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E-grāmata: In Vitro Drug Release Testing of Special Dosage Forms

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Guides readers on the proper use of in vitro drug release methodologies in order to evaluate the performance of special dosage forms

In the last decade, the application of drug release testing has widened to a variety of novel/special dosage forms. In order to predict the in vivo behavior of such dosage forms, the design and development of the in vitro test methods need to take into account various aspects, including the dosage form design and the conditions at the site of application and the site of drug release. This unique book is the first to cover the field of in vitro release testing of special dosage forms in one volume. Featuring contributions from an international team of experts, it presents the state of the art of the use of in vitro drug release methodologies for assessing special dosage forms’ performances and describes the different techniques required for each one.

In Vitro Drug Release Testing of Special Dosage Forms covers the in vitro release testing of: lipid based oral formulations; chewable oral drug products; injectables; drug eluting stents; inhalation products; transdermal formulations; topical formulations; vaginal and rectal delivery systems and ophthalmics. The book concludes with a look at regulatory aspects. 

  • Covers both oral and non-oral dosage forms
  • Describes current regulatory conditions for in vitro drug release testing
  • Features contributions from well respected global experts in dissolution testing

In Vitro Drug Release Testing of Special Dosage Forms will find a place on the bookshelves of anyone working with special dosage forms, dissolution testing, drug formulation and delivery, pharmaceutics, and regulatory affairs.

List of Contributors xvii
Series Preface xix
Preface xxi
Part I Oral Dosage Forms 1(54)
1 Lipid-Based Oral Formulations
3(24)
Murat Kilic
Aikaterini Avzoti
Jennifer Dressman
Christos Reppas
1.1 Introduction
3(4)
1.2 Levels of Release Testing for Lipid-Based Dosage Forms
7(9)
1.2.1 Dilution
7(2)
1.2.2 Dispersion and Drug Release
9(4)
1.2.3 Digestion
13(3)
1.2.4 Assessing Direct Uptake from the Vehicle
16(1)
1.3 Case Examples
16(6)
1.3.1 Compendial or Fed State Biorelevant Media to Evaluate Fenofibrate Lipid-based Formulations?
17(1)
1.3.2 Paddle or Biodis Method for Testing a Lipid-based Formulation?
17(2)
1.3.3 Does Nifedipine Precipitate after Administration as a Soft Gelatin Capsule?
19(1)
1.3.4 Screening of Indomethacin Lipid-Based Formulations
19(3)
1.3.5 Effect of Supersaturation on In Vivo Performance
22(1)
1.4 Conclusions and Future Directions
22(1)
References
23(4)
2 Chewable Oral Drug Products
27(28)
Johannes Kramer
Jayachandar Gajendran
Alexis Guillot
Abdulwahab Barakat
2.1 Introduction
27(3)
2.1.1 Dosage Forms for Which Drug Release Occurs in the Oral Cavity
27(1)
2.1.2 Chewable Dosage Forms Classification
28(2)
2.2 The Oral Cavity
30(3)
2.2.1 Anatomy of the Oral Cavity
30(1)
2.2.2 Physiological Conditions from the Perspective of In Vivo Performance
30(1)
2.2.3 Mechanical Forces
31(1)
2.2.4 Need for Masticatory Action
31(1)
2.2.5 Saliva Composition
32(1)
2.2.6 Oral Absorption vs. Subsequent Absorption in the GI Tract
32(1)
2.3 Drug Substances Used in Chewable Dosage Forms
33(1)
2.4 Technology
33(2)
2.4.1 Chewable Tablets
34(1)
2.4.2 Medicated Gums
34(1)
2.4.2.1 Conventional Method (Extrusion)
34(1)
2.4.2.2 Direct Compression Method
34(1)
2.4.3 Soft Gel Capsules as Chewable Dosage Forms
35(1)
2.5 Pharmacopoeial Requirements
35(14)
2.5.1 Chewable Tablets and Capsules
35(1)
2.5.1.1 US FDA and USP Requirements for In Vitro Performance Testing of Chewable Tablets
35(1)
2.5.1.2 Rationale for Use of the Reciprocating Cylinder Apparatus (USP Apparatus 3)
36(1)
2.5.1.3 Current Status of Drug Release/Dissolution Testing Apparatus for Chewable Drug Products
36(1)
2.5.2 Medicated Gums
36(1)
2.5.2.1 Rationale for In Vitro Performance Testing of Medicated Gums
41(1)
2.5.3 Apparatus for In Vitro Drug Release Testing of Medicated Gums
41(1)
2.5.3.1 Non-Compendial Setup: A USP Apparatus 2-based Method with Modified Gums
41(3)
2.5.4 Compendial Apparatus
44(1)
2.5.4.1 Ph.Eur. Chewing Apparatus A (Chapter 2.9.25)
44(1)
2.5.4.2 Ph.Eur. Chewing Apparatus B (Chapter 2.9.25)
44(1)
2.5.5 In Vitro-In Vivo Correlation (IVIVC)
45(4)
2.6 Summary and Conclusion
49(1)
References
50(5)
Part II Non-oral Dosage Forms 55(230)
3 Injectables
57(30)
Susan D'Souza
3.1 Introduction
57(3)
3.2 Significance of In Vitro Release Testing
60(1)
3.3 Considerations in Method Development
61(5)
3.3.1 Sink Conditions
63(1)
3.3.2 Burst Release
63(1)
3.3.3 Stability of Drug
64(1)
3.3.4 Completeness of In Vitro Release
64(1)
3.3.5 Robustness of Technique
65(1)
3.3.6 Accelerated Release
65(1)
3.3.7 In Vitro - In Vivo Correlations (IVIVCs)
66(1)
3.4 In Vitro Release Methods
66(5)
3.4.1 Sample and Separate
67(1)
3.4.1.1 Volume of Release Media
67(1)
3.4.1.2 Agitation Conditions
67(1)
3.4.1.3 Sampling Techniques
67(1)
3.4.1.4 Sampling Volume
68(1)
3.4.2 Continuous Flow
68(1)
3.4.2.1 CF Setups
69(1)
3.4.2.2 Pumps and Flow Rates
70(1)
3.4.2.3 Sampling Techniques
70(1)
3.5 Dialysis Method
71(3)
3.5.1 Dialysis Setup
72(1)
3.5.2 Volume of Release Media
73(1)
3.5.3 Sampling Technique and Volume
73(1)
3.6 Accelerated In Vitro Release
74(2)
3.7 In Vitro - In Vivo Correlations (IVIVCs)
76(2)
References
78(9)
4 Drug-Eluting Stents
87(32)
Anne Seidlitz
4.1 Drug-Eluting Stents: Combination Products at the Interface of Medical Devices and Medicinal Products
87(1)
4.2 DES Characteristics
88(2)
4.3 In Vivo Stent Position and the Resulting Challenges for In Vitro Release Testing of Coronary Stents
90(2)
4.4 Guidelines, Prerequisites, and General Recommendations on DES Testing
92(1)
4.5 Currently Used Test Methods
93(8)
4.5.1 Media
93(3)
4.5.2 Apparatus
96(5)
4.6 Toward More Biorelevant Testing Conditions and New Challenges for DES Testing
101(6)
4.7 Non-Vascular Stents
107(1)
4.8 Drug-Coated Balloons: An Alternative to DESs for a Wide Range of Indications?
108(1)
4.9 Concluding Remarks
109(1)
References
110(9)
5 In Vitro Dissolution for Inhalation Products
119(36)
Annalisa Mercuri
Nikoletta Fotaki
5.1 Introduction
119(1)
5.2 The Environment of the Human Lungs
120(5)
5.2.1 The Anatomy of Bronchi and Alveoli
121(1)
5.2.2 Airway Surface Liquid (ASL)
121(1)
5.2.2.1 The Composition of Humans Lung Fluids in the Disease State
123(1)
5.2.2.2 Surface Tension
125(1)
5.2.2.3 Mucus Production and Mucociliary Clearance
125(1)
5.3 Regulatory Perspectives and Current Practices for Testing Inhaled Products
125(14)
5.3.1 Compendial Methods for Testing Inhaled Products
126(1)
5.3.1.1 Andersen Cascade Impactor (ACI)
127(1)
5.3.1.2 Glass Twin Impinger
127(1)
5.3.1.3 Marple-Miller Impactor (MMI)
129(1)
5.3.1.4 Multi-Stage Liquid Impinger (MSLI)
129(1)
5.3.1.5 Next Generation Impactor (NGI)
130(1)
5.3.1.6 Analysis of the In Vitro Deposition Data of Inhaled Particles
130(1)
5.3.1.7 In Vitro-In Vivo Deposition Correlations
131(1)
5.3.2 Dissolution Methods for Inhaled Products
132(1)
5.3.2.1 Two-Stage Impinger
133(1)
5.3.2.2 Horizontal Diffusion Cell
133(1)
5.3.2.3 Static Dissolution Cell
133(1)
5.3.2.4 Shaking Incubator
133(1)
5.3.2.5 Paddle Dissolution Apparatus (USP II Apparatus)
135(1)
5.3.2.6 Dialysis Membranes
136(1)
5.3.2.7 Flow-through Cell (USP IV Apparatus)
137(1)
5.3.2.8 Transwell™ Method
137(1)
5.3.2.9 Franz Cell Method
137(1)
5.3.3 Dissolution Methods with Integrated Deposition and Cell Permeation Models
138(1)
5.4 Simulated Lung Fluids
139(4)
5.5 Pulmonary Biopharmaceutical Classification System
143(1)
5.6 Conclusions
143(1)
References
144(11)
6 Topicals and Transdermals
155(22)
Kailas Thakker
6.1 Introduction
155(1)
6.2 In Vitro Release Studies for Topical Dosage Forms
156(11)
6.2.1 Drug Release from Semisolid Dosage Forms - Theory and Calculations
157(1)
6.2.2 Compendial Apparatus
158(1)
6.2.2.1 Vertical Diffusion Cell
158(1)
6.2.2.2 Immersion Cell
160(1)
6.2.2.3 USP Apparatus 4
163(1)
6.2.3 Method Development: Points to Consider
163(1)
6.2.3.1 Selection of the Receiving Medium
165(1)
6.2.3.2 Selection of the Membrane
166(1)
6.2.3.3 Apparatus Qualification
166(1)
6.2.3.4 Test Procedure
166(1)
6.2.4 Custom-Designed Cells
167(1)
6.3 In Vitro Release Studies for Transdermal Systems
167(4)
6.3.1 Compendial Apparatus
168(1)
6.3.1.1 The Paddle over Disc Apparatus
168(1)
6.3.1.2 The Reciprocating Holder Apparatus
168(3)
6.4 Conclusions
171(1)
References
171(6)
7 Vaginal and Intrauterine Delivery Systems
177(34)
Sandra Klein
Katharina Tietz
7.1 Vaginal and Uterine Anatomy and Physiology Relevant to Drug Delivery
177(5)
7.1.1 Vaginal Anatomy
177(2)
7.1.2 Vaginal Secretions/Vaginal Fluid
179(1)
7.1.3 Vaginal Microflora and pH
179(1)
7.1.4 Uterine Anatomy
179(1)
7.1.5 Cervix Anatomy
180(1)
7.1.6 Uterine and Cervical Secretions/Cervical and Uterine Fluid
180(2)
7.2 Vaginal and Intrauterine Drug Delivery
182(1)
7.3 Standard Dissolution Test Methods for Vaginal and Intrauterine Delivery Systems
183(3)
7.3.1 Official Dissolution Methods
183(3)
7.4 Predictive Dissolution Test Methods for Vaginal and Intrauterine Delivery Systems
186(20)
7.4.1 Test Equipment
187(1)
7.4.2 Test Media
188(1)
7.4.2.1 Simulated Vaginal Fluids
188(1)
7.4.2.2 Simulated Intrauterine Fluids
192(1)
7.4.2.3 Other Genital Fluids
193(1)
7.4.2.4 Summary
194(1)
7.4.3 Case Studies
194(1)
7.4.3.1 Dissolution Test Methods for Vaginal Tablets
195(1)
7.4.3.2 Dissolution Test Methods for Vaginal Suppositories
198(1)
7.4.3.3 Dissolution Test Methods for Vaginal Gels
199(1)
7.4.3.4 Dissolution Test Methods for Vaginal Films
201(1)
7.4.3.5 Dissolution Test Methods for Vaginal Rings
202(1)
7.4.3.6 Dissolution Test Methods for Intrauterine Delivery Systems
205(1)
7.4.4 Conclusion and Future Directions
205(1)
References
206(5)
8 Rectal Dosage Forms
211(24)
Sandra Klein
8.1 Rectal Anatomy and Physiology Relevant to Drug Delivery
211(2)
8.1.1 Rectal Anatomy and Physiology
211(2)
8.1.2 Rectal Secretions and Rectal Fluid Properties
213(1)
8.2 Rectal Drug Delivery
213(2)
8.3 Standard Dissolution Test Methods for Rectal Dosage Forms
215(3)
8.3.1 Official Dissolution Methods
215(3)
8.4 Predictive Dissolution Test Methods for Rectal Dosage Forms
218(13)
8.4.1 Test Equipment
218(1)
8.4.2 Test Media
219(1)
8.4.3 Case Studies
219(1)
8.4.3.1 Dissolution Test Methods for Suppositories
220(1)
8.4.3.2 Dissolution Test Methods for Rectal Capsules
229(1)
8.4.3.3 Dissolution Test Methods for Rectal Gels
229(1)
8.4.4 Conclusion and Future Directions
230(1)
References
231(4)
9 Ophthalmic Dosage Forms
235(18)
Christian Simroth-Loch
Werner Weitschies
Clive G. Wilson
9.1 Introduction
235(1)
9.2 The Tear Film
236(2)
9.2.1 Tear Characteristics
236(1)
9.2.2 Tear Secretion: Enzymes and Proteins
237(1)
9.2.3 Tear Secretion: Lipids
237(1)
9.2.4 Osmolality
237(1)
9.2.5 Tear Secretion: pH
237(1)
9.2.6 Tear Secretion: Surface Tension
237(1)
9.2.7 Tear Viscosity
238(1)
9.3 Delivery Volume
238(1)
9.4 Ophthalmic Formulations
239(2)
9.4.1 Drug Salts
239(1)
9.4.2 Tonicity Adjusters
240(1)
9.4.3 Buffers
240(1)
9.4.4 Preservatives
240(1)
9.4.5 Polymers
240(1)
9.4.6 Ethylenediaminepentaacetic acid (EDTA)
241(1)
9.5 In Vitro Testing for Ophthalmic Formulations
241(5)
9.5.1 Media to Simulate Ocular Fluids
241(1)
9.5.2 Topical Ocular Delivery Systems and In Vitro Testing
242(1)
9.5.3 Intraocular Delivery Systems and In Vitro Testing
243(1)
9.5.3.1 Periocular Injections and Implants
243(1)
9.5.3.2 Intravitreal Injections and Implants
245(1)
9.6 Concluding Remarks
246(1)
References
247(6)
10 Regulatory Considerations
253(32)
Vivian A. Gray
10.1 Introduction
253(1)
Part One: Review of Documents Related to In Vitro Release Testing
253(22)
10.2 Compendial
Chapters with Legal Implications
253(1)
10.2.1 USP General
Chapter 711 Dissolution
254(1)
10.2.2 Ph.Eur.
Chapters on Dissolution
254(1)
10.2.2.1 Ph.Eur. 2.9.3 Dissolution Test for Solid Dosage Forms
254(1)
10.2.2.2 Ph.Eur. 2.9.42 Dissolution Test for Lipophilic Solid Dosage Forms
255(1)
10.2.3 JP 6.10 Dissolution Test
255(1)
10.2.4 Harmonization of Dissolution
Chapters
256(1)
10.2.5 The International Pharmacopoeia
256(1)
10.2.6 Testing of Transdermal Dosage Forms
257(1)
10.2.6.1 USP General
Chapter Drug Release 724
257(1)
10.2.6.2 Dissolution Testing for Transdermal Patches EP 2.9.4
257(1)
10.2.7 Dissolution Test for Medicated Chewing Gums, EP 2.9.25
258(1)
10.2.8 Disintegration Testing
258(1)
10.2.8.1 USP General
Chapter Disintegration 701
258(1)
10.2.8.2 Ph.Eur. Disintegration Testing
259(1)
10.2.8.3 JP Disintegration Test 6.09
260(1)
10.3 Compendial
Chapters, Non-binding
261(1)
10.3.1 The Dissolution Procedure: Development and Validation USP General
Chapter 1092
261(1)
10.3.2 Ph.Eur. Recommendations on Dissolution Testing 5.17.1
261(1)
10.3.3 USP General
Chapter In Vitro and In Vivo Evaluation of Dosage Forms 1088
262(1)
10.3.4 USP General
Chapter Semisolid Drug Products- Performance Tests 1724
262(1)
10.3.5 Capsules-Dissolution Testing and Related Quality Attributes USP General
Chapter 1094
262(1)
10.3.6 Assessment of Drug Performance-Bioavailability, Bioequivalence, and Dissolution USP General
Chapter 1090
263(1)
10.4 Guidances Related to In Vitro Release Testing
263(1)
10.4.1 FDA Guidances
264(1)
10.4.1.1 Dissolution Testing of Immediate-Release Solid Oral Dosage Forms
264(1)
10.4.1.2 Extended-Release Oral Dosage Forms: Development, Evaluation, and Application of In Vitro-In Vivo Correlations
265(1)
10.4.1.3 Waiver of In Vivo Bioavailability and Bioequivalence Studies for Immediate-Release Solid Oral Dosage Forms Based on a BCS
265(1)
10.4.1.4 Bioavailability and Bioequivalence Studies for Orally Administered Drug Products - General Considerations
266(1)
10.4.1.5 SUPAC Guidances for Immediate-Release [ 36], Extended-Release [ 37], and Non-Sterile Semisolids [ 19]
266(1)
10.4.1.6 Orally Disintegrating Tablets
268(1)
10.4.1.7 The Use of MC of Dissolution Apparatus 1 and 2 - Current Good Manufacturing Practice (CGMP)
268(1)
10.4.1.8 Dissolution Testing and Specification Criteria for Immediate-Release Solid Oral Dosage Forms Containing BCS Class 1 and 3 Drugs
268(1)
10.4.1.9 Quality Attribute Considerations for Chewable Tablets
269(1)
10.4.2 EMA Guidances
269(1)
10.4.2.1 Guideline on Quality of Oral Modified-Release Products
269(1)
10.4.2.2 Guideline on Quality of Transdermal Patches
270(1)
10.4.2.3 Guideline on the Investigation of Bioequivalence
270(1)
10.4.3 Japanese Guidelines
271(1)
10.4.3.1 Guideline for the Design and Evaluation of Oral Prolonged-Release Dosage Forms
271(1)
10.4.3.2 Guideline for Bioequivalence Studies of Generic Products
271(1)
10.4.3.3 Guideline for Bioequivalence Studies for Different Strengths of Oral Solid Dosage Forms
272(1)
10.4.3.4 Guideline for Bioequivalence Studies for Formulation Changes of Oral Solid Dosage Forms
272(1)
10.4.3.5 Guideline for Bioequivalence Studies for Different Oral Solid Dosage Forms
272(1)
10.4.4 ICH Guidelines
272(1)
10.4.4.1 Q6A Specifications: Test Procedures and Acceptance Criteria for New Drug Substances and New Drug Products: Chemical Substances
273(1)
10.4.4.2 Evaluation and Recommendation of Pharmacopeial Texts for Use in the ICH Regions on Dissolution Test General
Chapter Q4B Annex 7(R2)
273(1)
10.4.4.3 Evaluation and Recommendation of Pharmacopeial Texts for Use in the ICH Regions on Disintegration Test General
Chapter Q4B Annex 5(R1)
273(1)
10.4.5 Other Guidelines
273(1)
10.4.5.1 FIP Guidelines for Dissolution Testing of Solid Oral Products
273(1)
10.4.5.2 FIP/AAPS Guidelines for Dissolution/In Vitro Release Testing of Novel/Special Dosage Forms
274(1)
10.4.5.3 Specifications for Pharmaceutical Preparations (Forty-Sixth Report), WHO Technical Report Series 970
274(1)
Part Two: Role of Method Development in Setting Clinically Relevant Specifications
275(3)
10.5 Considerations in Early Method Development
275(1)
10.6 Choice of Media
276(1)
10.7 Discriminatory Power of the Method
277(1)
10.8 In Vitro Release Testing for Special Dosage Forms
278(1)
10.9 Resources
278(1)
Useful Web Sites
278(1)
Bibliography
279(1)
Acknowledgments
279(1)
References
279(6)
Index 285
Editors

Nikoletta Fotaki, PhD, is Reader in Pharmaceutics, Department of Pharmacy and Pharmacology, University of Bath, UK. Her research interests are focused on the prediction of drug absorption through the oral and non-oral route; prediction of drug absorption in special populations (paediatrics; disease states), biorelevant dissolution methods, formulation development, and physiologically based pharmacokinetic modeling.

Sandra Klein, PhD, is Professor of Pharmaceutical Technology, Department of Pharmacy, University Greifswald, Germany. Her research is focused on developing bio-predictive in vitro models and oral dosage forms for special patient groups, particularly the paediatric and geriatric population; the design of predictive and accelerated test methods for lozenges, vaginal delivery systems and depot parenterals, and in establishing formulation strategies for enhancing the bioavailability of poorly soluble drugs.
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