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Role of racemization in optically active drugs development
Author(s) -
Ali Imran,
Gupta Vinod K.,
AboulEnein Hassan Y.,
Singh Prashant,
Sharma Bhavtosh
Publication year - 2007
Publication title -
chirality
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.43
H-Index - 77
eISSN - 1520-636X
pISSN - 0899-0042
DOI - 10.1002/chir.20397
Subject(s) - racemization , chemistry , optically active , enantiomer , drug , active ingredient , in vivo , pharmacology , food and drug administration , combinatorial chemistry , stereochemistry , organic chemistry , microbiology and biotechnology , medicine , biology
U.S. Food and Drug Administration issues certain guidelines for marketing of optically active drugs as some enantiomers racemize into human body, leading to the generation of other antipodes, which may be toxic or ballast to the human beings. Moreover, racemization reduces the administrated dosage concentration as optically active enantiomer converted into its inactive counter part. Therefore, the study of racemization of such type of drugs is an important and urgent need of today. This article describes in vitro and in vivo racemization of optically active drugs. The racemization process of various optically active drugs has been discussed considering the effect of different variables i.e. pH, temperature, concentration of the drug, ionic concentration, etc. Attempts have also been made to discuss the mechanisms of racemization. Besides, efforts have been made to suggest the safe dosages of such type of drugs too. Chirality, 2007. © 2007 Wiley‐Liss, Inc.