Theory and Practice of Physical Pharmacy

Author: Jain> Gaurav  

Publisher: Elsevier Health Sciences APAC‎

Publication year: 2013

E-ISBN: 9788131232651

P-ISBN(Paperback): 9788131228241

Subject: R9 Pharmacy

Keyword: 药学

Language: ENG

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Description

A core subject in pharmaceutics, physical pharmacy is taught in the initial semesters of B. Pharm. The methodical knowledge of the subject is required, and is essential, to understand the principles pertaining to design and development of drug and drug products. Theory and Practice of Physical Pharmacy is unique as it fulfils the twin requirements of physical pharmacy students: the authentic text on theoretical concepts and its application including illustrative exercises in the form of practicals.Covers all the topics included in various existing syllabi of physical pharmacy Provides an integrated understanding of theory and practical applications associated with physicochemical concepts Explore the latest developments in the field of pharmaceutics Reviews the relevance of physicochemical principles in the design of dosage form Ensures proper recapitulation through sufficient end-of-chapter questions Provides valuable learning tool in the form of multiple choice questions Multiple choice questions section especially useful for GPAT aspirants

Chapter

Charles' law

Gay-Lussac's law

Avogadro's law

Molecular Weight Determination

Real Gases

Liquid State

Viscosity

Surface Tension

Vapour Pressure

Solid State

Crystalline Solids

Types of crystalline solids

Polymorphism

Polycrystalline Solids

Amorphous Solids

Liquid Crystal State

Characteristics of Liquid Crystal State

Types of Liquid Crystals

Supercritical Fluid State

Plasma

Changes in the State of Matter

Liquefaction of Gases

Aerosols

Boiling Point

Melting Point

Phase Rule

Single component (C=1) system (Fig. 1.7)

At triple point

At points 1, 2 and 3

Two-component (C=2) system containing liquid phases (Fig. 1.8)

Two-component (C=2) system containing solid and liquid phases (Fig. 1.9)

Three-component (C=3) system (Fig. 1.10)

Chapter 2 - Micromeritics

Fundamental Properties of Particles

Particle Size and Size Distribution

Spherical or symmetrical particle

Nonspherical or asymmetrical particle

Particle size distribution

Average particle size

Frequency distribution curve

Cumulative frequency distribution curve

Log-probability curve

Particle Size Determination Methods

Optical Microscopy

Advantage

Disadvantages

Alternative techniques

Sieving Technique

Advantages

Disadvantages

Alternative techniques

Sedimentation Technique

Advantages

Disadvantages

Alternative techniques

Coulter Counter Method (Particle Volume Measurement)

Advantages

Disadvantages

Hatch-Choate equation

Particle Number

Particle Shape

Shape factors

Surface-volume shape coefficient

Sphericity

Elongation

Convexity

Circularity

Particle Surface Area

Specific surface

Surface Area Determination Methods

Adsorption Method

Solute adsorption method

Gas adsorption method

Air Permeability Method

Derived Properties Of Powders

Packing Geometry

Porosity (E)

Density (ρ)

Density Determination Methods

Bulk Density

Method I-Graduated cylinder method

Method II-Scott volumeter

Tapped Density

Method I

True Density

Gas pycnometer

Liquid displacement

Granular Density

Mercury displacement method or mercury porosimetry

Bulkiness

Flow Property

Characterization Of Powder Flow

Compressibility Index

Angles of repose

Static angle of repose

Dynamic or kinetic angle of repose

Flow Rate Through an Orifice

Improvement of Flow Property

Chapter 3 - Pharmaceutical Rheology

Fundamental Concepts

Elastic Deformation and Viscous Flow

Elasticity

Hooke's law of elasticity

Viscosity

Newton's law of viscous flow

Temperature Dependence of Viscosity

Newtonian Fluids

Rheogram and viscogram

Non-Newtonian Fluids

Time-Independent Non-Newtonian Fluids

Plasticity

Rheogram and viscogram

Reason

Pseudoplasticity

Rheogram and viscogram

Reason

Dilatancy

Rheogram and viscogram

Reason

Time-Dependent Non-Newtonian Flow

Thixotropy

Hysteresis loop

Bulges and spurs in thixotropy

Rheopexy

Negative Thixotropy or Antithixotropy

Negative Rheopexy

Determination of Rheological Properties: Measurement of Viscosity

Capillary Viscometers

Ostwald viscometer

Ubbelohde suspended level viscometer

Extrusion rheometer

Density-Dependent Viscometers

Falling sphere viscometer

Bubble viscometer

Rotational Viscometers

Cup and bob viscometers

Cone and plate viscometers

Penetrometers

Non-Newtonian Corrections

Measurement of Thixotropy

Structural Breakdown with Increasing Rates of Shear (M)

Structural Breakdown with Time at Constant Rate of Shear (B)

Viscoelasticity

Viscoelasticity Mechanism

Viscoelastic Models

Maxwell model

Kelvin-Voigt model

Standard linear solid model (Maxwell form)

Weichert model

Viscoelastic Creep

Specialized Pharmaceutical Applications of Rheology

Yield Value and Suspensions

Plug Flow-Artifactual Observations

Rheological Use of Mixing Equipment

Biorheology

Chapter 4 - Surface and Interfacial Phenomena

Surface-Active Agents (Surfactants)

Classification of Surfactants

Anionic surfactants

Alkali soaps (sodium and potassium stearate)

Metallic soaps (calcium stearate)

Amine soaps

Alkyl sulphates and phosphates (sodium lauryl sulphate)

Alkyl sulphonates (sodium dioctyl sulphosuccinate also known as aerosol AT)

Cationic surfactants

Ampholytic surfactants

Nonionic surfactants

Sorbitan esters (Spans)

Polysorbates (Tweens)

Polymeric surfactants

Hydrophilic-Lipophilic Balance Concept

Calculation of HLB value

Required HLB

Determination of Surfactant Amount

Application of Surfactants

Medicinal applications

Pharmaceutical applications

Surface And Interfacial Tension

Expression of Surface Tension

In terms of force per unit length

In terms of energy per unit area increase

In terms of pressure difference across curved surface

Measurement Of Surface And Interfacial Tension

Capillary Rise Method

Upward force due to surface tension

Downward force due to the weight of the liquid

Drop Weight and Drop Count Methods

Wilhelmy Plate Method

Ring Detachment Method (du Nouy tensiometer)

Spinning Drop Method

Wetting And Contact Angle

Spreading

Spreading Coefficient (S)

Work of adhesion (WJa)

Work of cohesion (WJc)

Critical Micelle Concentration

Influence of CMC on the Physical Properties

Factors Affecting CMC

Molecular structure of the surfactant

Hydrocarbon chain in the hydrophobic group

Hydrophilic group

Effect of additives

Effect of temperature

Effect of counterions

Surface Films

Insoluble Monomolecular Films

Interfacial Complex Condensed Films

Lamellar Liquid Crystalline Films

Adsorption Phenomena

Adsorption Isotherm

Langmuir isotherm

Freundlich isotherm

BET isotherm

Factors Affecting Adsorption

Applications of Adsorption

Electrical Properties Of Interfaces

Electrical Double Layer

Specialized Surfactant Based Systems

Liquid Crystals

Vesicular Systems

Liposomes

Niosomes

Chapter 5 - Buffers and Isotonic Solutions

Buffer equation

Autoionization of Water

Buffer Equation for Weak Acid and Its Salt

Buffer Equation for Weak Base and Its Salt

Buffer Capacity

Buffer Preparation

Standard Buffer Solution

Selection of Buffer System

Pharmaceutical Buffers

Stabilization of Drug Substances in Formulations by Buffers

Use of Buffers to Study the pH-stability Profile of Drug Substances

Use of Buffers to Study the pH Dependence of Drug Substance Solubility

Biological Buffers

Buffered Isotonic Solutions

Methods of Adjusting Tonicity

Class I Methods

Cryoscopic method

Sodium chloride equivalent method

Class II Methods

White-Vincent method

Sprowls method

Tonicity Application

Ophthalmic medication

Parenteral medication

Chapter 6 - Complexation and Protein Binding

Classification of Complexes

Coordination Complexes

Inorganic Complexes

Chelates

Olefin Complexes

Aromatic Complexes

Organic Molecular Complexes

Charge-Transfer Complexes

Quinhydrone Complex

Picric Acid Complexes

Hydrogen-Bonded Complexes

Caffeine complexes

Polymeric Complexes

Inclusion Compound (Or No Bond Complexes)

Clathrates

Example

Channel Lattice Complexes

Intercalation Compound or Layer-type Complexes

Monomolecular Inclusion Compounds

Example: Cyclodextrins

Macromolecular Inclusion Compounds

Methods of Analysis

Job's Method of Continuous Variation

pH Titration Method

Phase-Distribution Method

Solubility Method

Protein Binding: Small Molecule-Macromolecule Complexes

Significance of Protein Binding

Binding Equilibria

Methods for Determining Protein Binding

Equilibrium dialysis method

Dynamic dialysis

Ultracentrifugation

Thermodynamic Treatment of Stability Constants

Chapter 7 - Colloidal Dispersions

Classification of Colloids

Lyophilic Colloids

Lyophobic Colloids

Association Colloids (Micelles)

Preparation of Colloidal Dispersions

Lyophilic Colloids

Lyophobic Colloids

Condensation methods

Dispersion methods

Properties of Colloidal Dispersions

Kinetic Properties

Brownian motion

Diffusion

Sedimentation

Osmotic pressure

Viscosity

Optical Properties

Light scattering

Electrical Properties

Stability of Colloidal Systems

Stability of lyophobic colloids-DLVO theory

Stability of lyophilic colloids

Interaction of Colloids

Colloidal Drug-Delivery Systems

Chapter 8 - Pharmaceutical Suspensions

Utility Of Suspensions

Theoretical Considerations

Particle Size Consideration

Interfacial Region

Wetting and Contact Angle

Particle Behaviour and Interactions

Electric double layer

Flocculated and Deflocculated Suspensions

Formulation Components

Wetting Agents

Deflocculants and Dispersing Agents

Flocculating Agents

Suspending Agents

Organoleptic Agents

Suspension Formation

Precipitation Method

Dispersion Method

Controlled Flocculation

Structured Vehicle

Stability of Suspension

Chemical Stability

Physical Stability

Sedimentation rate

Particle growth

Crystal growth or Ostwald ripening

Polymorphic transformation

Crystal habit

Temperature cycling

Evaluation of Suspension Stability

Organoleptic Aspects (Colour, Taste and Flavour)

Sedimentation Parameters

Sedimentation volume

Degree of flocculation

Rheologic Methods

Electrokinetic Techniques

Particle Size Changes

Packaging

Pharmaceutical Nanosuspensions

Chapter 9 - Pharmaceutical Emulsions

Utility of Emulsions

Theoretical Considerations

Reduction of Interfacial Tension: Thermodynamic Stabilization

Interfacial Film Formation: Mechanical Barrier to Coalescence

Monomolecular film formation by surface-active agents

Multimolecular film formation by hydrophilic colloids

Solid particle film formation by finely divided solids

Electrical Repulsion: Electrical Barrier to Approach of Particles

Formulation Components

Oil Phase

Emulsifiers

Determination of emulsifier amount

Auxiliary Emulsifiers

Hydrophilic colloids

Finely divided solids

Viscosity Modifiers

Preservatives

Antioxidant

Emulsification Techniques (Emulsion Formation)

Conventional Method

Condensation Method

Phase Inversion Technique

Low-Energy Emulsification

Spontaneous Emulsification

Production Aspects

Foaming During Agitation

Emulsion Type

Microemulsions

O/w micellar solution

W/o micellar solution

Stability of Emulsions

Physical Stability

Symptoms of Instability

Flocculation

Creaming

Coalescence and breaking

Phase inversion

Chemical Stability

Oxidation

Microbial Contamination

Assessment of Emulsion Shelf Life

Stress Conditions

Ageing and temperature

Centrifugation

Agitation

Rheology of Emulsion

Chapter 10 - Diffusion and Drug Release

Laws of Diffusion

Fick's First Law

Fick's Second Law

Steady-State Diffusion

Measurement of Diffusion

Applications of Diffusion Principles

Drug Absorption by Passive Diffusion

Drug Absorption by Facilitated Diffusion

Percutaneous or Transdermal Absorption

Ostwald Ripening in Emulsions

Bioadhesion and Mucoadhesion

In Vitro Permeation Studies

Osmotically Controlled Delivery Systems

Drug Release from Polymer Matrices

Reservoir Systems

Matrix/monolithic Systems

Membrane-Matrix System

Diffusion During Swelling of Matrix

Diffusion in Matrix Erosion

Chapter 11 - Drug Dissolution

Dissolution Mechanism

Reaction-Limited Model

Interfacial barrier model (Limited solvation theory)

Danckwert model

Diffusion-Limited Model or Film Theory

Noyes-Whitney Relationship

Hixon-Crowell Cubic Root Law

Factors Affecting Dissolution

Factors Affecting the Surface Area of the Drug (S)

Particle size

Wetting

Manufacturing processes

Formulation ingredients

Factors Affecting the Saturation Solubility of the Drug (Cs)

GL pH

Crystalline state

Drug complex

pKa and pH profile

Temperature

Factors Affecting Dissolution Volume (V)

Factors Affecting Diffusivity (D)

Factors Affecting the Thickness of Hydrodynamic Layer (h)

Dissolution Test Parameters

Eccentricity of the stirring device

Alignment of the stirring element

Vibration

Agitation intensity

Intrinsic Dissolution

Compendial Dissolution Methods

Dissolution Apparatus

Basket Apparatus (USP Apparatus 1)

Paddle Apparatus (USP Apparatus 2)

Dissolution Conditions

Dissolution Profile Comparison

Difference factor (f1)

Similarity factor (f2)

In Vitro-In Vivo Correlation

Level A

Level B

Level C

Multiple level C

Biopharmaceutical Classification System

Solubility

Permeability

Dissolution

Chapter 12 - Kinetics, Degradation and Stability

Rate of Reaction

Elementary Reaction

Nonelementary Reaction

Order of Reaction

Molecularity of Reaction

Types of Reaction

Zero-Order Reaction

Example

First-Order Reaction

Example

Second-Order Reaction

Example

Apparent/Pseudo-Zero-Order Reaction

Pseudo-First-Order Reaction

Example

Determination of Order of Reaction

Graphical Substitution Method

Half-Life Method

Complex Reactions

Reverse/Opposing Reactions

Consecutive/Series Reactions

Side/Parallel Reactions

Factors Influencing Reaction Rates

Temperature

Collision theory

Transition-state theory

Influence of temperature

Calculation of Ea

Method 1

Method 2

Medium Effects: Solvent, Ionic Strength and Dielectric Constant

Solvent

Ionic strength

Dielectric constant

pH-Specific Acid-Base Catalysis

General Acid-Base Catalysis

Decomposition and Stabilization of Pharmaceuticals

Degradative Pathways

Hydrolysis

Ester hydrolysis

Amide hydrolysis

Ring alteration

Protection from hydrolysis

Oxidation

Initiation

Propagation

Hydroperoxide decomposition

Termination

Protection from Oxidation

Photolysis

Racemization

Stability Testing

ICH Stability Guidelines

Thermal cycling studies

Photostability studies

Expiration Dating of Pharmaceuticals

Accelerated Stability Studies (Shelf-Life Determination)

Prediction of shelf life from accelerated stability-testing data

Practical Example: Estimation of degradation from accelerated data: First-order case

Solution

Limitations of Accelerated Stability Testing

Other Techniques for Stability Prediction

Experiment 1 Ternary Phase Diagram

Objective

Requirements

Procedure

Observation and Calculation

Result

Experiment 2 Particle Size By Optical Microscopy

Objective

Requirements

Procedure

Observations and Calculations

Result

Experiment 3 Particle Size By Sieving

Objective

Requirements

Procedure

Observations and Calculations

Result

Experiment 4 Flow Property Of Powder

Objective

Requirements

Procedure

Observations and Calculations

Result

Experiment 5 Angle Of Reposex

Objective

Requirements

Procedure

Observations and Calculations

Observations and Calculations

Result

Experiment 6 Density Determination

Objective

Requirements

Procedure

Observations and Calculations

Result

Experiment 7 Ostwald Viscometer

Objective

Requirements

Procedure

Observations and Calculations

Result

Experiment 8 Falling Sphere Viscometer

Objective

Requirements

Procedure

Observations and Calculations

Correction Factor

Result

Experiment 9 Spreading Coefficient

Objective

Requirements

Procedure

Observations and Calculations

Result

Experiment 10 Critical Micelle Concentration

Objective

Requirements

Procedure

Observations and Calculations

Calculation of Surface Tension

Determination of CMC

Result

Experiment 11 Buffer preparation

Objective

Requirements

Procedure

Observation and Calculation

Result

Experiment 12 Colloidal Solution

Objective

Requirements

Procedure

Observations

Result

Experiment 13 Physical Stability of Suspension

Objective

Requirements

Procedure

Observations and Calculations

Result

Experiment 14 Dissolutilution Profile of Tabltablet

Aim

Requirements

Procedure

Result

Experiment 15 Kinetics-I

Objective

Requirements

Procedure

Observations and Calculations

Table for λ max determination

Table for calibration curve

Result

Experiment 16 Kinetics-II

Objective

Requirements

Procedure

Observations and Calculations

Data Analysis (Record the following data in Table 5)

Result

Multiple Choice Questions (useful for GPAT aspirants)

MCQ Answer Key

Index

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