Chirality in Drug Design and Development by Indra K. Reddy, Reza Mehvar

By Indra K. Reddy, Reza Mehvar

Protecting each crucial point within the improvement of chiral items, this reference presents an excellent assessment of the formula, biopharmaceutical features, and regulatory matters impacting the creation of those pharmaceuticals—supporting researchers as they severely evaluation the pharmacodynamic, pharmacokinetic, and toxicological features of particular enantiomers and chiral drug compounds.

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Optical activity is the most characteristic index of optical purity in cases where the chiral excipients are suspected to be enantiomerically impure. Chiral excipients with no observable optical activity are assumed to be in a 1 : 1 ratio of enantiomers (racemates). However, the measurement may be accidental due to the storage conditions (such as temperature and medium) in which the determination was done, which could lead to changes in optical activity [15]. In such cases, the sample is not considered racemic but is said to be cryptochiral [16].

13. 14. ; Fitzpatrick, A. Commonly used chiral drugs: a survey. Chirality 1993, 5, 573–576. D. Pharmacological importance of stereochemical resolution of enantiomeric drugs. Drug Safety 1997, 17, 149–165. Wainer, I. ; Marcel Dekker: New York, 1993. Drayer, D. Pharmacodynamic and pharmacokinetic differences between drug enantiomers in humans: an overview. Clin. Pharmacol. Ther. 1986, 40, 125–133. ; McKay, G. W. The impact of stereoisomerism in bioequivalence studies. J. Pharm. Sci. 1998, 87, 797–802.

Pharm. 1999, 178, 111–120. Copyright 2004 by Marcel Dekker, Inc. All Rights Reserved. A. 1. INTRODUCTION A majority of the chiral excipients employed in pharmaceutical dosage forms are from natural sources and therefore exist in the optically pure form. Chiral excipients have been traditionally used, though unintentionally, in many pharmaceutical dosage forms [1–3] and as stationary phases for gas and liquid chromatography in qualitative and/or quantitative analysis of enantiomeric drugs [4–7].

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