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加工变量对醋氯芬酸微颗粒系统的影响。

Effect of processing variables on micro particulate system of aceclofenac.

作者信息

Dashora Kamlesh, Saraf S, Saraf Swarnlata

机构信息

Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur (C.G.) 492 010, India.

出版信息

Pak J Pharm Sci. 2006 Jan;19(1):6-10.

Abstract

Microparticulate systems of aceclofenac were prepared by modified solvent evaporation method using different variables such as polymer (cellulose acetate): drug ratios (1:9, 1:6, 1:3, and 1:1), agitation speeds (500-1,500 rpm) and stirring time (5-15 min). The effects of processing variables were evaluated by microparticle size and entrapment efficiency. The average microparticle size increases from 80.2+/-1.45 to 97.3+/-2.06 microm with increase in the polymer concentration while reduces with increase in agitation speed and stirring time; and at the higher speed gives irregular shape of particles. The highest entrapment efficiency, size uniformity, angle of repose (23.6+/-0.3 degree) and compressibility index (13.8+/-0.7%) of microparticles were found with 1:6 (polymer: drug ratio), at 1,000 rpm and 10 min stirring time among all microparticles. The in-vitro drug release study was carried out with prepared microcapsules (AC-1 to AC-4) of various polymer concentrations and optimized processing variables and compared with conventional and SR tablets. The conventional tablet and SR tablet releases maximum drug within 3 and 6h respectively while microparticulate system releases more than 12h. All formulations followed first order release kinetic and diffusion controlled drug release.

摘要

采用改良溶剂蒸发法,通过改变聚合物(醋酸纤维素)与药物的比例(1:9、1:6、1:3和1:1)、搅拌速度(500 - 1500转/分钟)以及搅拌时间(5 - 15分钟)等不同变量,制备了醋氯芬酸微粒系统。通过微粒尺寸和包封率评估加工变量的影响。随着聚合物浓度的增加,微粒平均尺寸从80.2±1.45微米增大至97.3±2.06微米,而随着搅拌速度和搅拌时间的增加微粒平均尺寸减小;且在较高速度下会产生不规则形状的颗粒。在所有微粒中,当聚合物与药物比例为1:6、搅拌速度为1000转/分钟、搅拌时间为10分钟时,微粒的包封率最高、尺寸均匀性最佳、休止角为23.6±0.3度、压缩指数为13.8±0.7%。对制备的不同聚合物浓度且加工变量优化的微胶囊(AC - 1至AC - 4)进行体外药物释放研究,并与普通片剂和缓释片剂进行比较。普通片剂和缓释片剂分别在3小时和6小时内释放最大量药物,而微粒系统释放药物超过12小时。所有制剂均遵循一级释放动力学且为扩散控制药物释放。

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