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阿昔洛韦载药聚合物微粒的制剂与体外评价:一项溶解度增强研究。

FORMULATION AND IN VITRO EVALUATION OF ACYCLOVIR LOADED POLYMERIC MICROPARTICLES: A SOLUBILITY ENHANCEMENT STUDY.

作者信息

Mahmood Asif, Ahmad Mahmood, Sarfraz Rai Muhammad, Minhas Muhammad Usman, Yaqoob Ayesha

出版信息

Acta Pol Pharm. 2016 Sep;73(5):1311-1324.

Abstract

Objective of present work was to formulate polymeric microparticles of acyclovir using 0-cyclodextrin by solvent evaporation method and kneading technique. Four different ratios were fabricated in each case. Sodium lauryl sulfate (4% was utilized as intestinal permeation enhancer in this study. Prepared microparticles were characterized for micromeritic properties i.e., angle of repose, Hausner's ratio, Carr's index, bulk density and tapped density, entrapment efficiency, zeta size and zeta potential, Fourier transform infrared spectroscopy, differential scanning calorimetry, powder x-ray diffraction, scanning electron microscopy, transmission electron microscopy, optical microscopy and permeability studies across chicken intestine. Kinetic models: zero order, first order, Higuchi and Korsmeyer Peppas were applied on release data. Based upon the results of entrapment efficiency (81.25% and 74.50%), product yield (92.50% and 85.50%), permeability (85.18% and 82.05%), x-ray diffraction (amorphous nature), and solubility etc., (1 : 2) drug-polymer ratio was declared the best. Moreover, solid dispersions (1 : 2) had shown promising results. A new potential approach for solubility, bioavailability and permeability enhancement of acyclovir and other BCS class IV drugs was successfully established.

摘要

本研究的目的是通过溶剂蒸发法和捏合技术,使用β-环糊精制备阿昔洛韦聚合物微粒。每种情况下制备了四种不同比例的微粒。本研究中使用十二烷基硫酸钠(4%)作为肠道渗透促进剂。对制备的微粒进行了微观性质表征,即休止角、豪斯纳比、卡尔指数、堆密度和振实密度、包封率、zeta粒径和zeta电位、傅里叶变换红外光谱、差示扫描量热法、粉末X射线衍射、扫描电子显微镜、透射电子显微镜、光学显微镜以及鸡肠道的渗透性研究。动力学模型:零级、一级、 Higuchi和Korsmeyer Peppas模型应用于释放数据。基于包封率(81.25%和74.50%)、产品收率(92.50%和85.50%)、渗透性(85.18%和82.05%)、X射线衍射(无定形性质)和溶解度等结果,药物与聚合物比例为(1:2)被判定为最佳。此外,(1:2)的固体分散体显示出良好的结果。成功建立了一种提高阿昔洛韦和其他BCS IV类药物溶解度、生物利用度和渗透性的新的潜在方法。

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