University College of Pharmacy, Mahatma Gandhi University, Ettumanoor , Kerala , India .
Drug Deliv. 2014 Mar;21(2):110-7. doi: 10.3109/10717544.2013.834414. Epub 2013 Sep 12.
Designing a sustained release system for Carvedilol to increase its residence time in the stomach.
Preparation of floating microsphere by the emulsion solvent diffusion method, studying the effect of various process parameters and optimize the formulation using full factorial design.
Different microsphere formulations were prepared by varying the ratio ethanol:dichloromethane (1:0 to 1:1.5), ethyl cellulose:hydroxypropyl methyl cellulose and stirring speed (800-1600 rpm). The effect of these variables on particle size, encapsulation parameters, surface topography, in vitro floatability and drug release were evaluated.
3(2) full factorial design was used for the optimization of the formulation. Drug entrapment efficiency, particle size and in vitro drug release were dependent on concentration of ethyl cellulose and stirring speed. Microspheres remained buoyant for more than 10 h and showed sustained release of the drug.
Floating microspheres of Carvedilol with good floating ability and sustained release were developed.
设计一种卡维地洛的缓释系统，以增加其在胃中的驻留时间。
采用乳化溶剂扩散法制备漂浮微球，通过全因子设计研究各种工艺参数的影响，并优化处方。
通过改变乙醇：二氯甲烷（1:0 至 1:1.5）、乙基纤维素：羟丙基甲基纤维素的比例和搅拌速度（800-1600 rpm）来制备不同的微球配方。评估这些变量对粒径、包封参数、表面形貌、体外漂浮性和药物释放的影响。
采用 3(2)全因子设计对处方进行优化。药物包封效率、粒径和体外药物释放均依赖于乙基纤维素的浓度和搅拌速度。微球具有良好的漂浮能力，能在 10 小时以上保持漂浮，并呈现出药物的持续释放。
制备了具有良好漂浮能力和持续释放性能的卡维地洛漂浮微球。
