The Significance of Chiral Separation, Determination of EnantiomericPurity in Drug Design, Safety and Development –An Overview

Abstract

Chiral separation, as well as the determination of the optical purity of chiral pharmaceuticals, has attracted a great deal of attention from the healthcare and pharmaceutical industries. Most pharmaceutical researches and drug development efforts have been concentrated on the production of enantiomerically pure products because of the increasing demand for such drugs to be administered in a highly optical purified form. Accordingly, chirality is also a major concern in the pharmaceutical industry. When the enantiomers of a drug are administered into a chirally selective living system, these enantiomers frequently exhibit differences in bioavailability, distribution, metabolic and excretion behavior and action. The determination of optical impurity in a drug is very important from the efficacy and safety point of view, and is rapidly becoming one of the key issues in the development of new drugs. Chirality influences drug delivery because a single enantiomer or a non-racemic blend may have improved solubility, dissolution, and stability. Chirality is a major concern in the modern pharmaceutical industry. This interest can be attributed largely to a heightened awareness that enantiomers of a racemic drug may
have different pharmacological activities, as well as different pharmacokinetic and pharmacodynamic effects. To assure patient safety and clinical efficacy, the pharmacological evaluation of stereoisomers is an integral part of new drug development. Analytical methods to determine the enantiomeric purity of new investigational drugs are often attained through a series of generic or screening methodologies. The main methods used for chiral drug separation are GC, HPLC, and CE. Other techniques, such as chiral crystallization and enzyme-based kinetic separation.