Jelvehgari Mitra, Hassanzadeh Davoud, Kiafar Farhad, Delf Loveym Badir, Amiri Sara
Department of Pharmaceutics, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran. ; Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
Iran J Pharm Res. 2011 Summer;10(3):457-67.
The objective of this study was to formulate and evaluate the drug-polymer interaction of mefenamic acid (MA) using two polymers with different characteristics as ethylcellulose (EC) and/or cellulose acetate phthalate (CAP). Microspheres were prepared by the modified emulsion solvent evaporation (MESE). The effect of drug-polymer interaction was studied for each of microspheres. Important parameters in the evaluation of a microencapsulation technique are encapsulation efficiency, yield production, particle size, surface characteristics of microspheres, scanning electronic microscopy (SEM), powder X-ray diffraction analysis (XRD), and differential scanning calorimetry (DSC). The in-vitro release studies are performed in Tris buffer (pH 9) with Sodium lauryl sulfate (SLS). Microspheres containing CAP and EC showed 68-97% and 63-76% of entrapment efficiency, respectively. The thermogram X-ray and DSC showed stable character of MA in the microspheres and revealed an absence of drug polymer interaction. The prepared microspheres were spherical in shape and had a size range of 235-436 μm for CAP-microspheres and 358-442 μm for EC-microspheres. The results suggest that MA was successfully and efficiently encapsulated; the release rates of matrix microspheres are related to the type of polymer, only when polymers (EC and CAP combine with 1 : 1 ratio) were used to get prolonged drug release with reducing the polymers content in the microspheres. Data obtained from in-vitro release for microspheres and commercial capsule were fitted to various kinetic models and the high correlation was obtained in the peppas model. Mefenamic acid, Ethylcellulose, Cellulose acetate phthalate, Microparticles, Modified emulsion-solvent evaporation.
本研究的目的是使用两种具有不同特性的聚合物,即乙基纤维素(EC)和/或邻苯二甲酸醋酸纤维素(CAP),来制备并评估甲芬那酸(MA)与聚合物的相互作用。通过改良的乳液溶剂蒸发法(MESE)制备微球。对每种微球研究了药物 - 聚合物相互作用的影响。微囊化技术评估中的重要参数包括包封率、产率、粒径、微球的表面特性、扫描电子显微镜(SEM)、粉末X射线衍射分析(XRD)和差示扫描量热法(DSC)。体外释放研究在含有十二烷基硫酸钠(SLS)的Tris缓冲液(pH 9)中进行。含有CAP和EC的微球的包封率分别为68 - 97%和63 - 76%。X射线热分析图和DSC显示MA在微球中具有稳定特性,且未显示出药物 - 聚合物相互作用。制备的微球呈球形,CAP微球的粒径范围为235 - 436μm,EC微球的粒径范围为358 - 442μm。结果表明MA已成功且有效地被包封;基质微球的释放速率与聚合物类型有关,仅当聚合物(EC和CAP以1:1比例组合)用于减少微球中聚合物含量以实现药物缓释时。从微球和市售胶囊的体外释放获得的数据拟合到各种动力学模型,在Peppas模型中获得了高度相关性。甲芬那酸、乙基纤维素、邻苯二甲酸醋酸纤维素、微粒、改良乳液 - 溶剂蒸发法