Essential chemistry for formulators of semisolid and liquid dosages / authors, Vitthal S. Kulkarni, Charles Shaw.

Format:

Book

Author/Creator:

Kulkarni, Vitthal S., author.

Shaw, Charles, author.

Language:

English

Subjects (All):

Drugs--Dosage forms.

Drugs.

Physical Description:

1 online resource (0 p.)

Edition:

1st ed.

Place of Publication:

Amsterdam, [Netherlands] : Academic Press, 2016.

Language Note:

English

Summary:

A needed resource for pharmaceutical scientists and cosmetic chemists, "Essential Chemistry for Formulators of Semisolid and Liquid Dosages" provides insight into the basic chemistry of mixing different phases and test methods for the stability study of nonsolid formulations. The book covers foundational surface/colloid chemistry, which forms the necessary background for making emulsions, suspensions, solutions, and nano drug delivery systems, and the chemistry of mixing, which is critical for further formulation of drug delivery systems into semisolid (gels, creams, lotions, and ointments) or liquid final dosages. Expanding on these foundational principles, this useful guide explores stability testing methods, such as particle size, rheological/viscosity, microscopy, and chemical, and closes with a valuable discussion of regulatory issues. "Essential Chemistry for Formulators of Semisolid and Liquid Dosages" offers scientists and students the foundation and practical guidance to make and analyze semisolid and liquid formulations. Unique coverage of the underlying chemistry that makes possible stable dosagesQuality content written by experienced experts from the drug development industryValuable information for academic and industrial scientists developing topical and liquid dosage formulations for pharmaceutical as well as skin care and cosmetic products

Contents:

Front Cover

Essential Chemistry for Formulators of Semisolid and Liquid Dosages

Copyright

CONTENTS

PREFACE

1 - Introduction

2 - Surfactants, Lipids, and Surface Chemistry

2.1 INTRODUCTION

2.2 TYPES OF SURFACTANTS

2.2.1 Surfactant Micelles

2.2.2 Anionic Surfactants

2.2.3 Cationic Surfactants

2.2.4 Nonionic Surfactants

2.3 NATURAL SURFACTANTS

2.3.1 Lipids

2.4 THE ROLE OF SURFACTANTS IN PHARMACEUTICAL FORMULATIONS

2.4.1 Skin Penetration Enhancers

2.4.2 Emulsifying Agents

2.4.2.1 Hydrophile-Lipophile Balance (HLB) System

2.4.3 Aerosol Formulations

2.4.4 Surfactant Gels

2.5 SURFACE CHEMISTRY FOR PHARMACEUTICAL FORMULATIONS

2.5.1 Surface and Interfacial Tension

2.5.2 Contact Angle

2.6 CONCLUSION

REFERENCES

3 - Drug Delivery Vehicles

3.1 INTRODUCTION

3.2 EMULSION DRUG DELIVERY SYSTEMS

3.3 LIPOSOME DRUG DELIVERY SYSTEMS

3.3.1 Methods of Making Liposomes

3.4 OTHER NANODRUG DELIVERY SYSTEMS

3.5 CONCLUSION

4 - Formulating Creams, Gels, Lotions, and Suspensions

4.1 INTRODUCTION

4.2 CREAMS AND LOTIONS

4.3 GELS, OINTMENTS, AND SUSPENSIONS

4.4 FORMULATING WITH LIPOSOMES

4.5 EXCIPIENTS

4.6 CONCLUSION

5 - Use of Polymers and Thickeners in Semisolid and Liquid Formulations

BACKGROUND

5.1 POLYMERS AS STYLING AGENTS

5.2 POLYMERS AS CONDITIONING AGENTS

5.2.1 Cationic Polymers

5.2.2 Silicones

5.2.3 Proteins

5.3 POLYMERS AS PRESERVATIVES [3,4]

5.4 POLYMERS AS PENETRATION ENHANCERS

5.5 POLYMERS AS THICKENING AND SUSPENDING AGENTS [11]

5.5.1 Emulsions

5.5.2 Gels

5.5.2.1 Examples of Gelling Agents

5.5.3 Suspensions

5.5.3.1 Examples of Suspending Agents

5.6 CHARACTERISTICS OF COMMONLY USED THICKENING, GELLING, AND SUSPENDING AGENTS

5.6.1 Natural Hydrocolloids

5.6.1.1 Agar.

5.6.1.2 Alginates

5.6.1.3 Carrageenan

5.6.1.4 Chitin and chitosan

5.6.1.5 Gelatin

5.6.1.6 Guar gum

5.6.1.7 Gum acacia/gum arabic

5.6.1.8 Locust bean gum

5.6.1.9 Pectin

5.6.1.10 Starch

5.6.1.11 Tragacanth

5.6.1.12 Xanthan Gum

5.6.2 Cellulose and Derivatives

5.6.2.1 Cellulose/Microcrystalline Cellulose (MCC)

5.6.3 Synthetic Polymers

5.6.4 Clays

6 - Aerosols and Nasal Sprays

6.1 AEROSOLS

6.1.1 Types of Formulation

6.1.2 Typical Aerosol Excipients

6.1.2.1 Examples of Uses and Effects of Aerosol Formulation Excipients

6.1.3 Propellants

6.1.3.1 Numerical Designations for Fluorinated Hydrocarbon Propellants

6.1.3.2 Chlorofluorocarbon (CFC) Propellants

6.1.3.3 Hydrochlorofluorocarbon (HCFC) and Hydrofluorocarbon (HFC) Propellants

6.1.3.4 Hydrocarbon Propellants

6.1.3.5 Compressed Gases

6.1.4 Particle Engineering and pMDIs

6.1.5 Manufacturing Process

6.2 NASAL SPRAYS

6.2.1 Types of Formulation

6.2.2 Typical Nasal Spray Excipients

6.2.2.1 Examples of Uses and Effects of Nasal Spray Formulation Excipients

6.2.3 Nasal Spray Devices

6.2.4 Manufacturing Process

7 - Preparation and Stability Testing

7.1 HOW FORMULATIONS ARE PUT TOGETHER

7.1.1 General Comments

7.1.2 Solutions

7.1.3 Suspensions

7.1.4 Ointments

7.1.5 Gels

7.1.6 Emulsions

7.2 MIXING SYSTEMS

7.3 QUALITY BY DESIGN (QBD) FOR FORMULATION AND PROCESS DEVELOPMENT

7.3.1 Example of QbD Formulation Development [3]

7.3.1.1 Preformulation

7.3.1.2 Formulation Development

7.3.1.3 Preliminary Risk Assessment

7.3.1.4 Stress Testing Assessment

7.3.1.5 Formulation Modifications

7.3.1.6 Informal Stability Testing

7.4 STABILITY TESTING

7.4.1 Examples of Physical Instability

7.4.2 Examples of Chemical Instability.

7.4.3 Examples of Biological Instability

7.4.4 Examples of Microbiological Instability

7.4.5 Stress Testing

7.4.5.1 Stress Conditions

7.4.6 Informal Stability Testing

7.4.7 Formal Stability Testing-ICH Guidelines

7.4.7.1 Testing Frequency (ICH Q1A(R2) [1])

7.4.7.2 Storage Conditions (ICH Q1A(R2) [1])

7.4.7.3 Short-term Excursions Outside the Label Storage Condition

8 - Particle Size Analysis: An Overview of Commonly Applied Methods for Drug Materials and Products

8.1 INTRODUCTION

8.2 LASER DIFFRACTION

8.2.1 Development and Validation of Laser Diffraction Particle-Size Methods

8.2.2 Method Development and Validation

8.2.3 Concerns about Laser Diffraction Technique

8.3 PARTICLE SIZE EVALUATION BY MICROSCOPY

8.4 CONCLUSION

9 - Rheological Studies

9.1 GENERAL TERMS AND DEFINITIONS [3]

9.2 INSTRUMENTS AND MEASURING GEOMETRIES

9.2.1 Glass Capillary Viscometers

9.2.2 Rotational Instruments [3]

9.2.2.1 Rotational Viscometers [5]

9.2.2.2 Rotational Rheometers

9.2.3 Measuring Geometries [5]

9.3 MATERIAL BEHAVIOR

9.3.1 Newtonian Fluids

9.3.2 Non-Newtonian Fluids

9.3.3 Zero-Shear Viscosity

9.3.4 Yield Stress Testing [9]

9.3.5 Factors Affecting Rheological Measurements

9.3.6 Characteristics of Dispersions and Emulsions [5]

9.4 RHEOLOGICAL STUDIES

9.4.1 Viscosity

9.4.2 Flow

9.4.3 Creep [11,12]

9.4.4 Oscillation

9.5 PRACTICAL APPLICATION OF RHEOLOGICAL DATA

9.5.1 Reported Examples

10 - Microscopy Techniques

10.1 INTRODUCTION

10.2 OPTICAL MICROSCOPY

10.2.1 Particle Size Testing

10.2.2 Morphology

10.2.3 Thermal or Hot-Stage Microscopy

10.2.4 Evaluation of Particulate Matter

10.2.5 Evaluation of Foreign Particulate Matter

10.2.6 Evaluation of Material Compatibility.

10.2.7 Testing of Tablets

10.2.8 Ingredient-Specific Particle Sizing

10.2.9 Fourier-Transform Infrared Microscopy

10.3 SCANNING ELECTRON MICROSCOPY

10.4 TRANSMISSION ELECTRON MICROSCOPY

10.5 ATOMIC FORCE MICROSCOPY

10.6 CONCLUSION

11 - Miscellaneous Physical, Chemical, and Microbiological Test Methods

11.1 GENERAL PHYSICAL TESTS

11.1.1 Description/Appearance

11.1.2 Color

11.1.3 pH (US Pharmacopeia [USP]&lt

791&gt

)

11.1.4 Osmolality (USP&lt

785&gt

11.1.5 Viscosity (USP&lt

911&gt

, &lt

912&gt

913&gt

11.1.6 Rheology (USP&lt

11.1.7 Specific Gravity (USP&lt

841&gt

11.1.8 Net Content/Minimum Fill (USP&lt

755&gt

11.1.9 Particle Size Distribution

11.1.10 Particulate Matter (USP&lt

788&gt

789&gt

11.1.11 Weight Loss

11.1.12 Container Closure Integrity

11.1.13 Temperature Cycling and Freeze/Thaw

11.1.14 Photostability

11.1.15 Conductivity

11.1.16 Microscopy

11.1.17 In Vitro Release Testing

11.1.18 Transit Trials

11.1.19 Differential Scanning Calorimetry/Thermal Analysis (USP&lt

891&gt

11.2 GENERAL CHEMICAL TESTS

11.2.1 Identification Test

11.2.2 Assays for Active Ingredient, Degradants, and Impurities

11.2.3 Preservative and Other Chemical Assays

11.2.4 Content Uniformity

11.2.5 Extractables/Leachables

11.3 GENERAL MICROBIOLOGICAL TESTS

11.3.1 Microbial-Limits Testing

11.3.2 Antimicrobial Effectiveness Testing

11.3.3 Sterility Testing

11.3.4 Endotoxin Testing (USP&lt

85&gt

11.4 PRODUCT-SPECIFIC TESTS

11.4.1 Tests Performed on Metered Dose Nasal Sprays and Pressurized Aerosols (e.g., pMDIs)

Sublingual Sprays [17]

11.4.1.1 Spray Pattern

11.4.1.2 Plume Geometry.

11.4.1.3 Spray Content Uniformity/Delivered Dose Uniformity (USP&lt

601&gt

11.4.1.4 Droplet Size Distribution

11.4.1.5 Dose Weight

11.4.1.6 Priming/Repriming

11.4.1.7 Number of Doses

11.4.1.8 Tail-Off Characteristics

11.4.2 Tests Performed on Pressurized Aerosols Fitted with Continuous Valves (e.g., Topical Aerosols) (USP&lt

11.4.2.1 Container Pressure

11.4.2.2 Delivery Rate/Delivered Amount

11.4.2.3 Leakage Test

11.4.3 Aerodynamic Size Distribution

11.4.4 Stress Tests (Section 7.4.5.1)

11.4.4.1 Centrifugation

11.4.4.2 Wick Test

11.4.5 Drop Weight

11.4.6 Resuspendability

11.4.7 Penetration

11.4.8 Drop Point/Congealing Temperature

11.4.9 Metal Particles

12 - An Overview of Regulatory Aspects for Pharmaceutical Semisolid Dosages

12.1 QUALITY DATA [1]

12.1.1 Stability

12.1.2 Analytical Validation

12.1.3 Impurities

12.1.4 Biotechnological Products

12.1.5 Specifications

12.1.6 Pharmaceutical Development

12.1.7 Quality Risk Management

12.2 TYPES OF REGULATORY SUBMISSIONS

12.3 RESOURCES-ICH

12.3.1 Quality Guidelines Relating to Drug Products

12.3.2 Other Quality Guidelines

12.3.3 Safety Guidelines

12.3.4 Efficacy Guidelines

12.3.5 Multidisciplinary Guidelines

12.4 RESOURCES-FDA

12.5 RESOURCES-WHO

INDEX

A

B

C

D

E

F

G

H

I

J

L

M

N

O

P

Q

R

S

T

U

V

W

X

Z

Back Cover.

Notes:

Description based upon print version of record.

Includes bibliographical references at the end of each chapters and index.

Description based on online resource; title from PDF title page (ebrary, viewed December 04, 2015).

ISBN:

9780128010723

012801072X