Solubility and dissolution enhancement of saquinavir mesylate by inclusion complexation technique
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The objective of the present study was to formulate inclusion complex of saquinavir mesylate to improve the aqueous solubility and dissolution rate. Saquinavir mesylate is a BCS class II drug having low aqueous solubility and therefore low oral bioavailability. In the present study, inclusion complex of saquinavir mesylate with hydroxypropyl-β-cyclodextrin were prepared by kneading method. Inclusion complex were characterized by differential scanning calorimetry (DSC), X-ray diffractometry (XRD), 1H NMR studies, and Fourier transform infrared spectroscopy and evaluated for in vitro dissolution, and phase solubility studies. DSC and XRD study demonstrated that there was a significant decrease in crystallinity of pure drug present in inclusion complex, which resulted in an increased dissolution rate of saquinavir mesylate and 1H NMR studies strongly, confirmed that the inclusion complex has formed. Inclusion complexation results in improvement in solubility and dissolution rate. The inclusion complexation would be suitable method for dissolution and bioavailability enhancement of saquinavir mesylate.
KeywordsHPβCD Inclusion complexation Saquinavir mesylate Kneading method Dissolution enhancement
Authors are thankful to Panacea Biotech Pvt. Ltd., Mumbai, India, for providing gift sample of saquinavir mesylate. The authors are also grateful to Principal (R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur) for providing necessary facilities and infrastructure for carrying out this work. Support of Mr. Vipul Rane, is kindly acknowledged.
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