Pharmaceutical Dissolution Testing

Offering a regulatory perspective on the role of dissolution testing in the regulation of pharmaceuticals, this reference focuses on drug bioavailability via the oral route of administration and supplies the latest research on topics such as the physiological parameters relevant to dissolution testing, pharmacokinetic study design, quality control, and the qualification of automated dissolution systems.

Preface

v

Contributors

xiii

1. Historical Development of Dissolution Testing

1

(38)

Johannes Krämer, Lee Timothy Grady, and Jayachandar Gajendran

Introduction

1

(1)

From Disintegration to Dissolution

2

(2)

Dissolution Methodologies

4

(1)

Perspective on the History of Compendial

Dissolution Testing

5

(10)

Compendial Apparatus

15

(9)

Qualification of the Apparatus

24

(2)

Description of the Sartorius Absorption

Model

26

(3)

Introduction to IVIVC

29

(3)

Dissolution Testing: Where Are We Now?

32

(2)

References

34

(5)

2. Compendial Testing Equipment: Calibration, Qualification, and Sources of Error

39

(30)

Vivian A. Gray

Introduction

39

(1)

Qualification

40

(1)

Qualification of Non-Compendial Equipment

41

(2)

Compendial Apparatus

43

(15)

Sources of Error

58

(7)

References

65

(4)

3. Compendial Requirements of Dissolution Testing-European Pharmacopoeia, Japanese Pharmacopoeia, United States Pharmacopeia

69

(12)

William E. Brown

Pharmacopeial Specifications

69

(1)

Historical Background and Legal Recognition

70

(2)

Necessity for Compendial Dissolution Testing Requirements

72

(1)

Introduction and Implementation of Compendial Dissolution Test Requirements

73

(5)

Harmonization

78

(1)

References

78

(3)

4. The Role of Dissolution Testing in the Regulation of Pharmaceuticals: The FDA Perspective

81

(16)

Vinod P. Shah

Introduction

81

(2)

Dissolution-Related FDA Guidances

83

(3)

Changes in Dissolution Science Perspectives

86

(1)

Dissolution-Based Biowaivers-Dissolution as a Surrogate Marker of BE

87

(2)

Dissolution/In Vitro Release of Special Dosage Forms

89

(1)

Dissolution Profile Comparison

90

(3)

Future Directions

93

(1)

Impact of Dissolution Testing

94

(1)

References

95

(2)

5. Gastrointestinal Transit and Drug Absorption

97

(30)

Clive G. Wilson and Kilian Kelly

Introduction

97

(2)

Esophageal Transit

99

(1)

Gastric Retention

100

(6)

Small Intestine

106

(1)

Motility and Stirring in the Small Intestine

107

(4)

Colonic Water

111

(1)

Colonic Gas

112

(1)

Distribution of Materials in the Colon

113

(1)

The Importance of Time of Dosing

114

(2)

Effects of Age, Gender, and Other Factors

116

(1)

Concluding Remarks

117

(1)

References

118

(9)

6. Physiological Parameters Relevant to Dissolution Testing: Hydrodynamic Considerations

127

(66)

Steffen M. Diebold

Hydrodynamics and Dissolution

127

(24)

Hydrodynamics of Compendial Dissolution Apparatus

151

(10)

In Vivo Hydrodynamics, Dissolution, and Drug Absorption

161

(22)

Conclusion

183

(1)

References

183

(10)

7. Development of Dissolution Tests on the Basis of Gastrointestinal Physiology

193

(36)

Sandra Klein, Erika Stippler, Martin Wunderlich, and Jennifer Dressman

Introduction

193

(2)

Getting Started: Solubility and the Dose: Solubility Ratio

195

(29)

Future Directions of Biorelevant Dissolution Test Design

224

(1)

References

225

(4)

8. Orally Administered Drug Products: Dissolution Data Analysis with a View to In Vitro-In Vivo Correlation

229

(22)

Maria Vertzoni, Eleftheria Nicolaides, Mira Symillides, Christos Reppas, and Athanassios Iliadis

Dissolution and In Vitro-In Vivo Correlation

229

(6)

Analysis of Dissolution Data Sets

235

(9)

Conclusions

244

(2)

References

246

(5)

9. Interpretation of In Vitro-In Vivo Time Profiles in Terms of Extent, Rate, and Shape

251

(30)

Frieder Langenbucher

Introduction

251

(1)

Characterization of Time Profiles

252

(7)

Comparison of Time Profiles

259

(17)

References

276

(5)

10. Study Design Considerations for IVIVC Studies

281

(34)

Theresa Shepard, Colm Farrell, and Myriam Rochdi

Introduction

281

(3)

Regulatory Guidance Documents

284

(2)

Study Design Elements

286

(18)

Usefulness of an IVIVC

304

(7)

Conclusion

311

(1)

Appendix A

311

(2)

References

313

(2)

11. Dissolution Method Development with a View to Quality Control

315

(36)

Johannes Krämer, Ralf Steinmetz, and Erika Stippler

Implementation of USP Methods for a U.S.-Listed Formulation Outside the United States

315

(6)

How to Proceed if no USP Method is Available?

321

(4)

What Are the Pre-Requisites for a Biowaiver?

325

(15)

IVIVC: In Vivo Verification of In Vitro Methodology-An Integral Part of Dissolution Method Development

340

(7)

References

347

(4)

12. Dissolution Method Development: An Industry Perspective

351

(22)

Cynthia K Brown

Introduction

351

(3)

Physical and Chemical Properties

354

(1)

Dissolution Apparatus Selection

355

(1)

Dissolution Medium Selection

356

(4)

Key Operating Parameters

360

(5)

Method Optimization

365

(1)

Validation

366

(2)

Automated Systems

368

(1)

Conclusions

368

(1)

References

369

(4)

13. Design and Qualification of Automated Dissolution Systems

373

(34)

Dale VonBehren and Stephen Dobro

Functional Design of an Automated Dissolution Apparatus

373

(19)

System Qualification

392

(12)

Re-Qualification Policy

404

(1)

Summary

405

(1)

References

406

(1)

14. Bioavailability of Ingredients in Dietary Supplements: A Practical Approach to the In Vitro Demonstration of the Availability of Ingredients in Dietary Supplements

407

(14)

V. Srini Srinivasan

Approach to In Vitro Dissolution in Different Categories of Dietary Supplements

412

(6)

References

418

(3)

Index

421

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Pharmaceutical Dissolution Testing

Summary

Table of Contents

Supplemental Materials