The document discusses various physicochemical properties that should be evaluated for new drug compounds, including solubility, crystallinity, polymorphism, particle size, density, moisture content, and flow properties. Understanding these properties is important for drug development and formulation design to ensure efficacy, stability, and manufacturability of drug products. Key properties discussed include the difference between amorphous and crystalline forms, how polymorphism can impact stability and solubility, and analytical techniques for characterizing these properties.
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 and physicochemical property of the drugSHIVANEE VYAS
“It is the study of the physical and chemical properties of the
drug prior to compounding process”.
Preformulation commences when a newly synthesized drug shows sufficient pharmacologic promise in animal models towarrant evaluation in man.
These studies should focus on physicochemical properties of new compound that affect drug performance & development of efficaciouss dosage form.
This properties may provide;
A rationale for formulation design
Support the need for molecular modification.
The document provides an overview of pre-formulation, which involves determining the physicochemical properties of a drug substance prior to developing a dosage form. It discusses the goals of pre-formulation to formulate an efficacious dosage form with good bioavailability. The protocol involves characterizing the physical, chemical, solubility, stability and compatibility properties of the drug. Key aspects covered include polymorphism, hygroscopicity, particle size, solubility, dissolution, stability in solution and solid state, and compatibility with excipients. The information guides subsequent formulation development.
This document discusses various parameters used to characterize drug release from pharmaceutical formulations. It describes diffusion parameters defined by Higuchi's equation and plots. Dissolution parameters like the effects of agitation, pH, temperature, and medium properties are outlined. Pharmacokinetic parameters including Cmax, Tmax, and AUC are defined. The Heckel equation is presented as a method to analyze powder compaction. Similarity factors f1 and f2 are introduced to compare dissolution profiles. The Higuchi and Korsmeyer-Peppas models for drug release are presented.
This document discusses various mathematical models used to study consolidation parameters and drug release from pharmaceutical formulations, including the Heckel, Higuchi, Korsmeyer-Peppas, and similarity factor (F1 and F2) models. It provides details on interpreting Heckel plots, limitations of the models, and their applications in understanding drug release mechanisms and comparing dissolution profiles. The summary concludes that these models are important tools for predicting drug release behavior from different drug delivery systems.
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 testing, which involves investigating the physical and chemical properties of a new drug substance alone and when combined with excipients. The overall objective is to generate information to help formulate stable and bioavailable dosage forms. Key aspects covered include organoleptic properties, purity, particle size and surface area. Common methods for analyzing these parameters, such as chromatography, microscopy, and gas adsorption, are also summarized. The goals are to provide critical data for developing optimized dosage forms that can be mass produced.
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 and physicochemical property of the drugSHIVANEE VYAS
“It is the study of the physical and chemical properties of the
drug prior to compounding process”.
Preformulation commences when a newly synthesized drug shows sufficient pharmacologic promise in animal models towarrant evaluation in man.
These studies should focus on physicochemical properties of new compound that affect drug performance & development of efficaciouss dosage form.
This properties may provide;
A rationale for formulation design
Support the need for molecular modification.
The document provides an overview of pre-formulation, which involves determining the physicochemical properties of a drug substance prior to developing a dosage form. It discusses the goals of pre-formulation to formulate an efficacious dosage form with good bioavailability. The protocol involves characterizing the physical, chemical, solubility, stability and compatibility properties of the drug. Key aspects covered include polymorphism, hygroscopicity, particle size, solubility, dissolution, stability in solution and solid state, and compatibility with excipients. The information guides subsequent formulation development.
This document discusses various parameters used to characterize drug release from pharmaceutical formulations. It describes diffusion parameters defined by Higuchi's equation and plots. Dissolution parameters like the effects of agitation, pH, temperature, and medium properties are outlined. Pharmacokinetic parameters including Cmax, Tmax, and AUC are defined. The Heckel equation is presented as a method to analyze powder compaction. Similarity factors f1 and f2 are introduced to compare dissolution profiles. The Higuchi and Korsmeyer-Peppas models for drug release are presented.
This document discusses various mathematical models used to study consolidation parameters and drug release from pharmaceutical formulations, including the Heckel, Higuchi, Korsmeyer-Peppas, and similarity factor (F1 and F2) models. It provides details on interpreting Heckel plots, limitations of the models, and their applications in understanding drug release mechanisms and comparing dissolution profiles. The summary concludes that these models are important tools for predicting drug release behavior from different drug delivery systems.
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 testing, which involves investigating the physical and chemical properties of a new drug substance alone and when combined with excipients. The overall objective is to generate information to help formulate stable and bioavailable dosage forms. Key aspects covered include organoleptic properties, purity, particle size and surface area. Common methods for analyzing these parameters, such as chromatography, microscopy, and gas adsorption, are also summarized. The goals are to provide critical data for developing optimized dosage forms that can be mass produced.
This document provides an overview of preformulation studies, which characterize the physical and chemical properties of new drug molecules to aid in the development of safe, effective, and stable dosage forms. Some key points covered include:
- Preformulation studies give direction for dosage form selection, excipient choice, composition, and process development.
- Important physicochemical properties to determine include solubility, partition coefficient, pKa, stability, and interactions with excipients.
- Methods are described for evaluating properties like solubility, dissolution, oxidation, hydrolysis, and polymorphism which can impact stability and bioavailability.
- Understanding these properties aids in developing robust formulations and setting appropriate storage conditions for drug products
This document discusses various pharmaceutical factors that should be considered during preformulation studies to develop safe and effective dosage forms. It outlines 7 key factors: 1) flow properties, determined through angle of repose, Hausner ratio, and Carr's index; 2) density; 3) compressibility; 4) hygroscopicity; 5) electrostatic charge, measured using devices like INOSTAT; 6) rheology, examining viscosity using various techniques; and 7) wettability, determined by contact angle between liquid and solid surface. The preformulation study aims to characterize the physical, chemical and mechanical properties of new drug molecules.
The document discusses key concepts and steps in preformulation testing. Preformulation involves investigating the physical and chemical properties of a drug substance alone and when combined with excipients. This generates useful information for formulating stable and safe dosage forms with good bioavailability. Some important properties discussed include solubility, particle size and shape, melting point, thermal analysis profile, hygroscopicity, and polymorphism potential. Determining these properties of a new drug substance is an important first step before developing drug formulations.
This document discusses pre-formulation studies, which involve investigating the physical and chemical properties of drug substances alone and when combined with excipients. Some key areas covered include polymorphism, hygroscopicity, particle size characterization, and solubility analysis. Thermal analysis techniques like DSC and XRD are described as useful for characterizing polymorphs. The importance of solubility studies at various pH levels and temperatures is highlighted for developing oral dosage forms with appropriate dissolution profiles.
Preformulation studies for bulk characterizationmangu3107
The document discusses preformulation studies, which generate information to help formulate stable and effective drug dosage forms. The overall goals of preformulation are to improve drug stability, bioavailability, and reduce incompatibility. Some key tests described include determining the drug's physical properties like color, odor, taste, purity, and thermal behavior. Melting point analysis can provide information on a drug's identity and purity. Preformulation studies are important to identify suitable drug candidates and formulations before clinical development.
This document provides an overview of preformulation factors affecting dosage forms. It discusses properties like flow, density, compressibility, and others that influence the development of safe and effective drug dosage forms. The goal of preformulation is to design dosage forms with good bioavailability. Various methods for characterizing properties are described, along with their importance in determining the suitable dosage form for a drug.
The document discusses preformulation and summarizes some of its key aspects. Preformulation involves determining the physicochemical properties of new drug substances to aid in developing effective dosage forms. It covers topics like organoleptic properties, purity, particle size and shape, solubilization using surfactants, and the effect of temperature, pH and co-solvents on solubility. It also mentions the importance of preformulation stability studies and considering drug characteristics for different dosage forms. The goals of preformulation are establishing parameters, kinetic profiles, physical characteristics and compatibility with excipients.
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.
The document discusses preformulation studies for solids. The objectives are to develop a stable, safe and effective dosage form with maximum bioavailability. Preformulation testing characterizes the physical, chemical and other properties of a new drug to aid in dosage form development. Studies include analyzing the drug's crystallinity, polymorphism, particle size, solubility, stability and compatibility with excipients. Analytical techniques used include microscopy, spectroscopy, chromatography and thermal analysis to understand the drug's properties and develop an optimal dosage form.
The document discusses suspensions, which are two-phase systems composed of solid particles dispersed in a liquid. Suspensions can be classified based on particle size as molecular, colloidal, or coarse dispersions. They can also be classified as flocculated or deflocculated based on how the particles interact. Factors like particle size, viscosity, density, and interfacial properties affect suspension stability. Common methods for producing suspensions include precipitation, dispersion, and controlled flocculation. The stability of suspensions is evaluated through sedimentation volume, degree of flocculation, and zeta potential measurements. Equipment like colloid mills and ultrasonic devices can be used to formulate suspensions.
The document discusses various techniques to improve the solubility of poorly soluble drugs, including salt formation, co-solvency, and particle size reduction. It focuses on using salt formation between flurbiprofen and tris(hydroxymethyl)aminomethane to increase solubility. Analytical techniques like DSC, TGA, HPLC, and UV were used to characterize the flurbiprofen-tris salt and showed improved solubility over flurbiprofen alone. The conclusion states that increasing water solubility of insoluble drugs is important for developing effective dosage forms and delivering drugs to the absorption site.
The document provides an overview of preformulation studies. It discusses the importance of characterizing the physical and chemical properties of new drug molecules during preformulation to aid in the development of stable dosage forms. Some of the key areas covered include drug-excipient compatibility studies, stability kinetics testing, and determining properties like solubility, partition coefficient, and polymorphism that can help dictate the suitable dosage form. The goal of preformulation is to gather necessary data to rationally develop safe and efficacious dosage forms.
Preformulation involves characterizing the physicochemical properties of a drug prior to formulation development. Key aspects of preformulation studied include determining solubility, stability, and bulk properties of the drug substance. Analytical methods are also developed to quantitatively analyze the drug. This information guides the selection of appropriate excipients and dosage forms that will deliver the drug safely and effectively.
This document discusses various parameters used to characterize drug release from pharmaceutical formulations, including diffusion parameters described by Higuchi's equation, dissolution parameters like the effects of agitation and pH, and pharmacokinetic parameters like Cmax, Tmax, and AUC. It also covers models like the Heckel equation that can be applied to understand powder compaction and the Korsmeyer-Peppas model for characterizing drug release mechanisms.
This document discusses several key areas of preformulation research for new drug candidates. These include analyzing organoleptic properties like color, odor and taste; bulk characterization of crystallinity, polymorphism and particle size; powder flow properties; solubility analysis including pH solubility profiles, partition coefficients and dissolution; and stability studies of solutions and solids, including compatibility with excipients. The goal of preformulation research is to better understand the physical and chemical properties of new drug substances to guide successful formulation development and scale-up of drug products.
This document discusses preformulation studies, which are important steps in developing an effective dosage form for a new drug. The objectives of preformulation studies are to establish the physico-chemical properties of the drug substance and generate information to design an optimal drug delivery system. Key aspects investigated include solubility, stability, compatibility with excipients, and parameters like particle size, bulk density and flow properties. Thorough preformulation work provides a foundation for formulation development and identifies potential problems to address.
This document summarizes key parameters related to consolidation and drug release from solid dosage forms. It discusses diffusion parameters defined by Higuchi's equation that are used to characterize drug release from modified release formulations. Dissolution parameters influenced drug release including effects of agitation, fluid properties, pH, surface tension and temperature. Pharmacokinetic parameters like Cmax, Tmax, and AUC that describe the plasma concentration time profile are also covered. The document also briefly mentions Heckel plots used to analyze powder deformation during compression and similarity factors F1 and F2 used to compare dissolution profiles.
This document summarizes various consolidation and dissolution parameters relevant to pharmaceutical dosage forms. It discusses diffusion parameters per Higuchi kinetics, dissolution parameters like effect of agitation and pH, pharmacokinetic parameters like Cmax and AUC, and methods to compare dissolution profiles using similarity factors f1 and f2. The Heckel plot is also introduced as a method to study mechanisms of powder consolidation under compression.
Preformulation involves characterizing the physicochemical properties of a new drug substance. This includes determining properties like solubility, melting point, particle size, and powder flow. Understanding these properties helps formulators design an optimal dosage form. Key goals of preformulation are generating useful data for formulators and establishing properties that may impact drug performance or development.
This document discusses the importance of preformulation studies, which involve characterizing the physical and chemical properties of a drug prior to formulation development. The major areas covered in preformulation include physical characterization of the drug's solid state, solubility analysis, and stability studies. Understanding properties like crystallinity, hygroscopicity, and solubility is crucial for developing a stable, safe, and effective dosage form. Key tests described are used to determine the drug's particle size, surface morphology, thermal behavior, polymorphism, and compatibility with excipients. The results of preformulation studies provide critical guidance for dosage form design and regulatory approval.
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, which characterize the physical and chemical properties of new drug molecules to aid in the development of safe, effective, and stable dosage forms. Some key points covered include:
- Preformulation studies give direction for dosage form selection, excipient choice, composition, and process development.
- Important physicochemical properties to determine include solubility, partition coefficient, pKa, stability, and interactions with excipients.
- Methods are described for evaluating properties like solubility, dissolution, oxidation, hydrolysis, and polymorphism which can impact stability and bioavailability.
- Understanding these properties aids in developing robust formulations and setting appropriate storage conditions for drug products
This document discusses various pharmaceutical factors that should be considered during preformulation studies to develop safe and effective dosage forms. It outlines 7 key factors: 1) flow properties, determined through angle of repose, Hausner ratio, and Carr's index; 2) density; 3) compressibility; 4) hygroscopicity; 5) electrostatic charge, measured using devices like INOSTAT; 6) rheology, examining viscosity using various techniques; and 7) wettability, determined by contact angle between liquid and solid surface. The preformulation study aims to characterize the physical, chemical and mechanical properties of new drug molecules.
The document discusses key concepts and steps in preformulation testing. Preformulation involves investigating the physical and chemical properties of a drug substance alone and when combined with excipients. This generates useful information for formulating stable and safe dosage forms with good bioavailability. Some important properties discussed include solubility, particle size and shape, melting point, thermal analysis profile, hygroscopicity, and polymorphism potential. Determining these properties of a new drug substance is an important first step before developing drug formulations.
This document discusses pre-formulation studies, which involve investigating the physical and chemical properties of drug substances alone and when combined with excipients. Some key areas covered include polymorphism, hygroscopicity, particle size characterization, and solubility analysis. Thermal analysis techniques like DSC and XRD are described as useful for characterizing polymorphs. The importance of solubility studies at various pH levels and temperatures is highlighted for developing oral dosage forms with appropriate dissolution profiles.
Preformulation studies for bulk characterizationmangu3107
The document discusses preformulation studies, which generate information to help formulate stable and effective drug dosage forms. The overall goals of preformulation are to improve drug stability, bioavailability, and reduce incompatibility. Some key tests described include determining the drug's physical properties like color, odor, taste, purity, and thermal behavior. Melting point analysis can provide information on a drug's identity and purity. Preformulation studies are important to identify suitable drug candidates and formulations before clinical development.
This document provides an overview of preformulation factors affecting dosage forms. It discusses properties like flow, density, compressibility, and others that influence the development of safe and effective drug dosage forms. The goal of preformulation is to design dosage forms with good bioavailability. Various methods for characterizing properties are described, along with their importance in determining the suitable dosage form for a drug.
The document discusses preformulation and summarizes some of its key aspects. Preformulation involves determining the physicochemical properties of new drug substances to aid in developing effective dosage forms. It covers topics like organoleptic properties, purity, particle size and shape, solubilization using surfactants, and the effect of temperature, pH and co-solvents on solubility. It also mentions the importance of preformulation stability studies and considering drug characteristics for different dosage forms. The goals of preformulation are establishing parameters, kinetic profiles, physical characteristics and compatibility with excipients.
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.
The document discusses preformulation studies for solids. The objectives are to develop a stable, safe and effective dosage form with maximum bioavailability. Preformulation testing characterizes the physical, chemical and other properties of a new drug to aid in dosage form development. Studies include analyzing the drug's crystallinity, polymorphism, particle size, solubility, stability and compatibility with excipients. Analytical techniques used include microscopy, spectroscopy, chromatography and thermal analysis to understand the drug's properties and develop an optimal dosage form.
The document discusses suspensions, which are two-phase systems composed of solid particles dispersed in a liquid. Suspensions can be classified based on particle size as molecular, colloidal, or coarse dispersions. They can also be classified as flocculated or deflocculated based on how the particles interact. Factors like particle size, viscosity, density, and interfacial properties affect suspension stability. Common methods for producing suspensions include precipitation, dispersion, and controlled flocculation. The stability of suspensions is evaluated through sedimentation volume, degree of flocculation, and zeta potential measurements. Equipment like colloid mills and ultrasonic devices can be used to formulate suspensions.
The document discusses various techniques to improve the solubility of poorly soluble drugs, including salt formation, co-solvency, and particle size reduction. It focuses on using salt formation between flurbiprofen and tris(hydroxymethyl)aminomethane to increase solubility. Analytical techniques like DSC, TGA, HPLC, and UV were used to characterize the flurbiprofen-tris salt and showed improved solubility over flurbiprofen alone. The conclusion states that increasing water solubility of insoluble drugs is important for developing effective dosage forms and delivering drugs to the absorption site.
The document provides an overview of preformulation studies. It discusses the importance of characterizing the physical and chemical properties of new drug molecules during preformulation to aid in the development of stable dosage forms. Some of the key areas covered include drug-excipient compatibility studies, stability kinetics testing, and determining properties like solubility, partition coefficient, and polymorphism that can help dictate the suitable dosage form. The goal of preformulation is to gather necessary data to rationally develop safe and efficacious dosage forms.
Preformulation involves characterizing the physicochemical properties of a drug prior to formulation development. Key aspects of preformulation studied include determining solubility, stability, and bulk properties of the drug substance. Analytical methods are also developed to quantitatively analyze the drug. This information guides the selection of appropriate excipients and dosage forms that will deliver the drug safely and effectively.
This document discusses various parameters used to characterize drug release from pharmaceutical formulations, including diffusion parameters described by Higuchi's equation, dissolution parameters like the effects of agitation and pH, and pharmacokinetic parameters like Cmax, Tmax, and AUC. It also covers models like the Heckel equation that can be applied to understand powder compaction and the Korsmeyer-Peppas model for characterizing drug release mechanisms.
This document discusses several key areas of preformulation research for new drug candidates. These include analyzing organoleptic properties like color, odor and taste; bulk characterization of crystallinity, polymorphism and particle size; powder flow properties; solubility analysis including pH solubility profiles, partition coefficients and dissolution; and stability studies of solutions and solids, including compatibility with excipients. The goal of preformulation research is to better understand the physical and chemical properties of new drug substances to guide successful formulation development and scale-up of drug products.
This document discusses preformulation studies, which are important steps in developing an effective dosage form for a new drug. The objectives of preformulation studies are to establish the physico-chemical properties of the drug substance and generate information to design an optimal drug delivery system. Key aspects investigated include solubility, stability, compatibility with excipients, and parameters like particle size, bulk density and flow properties. Thorough preformulation work provides a foundation for formulation development and identifies potential problems to address.
This document summarizes key parameters related to consolidation and drug release from solid dosage forms. It discusses diffusion parameters defined by Higuchi's equation that are used to characterize drug release from modified release formulations. Dissolution parameters influenced drug release including effects of agitation, fluid properties, pH, surface tension and temperature. Pharmacokinetic parameters like Cmax, Tmax, and AUC that describe the plasma concentration time profile are also covered. The document also briefly mentions Heckel plots used to analyze powder deformation during compression and similarity factors F1 and F2 used to compare dissolution profiles.
This document summarizes various consolidation and dissolution parameters relevant to pharmaceutical dosage forms. It discusses diffusion parameters per Higuchi kinetics, dissolution parameters like effect of agitation and pH, pharmacokinetic parameters like Cmax and AUC, and methods to compare dissolution profiles using similarity factors f1 and f2. The Heckel plot is also introduced as a method to study mechanisms of powder consolidation under compression.
Preformulation involves characterizing the physicochemical properties of a new drug substance. This includes determining properties like solubility, melting point, particle size, and powder flow. Understanding these properties helps formulators design an optimal dosage form. Key goals of preformulation are generating useful data for formulators and establishing properties that may impact drug performance or development.
This document discusses the importance of preformulation studies, which involve characterizing the physical and chemical properties of a drug prior to formulation development. The major areas covered in preformulation include physical characterization of the drug's solid state, solubility analysis, and stability studies. Understanding properties like crystallinity, hygroscopicity, and solubility is crucial for developing a stable, safe, and effective dosage form. Key tests described are used to determine the drug's particle size, surface morphology, thermal behavior, polymorphism, and compatibility with excipients. The results of preformulation studies provide critical guidance for dosage form design and regulatory approval.
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.
Techniques for enhancement of dissolution rateSagar Savale
The document discusses various techniques to enhance the dissolution rate of drugs, which is important for predicting bioavailability. It describes the process of dissolution and factors that influence the rate based on the Noyes-Whitney equation. Several methods are covered, including increasing surface area through particle size reduction, using surfactants, solid dispersions, polymorphism, molecular encapsulation, salt formation, and nanosuspensions. Enhancing dissolution rate can improve drug efficacy by increasing bioavailability.
Preformulation studies characterize the physical and chemical properties of new drug molecules to aid in developing safe, effective, and stable dosage forms. The objectives are to establish physico-chemical parameters, determine kinetics and stability, and establish compatibility with excipients. Major areas of investigation include organoleptic properties, bulk characterization like crystallinity and polymorphism, solubility analysis including pH effects, and stability analysis of solutions and solids. Understanding these properties provides insights for processing and storage to ensure drug quality.
The document discusses preformulation studies for new chemical entities. It defines preformulation studies and outlines their objectives. The major areas covered in preformulation research are physical description and bulk characterization, solubility analysis, and stability analysis. Key aspects studied include identification, purity, polymorphism, hygroscopicity, and thermal effects. Analytical methods are described for characterizing solid forms, solubility, and stability.
This document discusses preformulation studies, which characterize the physicochemical properties of new drug molecules to develop safe, effective, and stable dosage forms. It covers various areas of preformulation research like organoleptic properties, bulk characterization, crystallinity, polymorphism, hygroscopicity, micromeritic properties, solubility, pKa determination, and stability studies. Analytical techniques used for characterization include microscopy, DSC, IR, XRD, SEM, and TGA. The goals of preformulation are to establish the drug's properties, determine its kinetics and stability, ensure compatibility with excipients, and improve the drug product's manufacturing, storage and performance.
This document discusses various factors that influence drug delivery, including dissolution, absorption, and bioavailability. It covers topics like the balance between hydrophilic and lipophilic properties needed for drug delivery, how chemical and formulation modifications can impact bioavailability, and considerations for solid dosage forms like particle size and surface area. The purpose of drug formulation is to design a dosage form that safely delivers the right amount of active drug to the body at an optimal rate and extent.
This document discusses solubility and dissolution of solids in liquids, which are important processes in pharmaceutical solutions. It describes dissolution as a process where a substance goes into solution. Solubility is defined as the capacity of a solute to dissolve in a pure solvent. The document then discusses key steps in the dissolution process including removal of drug molecules from the solid state, formation of solvent cavities, and accommodation of drug molecules into the cavities. It presents the Noyes-Whitney equation, which describes dissolution rate in terms of surface area, concentration gradient, and diffusion coefficient. Finally, it notes that quality control dissolution testing is required by the FDA to ensure batch-to-batch uniformity of pharmaceutical formulations.
This document discusses preformulation studies, which involve characterizing the physical and chemical properties of drug substances prior to formulation development. It covers key topics like solubility profiling, polymorphism, particle size analysis, and flow properties. The goals are to establish parameters for new drugs and provide scientific data to support dosage form design and stability. Understanding preformulation can help develop stable, safe, and effective drug products.
consolidation parameters, consolidation definition, consolidation parameters,
diffusion parameters,
dissolution parameters,
heckle plot, consolidation process, cold welding, fusion bonding, mechanical theory, inter molecular forces theory, liquid surface film theory, factors effecting consolidation, driving froces that facilitate diffusion, parameters related to diffusion in drug release, parameters in dissolution process, affect of agitation on dissolution, effect of dissolution fluid on dissolution, pH on dissolution fluid, viscosity effect on dissolution, effect of temperature on dissolution, pharmacokinetics parameters, C max, T max, AUC(area under curve), heckel plot, application and limitations of heckel plot, methods to compare dissolution profile, model independent method(F1 AND F2)difference factor, similarity factors, limits of difference factor and similarity factors, higuchi model(Diffusion matrix formulation), korsmeyer peppas model(the power law).
Preformulation involves determining the physicochemical properties of new drug substances to establish parameters that may impact drug performance and dosage form development. Some key goals of preformulation testing include establishing a drug's physical characteristics, solubility, stability, and compatibility with excipients. Understanding properties like solubility, hygroscopicity, and powder flow help determine how a drug should be processed, stored, and formulated to ensure quality. Preformulation is an important first step in rational dosage form design.
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 presents information on preformulation studies, which involve characterizing the physicochemical properties of new drug molecules. The objectives are to generate stability and bioavailability data for formulation development. Key studies discussed include analyzing bulk properties, solubility, partitioning, hygroscopicity, ionization, dissolution, stability, and compatibility. Analytical techniques like spectroscopy, microscopy, thermal analysis, and chromatography are used to investigate properties and purity. Thorough preformulation provides critical information for designing dosage forms that are stable, safe, and effective.
PREFORMULATION STUDY IN DESIGNING OF TABLET DOSAGES FORM.pptxSWASTIKPATNAIK1
Preformulation studies are important for determining the physicochemical properties of new drug substances before developing dosage forms. This document outlines preformulation studies conducted for omeprazole magnesium and carbamazepine to aid in the development of enteric coated tablets and buccal mucoadhesive tablets, respectively. Key tests included solubility analysis, stability analysis, particle size characterization, and in vitro drug release studies. The results of these preformulation studies provided guidance on suitable excipients and helped establish formulation designs and processing parameters to achieve the desired drug delivery profiles.
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.
This document discusses various techniques for enhancing the solubility of poorly soluble drugs. It begins by defining solubility and factors that affect solubility such as particle size, temperature, and pressure. It then describes techniques like particle size reduction through micronization and nanosuspensions, modifying crystal habits through polymorphism, drug dispersion in carriers like solid dispersions and solid solutions, complexation using agents like cyclodextrins, and solubilization using surfactants to form microemulsions. Other approaches discussed include co-crystallization, cosolvency, hydrotrophy, and nanotechnology methods like producing nanocrystals. The conclusion emphasizes that solubility is a key factor in oral drug bioavailability and various
ISO/IEC 27001, ISO/IEC 42001, and GDPR: Best Practices for Implementation and...PECB
Denis is a dynamic and results-driven Chief Information Officer (CIO) with a distinguished career spanning information systems analysis and technical project management. With a proven track record of spearheading the design and delivery of cutting-edge Information Management solutions, he has consistently elevated business operations, streamlined reporting functions, and maximized process efficiency.
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Date: May 29, 2024
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A review of the growth of the Israel Genealogy Research Association Database Collection for the last 12 months. Our collection is now passed the 3 million mark and still growing. See which archives have contributed the most. See the different types of records we have, and which years have had records added. You can also see what we have for the future.
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.
The simplified electron and muon model, Oscillating Spacetime: The Foundation...RitikBhardwaj56
Discover the Simplified Electron and Muon Model: A New Wave-Based Approach to Understanding Particles delves into a groundbreaking theory that presents electrons and muons as rotating soliton waves within oscillating spacetime. Geared towards students, researchers, and science buffs, this book breaks down complex ideas into simple explanations. It covers topics such as electron waves, temporal dynamics, and the implications of this model on particle physics. With clear illustrations and easy-to-follow explanations, readers will gain a new outlook on the universe's fundamental nature.
How to Build a Module in Odoo 17 Using the Scaffold MethodCeline George
Odoo provides an option for creating a module by using a single line command. By using this command the user can make a whole structure of a module. It is very easy for a beginner to make a module. There is no need to make each file manually. This slide will show how to create a module using the scaffold method.
This slide is special for master students (MIBS & MIFB) in UUM. Also useful for readers who are interested in the topic of contemporary Islamic banking.
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.
2. These studies should focus on physicochemical properties of new
compound that affect drug performance & development of efficacious
dosage form.
Mostly investigation of physical and chemical property of a drug .
3. To establish the physicochemical parameters of a new drug.
To establish its physical characteristics .
To establish its compatibility with common excipients.
Providing a scientific data to support the dosage form design and
evaluation of the product efficacy and stability.
3
6. Drugs can be used therapeutically as solids, liquids and gases.
Liquid drugs are used to a much lesser extent than solid drugs
and even less frequently thangases.
Solid materials are preferred in formulation work because of
their ease of preparation into tablets and capsules.
The majority of drug substances in use occur as solid
materials.
Most of them are pure chemical compounds of either:
Amorphous or Crystalline in nature
7
7. CRYSTALLINITY AND POLYMORPHISM
Solid drug materials may occur as:
a. Amorphous (higher solubility)
b. Crystalline(higher stability)
The amorphous or crystalline characters of drugsare of
great importance to its ease of formulation and handling, its
chemical stability and its biological activity.
9
8. Amorphous drugs have randomly arranged atoms or
molecules.
Amorphous forms are typically prepared by ;
precipitation, lyophilization, or rapid cooling method.
Advantage:
Amorphous forms have higher solubilities as well as
dissolution rates as compared to crystalline forms.
Disadvantage:
Upon storage, sometimes amorphous solids tend to
revert to more stable forms. This instability can occur
during bulk processing or within dosageforms. 10
9. It is inactive when administered in crystalline form, but
when they are administered in the amorphous form,
absorption from the gastrointestinal tract proceeds
rapidly with good therapeutic response.
11
10. Crystals are characterized by repetitious spacing of constituent
atoms or molecules in a three dimensional array.
Crystalline forms of drugs may be used because of greater
stability than the corresponding amorphous form.
For example: the crystalline forms of penicillin G as
potassium or sodium salt is considerably more stable and
result in excellent therapeutic response than amorphous forms.
12
11. identical depending on the variation in;
a. Temperature
b. Solvent
c. Time
Polymorphism is the ability of a compound to
crystallize as more crystalline
different internal
than one distinct
lattices or crystalspecies with
packing arrangement even they are chemically
13
12. Different polymorphs exhibits different solubilities,
therapeutic activity and stability.
Chemical stability and solubility changes due to
polymorphism can have an impact on drug’sactivity.
14
15. Differential scanning calorimetry and Differential
thermal analysis: [DSC & DTA]
Measure the heat loss or gain resulting from physical or
chemical changes within a sample as function of temperature.
Thermo gravimetric analysis (TGA):
It measure changes in sample weight as a function of time
(isothermal) or function of time (isothermal) or temperature.
Desolvation and decomposition processes are frequently
monitored by TGA.
17
16. Purity, polymorphism, solvation, degradation, and
excipient compatibility.
Thermal analysis can be used to investigate and
predict any physicochemical interactions between
components in the formulation.
It is used for selection of chemically compatible
excipients.
18
17. It is an important technique for establishing the batch- to batch
reproducibility of a crystallineform.
Each diffraction pattern is characteristic of a specific
crystalline lattice for a givencompound.
Applications:
Quantitative ratios of two polymorphs and their
percentages of crystallinity may be determined.
crystalline forms can be Mixtures of different
analyzed using normalized intensities at specific
angles, which are unique for each crystallineform.
19
18. Many drugs , particularly water-soluble salts, have a
tendency to adsorb atmospheric moisture.
Changes in moisture level can greatly influence many
parameters such as ; chemical stability, flowability, and
compatibility.
Adsorption and equilibrium of moisture content can
depend upon ; atmospheric humidity, temperature,
surface area, exposure, and the mechanism for moisture
uptake.
20
19. It adsorbs water because of hydrate formation or
specific site adsorption.
Deliquescent materials:
Adsorb sufficient water to dissolve completely,
as observed with sodium chloride on a humidday.
Analytic methods for monitoring the moisture level
are ; gravimetric (weight gained), Karl Fischer
titration, or gas chromatography) according to the
desired precision & the amount of moisture adsorbed
onto the drug sample.
21
20. Certain physical and chemical properties of drug
substances are affected by the particle size
Size, shape & surface morphology of drug particles
affect the flow property, dissolution &chemical
reactivity of drugs.
Significance of Particle Size:
Particle size of drugs may affect formulation and
product efficacy.
distribution including; drug dissolution rate, content
uniformity, texture, stability, flow characteristics, and22
sedimentation rates.
21. Particle size significantly influences the oral
absorption profiles of certain drugs.
Satisfactory content uniformity in solid dosage
forms depends to a large degree on particle size and
the equal distribution of the active ingredient
throughout the formulation.
23
22. 1. Sieving or screening
2. Optical microscopy
3. Sedimentation
4. Stream scanning.
a relatively large sample
Sieving or screening:
Disadvantage: It requires
size.
Advantage: Simplicity in technique and equipment
requirements.
24
23. Disadvantage: Quantitative evaluations need minimum
1000 particles (tedious and time consuming). The slide
must be representative of the bulk of thematerial.
Sedimentation:
It utilize the relationship between rate of fall of
particles and their size.
Disadvantage:
Proper dispersion, consistent sampling temperature
control, must be carefully controlled to obtain
consistent and reliable results.
25
24. Technique utilizes a fluid suspension of particles which
pass the sensing zone where individual particles are
sized, counted & tabulated.
Sensing units are based on ; light scattering
transmission, as well as conductance.
The popular unit in the pharmaceutical industry for this
purpose is the Coulter Counter
Advantages:
The unit electronically size, count and tabulate the
individual particles that pass through the sensing zone
and data is obtained in a short time with reasonable
accuracy. 26
25. Thousands of particles can be counted in seconds and
used to determine the size distributioncurve.
It is a powerful tool and can be used for evaluation of
parameters as crystal growth in suspension
formulation.
27
26. It is observed by Scanning Electron Microscopy (SEM),
which serves to confirm the physical observations related to
surface area.
Surface morphology of drug can provide greater area for
various surface reactions such as; degradation, dissolution, or
hygroscopicity.
Surface roughness leads to poor powder flow characteristics
of powders due to friction and cohesiveness
28
27. Bulk density of a compound varies with the method
of crystallization, milling, or formulation.
Importance of bulk density:
Knowledge of the true and bulk densities of the drug
substance is useful in forming idea about the size of
the final dosage form.
The density of solids also affects their flow
properties.
29
28. Flow properties are significantly affected by:Changes in
particle size, density, shape, and adsorbed moisture, which
may arise from processing or formulation.
The powder flow properties can be characterized by the
following methods:
30
29. It is the maximum angle between the surface of a pile
of powder and horizontal plane
Tan θ= h/r
The rougher and more irregular the surface of the
particles, the higher will be the angle ofrepose.
Lower values indicates better flow characteristics.
31
30. Angle of repose Type of flow
< 20 Excellent flow
20-30 Good flow
30-34 Passable
>40 Poor flow
The acceptance criteria for angle of reposeare:
32
31. Compressibility:
It can be characterized by the followingmethods;
1. Carr’s compressibility index
2. Hausner`s ratio
1. Carr’s compressibility index:
Carr’s index (%) =Tapped density–bulk density x100
Tapped density
By decreasing the bulk and tapped density good flow
properties can be obtained. 33
32. Carr’s index Type of flow
5-15 Excellent
12-16 Good
18-21 Fair to passable
23-35 Poor
33-38 Very poor
>40 Extremely poor 34
33. Hausner `s ratio = Tapped density X 100
bulk density
The acceptance criteria for Hausner`s ratio are:
:
Hausner`s ratio Type of flow
< 1.25 Good flow
> 1.5 Poor flow
1.25-1.5 Glidant addition required
>1.5 Glidant doesn’t improve
flow
35
34. The solubility of drug is an important
physicochemical property because it affects the rate of
drug release
consequently,
into the dissolution medium and
the therapeutic efficacy of the
pharmaceutical product.
The solubility of a material is usually determined by
the equilibrium solubility method, which employs a
saturated solution of the material, obtained by stirring
an excess of material in the solvent for a prolonged
period until equilibrium is achieved.
General rules –
1. Polar solutes dissolve in polarsolvents
2. Non-polar solutes dissolve in non-polarsolvents
36
36. Description Approximate
weight of
solvent(g)
necessary to
dissolve 1g of
solute
Solubility(%w/v)
Very soluble <1 10-50
Freely soluble 1-10 3.3-10
Soluble 10-30 1-3.3
Sparingly soluble 30-100 0.1-1
Slightly soluble 100-1000 0.01-.1
Very slightly soluble 1000-10000 0.01-0.1 38
Poorly soluble >10000 <0.01
37. For a compound containing basic or acidic functional
groups, solubility at a given pH is influenced by the
compound’s ionization characteristics.
The solubility of a compound in aqueous media is
greater in the ionized state than in the neutral state.
Thus, solubility of ionizable compounds isdependent
on the pH of the solution.
The method for the determination of pKaaccording
to the nature of drug can be explainedas:
39
38. Nature of drug Ionization pKa
Very weak acid Unionized at all pH >8
Moderately weak
acid
Unionized at
gastric pH-1.2
2.5-7.3
Strong acid Ionize at all pH <2.5
Very weak base Unionize at all pH <5
Moderately weak
base
Unionize at
intestinal pH
5-11
Strong base Ionize at all pH
40
>11
39. Determination of the dissociation constant for a drug
capable of ionization within a pH range of 1 to
10 is important since solubility, and consequently
absorption, can be altered by changing pH.
The Henderson-Hasselbalch equation provides an
estimate of the ionized and un-ionized drug
concentration at a particular pH.
For acidic compounds:
pH = pKa + log ([ionized drug]/[un-ionized
drug])
For basic compounds:
pH = pKa + log ([un-ionized drug]/[ionized
drug])
41
40. The various methods for the determination of pKaare;
a. Potentiometric method
b. Spectrophotometric method
c. Solubility method
d. Conductometric method
42
41. Partition coefficient (oil/water) is a measure of a
drug's lipophilicity and an indication of its ability to
cross cell membranes.
Define:
It is defined as the ratio of un-ionized drug
distributed between the organic and aqueous phases at
equilibrium.
Po/w = (Coil/C water)equilibrium
Drugs having values of P much greater than 1 are
classified as lipophilic, whereas those withpartition
coefficients much less than 1 are indicative of a
hydrophilic drug
43
42. Preformulation stability studies are usually the first
quantitative assessment of chemical stability of a
new drug.
These studies include both solution and solid state
experiments under conditions typical for the
handling, formulation, storage, and administration of
a drug candidate as well as stability in presence of
other excipients.
critical in Factors affecting chemical stability
rational dosage form design include;
Temperature
pH
Dosage form diluents
44
43. e.g. acid labile drugs intended for oral
administration must be protected from the highly
The effect of pH on drug stability is important in the
development of both oral and parenteral dosage
forms
acidic environment of the stomach.
Buffer selection for parenteral dosage forms will
also be largely based on the stability characteristics
of the drug.
45
44. PHARMACEUTICAL DISPERSION
The term "Disperse System" refers to a system in which one
substance (the dispersed phase) is distributed, in discrete units,
throughout a second substance (the continuous phase or
vehicle). Each phase can exist in solid, liquid, or gaseous state.
COARSE DISPERSION SYSTEM
• Emulsion
• Colloids
• Suspension
EMULSION
An emulsion may be defined as a biphasic system
consisting of two immiscible liquids, one of which
(the dispersed phase) is finely and uniformly dispersed
as globules throughout the second phase (the
continuous phase). Since emulsions are a
thermodynamically unstable system, a third agent, the
emulsifier is added to stabilize the system. The particle
size of the dispersed phase commonly ranges from 0.1 to
100 µm
45. •Oil in water emulsion
•Water in oil emulsion
•Multiple emulsion
PREPARATION OF EMULSION
General method
Generally, an O/W emulsion is prepared by dividing the oily
phase completely into minute globules surrounding each globule
with an envelope of emulsifying agent and
finally suspends the globules in the aqueous phase. Conversely,
the W/O emulsion is prepared by dividing aqueous phase
completely into minute globules surrounding each globule with an
envelope of emulsifying agent and finally suspending the
globules in the oily phase.
46. Phase inversion method
In this method, the aqueous phase is first added to the
oil phase so as to form a W/O emulsion. At the
inversion point, the addition of more water results in
the inversion of emulsion which gives rise to an O/W
emulsion.
Continental and dry gum method
Extemporaneously emulsions are usually made by
continental or dry gum method. In this method, the
emulsion is prepared by mixing the emulsifying
agent (usually acacia) with the oil which is then mixed
with the aqueous phase. Continental and dry gum
methods differ in the proportion of constituents.
47. In this method, the proportion of the constituents is same as
those used in the dry gum method; the only difference is the
method of preparation. Here, the mucilage of the emulsifying
agent (usually acacia) is formed. The oil is then added to the
mucilage drop by drop with continuous titration.
Membrane emulsification method
It is a method, which is based on a novel concept of
generating droplets “drop by drop” to produce emulsion.
Here, a pressure is applied direct to the dispersed phase which
seeps through a porous membrane into the continuous phase
and in this way the droplets formed are then detached from
the membrane surface due to the relative shear motion
between the continuous phase and membrane surface.
48. Stability of emulsions A very important parameter for emulsion
products is their stability; however, the evaluation of emulsion
stability is not easy. Pharmaceutical emulsion stability is
characterized by the absence of coalescence of dispersed phase,
absence of creaming and retaining its physical characters like
elegance, odour, colour and appearance. The instability of emulsion
may be classified into four phenomenons Flocculation,
creaming, coalescence and breaking.
Creaming is the phenomenon in which the dispersed phase
separates out, forming a layer on the top of the continuous phase.
It is notable that in creaming, the dispersed phase remains in
globules state so that it can be redispersed on shaking. Creaming can
be minimized if the viscosity of the continuous phase is increased.
49. EMULSION STABILITY ASSESSMENT
Emulsion stability must be regarded in terms of physical
stability of emulsion system examined and the physical and
chemical stability of the emulsion components .
Macroscopic examination
The degree of creaming or coalescence occurring per unit
period of time can give the assessment of emulsion physical
satiability. This procedure is carried out by calculating the
ratio of the volume of the creamed part (separated part) of
the emulsion and the total volume of
the product.
Determination of particle size and particle count/globule
size analysis
Determination of changes in the average particle size is one
of the parameters used for assessing emulsion stability.
Optical microscopy, Andreasen apparatus and Coulter
counter apparatus are used for this purpose.
50. Determination of viscosity/viscosity changes
A change in the globule size or number or migration of
emulsifying agent during aging may be detected by a
change in apparent viscosity. Emulsions follow non-Newtonian
flow characteristics. Flocculation in O/W emulsions results in an
immediate increase in Viscosity.
Determination of electrophoretic properties
Zeta potential is an important parameter used for assessing
emulsion stability, since electric charges on the particles
affect the rate of flocculation. Electrostatically emulsion
stabilization is due to the mutual repulsion between electrical
double layer of both phases. Such type of stability is very
sensitive to the ionic strength of solution, as the concentration
of electrolyte increases the electrical double layer compressed
and the distance of electrostatic repulsion is reduced resulting in
flocculation.
51. Dilution test/miscibility test
Miscibility test involves the addition of continuous phase, e.g.
in case of O/W emulsion; the emulsion remains stable upon
unlimited addition of water but will become unstable upon
unlimited addition of oil, that is, the oil will separate. Vice
versa is the case with W/O emulsion
Electrical conductivity test
Water is a good conductor of electricity; hence, an emulsion
with water continuous phase will readily conduct electricity
while that with oil continuous phase will not.
Staining test/dye-solubility test
In this test, a small amount of water soluble dye, such as
methylene blue is added to the emulsion, now if water is the
continuous phase (O/W emulsion), dye will dissolve uniformly
throughout the system. If oil is the continuous phase (W/O
emulsion), dye will remain as cluster on the surface of the
system.
52. A Pharmaceutical suspension is a disperse system in which
internal phase is dispersed uniformly as finely divided
insoluble particles throughout the external phase. The internal
phase consisting of insoluble solid particles having a specific
range of size which is maintained uniformly throughout the
suspending vehicle with aid of single or combination of
suspending agent.The external phase (suspending medium) is
generally aqueous in some instance, may be an organic or oily
liquid for non oral use.
FORMULATION OF SUSPENSIONS
The three steps that can be taken to ensure formulation of an
elegant pharmaceutical suspension are:
1.CONTROL PARTICLE SIZE. On a small scale, this can be
done using a mortar and a pestle to grind down ingredients to
a fine powder.
2. Use thickening agent to increase viscosity of the vehicle by
using suspending agents or viscosity increasing agents.
3. Use of a wetting agent/ surfactants
53. Factors that contribute to appreciable stability of a suspension
include:
a)Small particle size- reduce the size of the dispersed particle
increases the total surface area of the solid. The greater the
degree of subdivision of a given solid the larger the surface
area. The increase in surface area means also an increase in
interface between the solids and liquids leading to an increase in
viscosity of a system.
b). Increasing the viscosity – increasing the viscosity of the
continuous phase can lead to the stability of suspensions. This is
so because the rate of sedimentation can be reduced by increase
in viscosity.
Viscosity increase is brought about by addition of thickening
agents to the external phase. In water these must be either
soluble or swell. It is important to note that the rate of release of
a drug from a suspension is also dependent on viscosity. of a
product. The more viscous the preparation, the slower is likely to
be the release of a drug. Sometimes this property may be
desirable for depot preparation.
54. C). TEMPERATURE.
Another factor which negatively affects the stability and
usefulness of pharmaceutical suspensions is fluctuation of
temperature.
Temperature fluctuations can lead to caking and claying.
55. Self-microemulsifying drug delivery (SMEDDS) is the one of
the method for the improvement of oral bioavailability.
SMEDDS are class of emulsion that has received particular
attention as a means of enhancing oral bioavailability of
poorly absorbed drugs. These systems are essentially mixes of
oil and surfactant (sometimes with added co surfactant) that
form emulsion on mixing with water with little or no energy
input.
SMEDDS or self-emulsifying oil formulations (SEOF) are
defined as isotropic mixtures of natural or synthetic oils,
solid or liquid surfactants, or alternatively, one or more
hydrophilic solvents and co-solvents/surfactants. Upon mild
agitation followed by dilution in aqueous media, such as GI
fluids, these systems can form fine oil-in-water (o/w)
emulsions or microemulsions. Self-emulsifying formulations
spread readily in the GI tract, and the digestive motility of
the stomach and the intestine provide the agitation necessary
for self-emulsification.
56. Viscosity Theory
As per this theory, an increase in viscosity of emulsions will lead
to an increase in stability.
Film theory Or absorption theory
As per this theory an added emulsifying agenagent forms a
mechanical film by getting adsorbed at Interfaces of liquid. This
offers stability to the emulsions.
Wedge theory
As per this theory monovalent soaps like sodium sterate gives o/w
type emulsions and divalent soaps like calcium sterate gives w/o
type emulsions. This was successfully explained by
accommodation of soap molecules at the interface and subsequent
possible orientation of the soap molecule to give the type of
emulsions. Limitation of this theory is that it could not explain the
stability of emulsions.
Interfacial tension theory
Initially when the oil and water are mixed together they will
become immiscible due to interfacial tension. The added
emulsifying agent reduce the interfacial tension and hence a stable
emulsion is formed.
57. Parenterals are the sterile dosage form intended for
administration other than enteral route and extent
their action by directly entering into systemic
circulation.
CLASSIFICATION :
Based on volume they are classified into two types :
Small volume parenterals (SVP’s)
E.g. Paracetamol IP150 mg(2ml)
Large volume parenterals (LVP’s)
E.g. Piracetam I.P. -200 mg /ml15 ml(20ml)/ 60
ml(100ml)
58. Based on volume they are classified into two types :
Small volume parenterals (SVP’s)
E.g. Paracetamol IP150 mg(2ml)
Large volume parenterals (LVP’s)
E.g. Piracetam I.P. -200 mg /ml15 ml(20ml)/ 60
ml(100ml)
59.
60. Leakage test
The leaker test is intended
to detect incompletely
sealed ampoules, so that
they may be discarded.
Tip sealed ampoules are
more prone to leak than
pull sealed. ... The visual
inspection is done by
holding the ampule by its
neck against highly
illuminated screens.
62. 30 Sterile units are selected from each batch.
The weight of 10 individual sterile units is noted and
the content is removed from them and empty
individual sterile units is weighed accurately
Then net weight is calculated by subtracting empty
sterile unit weight from gross weight.
PYROGEN TEST : The test involves measurement of the
rise in body temperature of rabbit following the IV
injection of a sterile solution into ear vein of rabbit
Dose not exceeding 10ml per Kg injected intravenously
within a period of not more than 10 min
63. 1. Handbook of preformulation by Srafaraz K. niazi
2. Dosage form design by Dr. Javed ali, Dr. khar
,Dr.Ahuja,1st edition ,2004-2005
3. H. Brittain, Polymorphism in Pharmaceutical Solids,
Marcel Dekker, Inc., 1999.
46