Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


2-Hydroxypropyl β-Cyclodextrin: A New Tool for the Improvement of Chemical Stability of Tiagabine HCl

Author(s): Abdussalam Sughir, Malika Lahiani-Skiba, Hassan Oulyadi, Mohamed Skiba.


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

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Article Details

Year: 2009
Page: [236 - 241]
Pages: 6
DOI: 10.2174/157018009787847800
Price: $58