Formulation development and evaluation of Glibenclamide loaded Eudragit RLPO microparticles

B. P. Kumar, I. S. Chandiran, K. N. Jayaveera
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引用次数: 10

Abstract

The objective of the present investigation was to formulate and evaluate microencapsulated Glibenclamide produced by the emulsion – solvent evaporation method. Microparticles were prepared using Eudragit RLPO by emulsion solvent evaporation method and characterized for their micromeritic properties, encapsulation efficiency, particle size, drug loading, FTIR, DSC, SEM analysis. In vitro release studies were performed in phosphate buffer (pH 7.4). Stability studies were conducted as per ICH guidelines. The resulting microparticles obtained by solvent evaporation method were free flowing in nature. The mean particle size of microparticles ranges from 134.49 – 179.72 µm and encapsulation efficiency ranges from 92.30-98.32%. The infrared spectra and differential scanning calorimetry thermographs confirmed the stable character of Glibenclamide in the drug-loaded microparticles. Scanning electron microscopy revealed that the microparticles were spherical in nature. In vitro release studies revealed that the drug release was sustained up to 12 hrs. The release kinetics of Glibenclamide from optimized formulation followed zero-order and peppas mechanism. The mechanism of drug release from the microparticles was found to be non-Fickian type. Eudragit RLPO microparticles containing Glibenclamide could be prepared successfully by using an emulsion solvent evaporation technique, which will not only sustain the release of drug but also manage complicacy of the diabetes in a better manner. DOI:  http://dx.doi.org/10.3329/icpj.v2i12.17016 International Current Pharmaceutical Journal, November 2013, 2(12): 196-201
载格列本脲的芡实RLPO微粒的研制与评价
本研究的目的是制备并评价乳状溶剂蒸发法制备的微胶囊格列本脲。采用乳化溶剂蒸发法制备了乌龙茶RLPO微颗粒,并对其微观性能、包封效率、粒径、载药量、FTIR、DSC、SEM等进行了表征。在磷酸盐缓冲液(pH 7.4)中进行体外释放研究。稳定性研究是按照ICH指南进行的。溶剂蒸发法制得的微颗粒是自由流动的。微颗粒平均粒径为134.49 ~ 179.72µm,包封效率为92.30 ~ 98.32%。红外光谱和差示扫描量热图证实了格列本脲在载药微粒中的稳定性。扫描电镜显示,微颗粒为球形。体外释放研究表明,药物释放持续长达12小时。优化后的格列本脲释放动力学遵循零级和胡椒动力学。发现微颗粒的药物释放机制为非菲克型。采用乳化液溶剂蒸发技术成功制备了含格列本脲的乌龙茶RLPO微颗粒,既能维持药物的释放,又能较好地控制糖尿病的复杂性。DOI: http://dx.doi.org/10.3329/icpj.v2i12.17016国际现代医药杂志,2013年11月,2(12):196-201
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