乙基纤维素、醋酸纤维素和芡实RS100微球的释药和透性比较

Prakash Katakam, Saousen R. Diaf, B. Dey, S. K. Adiki, B. Chandu, K. Chowdary
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引用次数: 1

摘要

本研究旨在比较评价双氯芬酸钠载乙基纤维素(EC)、醋酸纤维素(CA)和苦楝油(EU)微球的释药和通透性。采用乳化-溶剂蒸发(油中油,o/o)法制备了双氯芬酸钠的EC、CA和EU微球,并对各参数进行了比较评价。微球具有离散、自由流动、多核、整体和球形等特点。制备的微球中约有55.60%在-20+30(715m)孔径范围内。不同聚合物的包封效率为97.1±106.4%。微球的壁厚范围为13.69 ~ 74.97m,与聚合物用量有关,与聚合物浓度成正比。双氯芬酸在较长时间内从微球中缓慢释放,这取决于所使用的聚合物和包芯比。释放受扩散控制,符合一级动力学。三种聚合物的涂膜率、壁厚和释放速率常数均呈良好的线性关系。被膜百分比与释放率(k1)的斜率分别为0.4117、0.2351和0.9762;EC、CA和EU微球的壁厚(h)与药物释放率(k1)的比值分别为0.2549、0.1863和0.7850。坡度越小,控制效果越好。醋酸纤维素的控释效果优于乙基纤维素和苦苣苔。不同微球对双氯芬酸的释放率和渗透性的增大顺序为醋酸纤维素<乙基纤维素<乌龙油RS100。药物从制备的多孔微球的渗透性可能是由于双氯芬酸产生的渗透压。
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A Comparative Evaluation of Drug Release and Permeability of Ethylcellulose, Cellulose Acetate and Eudragit RS100 Microspheres
Present study aims at comparative evaluation of drug release and permeability of diclofenac sodium loaded ethylcellulose (EC), cellulose acetate (CA) and eudragit (EU) microspheres. Microspheres of EC, CA and EU containing diclofenac sodium were prepared by an emulsification-solvent evaporation (oil-in-oil, o/o) method and were investigated for a comparative evaluation of various parameters. The microspheres were found discrete, free flowing, multinucleate, monolithic and spherical. About 5560% of all microspheres prepared were in the size range of -20+30 (715 m) mesh size. The encapsulation efficiency was in the range of 97.1106.4% with various polymers. The wall thickness of microspheres was in the range of 13.69-74.97m which depended on polymer employed and was directly proportional to polymer concentration. Diclofenac release from the microspheres was slow over longer periods of time and depended on the polymer used and coat:core ratio. Release was diffusion controlled and followed first order kinetics. Good linear relationships were observed between percent coat, wall thickness and release rate constant with all the three polymers. The slopes of percent coat vs release rate (k1) plots were found to be 0.4117, 0.2351 and 0.9762; and those of wall thickness (h) vs drug release rate (k1) plots were found 0.2549, 0.1863 and 0.7850 respectively for EC, CA and EU microspheres. The lower the slope the better is the controlling effect. Cellulose acetate exhibited better release-controlling effect than that of ethylcellulose and eudragit. The increasing order of diclofenac release rate and permeability observed with various microspheres was, cellulose acetate < ethylcellulose < eudragit RS100. The possible permeability of drug from the prepared porous micrsopheres could be due to osmotic pressure generated by diclofenac.
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