In Vitro Drug Release Testing of Special Dosage Forms

Nikoletta Fotaki, Sandra Klein, Nikoletta Fotaki, Sandra Klein

• Publisher: Wiley
• Year: 2019
• Print ISBN: 9781118341476
• eBook ISBN: 9781118675830
• Edition: 1
• Topic: Physical Sciences
• Subtopic: Organic Chemistry

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.

Part I
Oral Dosage Forms

1
Lipid‐Based Oral Formulations

Murat Kilic¹, Aikaterini Avzoti², Jennifer Dressman¹, and Christos Reppas²

¹ Goethe University, Frankfurt/Main, Germany

² National and Kapodistrian University of Athens, Athens, Greece

1.1 Introduction

Lipid‐based formulations have been used for oral dosage forms for many years, as there have always been drugs to be formulated which are oil‐soluble, e.g. the fat‐soluble vitamins and their derivatives. Whereas 25 years ago drugs that are poorly water‐soluble but very oil‐soluble were few and far between, these days drugs in this category are encountered more and more frequently in drug discovery. As a result, the need for lipid‐based oral formulations is on the increase. But lipid‐based formulations can be used for other purposes than to adapt the vehicle to the drug’s solubility characteristics. For example, preparing a drug in a lipid‐based suspension can also be a good way of avoiding safety problems due to dusting during the manufacturing process for drugs that are toxic.

Several years ago, David Hauss published a book that was devoted to oral lipid dosage forms [1]. In this book the lipid‐based dosage forms on the market at the time of writing [2] were summarized and some key examples are shown in Table 1.1.

Table 1.1 Some examples of drugs which are formulated in lipid‐based dosage forms.

Source: Adapted from Strickley [2].

Drug	Trade name and manufacturer	Date introduced to the market	Indication and dose in adults	Type of formulation
Amprenavir	Agenerase; GSK	2000	HIV, 1200 mg (8 capsules bid)	Soft gelatin capsule
α‐Calcidiol	One‐Alpha; Leo	2000	Calcium regulator, 0.5–1 μg qd	Soft gelatin capsule
Bexarotene	Tagretin; Ligand	2001	Antineoplastic, 300–750 mg (4–10 capsules bid)	Soft gelatin capsule
Calcitriol	Rocatrol; Roche	1996	Calcium regulator, 0.25–0.5 μg qd	Soft gelatin capsule
Ciprofloxacin	Cipro; Bayer		Antibiotic, 15 mg/kg bid bis max 500 mg/dose	Microcapsules
Clofazamine	Lamprene; Alliance	1998	Leprosy, max 300 mg (3 capsules qd)	Soft gelatin capsule (suspension)
Clomethiazole edilisate	Heminevrin; AZ	2002	Sedative, 192 mg, 1–4 capsules prn	Soft gelatin capsule
Cyclosporin A	a. Neoral; Novartis b. Sandimmun; Novartis	1995	Immunosuppressant, 2–10 mg/kg/day, bid (1–7 capsules or 1–7 ml)	Soft gelatin capsules; oral solution (generic version as hard gelatin capsule: Gengraf, Abbott)
Doyercalciferol	Hectorol; Bone Care		2° Hyper‐parathyroidism, 10–20 μg, thrice weekly (4–8 capsules)	Soft gelatin capsule
Dronabinol	Marinol; Roxane, Unimed		Anorexia, Nausea; 2.5–10 mg bid	Soft gelatin capsule
Dustasteride	Avodart; GSK	2003	Benign prostate hyperplasia, 0.5 mg qid	Soft gelatin capsule
Efivarenz	Sustiva; BMS	1999	HIV, 600 mg qd	Oral solution
Ethylicosapentate	Epadel; Mochida	1990	Hyperlipidemia, 600 mg tid (2 capsules)	Soft gelatin capsule
Fenofibrate	Fenogal; Genus	2002	Hyperlipidemia, 200 mg qd	Hard gelatin capsule
Ibudilast	Ketas; Kyorin	1989	Asthma, cerebrovascular disorders, 10 mg bid or tid	ER granules in a hard gelatin capsule
Indomethacin farnesil	Infree; Eisai	1991	Anti‐inflammatory and analgesia, 200 mg bid	Hard and soft gelatin capsules available
Isotretinoin	Accutane; Roche	1983	Acne, 0.5–1 mg/kg/day admin in 2 doses	Soft gelatin capsule
Lopinavir and Ritonavir	Kaletra; Abbott	2001	HIV, 400 mg/ 100 mg bid (5 ml)	Oral solution
Menanetrenone	Glakay; Eisai	1995	Osteoporosis, 45 mg tid (3 capsules)	Soft gelatin capsule
Morphine sulfate	MXL; Napp	1996	Analgesic, 30–200 mg qd	Hard gelatin capsule containing multiparticulate
Progesterone	Prometrium; Solvay		Hormone replacement, 200–400 mg qd (2–4 capsules)	Soft gelatin capsule containing a micronized suspension
Ritonavir	Norvir; Abbott	1999	HIV, 600 mg bid (6 capsules)	Soft gelatin capsule
Sirolimus	Rapamune; Wyeth‐Ayerst	2001	Immunosuppressant, 6 mg loading dose (6 ml), then 2 mg qd	Oral solution
Testosterone undecanoate	Restandol; Organon	1981	Hormone replacement, 40–160 mg qd (1–4 c...

Table of contents

• Cover
• Table of Contents
• List of Contributors
• Series Preface
• Preface
• Part I: Oral Dosage Forms
• Part II: Non-oral Dosage Forms
• Index
• End User License Agreement