Authors: Sughir, Abdussalam; Lahiani-Skiba, Malika; Oulyadi, Hassan; Skiba, Mohamed

Source: Letters in Drug Design & Discovery, Volume 6, Number 3, April 2009 , pp. 236-241(6)

Publisher: Bentham Science Publishers

Abstract:

The aim of this paper was to describe the use of a 2-hydroxypropyl beta-cyclodextrin (2-HPβCD) as a tool to improve the chemical stability of tiagabine hydrochloride (TGB). HPLC method was used to quantify TGB. The correlation coefficient of the linearity (r2) of HPLC method was more than 0.999 whilst the limit of detection and the limit of quantification of TGB were 0.6494 μg ml-1 and 1.765μg ml-1 respectively. The effect of 2-HPβCD on the chemical stability of TGB was compared with α-tocopherol and ascorbic acid, the most recognized antioxidants used to enhance the stability of TGB. The stability was expressed by (% w/w) of the total related substances (TRS) of TGB. When TGB was exposed for 24 h to 50°C, the TRS were 3.264% (SD ±0.077) and 3.125% (SD ±0.053) in the presence of α-tocopherol and ascorbic acid, respectively. The TRS of TGB complexed with 2-HPβCD was 2.142% (SD ±0.045). This study demonstrates that 2-HPβCD exhibits an obvious enhancement of TGB chemical stability with a different mechanism compared with the usual antioxidants.

Keywords: Cyclodextrin; Tiagabine; Chemical stability; Inclusion complex; HPLC analysis

Document Type: Research article

DOI: http://dx.doi.org/10.2174/157018009787847800

Publication date: 2009-04-01

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• Letters in Drug Design & Discovery publishes original letters on all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis will be on publishing quality papers very rapidly. Letters will be processed rapidly by taking full advantage of Internet technology for both the submission and review of manuscripts. The journal is essential reading to all pharmaceutical scientists involved in research in drug design and discovery.

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