Formulation development & invitro evaluation of efavirenz cyclodexprin complexes im-mediate release tablets

Prasad Bingidoddi, V. J. Marabathuni, Naidu Narapusetty
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Abstract

The study was designed to investigate the effect of cyclodextrins (CDs) on the solubility, dissolution rate, and bioavailability of efavirenz by forming inclusion complexes. Prepared inclusion complexes were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction (XRD) studies. In vitro dissolution study was performed using phosphate buffer pH 6.4, distilled water, and HCl buffer pH 1.2 as dissolution medium. Among all efavirenz–cyclodextrins complexes, efavirenz–DM-β-CD inclusion complex (1:3) prepared by coprecipitation method showed 1.53-fold and 4.11-fold increase in absorption along with 2.1-fold and 2.97-fold increase in dissolution rate in comparison with Pletoz-50 and pure efavirenz, respectively.
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依非韦伦环dexprin配合物速释片的处方研制及体外评价
本研究旨在探讨环糊精(CDs)通过形成包合物对依非韦伦溶解度、溶出率和生物利用度的影响。采用傅里叶变换红外光谱、差示扫描量热法(DSC)和x射线衍射(XRD)对所制备的包合物进行了表征。以pH 6.4的磷酸盐缓冲液、蒸馏水、pH 1.2的盐酸缓冲液为溶出介质进行体外溶出研究。在所有依非韦伦-环糊精配合物中,共沉淀法制备的依非韦伦- dm -β-CD包合物(1:3)的吸光度比Pletoz-50和纯依非韦伦分别提高1.53倍和4.11倍,溶出率分别提高2.1倍和2.97倍。
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