Journal ArticleDOI
Molecular Properties of WHO Essential Drugs and Provisional Biopharmaceutical Classification
Nehal A. Kasim,Marc Whitehouse,Chandrasekharan Ramachandran,Marival Bermejo,H Lennernäs,Ajaz S. Hussain,Hans E. Junginger,Salomon A Stavchansky,Kamal K. Midha,Vinod P. Shah,Gordon L. Amidon +10 more
TLDR
The results suggest that a satisfactory bioequivalence (BE) test for more than 55% of the high-solubility Class 1 and Class 3 drug products on the WHO Essential Drug List may be based on an in vitro dissolution test.Abstract:
The purpose of this study is to provisionally classify, based on the Biopharmaceutics Classification System (BCS), drugs in immediate-release dosage forms that appear on the World Health Organization (WHO) Essential Drug List. The classification in this report is based on the aqueous solubility of the drugs reported in commonly available reference literature and a correlation of human intestinal membrane permeability for a set of 29 reference drugs with their calculated partition coefficients. The WHO Essential Drug List consists of a total of 325 medicines and 260 drugs, of which 123 are oral drugs in immediate-release (IR) products. Drugs with dose numbers less than or equal to unity [Do = (maximum dose strength/250 mL)/solubility ≤ 1] are defined as high-solubility drugs. Drug solubility for the uncharged, lowest-solubility form reported in the Merck Index or USP was used. Of the 123 WHO oral drugs in immediate-release dosage forms, 67% (82) were determined to be high-solubility drugs. The classificati...read more
Citations
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Journal ArticleDOI
Predicting Drug Disposition via Application of BCS: Transport/Absorption/ Elimination Interplay and Development of a Biopharmaceutics Drug Disposition Classification System
Chi-Yuan Wu,Leslie Z. Benet +1 more
TL;DR: It is suggested that a Biopharmaceutics Drug Disposition Classification System (BDDCS) using elimination criteria may expand the number of Class 1 drugs eligible for a waiver of in vivo bioequivalence studies and provide predictability of drug disposition profiles for Classes 2, 3, and 4 compounds.
Journal ArticleDOI
Strategies to Address Low Drug Solubility in Discovery and Development
Hywel David Williams,Natalie L. Trevaskis,Susan A. Charman,Ravi Mysore Shanker,William N. Charman,Colin W. Pouton,Christopher J.H. Porter +6 more
TL;DR: The article provides an integrated and contemporary discussion of current approaches to solubility and dissolution enhancement but has been deliberately structured as a series of stand-alone sections to allow also directed access to a specific technology where required.
Journal ArticleDOI
A century of dissolution research: from Noyes and Whitney to the biopharmaceutics classification system.
TL;DR: In this paper, a review of the most important developments in the field of drug dissolution from a historical point of view is presented, which is structured in a chronological order, from the theoretical foundations of dissolution, developed in the first half of the 20th century, and the development of a relationship between dissolution and bioavailability in the 1950s, going to the more recent development in the framework of the Biopharmaceutics Classification System (BCS).
Journal ArticleDOI
A provisional biopharmaceutical classification of the top 200 oral drug products in the United States, Great Britain, Spain, and Japan.
Toshihide Takagi,Chandrasekharan Ramachandran,Marival Bermejo,Shinji Yamashita,Lawrence X. Yu,Gordon L. Amidon +5 more
TL;DR: More than 55% of the drug products were classified as high-solubility (Class 1 and Class 3) drugs in the four lists, suggesting that in vivo bioequivalence (BE) may be assured with a less expensive and more easily implemented in vitro dissolution test.
Historical Perspectives A century of dissolution research: From Noyes and Whitney to the Biopharmaceutics Classification System
TL;DR: This review attempts to account the most important developments in the field of dissolution research, from a historical point of view, in the framework of the Biopharmaceutics Classification System (BCS).
References
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Journal ArticleDOI
A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability
TL;DR: A biopharmaceutics drug classification scheme for correlating in vitro drug product dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling rate and extent of drug absorption.
Book
Substituent constants for correlation analysis in chemistry and biology
Corwin Hansch,Albert J. Leo +1 more
TL;DR: In this paper, the book is the window to get in the world and you can open the world easily, and these wise words are really familiar with you, so bring home now the book enPDFd substituent constants for correlation analysis in chemistry and biology to be your sources when going to read.
Journal ArticleDOI
Atomic physicochemical parameters for three dimensional structure directed quantitative structure-activity relationships. 4. Additional parameters for hydrophobic and dispersive interactions and their application for an automated superposition of certain naturally occurring nucleoside antibiotics
TL;DR: Les valeurs d'hydrophobicite de 120 types d'atomes sont evalues pour 893 composes a partir des refractivites molaires de 538 composes and la methode de superposition a ete appliquee a des antibiotiques nucleosides naturels isabelle d'un nombre important de composes.
Journal ArticleDOI
Dissolution Testing as a Prognostic Tool for Oral Drug Absorption: Immediate Release Dosage Forms
TL;DR: The aims of this article are to clarify under which circumstances dissolution testing can be prognostic for in vivo performance, and to present physiological data relevant to the design of dissolution tests, particularly with respect to the composition, volume, flow rates and mixing patterns of the fluids in the gastrointestinal tract.
Journal ArticleDOI
Evaluation of Various Dissolution Media for Predicting In Vivo Performance of Class I and II Drugs
Eric Galia,Eleftheria Nicolaides,D. Hörter,Raimar Löbenberg,Christos Reppas,Jennifer B. Dressman +5 more
TL;DR: With the array of compendial and physiological media available, it should be possible to design a suitable set of tests to predict the in vivo dissolution of both class I and II drugs from immediate release formulations.
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Predicting Drug Disposition via Application of BCS: Transport/Absorption/ Elimination Interplay and Development of a Biopharmaceutics Drug Disposition Classification System
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