Preformulation studies are important to develop a safe, effective, and stable dosage form. The goals are to establish physicochemical parameters of the drug substance for stability and compatibility with excipients. Key preformulation considerations include physical properties like polymorphism, particle size and shape, and chemical properties like hydrolysis and oxidation. These factors impact the drug's solubility, dissolution, and stability in a dosage form. Understanding preformulation is essential for optimizing the drug development process and producing dosage forms with consistent therapeutic effects.
The document discusses various chemical properties and processes that can affect drug stability during preformulation, including oxidation, hydrolysis, racemization, and polymerization. It provides details on the mechanisms and factors that influence these processes, as well as methods to prevent or reduce degradation, such as adjusting pH, adding antioxidants or chelating agents, and controlling temperature and light exposure. Racemization can impact a drug's pharmacological and toxicological properties due to differences between its enantiomers. Polymerization involves monomers reacting to form polymer chains or networks and is exemplified by the darkening of glucose solutions.
This document discusses preformulation studies and biopharmaceutical classification system (BCS) classification. It provides an introduction to preformulation studies, which characterize the physical and chemical properties of drug substances alone and with excipients. The goals and types of preformulation studies are described. Key parameters evaluated in preformulation studies include physical characteristics, chemical characteristics, organoleptic properties, polymorphism, particle size and shape, powder flow properties, hygroscopicity, solubility, pH solubility profile and common ion effects, dissolution, and permeability. Methods for various preformulation tests are also outlined.
This document discusses pellets, which are small spherical units used to deliver drugs. It covers pellet formulation requirements, manufacturing processes like extrusion-spheronization, and characterization methods. Pellets offer benefits like uniform dosing and controlled release. They are made by agglomerating powders using water or other liquids to form nuclei that grow in size. Key processes include granulation, extrusion, spheronization, and coating layers onto seeds or cores. Pellets are characterized based on size, shape, porosity, and dissolution profile. Controlling these properties allows pellets to improve drug delivery.
The document discusses preformulation studies, which involve characterizing the physical and chemical properties of a drug substance before developing a dosage form. The goals are to generate stability-indicating parameters and select an appropriate dosage form. Key topics covered include the physical properties tested (such as solubility, polymorphism, particle size), chemical degradation pathways (such as hydrolysis, oxidation), and how these properties influence dosage form design and drug performance. Understanding a drug's preformulation behavior is critical for developing a safe, effective, and stable drug product.
Preformulation Studies (Chemical Properties) Industrial Pharmacy 1stRAHUL PAL
This document discusses preformulation studies focusing on chemical properties. It describes common degradation pathways like oxidation, hydrolysis, reduction, racemization, and polymerization. For each pathway, it provides examples and discusses factors that catalyze the reactions as well as methods to prevent degradation, such as using antioxidants, buffers, and removing water. The goal of preformulation studies is to generate information useful for developing stable drug formulations that can be mass produced and reproduced consistently.
The document discusses preformulation, which involves determining the physicochemical properties of a new drug substance to aid in developing a stable dosage form. Key goals are to formulate a safe, effective dosage form with good bioavailability. The document outlines areas studied in preformulation including solubility, polymorphism, hygroscopicity, and particle characterization. Understanding these properties helps ensure the drug will perform as intended.
This document summarizes formulations for various cosmetic preparations including lipsticks, shampoos, cold cream, vanishing cream, toothpastes, hair dyes, and sunscreens. It provides information on the definition, key ingredients, preparation methods, and evaluation of these products. The main formulations covered are lipsticks, shampoos, cold cream, and toothpastes. It also briefly discusses packaging materials science and factors that influence the choice of packaging for pharmaceutical products.
A comprehensive interpretation of pellets based on their definitions, advantages, disadvantages, mechanism of pellet formation and growth, pelletization techniques, formulation requirements, and the equipment system for manufacture of pellets.
The document discusses various chemical properties and processes that can affect drug stability during preformulation, including oxidation, hydrolysis, racemization, and polymerization. It provides details on the mechanisms and factors that influence these processes, as well as methods to prevent or reduce degradation, such as adjusting pH, adding antioxidants or chelating agents, and controlling temperature and light exposure. Racemization can impact a drug's pharmacological and toxicological properties due to differences between its enantiomers. Polymerization involves monomers reacting to form polymer chains or networks and is exemplified by the darkening of glucose solutions.
This document discusses preformulation studies and biopharmaceutical classification system (BCS) classification. It provides an introduction to preformulation studies, which characterize the physical and chemical properties of drug substances alone and with excipients. The goals and types of preformulation studies are described. Key parameters evaluated in preformulation studies include physical characteristics, chemical characteristics, organoleptic properties, polymorphism, particle size and shape, powder flow properties, hygroscopicity, solubility, pH solubility profile and common ion effects, dissolution, and permeability. Methods for various preformulation tests are also outlined.
This document discusses pellets, which are small spherical units used to deliver drugs. It covers pellet formulation requirements, manufacturing processes like extrusion-spheronization, and characterization methods. Pellets offer benefits like uniform dosing and controlled release. They are made by agglomerating powders using water or other liquids to form nuclei that grow in size. Key processes include granulation, extrusion, spheronization, and coating layers onto seeds or cores. Pellets are characterized based on size, shape, porosity, and dissolution profile. Controlling these properties allows pellets to improve drug delivery.
The document discusses preformulation studies, which involve characterizing the physical and chemical properties of a drug substance before developing a dosage form. The goals are to generate stability-indicating parameters and select an appropriate dosage form. Key topics covered include the physical properties tested (such as solubility, polymorphism, particle size), chemical degradation pathways (such as hydrolysis, oxidation), and how these properties influence dosage form design and drug performance. Understanding a drug's preformulation behavior is critical for developing a safe, effective, and stable drug product.
Preformulation Studies (Chemical Properties) Industrial Pharmacy 1stRAHUL PAL
This document discusses preformulation studies focusing on chemical properties. It describes common degradation pathways like oxidation, hydrolysis, reduction, racemization, and polymerization. For each pathway, it provides examples and discusses factors that catalyze the reactions as well as methods to prevent degradation, such as using antioxidants, buffers, and removing water. The goal of preformulation studies is to generate information useful for developing stable drug formulations that can be mass produced and reproduced consistently.
The document discusses preformulation, which involves determining the physicochemical properties of a new drug substance to aid in developing a stable dosage form. Key goals are to formulate a safe, effective dosage form with good bioavailability. The document outlines areas studied in preformulation including solubility, polymorphism, hygroscopicity, and particle characterization. Understanding these properties helps ensure the drug will perform as intended.
This document summarizes formulations for various cosmetic preparations including lipsticks, shampoos, cold cream, vanishing cream, toothpastes, hair dyes, and sunscreens. It provides information on the definition, key ingredients, preparation methods, and evaluation of these products. The main formulations covered are lipsticks, shampoos, cold cream, and toothpastes. It also briefly discusses packaging materials science and factors that influence the choice of packaging for pharmaceutical products.
A comprehensive interpretation of pellets based on their definitions, advantages, disadvantages, mechanism of pellet formation and growth, pelletization techniques, formulation requirements, and the equipment system for manufacture of pellets.
This document discusses tablet coating processes. There are three main types of coatings: sugar coating, film coating, and enteric coating. Sugar coating involves applying a sucrose solution to tablets to make them easier to swallow. Film coating deposits a thin polymer film around tablet cores. Enteric coatings are designed to pass through the stomach and dissolve in the intestines. Tablet coating is done in pans or fluidized beds to evenly apply coatings and dry the tablets. Coatings are used to mask tastes, protect medications, and control drug release.
Liquid oral topic in Industrial Pharmacy contains many topics like solution, elixirs, syrups, emulsion, and suspension. This topic includes general introduction, types, formulation, components, uses, and Quality control tests. These are also beneficial in other subjects like Pharmaceutics.
Physical Properties of Pre-formulation.pptxRAHUL PAL
Preformulation studies provide a path for formulation development and drug product development in respect of drug form, adjuvants, composition, physical structure, and chemistry of drug molecules, facilitating pharmacokinetic and biopharmaceutical properties evaluation, adjustments, and their implementation.
Preformulation studies focus on the concepts of physicochemical properties which are vital for any new drug molecule and/or proteins/peptides. These properties not only affect their therapeutic efficacy but also the development process of their specific dosage form.
This document summarizes the key aspects of manufacturing and evaluating aerosol products. It discusses the components of aerosol formulations including the product concentrate and propellant. It describes various aerosol systems like solution, water-based, suspension, and foam. It also outlines the different methods for filling aerosol containers and evaluating properties such as flammability, performance, and biological activity.
The presentation deals with a detailed study of soft gelatin capsules. this involves the production of soft gelatin capsule based on the importance of base adsorption factor and minim/gram factor. also quality control studies was also elaborated.
The document discusses parenteral products and their administration. It defines parenteral as referring to administration by injection rather than orally, bypassing the gastrointestinal tract. It then discusses the advantages and disadvantages of the parenteral route, including faster systemic delivery but also risks of infection. The document outlines various routes of parenteral injection and provides details on procedures like subcutaneous, intramuscular, and intravenous injection. It also discusses formulation, processing, and quality testing of parenteral products.
Bioassay of Digitalis, d-tubocurarine , OxytocinHeena Parveen
This document summarizes several bioassay methods for determining the potency of digitalis, oxytocin, and d-tubocurarine (d-tb) extracts, including guinea pig, cat, and pigeon methods for digitalis; depression of blood pressure in chickens, contraction of rat uterus, and measurement of milk ejection pressure in lactating rats for oxytocin; and rabbit head drop and frog rectus abdominis muscle preparation methods for d-tb. Standard preparations and procedures for administering test and standard extracts and measuring responses are described for each method.
Pharmaceutical Aerosols: Definition, propellants, containers, valves, types of aerosol systems; formulation and manufacture of aerosols; Evaluation of aerosols; Quality control and stability studies
This document discusses tablet coating, which involves covering tablet surfaces with a polymeric film to provide benefits like masking taste, protecting drugs, and controlling drug release. It describes the main types of tablet coating - sugar coating, film coating, enteric coating, vacuum film coating, electrostatic coating, and dip coating. For each coating type, it outlines the basic process and materials used. The document also explains the need for tablet coating and lists the ideal characteristics of coating materials.
This document provides an overview of drug stability for a pharmaceutical chemistry and pharmaceutics course. It defines drug stability as the ability of a dosage form to maintain its physical, chemical, therapeutic, and microbial properties during storage and usage. It discusses factors that influence stability such as temperature, pH, moisture, light, and packaging. It also describes different types of instability like physical changes, chemical degradation through hydrolysis, oxidation, or isomerization, and microbial contamination. The document aims to help predict and ensure drug stability.
Application of preformulation consideration in the development ofArpan Dhungel
This document discusses preformulation studies for developing parenteral dosage forms. Preformulation involves studying a new drug's physicochemical properties to create stable, effective formulations. Key aspects of preformulation include assessing solubility through methods like changing pH, adding co-solvents or complexing agents, and evaluating stability under various conditions like heat, light and pH to determine a drug's degradation profile. The goal of preformulation is to obtain information to guide formulation development and ensure the drug molecule is most stable.
Preformulation is the stage of development where the physicochemical properties of a drug substance are characterized and established. The objectives of preformulation study are to develop an elegant, stable, effective and safe dosage form by establishing the kinetic rate profile, compatibility with other ingredients, and physicochemical parameters of new drug substances. The physicochemical properties of a drug, such as its ability to elicit a pharmacological effect, are related to how those properties influence the biomolecule it interacts with.
pellets can be defined as multi particulate system or multiunit system
They are spherical particulates manufactured by agglomeration of the powder granules containing drug substance and excipients.
Pellets can be prepared by a special technique called Pelletization.
This technique is referred to an agglomeration process that convert fine powder or granules of bulk drug or excipient in to small , free flowing , spherical or semi spherical pellets .
Multi particular drug delivery system especially suitable for achieving controlled delay released oral formulation with low risk of dose dumping, flexibility of blending to attain different release patterns as well as reproducible and short gastric residence time.
Multi particulate drug delivery system are mainly oral dosage form consisting of a multiplicity of small discrete units each exhibiting some desire characteristics.
This document describes a bioassay method for determining the potency of oxytocin injections by comparing their activity to a standard oxytocin preparation. Female rats or guinea pigs are used as test animals. One uterine horn is suspended in a bath and contractions are recorded following the addition of two doses each of the standard preparation and the oxytocin injection being tested. The ratio of doses and intervals between doses are kept constant. Responses are measured and the potency determined using statistical analysis by comparing the responses to the standard.
This document describes several bioassay methods for measuring the potency of insulin samples, including rabbit, mouse, rat diaphragm, and rat epididymal fat pad methods. For the rabbit method, insulin samples and a standard are injected subcutaneously in rabbits and blood sugar levels are measured over time, comparing the hypoglycemic effect between samples. The mouse method compares the percentage of mice experiencing convulsions after insulin injection between samples and a standard. The rat diaphragm and epididymal fat pad methods measure glucose uptake in tissue samples incubated with insulin to determine insulin-like activity.
The document summarizes procedures for evaluating ophthalmic drug preparations. It discusses that evaluation includes sterility testing, clarity testing, leak testing, and testing for metal particles in ointments. It also describes that drug product quality tests assess attributes like identification, potency, purity, sterility and particulate matter, while performance tests evaluate drug release. Key quality tests discussed are identification, assay, pH, osmolarity, bacterial endotoxins, and uniformity of dosage units. Specific tests covered include viscosity and drop size.
This document provides information on the extraction and identification of several phytoconstituents including curcumin, artemisinin, atropine, citral, menthol, caffeine, and reserpine. For each constituent, it describes the biological source, properties, extraction method from the source, and thin layer chromatography conditions and results for identification, including mobile phase, detecting agent, and Rf value.
This document discusses different techniques for pelletization, including extrusion-spheronization, fluid bed granulation, spray drying, and spray congealing. Extrusion-spheronization involves extruding the material through a screen to form rods, which are then rounded into spheres using a spheronization machine. Fluid bed granulation coats particles in a fluidized bed with sprayed binding liquid. Spray drying and spray congealing involve spraying melted or dissolved formulations into cooled air to form solid spheres.
PMY 6120_1-1-Preformulation Characteristics of Pharmaceutical Product Systems...MuungoLungwani
The document discusses preformulation characterization of new drug candidates. It covers assessing key physical properties like crystallinity, polymorphism, hygroscopicity, particle size and shape, bulk density, and flow properties which influence formulation development, stability, and bioavailability. Solubility analysis including determining pKa, pH solubility profiles, and effects of temperature are also important to understand for formulation. Together, preformulation studies provide essential information to guide development of a stable, safe and effective dosage form with optimal bioavailability.
The document discusses preformulation studies, which characterize the physicochemical properties of drug substances. Some key points:
- Preformulation studies are conducted early in drug development to understand how a drug's properties will influence formulation, stability, bioavailability and the development process.
- Areas of study include bulk properties, solubility, stability and more. Properties like solubility, dissolution, polymorphism can impact the drug's performance.
- Various analytical techniques are used to characterize aspects like crystallinity, particle size, hygroscopicity and more which provide essential information for designing drug products.
- Understanding a drug's properties is important for selecting excipients, manufacturing processes, container closure systems and developing analytical
This document discusses tablet coating processes. There are three main types of coatings: sugar coating, film coating, and enteric coating. Sugar coating involves applying a sucrose solution to tablets to make them easier to swallow. Film coating deposits a thin polymer film around tablet cores. Enteric coatings are designed to pass through the stomach and dissolve in the intestines. Tablet coating is done in pans or fluidized beds to evenly apply coatings and dry the tablets. Coatings are used to mask tastes, protect medications, and control drug release.
Liquid oral topic in Industrial Pharmacy contains many topics like solution, elixirs, syrups, emulsion, and suspension. This topic includes general introduction, types, formulation, components, uses, and Quality control tests. These are also beneficial in other subjects like Pharmaceutics.
Physical Properties of Pre-formulation.pptxRAHUL PAL
Preformulation studies provide a path for formulation development and drug product development in respect of drug form, adjuvants, composition, physical structure, and chemistry of drug molecules, facilitating pharmacokinetic and biopharmaceutical properties evaluation, adjustments, and their implementation.
Preformulation studies focus on the concepts of physicochemical properties which are vital for any new drug molecule and/or proteins/peptides. These properties not only affect their therapeutic efficacy but also the development process of their specific dosage form.
This document summarizes the key aspects of manufacturing and evaluating aerosol products. It discusses the components of aerosol formulations including the product concentrate and propellant. It describes various aerosol systems like solution, water-based, suspension, and foam. It also outlines the different methods for filling aerosol containers and evaluating properties such as flammability, performance, and biological activity.
The presentation deals with a detailed study of soft gelatin capsules. this involves the production of soft gelatin capsule based on the importance of base adsorption factor and minim/gram factor. also quality control studies was also elaborated.
The document discusses parenteral products and their administration. It defines parenteral as referring to administration by injection rather than orally, bypassing the gastrointestinal tract. It then discusses the advantages and disadvantages of the parenteral route, including faster systemic delivery but also risks of infection. The document outlines various routes of parenteral injection and provides details on procedures like subcutaneous, intramuscular, and intravenous injection. It also discusses formulation, processing, and quality testing of parenteral products.
Bioassay of Digitalis, d-tubocurarine , OxytocinHeena Parveen
This document summarizes several bioassay methods for determining the potency of digitalis, oxytocin, and d-tubocurarine (d-tb) extracts, including guinea pig, cat, and pigeon methods for digitalis; depression of blood pressure in chickens, contraction of rat uterus, and measurement of milk ejection pressure in lactating rats for oxytocin; and rabbit head drop and frog rectus abdominis muscle preparation methods for d-tb. Standard preparations and procedures for administering test and standard extracts and measuring responses are described for each method.
Pharmaceutical Aerosols: Definition, propellants, containers, valves, types of aerosol systems; formulation and manufacture of aerosols; Evaluation of aerosols; Quality control and stability studies
This document discusses tablet coating, which involves covering tablet surfaces with a polymeric film to provide benefits like masking taste, protecting drugs, and controlling drug release. It describes the main types of tablet coating - sugar coating, film coating, enteric coating, vacuum film coating, electrostatic coating, and dip coating. For each coating type, it outlines the basic process and materials used. The document also explains the need for tablet coating and lists the ideal characteristics of coating materials.
This document provides an overview of drug stability for a pharmaceutical chemistry and pharmaceutics course. It defines drug stability as the ability of a dosage form to maintain its physical, chemical, therapeutic, and microbial properties during storage and usage. It discusses factors that influence stability such as temperature, pH, moisture, light, and packaging. It also describes different types of instability like physical changes, chemical degradation through hydrolysis, oxidation, or isomerization, and microbial contamination. The document aims to help predict and ensure drug stability.
Application of preformulation consideration in the development ofArpan Dhungel
This document discusses preformulation studies for developing parenteral dosage forms. Preformulation involves studying a new drug's physicochemical properties to create stable, effective formulations. Key aspects of preformulation include assessing solubility through methods like changing pH, adding co-solvents or complexing agents, and evaluating stability under various conditions like heat, light and pH to determine a drug's degradation profile. The goal of preformulation is to obtain information to guide formulation development and ensure the drug molecule is most stable.
Preformulation is the stage of development where the physicochemical properties of a drug substance are characterized and established. The objectives of preformulation study are to develop an elegant, stable, effective and safe dosage form by establishing the kinetic rate profile, compatibility with other ingredients, and physicochemical parameters of new drug substances. The physicochemical properties of a drug, such as its ability to elicit a pharmacological effect, are related to how those properties influence the biomolecule it interacts with.
pellets can be defined as multi particulate system or multiunit system
They are spherical particulates manufactured by agglomeration of the powder granules containing drug substance and excipients.
Pellets can be prepared by a special technique called Pelletization.
This technique is referred to an agglomeration process that convert fine powder or granules of bulk drug or excipient in to small , free flowing , spherical or semi spherical pellets .
Multi particular drug delivery system especially suitable for achieving controlled delay released oral formulation with low risk of dose dumping, flexibility of blending to attain different release patterns as well as reproducible and short gastric residence time.
Multi particulate drug delivery system are mainly oral dosage form consisting of a multiplicity of small discrete units each exhibiting some desire characteristics.
This document describes a bioassay method for determining the potency of oxytocin injections by comparing their activity to a standard oxytocin preparation. Female rats or guinea pigs are used as test animals. One uterine horn is suspended in a bath and contractions are recorded following the addition of two doses each of the standard preparation and the oxytocin injection being tested. The ratio of doses and intervals between doses are kept constant. Responses are measured and the potency determined using statistical analysis by comparing the responses to the standard.
This document describes several bioassay methods for measuring the potency of insulin samples, including rabbit, mouse, rat diaphragm, and rat epididymal fat pad methods. For the rabbit method, insulin samples and a standard are injected subcutaneously in rabbits and blood sugar levels are measured over time, comparing the hypoglycemic effect between samples. The mouse method compares the percentage of mice experiencing convulsions after insulin injection between samples and a standard. The rat diaphragm and epididymal fat pad methods measure glucose uptake in tissue samples incubated with insulin to determine insulin-like activity.
The document summarizes procedures for evaluating ophthalmic drug preparations. It discusses that evaluation includes sterility testing, clarity testing, leak testing, and testing for metal particles in ointments. It also describes that drug product quality tests assess attributes like identification, potency, purity, sterility and particulate matter, while performance tests evaluate drug release. Key quality tests discussed are identification, assay, pH, osmolarity, bacterial endotoxins, and uniformity of dosage units. Specific tests covered include viscosity and drop size.
This document provides information on the extraction and identification of several phytoconstituents including curcumin, artemisinin, atropine, citral, menthol, caffeine, and reserpine. For each constituent, it describes the biological source, properties, extraction method from the source, and thin layer chromatography conditions and results for identification, including mobile phase, detecting agent, and Rf value.
This document discusses different techniques for pelletization, including extrusion-spheronization, fluid bed granulation, spray drying, and spray congealing. Extrusion-spheronization involves extruding the material through a screen to form rods, which are then rounded into spheres using a spheronization machine. Fluid bed granulation coats particles in a fluidized bed with sprayed binding liquid. Spray drying and spray congealing involve spraying melted or dissolved formulations into cooled air to form solid spheres.
PMY 6120_1-1-Preformulation Characteristics of Pharmaceutical Product Systems...MuungoLungwani
The document discusses preformulation characterization of new drug candidates. It covers assessing key physical properties like crystallinity, polymorphism, hygroscopicity, particle size and shape, bulk density, and flow properties which influence formulation development, stability, and bioavailability. Solubility analysis including determining pKa, pH solubility profiles, and effects of temperature are also important to understand for formulation. Together, preformulation studies provide essential information to guide development of a stable, safe and effective dosage form with optimal bioavailability.
The document discusses preformulation studies, which characterize the physicochemical properties of drug substances. Some key points:
- Preformulation studies are conducted early in drug development to understand how a drug's properties will influence formulation, stability, bioavailability and the development process.
- Areas of study include bulk properties, solubility, stability and more. Properties like solubility, dissolution, polymorphism can impact the drug's performance.
- Various analytical techniques are used to characterize aspects like crystallinity, particle size, hygroscopicity and more which provide essential information for designing drug products.
- Understanding a drug's properties is important for selecting excipients, manufacturing processes, container closure systems and developing analytical
1.preformulation concept in Modern pharmaceutics.pptxPNMallikarjun
Preformulation is defined as the investigation of physical and chemical properties of a drug substance alone and when combined with excipients. The goal is to generate information to help formulators develop stable and safe dosage forms with good bioavailability. Some key tests include determining the drug's solubility, stability, and compatibility with various excipients using techniques like DSC, TLC, and HPLC. This provides critical data to guide the rational selection of dosage form and formulation components.
The document discusses preformulation studies that are conducted to characterize the physical, chemical, and mechanical properties of new drug substances. It covers topics like solubility, permeability, polymorphism, hygroscopicity, particle size, and powder flow properties. The objectives of preformulation are to develop stable, safe, and effective dosage forms and generate useful information for formulating an optimal drug delivery system. It also discusses various analytical methods used to characterize solid forms during preformulation.
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.
This document outlines the course content for a Pharmaceutical Technology course. It discusses topics like pre-formulation, dosage forms, liquid dosage forms, suspensions, emulsions, semisolids, suppositories, transdermal drug delivery systems, and case studies. Pre-formulation is described as investigating the physical and chemical properties of drug substances alone or with excipients to generate information for developing stable and bioavailable dosage forms. Key areas of pre-formulation research include solubility analysis, particle characterization, and stability analysis.
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 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
Presentation cover
Introduction of Preformulation
Goals of Preformulation
Usefulness of Preformulation
Classes of Preformulation
Factors to be consider before Preformulation
Steps in Preformulation
Principle area of Preformulation
Evaluated parameters in Preformulation
Conclusion
This document discusses preformulation, which involves studying the physical and chemical properties of a drug prior to developing a dosage form. The goals of preformulation are to establish the drug's physicochemical parameters, physical characteristics, compatibility with excipients, and provide data to support dosage form design and evaluation. The major areas of preformulation study include physical description and bulk characterization, solubility analysis, and stability analysis. Specific tests described include assessing crystallinity, polymorphism, hygroscopicity, particle size, thermal effects, and powder flow properties.
This document provides an overview of preformulation studies for a new drug. It discusses characterizing the physical and chemical properties of the drug molecule to develop a safe, effective, and stable dosage form. Key aspects of preformulation studies that are described include salt formation, prodrug design, polymorphism, crystallinity, hygroscopicity, particle characterization, bulk density, powder flow properties, solubility analysis, stability analysis, and drug-excipient compatibility testing. The goal of preformulation is to obtain essential information to guide formulation development and design robust evaluation of the new drug candidate.
This document provides an overview of preformulation studies for drug development. It discusses the importance of characterizing key physicochemical properties of drug substances such as solubility, ionization constants, melting point, and polymorphism. It also covers the role of excipients and how drug-excipient interactions can impact stability. The document concludes with sections on stability studies, factors that influence stability, and guidelines for stability testing procedures and frequencies.
This document discusses preformulation studies, which focus on the physical and chemical properties of a new drug compound and how those properties could impact drug performance and dosage form development. The goals of preformulation studies are to establish the physicochemical parameters, kinetics, stability, and compatibility of a new drug compound alone and when combined with excipients. Key physicochemical properties investigated include particle size, shape, crystallinity, solubility, hygroscopicity, and stability. Understanding these properties helps with rational dosage form design and evaluation of product efficacy and stability.
This document discusses preformulation for new drug development. A change in formulation, dosage, route of administration, or dosage form of an existing drug causes it to be considered "new" and requires safety and efficacy evaluation. Preformulation aims to optimize a drug's physical and chemical properties for a stable, effective dosage form. It involves characterizing the drug molecule and developing the dosage form. Some goals of preformulation include establishing the drug's physicochemical parameters, kinetic profile, physical characteristics, and compatibility with excipients. Polymorphism, or the ability of a drug to exist in different crystal forms, is also evaluated as it can impact properties like solubility, dissolution rate, and bioavailability.
Preformulation studies characterize the physical and chemical properties of drug molecules to develop safe, effective, and stable dosage forms. The goals are to develop formulations that are stable, safe, and effective. Major areas of study include physical characterization of properties like crystallinity and polymorphism, hygroscopicity, particle size, and powder flow. Solubility is analyzed through measurements of ionization, partition coefficient, aqueous solubility, and pH-solubility profiles. Stability is analyzed through studies of photolytic stability, stability to oxidation, and drug-excipient compatibility.
The document discusses preformulation of sterile products. It covers key areas of preformulation including bulk characterization, solubility analysis, and stability analysis. Bulk characterization involves assessing properties like crystallinity, polymorphism, particle size, powder flow, and hygroscopicity. Solubility analysis includes studying aqueous solubility, drug ionization at physiological pH, partition coefficient, and thermal effects. Stability analysis focuses on stability in toxicology formulations, solution stability, and solid state stability under various conditions. The goal of preformulation is to characterize important physicochemical properties of drug substances to aid in developing appropriate formulations.
The document summarizes key aspects of preformulation studies. It discusses the objectives of preformulation which are to establish physicochemical parameters, stability, and compatibility with excipients. It then examines various physicochemical properties of drugs including organoleptic characteristics, bulk properties, solubility, crystallinity and polymorphism. Methods for analyzing properties like hygroscopicity, powder flow, and partition coefficient are also outlined. The importance of preformulation in developing stable dosage forms is emphasized.
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How to Add Chatter in the odoo 17 ERP ModuleCeline George
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Exploiting Artificial Intelligence for Empowering Researchers and Faculty, In...Dr. Vinod Kumar Kanvaria
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LAND USE LAND COVER AND NDVI OF MIRZAPUR DISTRICT, UPRAHUL
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significant role in maintaining the ecological equilibrium of our planet.Land serves as the foundation for all human activities and provides the necessary materials for
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land.
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like India, rapid population growth and the emphasis on extensive resource exploitation can lead
to significant land degradation, adversely affecting the region's land cover.
Therefore, human intervention has significantly influenced land use patterns over many
centuries, evolving its structure over time and space. In the present era, these changes have
accelerated due to factors such as agriculture and urbanization. Information regarding land use and
cover is essential for various planning and management tasks related to the Earth's surface,
providing crucial environmental data for scientific, resource management, policy purposes, and
diverse human activities.
Accurate understanding of land use and cover is imperative for the development planning
of any area. Consequently, a wide range of professionals, including earth system scientists, land
and water managers, and urban planners, are interested in obtaining data on land use and cover
changes, conversion trends, and other related patterns. The spatial dimensions of land use and
cover support policymakers and scientists in making well-informed decisions, as alterations in
these patterns indicate shifts in economic and social conditions. Monitoring such changes with the
help of Advanced technologies like Remote Sensing and Geographic Information Systems is
crucial for coordinated efforts across different administrative levels. Advanced technologies like
Remote Sensing and Geographic Information Systems
9
Changes in vegetation cover refer to variations in the distribution, composition, and overall
structure of plant communities across different temporal and spatial scales. These changes can
occur natural.
This presentation was provided by Steph Pollock of The American Psychological Association’s Journals Program, and Damita Snow, of The American Society of Civil Engineers (ASCE), for the initial session of NISO's 2024 Training Series "DEIA in the Scholarly Landscape." Session One: 'Setting Expectations: a DEIA Primer,' was held June 6, 2024.
it describes the bony anatomy including the femoral head , acetabulum, labrum . also discusses the capsule , ligaments . muscle that act on the hip joint and the range of motion are outlined. factors affecting hip joint stability and weight transmission through the joint are summarized.
2. Content…..
Introduction.
Goals and objective of preformulation studies
Preformulation considerations
Application of Preformulation Considerations in the development
of dosage forms.
Impact of Preformulation considerations on Stability of dosage
form.
Conclusion
3. Introduction….
“Preformulation studies are the investigations of physical
and chemical properties of drug substance alone and in
combination with other excipients to develop a Safe
,Effective and Stable dosage form”
These are the first step in the rational development of
dosage forms of a drug substance.
It is the phase of research and development of drug
4. Goals and objective of preformulation studies….
• To establish the physicochemical parameters of drug molecules for
its stability for any desired dosage form.
• To determine the kinetic rate profile of a drug substance for drug
stability
• To establish compatibility of any drug with formulation excipients
for possible interactions
• Preparation of safe ,effective ,and stable dosage form with better
therapeutic values
7. Physical Considerations…
1. Physical form:-
Drug may exist in crystal or
amorphous form.
Crystal form:-
It is characterized by repeated arrangements of atoms in
three –dimensional (3-D) array.
Amorphous form:-
it has atoms or molecules randomly placed and does not
have any defined structure or molecular arrangement.
8. Physical Considerations…
2- Polymorphism:-
It is the ability of a solid material to
exist in more than one form of crystal structure.
Polymorphs may divided in to two types-
Enantiotropic :- Reversibly changes into another form at
varying in temperature & pressure .
Example- carbamazepine ,acetozolamide .
Monotropic:- Unstable at all temperature & pressure .
Example – flufenamic acid .
9. Physical Considerations…
3- Particle size:-
Particle diameter is also important
consideration in the preformulation studies.
4- Particle shape:-
Particles may exist in various shape.
Like- spherical, oval, rod-shaped etc.
Particle shape also important consideration in
preformulation studies .
10. Physical Considerations…
5- Flow properties:-
Flow properties of material can be measured by following
determinations.
Angle of repose:-
The angle of repose or the critical angle of repose, of a granular material
is the steepest angle relative to the horizontal plane which a material
can be piled without slumping or the surface material sliding.
[Angle of repose (ϑ)= tan−1(2H/D)]
Carr’s index( compressibility ):-
Carr’s index can be calculated by formula
[ C= tapped density – bulk density X100 ]
tapped density
11. Physical Considerations…
6- Solubility profile:-
In solubility profile following parameters are considered .
Partition co-efficient:-
“It is the ratio of drug amount dissolved in oil phase to the drug
amount dissolved in aqueous phase”
Partition co-efficient (P) = Xo
Xw
PKa :- it is also called dissociation constant .
This parameter gives information about drug ionization at any
physiological PH condition . It can be calculated by-
[Henderson-Hasselbalch equation pH = pKa + log([A-]/[HA])]
PH:- it is the measurement unit of acidity or alkalinity of any
chemical compound .
12. Chemical Considerations…
1- Hydrolysis:-
It is the chemically breakdown reaction of any compound
in the presence of water.
2- Oxidation – Reduction (Redox) reaction:-
An oxidation-reduction (redox) reaction is a type of -
chemical reaction that involves-
Oxidation is the gain of oxygen.
Reduction is the loss of oxygen.
Oxidation is the loss of hydrogen.
Reduction is the gain of hydrogen.
Oxidation is loss of electrons
Reduction is gain of electrons
13. Chemical Considerations…
3- Racemization:-
It is the formation of racemic mixture from any optically
active compound.
Racemic mixture is the equimolar mixture of enantiomers and
it is optically inactive.
4- polymerization:-
It is a continuous reaction between molecules , more
than one monomer reacts together to form a polymer.
14. Application of Preformulation Considerations in the development
of dosage forms……
All the considerations of preformulation studies are applicable to produce an
optimized and stable dosage form of any known or new drug substance.
1. Drug–excipient compatibility study:-
Excipients are the non-pharmacological substances which are
required to convert a drug into a desired dosage form.
Excipient should be compatible with drug and should be inert,
otherwise it may produce any other chemical entity by reacting
with the drug.
There are two methods for the assessment of drug-excipient
compatibility.
(a)D.S.C method ( digital scanning calorimeter)
(b) F.T.I.R method ( fourier transform infrared spectrometer )
15. Application of Preformulation Considerations in the development
of dosage forms……
2- Physical form:-
This is an important preformulation consideration related with the
drug form, is either crystalline or amorphous.
Physical form of drug may affect –
- Melting point
- Solubility
- Density
- Vapor pressure
- Compressibility
For the optimization of above factors we need to study about the physical
form of drug.
Amorphous drugs are generally have higher solubility and less stability
as compared to crystalline drug.
16. Application of Preformulation Considerations in the development
of dosage forms……
3- Polymorphism:-
Due to different shape of material, arrangement of
atoms also differ that leads to vary in crystal energy.
Hence every shape of material possess different reactivity ,
that affects-
- Chemical stability
- Solubility
- Bioavailability
- Melting point
To stabilize the above factors ,we should have proper
knowledge about the phenomenon of polymorphism
17. Application of Preformulation Considerations in the development
of dosage forms……
4- Particle size :-
Particle size & size distribution affects-
- Dissolution rate
- Absorption rate
- Content uniformity
- Taste
- Texture
- Color
- Stability
Particle size should be optimum for every dosage form.
18. Application of Preformulation Considerations in the development
of dosage forms……
5- Angle of repose:-
angle of repose tells about that flow properties of
material. flow properties affect-
- Production rate
- Uniformity of dose
- Efficacy of dosage form
Angle of repose Type of flow
<20 Excellent
20-30 Good
30-34 Passable
>40 Poor flow
19. Application of Preformulation Considerations in the development
of dosage forms……
6- Carr’s index(compressibility) :-
it is an indication about the compressibility of material, on
the basis of Carr’s index of powder we decide the
compression methods during tablet formulation.
- Direct compression ( if powder material compressible) .
- Dry granulation
- Wet granulation
Carr’s index Type of flow
5-15 Excellent
12-16 Good
18-21 Passable
23-35 Poor
33-38 Very poor
>40 Extremely poor
20. Application of Preformulation Considerations in the development
of dosage forms……
7- Partition co-efficient:-
It is the measurement of hydrophilicity and lipophilicity of any drug
substance.
Hydrophilicity and lipophilicity of any drug affects its-
- Absorption through biological membrane
- Solubility in aqueous media
If Partition co-efficient is more than one then drug is lipophilic in
nature, highly lipophilic drug may cross blood brain barrier and
blood-placental barrier.
If partition co-efficient is less than one then drug is hydrophilic in
nature and may easily dissolve in aqueous media.
21. Application of Preformulation Considerations in the development
of dosage forms……
8- Pka:-
This parameter gives information about drug ionization
at any physiological PH.
By determining the PH and Pka of any drug we can easily
predict the absorption rate of any drug at any PH.
9- Hydrolysis:-
H+ and OH- are the reactive species ,responsible for drug
hydrolysis in solutions.
Hydrolysis is mainly considered in solutions and deal with the
drug stability during shelf life and its degradation.
22. Application of Preformulation Considerations in the development
of dosage forms……
10- Racemization:-
Racemization may occurs due to heat or any chemical
reaction , in which half of the optically active compound
becomes its mirror image.
Racemization may affect-
- Solubility
- Dissolution rate
- Absorption
- Bioavailability
- Drug-receptor interaction
- Pharmacological efficacy
Hence it has to be establish that racemization does not occur under
the labeled conditions of storage until shelf life.
23. Impact of Preformulation considerations on Stability of dosage
form….
Preformuation considerations affect the stability of dosage
forms If they are not in optimized condition.
1-Physical form(Crystal or Amorphous):-
Crystalline form is more stable than amorphous
form because crystal has arranged internal structure.
Eg:- Crystalline Penicillin-G is more stable than amorphous form.
Tablet stability may affect due to crystal packing arrangement of
drug.
24. Impact of Preformulation considerations on Stability of dosage
form…
2- Polymorphism:-
polymorphism is the phenomenon of changing in shape
and size of solid material at different temperature and
pressure ,so it may cause instability in the dosage form
during storage.
Polymorphs are also evaluated to be sure that they are not
changing their shape and size during unit operations of
formulation ,like- drying , milling etc.
25. Impact of Preformulation considerations on Stability of dosage
form….
3- Particle size:-
Particle size reduction less than 10u causes incorporation of
gas/air between particles ,this prevents water penetration between
particles and reduce wetting properties of particles ,which may
cause-
- Sedimentation
- Creaming
- Cracking
Extreme size reduction increase higher surface area which may
leads to-
- Polymorphic changes
- Rapid degradation when exposed to- Air, Heat, Light, Humidity ,and
oxygen.
Larger particle size also cause instability in the formulations.
26. Impact of Preformulation considerations on Stability of dosage
form….
4- Carr’s Index:-
Powder material’s compressibility should be optimum otherwise
fragmentation may occur after formulation of tablet.
5- Hydrolysis :-
It mainly consider in preformuation study of solution.
In the presence of water certain drug are degraded.
Hydroxyl ions of water are strong nucleophiles
In solution of the acidic PH(<7), H+ ions cause hydrolysis reactions.
These degradation reactions are higher in alkaline solutions than in water.
Hydrolysis is affected by the PH of solution , presence of buffer salts & co-
solvents, complexing agents & surfactants .
27. Impact of Preformulation considerations on Stability of dosage
form…..
6- Oxidation:-
Most common cause of drug decomposition in solutions
It is promoted by the presence of oxygen and reaction can be
initiated by the action of heat , light or trace metal ions that
produce free radicals , these free radicals propagate the
oxidation reaction that cause drug degradation.
7- Racemization:-
Conversion of enantiomer in its mirror image may leads to
instability of drug ,because in this reaction drug’s structure is
changed that may propagate other reactions.
28. Impact of Preformulation considerations on Stability of dosage
form…
8- Polymerization:-
It leads to increase in viscosity of the
formulation that may cause difficulties in drug
stability during storage.
29. Conclusion ………..
Drug development is a very complex , Expensive and time
consuming process and there is higher risk of failure.
To minimize the risk of failure we have to optimize
preformulation considerations.
For optimization we should have proper knowledge about the
drug’s physicochemical properties
Hence preformulation study is the obligatory phase to
avoid loss of time and money and to develop a Safe , Effective
& Stable dosage form