Uniformity Of Content
2. Disintigration Test
3. Weight Variation Test
4. Dissolution Test
The tests are with Acceptance limits/Criteria as per Indian Pharmacopoeia (IP), British Pharmacopoeia (BP) & United States Pharmacopoeia (USP)
This document discusses important considerations for dosage form design and pharmaceutical formulation. It covers topics like pharmaceutics, drug substance characteristics, excipient selection and functions, preformulation studies, stability testing, and packaging. Preformulation studies help determine appropriate dosage forms and ensure drug stability. Stability is enhanced by protecting drugs from moisture, oxygen, light and other degradation factors through packaging and formulation choices. Proper dosage form design and formulation are essential for producing effective and safe drug products.
This lecture discusses pharmaceutical powders. It begins by defining a pharmaceutical powder as a solid dosage form containing finely divided drugs or chemicals meant for internal or external use. Powders permit drugs to be reduced to a very fine state, enhancing dissolution rate, absorption, and masking unpleasant tastes. The lecture then covers various types of powders including divided powders for internal use (simple, compound, cachet-enclosed), bulk powders (antacids, laxatives), and powders for external use. Methods for reducing particle size like trituration, pulverization, and levigation are also summarized.
This document summarizes the standards and testing methods for different types of tablets according to the Indian Pharmacopoeia. It describes 10 types of tablets and the standards that apply to all tablets, including content uniformity, weight variation, disintegration, friability, and dissolution testing. The document provides details on the acceptance criteria and testing procedures for each of these standards.
This document provides information about pharmacy internship programs and pharmaceutical dosage forms. It describes minor and major internships in community pharmacy, hospital pharmacy, and manufacturing pharmacy. It also outlines the specific objectives of community pharmacy internships. The document then discusses various pharmaceutical dosage forms including liquids, emulsions, suspensions, gels, and oral solid dosage forms like tablets and capsules. It provides examples of different dosage forms.
The document describes the process and key components of a tablet compression machine. The machine uses punches and dies to compress powder or granules into tablets. It has several stations that rotate to precisely fill the dies, compress the powder under high pressure, and eject the finished tablets. The main stages are filling the die cavity, adjusting the powder weight, compressing the powder between the punches, and ejecting the tablet. Critical parts include the hopper, feeder system, punches, dies, turret, cam tracks, and rollers which work together to automate tablet production.
This document provides information about various topical dermatological preparations including ointments, creams, gels, pastes, plasters, and others. It discusses the composition, properties, applications, and manufacturing of these preparations. Ointments are semisolid preparations intended for external application with an oily base that forms a protective, moisturizing layer on the skin. Creams are emulsions that are soft, smooth, and spreadable. Gels consist of a gelling agent suspended in water that forms a semirigid system. The document outlines the different types of bases used and key factors in selecting the appropriate base. It also reviews the production and quality control of these topical preparations.
This document discusses common manufacturing defects that can occur during tablet production such as picking and sticking, capping and lamination, mottling, double impression, poor mixing, poor flow, weight variation, and hardness variation. For each defect, the document provides the reason for why the defect occurs and recommendations for how to correct the issue, such as using properly designed punches, adequate drying, uniform granule size distribution, and controlling punch movement. The overall goal of the document is to outline typical tablet defects, their causes, and methods for prevention.
Superdisintegrants in Orally Administered Products of Pharmaceuticals A Reviewijtsrd
This document reviews superdisintegrants, which are added to pharmaceutical products to improve palatability and the performance of solid oral dosage forms. Superdisintegrants work by reducing the disintegration time of tablets, which improves drug dissolution rate. The review discusses various types of natural, synthetic, and semi-synthetic superdisintegrants. It also examines the mechanisms by which superdisintegrants cause rapid tablet disintegration, such as swelling, porosity, deformation, and particle repulsion. The ideal properties of superdisintegrants and their methods of incorporation into tablets are described. The document concludes that superdisintegrants can help advance the development of orally administered pharmaceutical products by improving acceptability and potency.
This document provides information about semi-solid dosage forms including ointments. It defines semi-solid dosage forms as products of semi-solid consistency applied to the skin or mucous membranes. Ointments are described as viscous semisolids used topically containing a drug and a base. Various types of bases are discussed including oleaginous, absorption, emulsion and water-soluble bases. Properties, examples and uses of different bases are provided. Other topics covered include ideal properties of semi-solid dosage forms, drug permeability through skin, and formulation ingredients like antimicrobial preservatives.
The most common method of drug delivery is oral dosage
form of which tablet and capsule are predominant.
Tablet is more accepted as compared to capsule due to
many reason such as cost, tamper resistance, ease of
handling, ease of identification and manufacturing efficiency.
Tablet compression process understanding is resulted in
development of formulation.
Recent advances in the design of tablet compression
equipment has conducted resulted in higher efficiency,
minimized tablet variation, greater flexibility.
This document discusses key considerations for dosage form design and formulation. It outlines the need to consider the physical and chemical properties of drug substances and ensure compatibility between ingredients. Preformulation studies are important to characterize drug properties like solubility, dissolution rate, and stability. These studies help determine the appropriate dosage form and ensure the drug is delivered effectively and safely. The goals of a proper design are to provide patient benefit while protecting drug integrity throughout production, storage, and use.
This document discusses dissolution testing techniques used in the pharmaceutical industry. It begins with introductions to dissolution testing, including its history and importance. It then covers development of dissolution methods, including characterizing drug substances and formulations, classifying drugs based on solubility and permeability, and selecting test conditions like apparatus, medium, agitation, and time points. The document discusses compendial and regulatory expectations for dissolution testing as well as validating dissolution methods.
The document discusses various quality control tests that are performed on tablets during manufacturing, including tests for general appearance, hardness, friability, weight variation, content uniformity, disintegration and dissolution. It provides details on procedures and limits for these tests according to pharmacopoeial standards like the British Pharmacopoeia, Indian Pharmacopoeia and United States Pharmacopoeia. The tests are important to ensure tablets meet requirements for reproducibility, stability and accurate dosing of the active drug.
This document discusses tablet tooling and the tablet compression process. It describes the main types of tablet tooling, including 'B', 'D', 'BB', and 'DB' tooling, and provides their dimensions and specifications. It also outlines the basic components of a tablet press, including the hopper, dies, punches, cam tracks, and feeding mechanism. Finally, it explains the three main steps of the tablet compression process: filling and dosing the dies, compressing the tablets, and ejecting and exiting the tablets from the press.
This document discusses various types of solid dosage forms, with a focus on tablets and capsules. Tablets can be film coated, enteric coated, effervescent, sublingual, buccal, troches, chewable, or modified/slow release. Capsules can be hard or soft shell and contain solids or oils. Powders can be simplex, complex, indivisi or divisi. The document provides examples and describes how to write prescriptions for different solid dosage forms.
This document discusses common tablet processing problems and their remedies. It describes visual defects like capping, lamination, cracking, chipping, sticking, picking, and binding that can occur during tablet manufacturing. The causes of each defect are explained in terms of formulation issues like moisture content, binder amount, granule size, and machine issues like die wear, concavity, and speed. Solutions provided include optimizing the formulation through proper drying, lubrication, and binder selection, as well as adjusting machine settings like tapered dies, lubricated punches, and reduced speed or pressure. Overall, the document aims to help industrial pharmacists address problems in tablet manufacturing.
The document discusses sterile formulations and parenteral products. It covers key topics like routes of parenteral administration, pre-formulation of sterile products, physicochemical properties, general requirements, and sterility testing. The different routes discussed are subcutaneous, intramuscular, intravenous, and others. Ideal properties of sterile dosage forms include sterility, isotonicity, being pyrogen-free and particle-free. The document also differentiates between small volume parenterals and large volume parenterals.
1. The document discusses quality control tests for tablets, including tests for tablet characteristics before and after compression. It describes tests for properties like hardness, friability, thickness, weight variation, drug content uniformity, and dissolution.
2. Official tests discussed include weight variation, disintegration, dissolution, and drug content/assay. Non-official tests include hardness and friability. Test conditions and acceptance criteria are provided for many of the tests.
3. The purpose of the quality control tests is to ensure tablets include the correct dose of drug, the drug is released in a controlled and reproducible manner, and the tablets have sufficient mechanical strength.
Selection and evaluation of pharmaceutical packaging materials, containers an...NRx Hemant Rathod
This document discusses pharmaceutical packaging materials and their characteristics. It describes the role of packaging in protecting pharmaceuticals and presenting information. The main packaging materials discussed are glass, plastic, metal, and paper. The ideal requirements for containers include being neutral and protecting the product from various environmental factors. Common container types include well-closed, single dose, and multi dose containers. The document also examines closures and their role in preventing contamination or loss of materials. Closures discussed include screw caps, lug caps and pilfer proof closures. The characteristics and uses of different packaging materials are summarized.
IPQC Tests for capsules As per IP, BP & USPPramod Ramane
IPQC- In Process Quality Control Tests for Capsules are
1. Uniformity Of Content
2. Disintigration Test
3. Weight Variation Test
4. Dissolution Test
The tests are with Acceptance limits/Criteria as per Indian Pharmacopoeia (IP), British Pharmacopoeia (BP) & United States Pharmacopoeia (USP)
This document discusses important considerations for dosage form design and pharmaceutical formulation. It covers topics like pharmaceutics, drug substance characteristics, excipient selection and functions, preformulation studies, stability testing, and packaging. Preformulation studies help determine appropriate dosage forms and ensure drug stability. Stability is enhanced by protecting drugs from moisture, oxygen, light and other degradation factors through packaging and formulation choices. Proper dosage form design and formulation are essential for producing effective and safe drug products.
This lecture discusses pharmaceutical powders. It begins by defining a pharmaceutical powder as a solid dosage form containing finely divided drugs or chemicals meant for internal or external use. Powders permit drugs to be reduced to a very fine state, enhancing dissolution rate, absorption, and masking unpleasant tastes. The lecture then covers various types of powders including divided powders for internal use (simple, compound, cachet-enclosed), bulk powders (antacids, laxatives), and powders for external use. Methods for reducing particle size like trituration, pulverization, and levigation are also summarized.
This document summarizes the standards and testing methods for different types of tablets according to the Indian Pharmacopoeia. It describes 10 types of tablets and the standards that apply to all tablets, including content uniformity, weight variation, disintegration, friability, and dissolution testing. The document provides details on the acceptance criteria and testing procedures for each of these standards.
This document provides information about pharmacy internship programs and pharmaceutical dosage forms. It describes minor and major internships in community pharmacy, hospital pharmacy, and manufacturing pharmacy. It also outlines the specific objectives of community pharmacy internships. The document then discusses various pharmaceutical dosage forms including liquids, emulsions, suspensions, gels, and oral solid dosage forms like tablets and capsules. It provides examples of different dosage forms.
The document describes the process and key components of a tablet compression machine. The machine uses punches and dies to compress powder or granules into tablets. It has several stations that rotate to precisely fill the dies, compress the powder under high pressure, and eject the finished tablets. The main stages are filling the die cavity, adjusting the powder weight, compressing the powder between the punches, and ejecting the tablet. Critical parts include the hopper, feeder system, punches, dies, turret, cam tracks, and rollers which work together to automate tablet production.
This document provides information about various topical dermatological preparations including ointments, creams, gels, pastes, plasters, and others. It discusses the composition, properties, applications, and manufacturing of these preparations. Ointments are semisolid preparations intended for external application with an oily base that forms a protective, moisturizing layer on the skin. Creams are emulsions that are soft, smooth, and spreadable. Gels consist of a gelling agent suspended in water that forms a semirigid system. The document outlines the different types of bases used and key factors in selecting the appropriate base. It also reviews the production and quality control of these topical preparations.
This document discusses common manufacturing defects that can occur during tablet production such as picking and sticking, capping and lamination, mottling, double impression, poor mixing, poor flow, weight variation, and hardness variation. For each defect, the document provides the reason for why the defect occurs and recommendations for how to correct the issue, such as using properly designed punches, adequate drying, uniform granule size distribution, and controlling punch movement. The overall goal of the document is to outline typical tablet defects, their causes, and methods for prevention.
Superdisintegrants in Orally Administered Products of Pharmaceuticals A Reviewijtsrd
This document reviews superdisintegrants, which are added to pharmaceutical products to improve palatability and the performance of solid oral dosage forms. Superdisintegrants work by reducing the disintegration time of tablets, which improves drug dissolution rate. The review discusses various types of natural, synthetic, and semi-synthetic superdisintegrants. It also examines the mechanisms by which superdisintegrants cause rapid tablet disintegration, such as swelling, porosity, deformation, and particle repulsion. The ideal properties of superdisintegrants and their methods of incorporation into tablets are described. The document concludes that superdisintegrants can help advance the development of orally administered pharmaceutical products by improving acceptability and potency.
This document provides information about semi-solid dosage forms including ointments. It defines semi-solid dosage forms as products of semi-solid consistency applied to the skin or mucous membranes. Ointments are described as viscous semisolids used topically containing a drug and a base. Various types of bases are discussed including oleaginous, absorption, emulsion and water-soluble bases. Properties, examples and uses of different bases are provided. Other topics covered include ideal properties of semi-solid dosage forms, drug permeability through skin, and formulation ingredients like antimicrobial preservatives.
The most common method of drug delivery is oral dosage
form of which tablet and capsule are predominant.
Tablet is more accepted as compared to capsule due to
many reason such as cost, tamper resistance, ease of
handling, ease of identification and manufacturing efficiency.
Tablet compression process understanding is resulted in
development of formulation.
Recent advances in the design of tablet compression
equipment has conducted resulted in higher efficiency,
minimized tablet variation, greater flexibility.
This document discusses key considerations for dosage form design and formulation. It outlines the need to consider the physical and chemical properties of drug substances and ensure compatibility between ingredients. Preformulation studies are important to characterize drug properties like solubility, dissolution rate, and stability. These studies help determine the appropriate dosage form and ensure the drug is delivered effectively and safely. The goals of a proper design are to provide patient benefit while protecting drug integrity throughout production, storage, and use.
This document discusses dissolution testing techniques used in the pharmaceutical industry. It begins with introductions to dissolution testing, including its history and importance. It then covers development of dissolution methods, including characterizing drug substances and formulations, classifying drugs based on solubility and permeability, and selecting test conditions like apparatus, medium, agitation, and time points. The document discusses compendial and regulatory expectations for dissolution testing as well as validating dissolution methods.
This document discusses key aspects of preformulation and formulation development. It begins with definitions of important terms like drug, dosage form, dose, and bioavailability. It then describes the basic preformulation studies conducted like solubility, pH, and stability testing. The document outlines the main components of a dosage form including active drug and excipients. It provides examples of various dosage forms like tablets, capsules, liquids, semisolids, and inhalations. Finally, it stresses the importance of following formulation development steps to create an efficient dosage form that is safe, effective and has minimal toxicity.
Biopharmaceutics is the study of physicochemical properties of drugs and how they influence the drug's bioavailability. Key factors that can impact bioavailability include the drug's solubility, dissolution rate, and permeability. For an orally administered drug, the drug must first dissolve in the gastrointestinal fluids before it can be absorbed through the gastrointestinal membranes and enter systemic circulation. The rate of dissolution is often the slowest step and thus rate-limiting for poorly water soluble drugs. Techniques such as reducing particle size, use of salt forms, and amorphous forms can increase dissolution rate and bioavailability.
The document discusses drug product performance evaluation through in vitro dissolution testing. It provides details on factors that influence drug dissolution like drug substance properties, formulation composition, manufacturing process, and dissolution test conditions. The key goals of in vitro drug product testing are to characterize drug potency and release rate from oral dosage forms, provide information for formulation development, and ensure quality, comparability and stability over time. Common tests include disintegration testing and dissolution testing using apparatus specified in pharmacopeias to simulate gastrointestinal conditions. The results of in vitro testing aid product development and assessment of shelf-life and quality.
2.Sagar Goda Biological classification system (BCS); its significance on diss...Sagar Goda
This presentation provides a detailed information about Biopharmaceutics classification system(BCS) and its significance on dissolution study as well as its application in dosage form development.
This document discusses key concepts in preformulation testing. It begins by defining preformulation as investigating the physical and chemical properties of a drug substance alone and combined with excipients. The overall goal is to generate information useful for developing stable and safe dosage forms.
It then outlines some of the main steps in preformation process including assessing organoleptic properties, purity, particle size, melting point, stability, excipient compatibility, solubility, polymorphism, pH and salt formation. Specific tests are mentioned for many of these areas.
The document emphasizes that preformulation is important for aiding drug candidate selection, product design, decreasing time to market, and ensuring overall safety and efficacy of the final product
1. Biopharmaceutics encompasses the relationship between physical, chemical and biological properties of drugs and drug products and their effects on the body.
2. Key considerations in biopharmaceutics include drug formulation, dosage form, route of administration, and physico-chemical properties which influence drug bioavailability.
3. The goal of biopharmaceutics is to optimize drug delivery and therapeutic effects through rational design of drug products based on an understanding of biopharmaceutic principles.
This document provides an overview of pharmacology and pharmaceutical dosage forms. It discusses the scope and objectives of understanding how pharmaceutical additives and dosage forms influence drug performance. The objectives are to understand various dosage forms and manufacturing techniques, considerations in dosage form development, and how to formulate and evaluate solid, liquid and semisolid dosage forms. It also discusses basic pharmacology concepts like how drugs work, are absorbed and distributed in the body, and the objective of drug therapy to deliver drugs to the right site of action. Preformulation studies are introduced, which involve characterizing the physical and chemical properties of drug substances and understanding how these properties impact dosage form development and stability.
Formulation development of pharmaceutical drugSriramPraveen5
The document discusses the importance of formulation development in the pharmaceutical industry. It outlines key steps in the formulation development process, including excipient compatibility studies, formulation optimization, evaluation, and stability testing. Proper formulation is crucial for ensuring patient safety and therapeutic efficacy. The summary discusses formulation development as a critical aspect of drug discovery that can enhance patient outcomes through improved drug delivery and compliance.
1. Biopharmaceutics encompasses the relationship between physical, chemical and biological properties of drugs and dosage forms and their effects on the body.
2. Key considerations in biopharmaceutics include drug properties like particle size and polymorphism, dosage form properties like coating and excipients, and route of administration.
3. Together these factors determine important metrics like bioavailability, therapeutic efficacy and dosing requirements. Understanding biopharmaceutics allows rational drug product design.
Biopharmaceutic considerations in drug product designMOHAMMAD ASIM
Biopharmaceutics considerations in drug product design include pharmacodynamic factors like the therapeutic objective and desired effects, drug properties such as solubility and polymorphism, drug product attributes regarding bioavailability and dosing, patient factors like acceptability and compliance, and manufacturing issues. Key drug properties evaluated are particle size, solubility-pH profile, stability-pH profile, and polymorphism which influence drug release and absorption. The desired dose, dosing frequency, and administration route are based on pharmacokinetic profiles and the drug's half-life. Patient acceptability, costs, and conditions are also weighed. Manufacturability, quality control, stability, and raw material availability are manufacturing priorities.
This document discusses the importance of preformulation studies in designing sustained release dosage forms. Preformulation studies provide important information about the drug substance including solubility, pH effects, partitioning, stability and compatibility with excipients. This information guides the selection of appropriate formulation components, manufacturing processes and container closure systems. Key preformulation tests described include determining intrinsic solubility, dissociation constant (pKa), partition coefficient, crystal properties, and dissolution rate. The results of preformulation studies help develop stable, bioavailable sustained release dosage forms that can be mass produced.
This document discusses the importance of preformulation studies in designing sustained release dosage forms. Preformulation studies provide important information about the drug substance that can be used to develop stable and bioavailable sustained release formulations. Key aspects of preformulation include determining solubility, pKa, partition coefficient, crystal properties, and compatibility with excipients. This information helps select appropriate formulation components, manufacturing processes, container closure systems and more. The overall goal of preformulation is to generate data to support the development of sustained release dosage forms that can be mass produced and provide a prolonged therapeutic effect.
This document discusses prodrug design. It defines prodrugs as pharmacologically inert derivatives that can be converted in vivo to the active drug molecule. The goals of prodrug design are to overcome undesirable drug properties related to absorption, distribution, metabolism and toxicity. Examples are given of prodrugs that increase oral absorption or provide targeted delivery to tumors. Prodrugs are evaluated based on their physicochemical properties and pharmacokinetic profile to ensure they are converted to the active drug molecule.
Preformulation is a group of studies that focus on the physicochemical properties of a new drug candidate that could affect the drug performance and the development of a dosage form. ... This property provides the framework for drugs combination with pharmaceutical ingredients in the fabrication of dosage form.
The document discusses guidelines for stability testing of pharmaceutical products. It defines stability testing as evaluating how environmental factors affect a drug substance or product's properties over time. This helps determine shelf life, proper storage conditions, and labeling instructions. Stability testing evaluates many factors like active ingredient stability, excipient interactions, manufacturing process, dosage form, and storage conditions. It also considers degradation reactions and how they are impacted by conditions. Stability testing parameters and timepoints are described for various dosage forms like tablets, capsules, solutions, injections etc. The document also discusses ICH guidelines for stability testing and recommendations for climatic zones III and IV.
preformulation studies by SeDeM expert system toolNagabhushanShet4
PREFORMULATION STUDIES OF TABLETS
IT ALSO INCLUDES SEDEM STUDIES WHICH IS BASED ON THE QBD DESCRIBED ICH Q 8 .
IN THIS STUDIES CANNABIDIOL IS CONSIDERED AND IT IS BCS CLASS 2 HENCE DISSOLUTION WAS CHALLENGING IN THEM SO IN THE ABOVE STUDIES THEY CAME UP WITH THE IDEA OF AN ORODISPERSIBLE TABLET OF CANNABIDIOL.
THE ABOVE CASE STDUY IS TAKEN FROM SAUDI JOURNAL OF PHARMACEUTICS AND HAS A IMPACT FACTOR OF 4.66.
THE CREDITS OF CASE STUDIES GO TO THE RESPECTIVE RESEARCH SCIENTIST.
This document outlines the syllabus for the final year B. Pharm course at Dr. Babasaheb Ambedkar Marathwada University in Aurangabad, India. It includes 7 subjects in the theory portion, totaling 21 hours per week. The practical portion totals 15 hours per week.
One of the subjects covered is Dosage Form Design, which focuses on topics like preformulation, solubility, stability, package development, sustained release drug delivery systems, scale up techniques, optimization, and dosage form design. The practical portion involves experiments related to stability testing, micromeritics, solubility analysis, and preparation/evaluation of various drug delivery systems.
It is a small presentation about the preformulation studies, which help students in their exams.
Preformulation is a crucial stage in pharmaceutical research and development that encompasses a series of scientific studies and experiments conducted before the formulation of a drug product begins. Its primary purpose is to gather essential information and data about the physical, chemical, and biopharmaceutical properties of a drug substance or active pharmaceutical ingredient (API).
Understanding the Drug Substance:
Preformulation starts with a comprehensive characterization of the drug substance. This includes identifying its chemical structure, molecular weight, and purity. Various analytical techniques are employed for this purpose, such as nuclear magnetic resonance (NMR) spectroscopy, mass spectrometry (MS), and high-performance liquid chromatography (HPLC).
2. Assessing Physicochemical Properties:
Preformulation studies delve into the physicochemical properties of the drug substance. Researchers investigate properties such as solubility, melting point, crystallinity, hygroscopicity, and polymorphism. These properties can profoundly affect formulation design and stability.
This document provides an overview of common instrumental analytical techniques used in chromatography and spectroscopy. It describes various chromatographic techniques including thin layer chromatography, column chromatography, gas chromatography, and high performance liquid chromatography. It also outlines several spectroscopic techniques such as atomic absorption spectroscopy, colorimetry, and UV-visible spectroscopy. The document explains the basic principles, components, and applications of these analytical methods for separating and analyzing mixtures.
The document discusses Investigational New Drug Applications (INDs), which are required for clinical trials of new drugs. It outlines the key components of an IND, including an introductory statement, investigator's brochure, protocols, chemistry/manufacturing information, and previous human experience. It also describes IND amendments, annual reports, and the roles of the sponsor and investigator. The overall purpose of an IND is to provide information to the FDA on a new drug's safety before it can be tested in humans.
Fractional factorial designs (FFDs) are used to efficiently study many factors using fewer experimental runs than a full factorial design. FFDs exploit redundancy in estimating interactions to select a subset of runs. Regular FFDs have desirable properties like balance and orthogonality. Resolution indicates how interactions are aliased, with higher resolutions preferred. FFDs are useful in screening experiments to identify important factors efficiently before further optimization. Software helps select appropriate FFDs based on desired resolution and aliasing.
This document discusses herbal medicines and their use in the pharmaceutical industry. It provides information on patient use of herbal remedies, why herbal products are in demand, approaches to developing herbal formulations, standardizing herbs, guidelines for using herbs safely, and interacting with other medications. The document addresses issues like herbal products not being well-tested, lacking quality control, and having imprecise potency, while also noting two sides to herbs in terms of benefits and risks.
Herbal medicine involves the use of whole plants to promote health and treat disease, drawing on a tradition of human use for over 60,000 years. It views disease more broadly by addressing underlying causes and individual expression rather than just symptoms. Herbal medicines are prescribed to restore homeostasis and promote optimal cellular nutrition and elimination. Around 1 in 5 people in the UK regularly use herbal medicine, and it is regulated through organizations like the National Institute of Medical Herbalists. Herbal medicines are prescribed individually based on a comprehensive medical history and clinical examination.
The document discusses Investigational New Drug Applications (INDs), which are required for clinical testing of new drugs. It describes the key components of an IND including an introductory statement, investigator's brochure, protocols, chemistry and manufacturing information, and annual reports. It also defines important terms like sponsor and investigator and outlines the regulatory requirements for INDs.
This document provides an introduction to water systems for pharmaceutical use. It discusses the importance of water quality for pharmaceutical processes and products. It outlines various water types like purified water, highly purified water, and water for injections. It emphasizes that water systems must be properly designed, installed, operated and maintained according to GMP to ensure consistent production of water meeting quality specifications. It also discusses common water contaminants and the need to monitor water sources and treat water appropriately based on its chemistry and contaminants.
Good Manufacturing Practices (GMPs) establish minimum standards for methods, facilities, and controls used in manufacturing drugs to ensure they are safe, have the appropriate identity and strength, and meet quality and purity standards. GMP violations can result in severe consequences for drug manufacturers such as product seizures, recalls, shutdown of facilities, and large financial penalties. Current trends in GMPs include a risk-based approach, international harmonization of quality standards, and proposed amendments regarding validation and cross-contamination prevention.
GMP (good manufacturing practices) and cGMP (current good manufacturing practices) are quality standards for the manufacture of pharmaceutical products and medical devices. They help ensure that products are consistently produced and controlled according to quality standards for safety and efficacy. Key aspects of GMP include establishing processes and procedures for production, cleaning, maintenance, personnel training, and quality testing of products. Following GMP guidelines helps manufacturers produce pharmaceuticals that meet the necessary quality standards.
The document discusses the FDA's Inactive Ingredient Guide (IIG), which lists inactive ingredients that are present in approved drug products. It provides information on obtaining the IIG and describes the contents and purpose of the guide. The IIG is intended to help identify inactive ingredients that may require less extensive review if they are already present in approved drug products for a particular route of administration. It lists ingredients alphabetically and provides information like routes of administration, CAS numbers, number of NDAs, and potency ranges.
The document discusses Drug Master Files (DMFs), which provide confidential detailed information to the FDA in support of applications. It defines 5 types of DMFs and outlines their typical contents. These include manufacturing processes and facilities, active pharmaceutical ingredients, packaging materials, excipients, and reference information. The summary provides guidelines on submitting DMFs, required content for each type, quality controls, stability testing, and the FDA review process. Holders must adhere to good manufacturing practices and be willing to allow inspections.
This document outlines the history of drug development and approval processes in the United States from 1820 to 1997. It describes key milestones and legislation that established regulations for new drug applications (NDAs). NDAs were first required in 1938 to show drug safety, and in 1962 were amended to require proof of efficacy. The FDA now reviews NDAs to ensure the benefits of new drugs outweigh the risks based on clinical trial data.
The EMEA (European Medicines Agency) is a decentralized body of the European Union headquartered in London. It was established in 1995 and coordinates the evaluation and supervision of medicines for human and veterinary use throughout the EU. It is composed of various committees including the CHMP (Committee for Medicinal Products for Human Use) and CVMP (Committee for Medicinal Products for Veterinary Use) which are responsible for assessment and authorization of medicines. The EMEA ensures that medicines are evaluated based on quality, safety and efficacy with the goal of protecting public health.
This document defines various microbiology terms related to sterilization and disinfection. It discusses sterilization techniques like heat, filtration, and radiation. It also covers chemical disinfectants including phenols, bisphenols, biguanides, halogens, and chlorine. Physical methods like heat, filtration, refrigeration, and radiation can kill microbes. Chemical disinfectants have varying mechanisms of action, with phenols and halogens damaging cell membranes and bisphenols inhibiting fatty acid synthesis. Proper evaluation of disinfectant efficacy involves tests against standard microbes.
This document provides an overview of computer validation and compliance with regulatory guidance. It discusses the need for computer validation and outlines key principles from guidance documents such as software validation, use of off-the-shelf software in medical devices, and validation of electronic records and signatures. Validation approaches for different systems and software are covered, including spreadsheets. The document provides references to FDA and international regulatory guidance on these topics.
This document discusses designing around patents from the perspectives of both patent holders and competitors. It notes that patent holders seek broad patent protection to maximize monopoly profits and minimize successful design around efforts, while competitors aim to create non-infringing alternative products without bearing the monopoly costs of the patent. The document outlines strategies for patent holders to draft claims to make designing around more difficult and for competitors to develop design around approaches in light of legal precedents like Festo v. Shoketsu, which impacted the doctrine of equivalents.
Clinical trials are conducted in phases to evaluate the safety and efficacy of new drugs. Phase 1 trials involve 10-20 healthy volunteers to determine toxicity and pharmacokinetics. Phase 2 trials involve 100-200 patients to identify effective doses and further evaluate safety. Phase 3 trials involve up to 1000 volunteers to study less common side effects, compare to standard treatments, and evaluate long-term safety and effectiveness. Phase 4 trials monitor drugs after approval in 5000-10,000 patients to identify rare or long-term issues.
Clinical trials progress through phases (preclinical, I-IV) to evaluate treatments safely in humans. Preclinical testing occurs in labs and animals. Phase I studies evaluate safety in 20-80 healthy volunteers. Phase II expands to 100-300 patient volunteers to assess efficacy. Phase III further tests efficacy in 1,000-3,000 patients. FDA approval requires compliance with Good Clinical Practice guidelines to protect subject rights and ensure credible data. Key elements include oversight by independent review boards, informed consent, qualified investigators and sponsors, adherence to protocols, and comprehensive record keeping.
Clinical research in India is growing rapidly due to several factors:
- India has a large population with a growing disease burden similar to developed countries. This provides opportunities for clinical trial recruitment.
- Regulatory reforms have made the approval process for clinical trials much faster, within 6-8 weeks for some applications.
- Costs for conducting clinical trials are around half of Western countries, providing significant cost savings for sponsors.
- There is an increasing pool of experienced investigators and staff familiar with Good Clinical Practice who can conduct trials to international standards.
- The pharmaceutical industry and contract research organizations see India as an important location for outsourcing various stages of drug development to take advantage of the opportunities.
The Center for Drug Evaluation and Research (CDER) is responsible for regulating prescription and over-the-counter drugs. CDER oversees new drug development and approval, drug safety, and drug advertising and promotion. It reviews New Drug Applications, monitors drug safety after approval, develops regulations and guidance, and communicates with industry and the public about drugs and drug development.
Main Java[All of the Base Concepts}.docxadhitya5119
This is part 1 of my Java Learning Journey. This Contains Custom methods, classes, constructors, packages, multithreading , try- catch block, finally block and more.
Macroeconomics- Movie Location
This will be used as part of your Personal Professional Portfolio once graded.
Objective:
Prepare a presentation or a paper using research, basic comparative analysis, data organization and application of economic information. You will make an informed assessment of an economic climate outside of the United States to accomplish an entertainment industry objective.
This presentation includes basic of PCOS their pathology and treatment and also Ayurveda correlation of PCOS and Ayurvedic line of treatment mentioned in classics.
Introduction to AI for Nonprofits with Tapp NetworkTechSoup
Dive into the world of AI! Experts Jon Hill and Tareq Monaur will guide you through AI's role in enhancing nonprofit websites and basic marketing strategies, making it easy to understand and apply.
A Strategic Approach: GenAI in EducationPeter Windle
Artificial Intelligence (AI) technologies such as Generative AI, Image Generators and Large Language Models have had a dramatic impact on teaching, learning and assessment over the past 18 months. The most immediate threat AI posed was to Academic Integrity with Higher Education Institutes (HEIs) focusing their efforts on combating the use of GenAI in assessment. Guidelines were developed for staff and students, policies put in place too. Innovative educators have forged paths in the use of Generative AI for teaching, learning and assessments leading to pockets of transformation springing up across HEIs, often with little or no top-down guidance, support or direction.
This Gasta posits a strategic approach to integrating AI into HEIs to prepare staff, students and the curriculum for an evolving world and workplace. We will highlight the advantages of working with these technologies beyond the realm of teaching, learning and assessment by considering prompt engineering skills, industry impact, curriculum changes, and the need for staff upskilling. In contrast, not engaging strategically with Generative AI poses risks, including falling behind peers, missed opportunities and failing to ensure our graduates remain employable. The rapid evolution of AI technologies necessitates a proactive and strategic approach if we are to remain relevant.
How to Fix the Import Error in the Odoo 17Celine George
An import error occurs when a program fails to import a module or library, disrupting its execution. In languages like Python, this issue arises when the specified module cannot be found or accessed, hindering the program's functionality. Resolving import errors is crucial for maintaining smooth software operation and uninterrupted development processes.
How to Add Chatter in the odoo 17 ERP ModuleCeline George
In Odoo, the chatter is like a chat tool that helps you work together on records. You can leave notes and track things, making it easier to talk with your team and partners. Inside chatter, all communication history, activity, and changes will be displayed.
1. Dosage Form Design: Pharmaceutical
and Formulation Considerations
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2. Dosage Form Design
Pharmaceutics
- study on the: formulation, manufacture, stability,
and effectiveness of pharmaceutical dosage forms
Pharmaceutical ingredients or excipients
-Selective use of these non medicinal agents
- Uses
solubilize thicken stabilize flavor
suspend dilute preserve efficacious
suspend emulsify color appealing closure forms.
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3. Requirements of a proper design & formulation
of dosage form
Consideration of drug substances:
Physical, chemical & biological characteristics
*compatible with one another - stable, efficacious, attractive,
easy to administer & safe
*manufactured under appropriate measures of quality control
& packaged in containers to make product stable
*labeled to promote correct use & stored under conditions to
maximize shell life
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4. The Need for Dosage Forms
To protect the drug substance from the destructive
influences of atmospheric oxygen or humidity.
(Coated tablets)
To protect the drug substance from the destructive
influence of gastric acid after oral administration.
(Enteric-coated)
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5. The Need for Dosage Forms
To conceal the bitter, salty or offensive taste or odor
of a drug substance. (Capsules, Flavored
syrups)
To provide liquid preparations of substances that are
either insoluble or unstable in the desired vehicle.
(Suspension
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6. The Need for Dosage Forms
To provide clear liquid dosage forms of substances.
(Syrups, Solutions)
To provide rate-controlled drug action. (Controlled-
release tablets)
To provide optimal drug action from topical
administration sites. (Ointments,Creams,
Transdermal patches)
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7. The Need for Dosage Forms
To provide for insertion of a drug into one of the body’s
orifices (Suppositories)
To provide placement of drugs directly in the
bloodstream or body tissues (Injections)
To provide for optimal drug action through inhalation
therapy (Inhalants, Inhalation aerosols)
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8. General Considerations in Dosage Form Design
Determine desired product type - framework for
product development.
develop and examine initial formulations of the
product:
- desired features: drug release profile bioavailability
clinical effectiveness
- pilot plant studies and production scale-up.
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9. master formula
- formulation that best meets the goals of the
product
Factors to consider before formulation of a
medicinal agent in one or more dosage forms
Therapeutic matters (nature of the illness)
manner it is treated (locally or through systemic
action)
age and anticipated condition of the patient.
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10. Preformulation Studies
drug be chemically and physically characterized
define the nature of the drug substance.
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11. Three ways liquid drug be given in solid form
Liquid substance:
Sealed in soft gelatin capsule
Developed into a solid ester or salt form suitable for
tablets or drug capsules
Mixed with a solid or melted semisolid material
- melted mixtrue is poured into hard gelatin capsules
to harden & capsules sealed
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12. Preformulation Studies
1. Physical Description
- physical description particle size
crystalline structure melting point solubility.
Chemical properties: structure form
reactivity
- purity of the chemical substance for:
identification and for evaluation of its
chemical, physical, and biologic properties
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13. Preformulation Studies
2. Microscopic Examination
indication of: particle size and size range of the
raw material along with the crystal structure.
information in formulation processing
attributable to changes in particle or crystal
characteristics of the drug.
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14. Preformulation Studies
3. Melting Point Depression
Determines the: purity of the substance
compatibility of various subs before
inclusion in the dosage form
- pure subs: sharp melting point
- impure subs: depressed melting point
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15. Preformulation Studies
4. Phase Rule
Phase diagrams constructed determines:
- existence & extent of the presence of solid and liquid
phases in binary, ternary & other mixtures
Particle Size
- affects : physical–chemical properties of drug subs’s:
*dissolution rate bioavailability content uniformity
stability taste texture
flow properties absorption sedimentation rate
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16. Preformulation Studies Polymorphism
- substances can exist in more than one crystalline form
Polymorphic forms – diff. physical-chemical
properties (incl. melting pt. & solubility)
Evaluation of:
*crystal structure (microscopy,
IR spectroscopy, thermal analysis, x-ray
diffraction)
*polymorphism & *solvate form
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17. Preformulation Studies
Solubility
Determined by equlibrium solubility method
- excess amount of drug + solvent = shaken at constant
temp. over a prolonged period of time until equilibrium is
obtained
Drug possess aqueous solubility - for therapeutic
efficacy.
Insoluble compounds: incomplete/erratic absorption
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18. Solubility & particle size
Solubility & pH
- drug formulated to liquid product:
adjustment of pH of solvent where drug is dissolved
to adjust solubility
- Weak acidic or basic drugs - require extremes in
pH outside or accepted physiologic limits or that
may cause stability problems with formulation
ingredients.
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19. Preformulation Studies
Dissolution Rate
time for the drug to dissolve in the fluids at the
absorption site (rate-limiting step in absorption).
Dissolution rate of drugs - increased by decreasing
the particle size.
for higher dissolution rate
- use a highly water soluble salt of the parent
substance.
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20. 2 methods in determining dissolution rates
of chemical compounds
1.Constant surface method
- intrinsic dissolution rate of the agent
- Characteristic of compound & solvent under fixed
experimental conditions
- mg dissolved/min/cm square
2.Particulate dissolution
- Weighed amount of powdered sample +
dissolution medium in constant agitation system
- to study the influence of particle size, surface area,
and excipients upon the active agent
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21. Fick’s law (law of diffusion)
- describes the:
* relationship of diffusion & dissolution of the active
drug in the dosage form & when administered in the
body
- 1st
law
*relates to a steady state flow
- 2nd
law
*relates to a change in conc. of drug with time, at any
distance, or a nonsteady state of flow
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22. Preformulation Studies
Membrane Permeability
Everted intestinal sac
- determines degree & rate of passage of drug through the
membrane sac by passive & active transport
early assessment of passage of drug molecules across
biologic membranes
To produce a biologic response - drug molecule must first
cross a biologic membrane
The biologic membrane (lipid barrier) - permits
absorption of lipid soluble substance by passive diffusion
Molecules’ lipophilic character – measured by the oil-
water coefficient
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23. Basis of pH-partition coefficient
Interrelationship at the absorption site & absorption
characteristics of various drugs:
Dissociation constant
lipid solubility
pH
Indication of absorption expectations:
Data from basic physicochemical studies: pKa, solubility &
dissolution rate
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25. Preformulation Studies
pKa / Dissociation Constants
extent of ionization of drug - strong effect on
formulation & pharmacokinetic parameters of the
drug
determined by potentiometric titration
- for the pharmacist important:
*predicting precipitation in admixtures
*calculating solubility of drugs at certain pH values
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26. Stability
-extent a product retains within specified
limits and through its period of storage and use
Stability studies conducted in the
preformulation phase:
Solid-state of the drug alone
Solution phase
with the expected excipients
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27. Drug and Drug Product Stability
Evaluation of:
- physical and chemical stability of pure drug
substances -important for preformulation.
Drug Stability : Mechanisms of Degradation
-Chemically drug substances with different susceptibilities
toward chemical instability:
alcohols, phenols, aldehydes, ketones, esters, ethers, acids,
salts, alkaloids, glycosides and others.
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28. most frequently encountered destructive
process:
Hydrolysis (solvolysis process)
- (drug) molecules interact with water molecule to
yield breakdown product.
- susceptible to the hydrolytic process: esters,
substituted amides, lactones, and lactams
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29. most frequently encountered destructive
process:
OXIDATION
- loss of electrons from an atom or molecule;
- involves free radicals (molecules or atoms
containing one or more unpaired electrons).
- destructive to: aldehydes, alcohols, phenols,
sugars, alkaloids & unsaturated fats & oils
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30. Drug and Drug Product Stability:
A. Kinetics and Shelf Life
Five types of stability
1. Chemical –active ingredient retains chemical integrity
and labeled potency within the specified limits.
- important for selecting:
*storage conditions (temp., light, humidity)
*proper container for dispensing
*anticipating interactions when mixing drugs & dosage
forms
- must know reaction order & rate
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31. 2. Physical - original physical properties, appearance,
palatability, uniformity, dissolution and
suspendability are retained.
3. Microbiologic –sterility/resistance to
microbial growth
4. Therapeutic –therapeutic effect remains
unchanged
5. Toxicologic - no significant increase in
toxicity occurs.
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32. Drug and Drug Product Stability:
B. RATE REACTIONS
- description of the drug concentration with
respect to time.
C. Q10 METHOD
- estimate the shelf life of a product that has
been stored or to be stored under a different set of
conditions.
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33. ENHANCING STABILITY
drugs subjected to hydrolysis
*water reduced or eliminated from the system.
*water-liable drugs - waterproof protective coating
applied in the tablet.
*in liquid formulation - water replaced by substitute
liquids.
*suspending them in nonaqueous vehicle
*for injectable products – anhydrous vegetable
oils may be used as solvent
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34. ENHANCING STABILITY
For unstable antibiotic drugs (aq. prepn desired)
- supplied in dry form for reconstitution before dispensing
For unstable prepns: storage under refrigeration
pH – major determinant in stability
- optimum stability: pH 5 & 6
- buffering agents increases stability
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35. ENHANCING STABILITY
oxygen sensitive drugs
* prepared in dry state
*packaged in sealed containers with air replaced by
inert gas (Nitrogen, carbon dioxide).
* add antioxidants (for stability):
- in aq. Prepns:
Na2SO3, NaHSO3, H3PO2, ascorbic acid
- in oleaginous/unctous prepns:
alpha tocopherol, butylhydroxyanisole &
ascorbyl parmitate
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36. ENHANCING STABILITY
trace metals in drug, solvent, container or
stopper
- source of difficulty in preparing stable solns
of oxidizable drugs
- eliminated by:
*purification of source of contaminant
*complexing or binding metal by using
specialized agents (chelating agents- Ca
disod edetate & EDTA)
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37. ENHANCING STABILITY
Light
- catalyst to oxidation reactions
- prepns packaged in light resistant or opaque
containers
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38. In summary : easily oxidizable drugsmay
be stabilized in formulation by:selective exclusion from the system of:
oxygen oxidizing agents trace metals
light heat other chemical
catalysis
add to create and maintain a favorable pH:
antioxidants chelating agents
buffering agents
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39. Other destructive process in pharmaceutical
preparations
Polymerization
- reaction between two or more identical molecules with
resultant formation of new & generally larger molecule
(formaldhyde)
Process where one or more active chemical groups removed:
Chemical decarboxylation
deamination
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40. Decarboxylation
- decomposition of RCOOH & release of CO2
Deamination
- removal of nitrogen containing group from organic
amine (ex. Insulin)
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41. Importance of Drug Stability
in preclin. testing and in clinical (human) trials
- for a true and accurate assessment of the
drug/drug prod evaluated
marketed drug product
- for the safety and effectiveness when distributed
and during the entire course of its shelf-life and use
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42. Product stability assessed before marketing:
Formulation
Influence of:
- pharmaceutic ingredients present
- container & closure
Manufacturing & processing conditions
Packaging components & conditions of
warehousing/storage
Conditions of shipping, temp., light & humidity
Shelf life & patient utilization
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43. stability testing considerations
product containers, closures, and other packaging
features
parenteral and other sterile prods must meet sterility
test stds
- to ensure protection against microbial
contamination
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44. Drug instability detected
Change in:
physical appearance, color, odor, taste or texture of
the formulation
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45. Scientific data pertaining to the stability of
a formulationleads to:
*prediction of the expected shelf-life of the
proposed product
*redesign of the drug (to more stable salt or
ester form)
*reformulation of the dosage form.
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46. Accelerated stability testing
Use of exaggerated conditions of temp., humidity, light &
others
accelerated temp
- 6 mons study at 40o
C with 75% relative humidity
Short tem accelerated studies
Determines most stable of the proposed formulations for a
drug product
lesser temp and humidity
- 30o
C and 60% humidity
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47. Stress testing
- temp. elevations in 10o
increments higher than used
in accelerated studies
- employed until chem.. or phy. Degradation
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48. Long term stability studies
product is subjected to different climatic zones
(temp. & humidity)nationally & internationally
predicted from the data generated from continuing
stability studies
12 months minimum and conducted at 25o
C +/- 2o
C
and at a relative humidity of 60% +/- 5%
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49. PACKAGING & STORAGE of
PHARMACEUTICALS
labeling is essential for:
*prod. stability
*efficacious use
CONTAINERS
- stds for packaging of pharmaceuticals by
manufacturers are contained in the CGMP
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50. Tests performed depending on the intended
use and type of container:
physicochem. tests
light-transmission tests for glass or plastic
drug compatibility
leaching and or migration tests,
vapor-transmission test for plastics, moisture barrier tests, toxicity
studies for plastics,
valve, actuator, metered-dose, partical size, spray characteristics, leak
testing for aerosols,
sterility and permeation tests for parenteral containers
drug stability for all packaging
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51. According to USP:
CONTAINER
- holds the article and is or may be in direct contact
with the article
IMMEDIATE CONTAINER
- in direct contact with the article at all times
Closure
- part of the container
Closure & container
- clean and dry prior to its being filled with the drug
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52. CLASSIFICATION OF CONTAINERS BY THE USP according
to their ability to protect their contents from external
conditions:
well-closed container
- protects the contents from extraneous solids and from:
*loss of the article under ordinary conditions of handling, shipment,
storage & distribution
tight container
- protects the contents from contamination by extraneous liqs., solids,
or vapors, from:
* loss of the articles, and from efflorescence, deliquescence, or
evaporation under the ordinary or customary conditions of handling,
shipment, storage and distribution and is capable of tight re-closure
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53. CLASSIFICATION OF CONTAINERS BY THE USP according
to their ability to protect their contents from external
conditions:
hermetic container
- impervious/resistant to air or any other gas under the ordinary or
customary conditions of handling, shipment, storage, and distribution
- those sterile are generally used to hold prepns intended for injection
or parenteral adm
single-dose container
- quantity of drug contained is intended as a single dose and when
opened cannot be resealed with assurance that sterility has been
maintained
- includes fusion-sealed ampules, pre-filled syringes and cartridges
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54. CLASSIFICATION OF CONTAINERS BY THE USP according
to their ability to protect their contents from external
conditions:
single-dose container
- designed to hold a quantity of drug intended for adm as a single dose promptly
after the container is opened
- single-unit package is termed a unit-dose package when dispensed to a
patient
- may be performed on a large scale by a manufacturer or distributor or on a
smaller scale by the pharmacy dispensing the medication
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55. CLASSIFICATION OF CONTAINERS BY THE USP according
to their ability to protect their contents from external
conditions:
multiple-dose container
- hermetic container that permits withdrawal of successive portions of
the contents without changing the strength or endangering the quality
or purity of the remaining portion
- referred as vials
- contain more than a single unit or dose of the medication
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56. Tablets, capsules & oral liquids
- packaged in single-unit or multiple-unit containers
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57. Single-unit packages
convenient & sanitary means of maintaining and utilizing the
medication
advantages:
*positive ID of each dosage unit and reduction of medication
errors
*reduced contamination of the drug due to its protective
wrapping
*reduced dispensing time
*greater ease of inventory control in the pharmacy or nursing
station
*elimination of waste through better medication management
with less discarded medication
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58. Packaging materials
- may be combinations of paper, foil, plastics or
cellophane
Packaging of solid dosage forms in:
*clear plastic or aluminum blister wells
- most popular method of single-unit
packaging
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59. Oral liquids
- may be single-unit dispensed in:
*paper *plastic *foil cups
*pre-packaged and dispensed in glass
containers (with threaded caps or crimped
aluminum caps)
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60. Light resistant containers
required by many pharmaceutical prods to protect them
from photochem. deterioration
amber glass or light resistant opaque plastic will reduce
light transmission sufficiently to protect a light-sensitive
pharmaceutical
UV absorbers may be added to plastic to decrease the
transmission of short UV rays
must meet the USP stds w/c define the acceptable limits of
light transmission at any wavelength of light between 290
and 450 nm
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61. Classification of glass used in packaging pharmaceuticals depending upon
the chem.. constitution of the glass and its ability to resist deterioration:
Type I highly resistant, borosilicate glass
II treated soda-lime glass
III soda-lime glass
NP gen. purpose soda-lime glass
Types I, II & III for parenteral prods
Type NP – for non-parenteral
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62. Newer plastic materials used:
PET – polyethylene terephthalate
amorphous PET (APET)
PET glycol (PETG)
APET & PETG
- excellent transparency, luster and can be sterilized
with gamma radiation
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63. Problems encountered in the use of plastics in
packaging:
permeability of the containers to atmospheric oxygen and
to moisture vapor
leaching of the constituents of the container to the internal
contents
absorption of drugs from the contents to the container
transmission of light through the container
alteration of the container upon storage
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64. properties of plastics may be altered
addition of:
- plasticizers, stabilizers, antioxidants, antistatic agts,
antimold agts, colorants, and others
drug subs’s subjected to oxidative degradation
- may undergo a greater degree of degradation when
packaged in plastic as compared to glass
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65. LEACHING
movement of components of a container into the contents
Cpds leached from the plastic containers:
polymer additives as the plasticizers, stabilizers or
antioxidants
occurs when liq. or semi-solid dosage forms are packaged
in plastic
little leaching occurs for tabs or caps packaged in plastic
Influenced by:
*temp *excessive agitation of the filled container
*solubilizing effect of liq. contents on one or more of the
polymer additives
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66. Soft-walled plastic containers of PVC – polyvinyl Cl
- used to package IV solns and blood for
transfusion
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67. SORPTION
binding of molecules to polymer materials
absorption and adsorption are considered
occurs through chem. or phy. means due to:
*chem.. structure of the solute molecules
*phy. and chem. properties of the polymer
occurs with active pharmacologic agts or with pharmaceu. excipients
thus, ings must be examined in the proposed plastic packaging to
determine its tendency
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68. Pharmacist should dispense medication to patients
in:
- same type & quality of container used by the
manufacturer of the product.
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69. Child-Resistant/Adult-Senior Use Packaging
Child-resistant container
- defined as:
*significantly difficult for children under 5 years of age to open
or to obtain a harmful amount of its contents within a
reasonable time
*not difficult for “normal adults” to use properly.
Child-proof closures
- initial regulations called for its use for
*aspirin products *certain household chemical products
- shown to have a significant potential for causing accidental poisoning
in youngsters
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70. Drugs intended for oral use
dispensed by the pharmacist to the patient in containers having child-
resistant closures unless the prescriber or the patient specifically
requests otherwise, or unless the product is specifically exempt from
the requirement
Adults, particularly the elderly or those with arthritis or weakened
hand-strength (with difficulty opening child-resistant packages)
- the regulations were amended and (1998) to require that child-
resistant containers be capable of being readily opened by senior adults
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71. STORAGE
product must be stored under proper conditions
- to ensure the stability of a pharmaceutical prepn
for the period of its intended shelf life
Labeling of each product
- includes the desired conditions of storage
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72. Terms employed for the desired conditions
as defined by the USP:
Cold
- any temp not exceeding 8o
C (46o
F)
- a refrigerator is a cold place where the temp. is
maintained bet. 2o and 8oC (36o and 46oF)
Cool
- any temp bet. 8o
and 15o
C (46o
and 59o
F)
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73. Terms employed for the desired conditions
as defined by the USP:
Room Temp.
- temp prevailing in a working area
- 20o
to 25o
C (68o
F to 77o
F) but also allows for temp variations
bet 15o
and 30o
C (59o
and 86o
F) experienced in pharmacies,
hospitals, and drug warehouses
Warm
- any temp bet 30o
and 40o
C (86o
and 104o
F)
Excessive Heat
- any temp above 40o
C (104o
F)
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74. Protection from Freezing
protects the product from:
*freezing
*risk of breakage of the container
*loss of strength or potency
*destructive alteration of the dosage form
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75. Stability Testing
Signs of degradation of the specific dosage forms
must be observed and reported.
Tablets : Apperance (cracking, chipping, mottling),
friability, hardness, color.
Capsules: Moisture tackiness, color appearance, shape,
brittleness and dissolution
Oral Solutions and Suspensions: Appearance, precipitation,
pH, color, odor, dispersibility (suspension) and clarity
(solutions)
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76. Oral Powders: Appearance, color, odor, moisture
Metered–dose inhalation aerosols delivered dose per
activation, number of metered doses, color, particle
size distribution, loss of propellant, pressure, valve
corrosion, spray pattern, absence of pathogenic
microorganism
Topical creams: ointments, lotions, solutions, and
gels. Appearance, color, homogeneity, odor, pH,
resuspendability (lotions), consistency, particle size,
distribution strength, weight loss.
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77. Opthalmic and Nasal and Oral inhalation
preparations: Appearance, color consistency,
pH, clarity (solutions), particle size, and
resuspendability (suspensions, ointments),
strength and sterility.
Small Volume Parenterals: Appearnace, color,
clarity, particulate matter, pH volumes and
extractables (when plastic containers are
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78. Suppositories: Softening range; appearance
and melting.
Emulsions: Appearance (such as phase
separation) color, odor, pH, and viscosity.
Controlled release membrane drug delivery
systems: seal strength of thr drug reservoir,
decomposition products, membrane integrity,
drug strength and drug release rate.
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79. FDA guidelines on stability for
extemporaneous compounding
Nonaqueous liquids & solid formulations
(source of active ingredient)’s
- not later than 25% of the time remaining until the
product’s expiration date or 6 months, whichever is earlier
Nonaqueous liqs & solid formulations in w/c USP or NF
substance (source of ing)
- beyond-use not later than 14 days in storage at cold
temperatures
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80. FDA guidelines on stability for
extemporaneous compounding
Other formulations beyond-use date of the
intended duration of therapy or 30 days
whichever is earlier
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81. PHARMACIST:
oral aq. liq prepns made from existing tab or cap formulation
- pharmacist should make up only at most a 14 days supply and
must be stored in a ref.
must dispense the medication in a container conducive to
stability and use
- advise the patient of the proper method of use and conditions
of storage of the medication
when compounding on the basis of extrapolated or less than
concrete information
- should keep the formulation simple and not to shortcut but
use the necessary pharmaceutical adjuvants to prepare the
prescription
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82. Stability testing
manufactured products - shelf life of 2 or more years
to ensure stability at the time of consumption.
expiration date - limits the time during which the
product may be dispensed by the pharmacist or used
by the patient.
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83. PHARMACEUTIC INGREDIENTS
required in preparing the drug subs. into a final
dosage form
for each dosage form:
*establish the primary features of the prod
*contribute to the physical form, texture,
stability, taste and over all appearance
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84. Pharmaceutical Ingredients and Excipients
Definition of terms
Solvents are used to dissolve the drug substance.
Flavors and sweeteners are used to make the product
more palatable
Colorants are added to enhance appeal
Preservatives may be added to prevent microbial
growth
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85. Pharmaceutical Ingredients and Excipients
Stabilizers (antioxidants and chelating) - to prevent
decomposition.
Diluents or fillers - to increase the bulk of the formulation.
Binders – to cause adhesion of the powdered drug and
pharmaceutical substances.
Antiadherents or lubricants to assist smooth tablet
information.
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86. Pharmaceutical Ingredients and Excipients
Disintegrating agents - promote tablet break up
after administration and coatings to improve
stability, control disintegration or enhance
appearance.
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87. Sweetening Pharmaceuticals
used in foods and pharmaceuticals:
*sucrose
*artificial sweetening agents
SWEETENING PHARMACEUTICALS
- mask unwanted taste
- commonly used - sucrose
-Delaney Clause: no new food additives may be
used if animal studies/appropriate tests showed that
it caused cancer
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88. Saccharin & cyclamate - used in foods
-“generally recognized as safe” (before the
amendment’s passage)
- use on rats: developed incidence of bladder
tumors (cancer)
- continued availability but warning labels be used
-cyclamates (banned) - possible carcinogenicity,
genetic damage, testicular atrophy
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89. Sweetening Pharmaceuticals
Aspartame –
- 1st artificial sweetener (1958 amendment)
w/ requirement for pre-marketing proof of safety.
- Acesulfame potassium (nonnutritive sweetener)
- structurally similar to saccharin (USP approved)
-130 times as sweet as sucrose, excreted unchanged in
the urine;
- more stable than aspartame
- Stevia (Stevia rebaudiana Bertoni)
– new sweetening agent: natural, nontoxic, safe,
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90. Sucrose Saccharin aspartame
Source Sugar cane;
sugar beet
Chemical
synthesis;
phthalic
anhydride
Methyl ester
dipeptide of
phenylalanine
and aspartic
acid
Relative
sweetness
1 300 180-200
Bitterness None Moderate to
strong
none
After taste None Moderate to
strong metallic
to bitter
none
Calories acid
stability
4/g 0 4/g
Acid stability good Excellent fair
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91. Coloring Pharmaceuticals
for esthetics.
Coal tar (pix carbonis)
- thick black viscid liquid
- by product of destructive distillation of coal.
- source of synthetic coloring agents in pharm.
products in the middle of the 19th
century
Dyes – added to pharmaceutical prens in the form of
diluted solutions
Lakes - commonly used in the form of fine
dispersions or suspensions.
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92. Coloring Pharmaceuticals
90% of the dyes used in the products - synthesized from
derivative of benzene (aniline)
FDA - regulates use color additives in foods, drugs, and
cosmetics (Federal Food, Drug, and Cosmetic Act of 1938)
- FD&C color additives - foods, drugs, and cosmetics
- D&C color additives - drugs, some in cosmetics &
medical devices
- external D&C color additives - restricted to external
parts
of the body (not including the lips and other parts that
are covered by mucous membrane)
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93. Factors in selecting dyes
Solubility of prospective dye
pH & pH stability of the preparation to be colored
Dyes must be photostable
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95. Sterilization and Preservation
some types of pharmaceutical products
(ex. Ophthalmic and injectable preparations)
- sterilized by physical methods :
*autoclaving (20min at 15 lb. press. &
121°C, dry heat at 180°C for 1 hr)
*bacterial filtration.
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96. Sterilization and Preservation
Preparations that provide excellent growth media for
microbes
- aqueous preparations: syrups, emulsions,
suspensions
- semi solid preparations particularly creams.
- hydro-alcoholic & most alcoholic preparation
*may not require addition of chemical
preservative
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97. Sterilization and Preservation
prevent microbial growth:
*15% alcohol in acid media
*18% alcohol in alkaline media.
Alcohol-containing pharmaceuticals (elixirs, spirits,
and tinctures) - self sterilizing and do not require
additional preservation.
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98. Preservative Selection
Considerations in selecting preservative in pharmaceutical
preparations:
1. prevents the growth of the type of microorganisms
( contaminants of the preparations)
2. soluble enough in water to achieve adequate
concentrations in aqueous phase with two or more phase
systems
3. proportion of preservative remaining undissociated at the pH
of preparation (can penetrate the microorganism &
destroy its integrity).
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99. Preservative Selection
4. concentration of the preservative does not affect the
safety/comfort of the patient
5. with adequate stability and not reduced in
concentration by chemical
decomposition/volatilization
6. compatible with all other formulative ingredients and
does not interfere with them
7. does not adversely affect the preparation’s container
or closure.
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100. Mode of action
Mechanisms preservative interfere with microbial growth,
multiplications, and metabolism:
1. Modifications of cell membrane permeability and leakage of
cell constituents (partial lysis)
2. Lysis and cytoplasmic leakage
3. Irreversible coagulation of cytoplasmic constituents
4. Inhibition of cellular metabolism by interfering with enzyme
systems/inhibition of cell wall synthesis
5. Oxidation of cellular constituents
6. Hydrolysis
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101. PRESERVATIVE UTILIZATION
PRESERVATIVES:
- suitable substances added to enhance its permanency
or usefulness
- examples: commonly employed:
benzoic acid alcohol
sodium benzoate phenylmercuric nitrate and acetate
phenol benzalkonium chloride
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102. IV prepns in large volumes as blood
replenishers/nutrients
- no bacteriostatic additives
Injectable prepns in small volumes
- can be preserved with suitable preservatives
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