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Enantiomeric purity evaluation of atenolol and nadolol using high-performance liquid chromatography with chiral stationary phase

Grant number: 15/20517-3
Support type:Scholarships in Brazil - Scientific Initiation
Effective date (Start): October 01, 2016
Effective date (End): September 30, 2017
Field of knowledge:Health Sciences - Pharmacy
Principal Investigator:Anil Kumar Singh
Grantee:Gabriela Souto Cardoso
Home Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil

Abstract

Most antihypertensive drugs prescribed are marketed under the racemic form, despite the well-known fact that the presence of different enantiomers in a pharmaceutical formulation can lead to different pharmacological activities, distinct pharmacokinetic and toxicological profiles. The use of the pure enantiomers in pharmaceutical formulations may result in better dose adjustment and reduction of adverse effects, a fact that makes studies on molecular chirality of utmost importance in the pharmaceutical field. The characterization and quantification of enantiomers in pharmaceutical drug substances and drug products became mandatory with the implementation of RDC n° 57, in 2009 by Brazilian drug regulatory agency (ANVISA). These regulatory changes lead to an increase in the demand of rapid, accurate and sensitive methods, for the determination of enantiomeric purity of chiral drug substances. Currently, the most analytical methods employed for separation and determination of enantiomeric purity of compounds are restricted to chromatographic techniques. On the other hand, for proper development and validation of enantioselective methods, the use of reference substance is indispensable. There is great scarcity of reference drug substances with adequate and acceptable purity, the situation with pure enantiomers is even more critical. This scientific initiation project aims to expand the scientific-academic knowledge on the proposed topic, namely importance of chirality, method of chiral separation and preparation of enantiomerically pure reference drug substances. Develop innovative strategies for enantiomeric separation of the two beta-blockers, atenolol and nadolol in semipreparative scale; use obtained pure enantiomers as reference standards in the development and validation of accurate and sensitive chromatographic methods and their application in the quantitative determination of enantiomers of atenolol and nadolol in pharmaceutical preparations. (AU)