Enantiomorphic Composition

Chirality plays an important role in pharmaceutical industries. The pharmaceuticals obtained by chemically synthesis are often chiral drugs, and more than half of the drugs currently in use are chiral compounds. Chiral drugs can exist in the form of enantiomers. Enantiomer drugs occupy a large proportion in the pharmaceutical industry. Enantiomers are a part and parcel of drug discovery and development. It is well-known that many pharmaceutical enantiomorphs show different pharmacokinetics and pharmacodynamics due to the difference of stereochemistry, and they often have significant differences in pharmacological actions, such as distribution, metabolism and excretion. Due to different pharmacological activity, the biological effects of a pair of enantiomers on humans or animals are quite different. In general, only one form of enantiomers pair has significant pharmacological activity, while the other enantiomer is low or inactive, even exhibiting opposite activity or toxic side effects. For example, the (l)-isomers of some barbiturates act as depressants while the (d)-isomers act as convulsants. The potency, toxicity and pharmacokinetics of a single enantiomer should be evaluated separately in the development of new chiral drugs. US Food and Drug Administration (FDA) regulations place major emphases on the characterizations of enantiomeric compositions of pharmaceutical products in order to ensure drugs containing only the therapeutically active enantiomers. Therefore, enantiomeric characterization and composition determination are important issues in pharmaceutical industry. Enantiomeric analysis in the pharmaceutical industry has been the focus of academic research and drug development.

It is very important to measure enantiomeric composition for a chiral molecule, in particular a chiral drug, because people working in this area need related information to evaluate the biological data to make sure they are viable. At present, a variety of analytical techniques mainly based on either separation or spectroscopic are utilized for analyzing and determining enantiomeric composition of a chiral compound, like high-performance liquid chromatographic (HPLC), gas chromatographic (GC), nuclear magnetic resonance (NMR), capillary electrophoretic (CE), and MS. Among these available methods, GC and HPLC are the most commonly used. All these techniques are available for Alfa Chemistry , our laboratories are equipped with various cutting-edge instruments. Our experts have extensive experience in the enantiomeric composition determination for a variety of drug substances, pharmaceutical intermediates and products.

Method to determine enantiomeric composition

• HPLC is a rapid and sensitive method for the determination of enantiomeric composition of some compounds, such as epinephrine, ibuprofen in human plasma, etc.;

• GC, as a rapid method, is the most common approach adopted for the enantiomeric analysis of amphetamine and related drugs and metabolites;

• NMR spectroscopy turns out to be a powerful and rapid tool for assessing drug enantiomeric composition, such as methamphetamine, selegiline, amphetamine and norephedrine;

•  CE is known to be one of the most powerful analytical techniques for enantiomeric composition determinations.

The expertise and facilities of Alfa Chemistry allow to perform accurate characterizations. For further information, please contact with us.