Dashora Kamlesh, Saraf S, Saraf Swarnlata
Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur (C.G.) 492 010, India.
Pak J Pharm Sci. 2006 Jan;19(1):6-10.
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.
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。