Preparation, Characterization and Dissolution Test of an Inclusion Complex of Atorvastatin in β-Cyclodextrin

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Abstract:

Inclusion complex of Atorvastatin (ATR) in β-cyclodextrin (β-CD) was prepared using co-evaporating technique. Characterization of the complex was carried out by the solubility method, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), 1H, 13C and fluorine nuclear resonance spectrometry (NMR). It was testified that the inclusion complex was formed between βCD and ATR. The stability constant K1:1 and the 1:1 steochiometry of complexation were determined. 1H, 13C and fluorine NMR analysis confirmed the inclusion and to provide information on the behavior of ATR inside the cavity of βCD. The dissolution rate of ATR/β-CD complex prepared by the co-evaporating technique was investigated and compared with this of the pure drug. Analysis of the dissolution samples was made by reversed phase liquid chromatographic method. The overall results showed that the dissolution rate of ATR/β-CD was significantly higher compared to the free ATR.

Keywords: Atorvastatin; Characterization dissolution test; Inclusion complex; Solubility; β-cyclodextrin

Document Type: Research Article

Publication date: May 1, 2013

More about this publication?
  • 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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