摘要
目的研究利用明胶与阿拉伯胶作为囊材制备水飞蓟宾缓释微囊及其缓释效果和机制。方法以药物与胶液比例(A)、胶液质量浓度(B)、pH值(C)和戊二醛(D)为影响微囊缓释性能的主要因素设计正交实验,以累积释放量为评价指标,选出最佳处方及工艺条件;在最佳处方配比的条件下研究了水飞蓟宾缓释微囊的药动学并对其缓释机制进行探究。结果各因素对水飞蓟宾微囊释放量影响大小顺序为B>A>D>C,最佳处方和工艺条件为A2B3C1D2,即药物与胶液比例为1∶5、胶液质量浓度<50.0g·L^(-1)、pH值为3.0和戊二醛质量浓度为0.01g·mL^(-1);经静脉给药后,水飞蓟宾缓释微囊在大鼠体内消除半衰期约为18h,明显比水飞蓟宾原料药消除半衰期延长;释药机制的研究表明,渗透压、扩散作用和释药动力源对水飞蓟宾缓释微囊的释药有影响;而释药介质的pH值对水飞蓟宾微囊的缓释作用影响不显著。结论采用明胶与阿拉伯胶作为囊材制备的水飞蓟宾微囊具有良好的缓释效果。
Objective To prepare Silybin Sustained-release Microcapsules with gelatin and acacia as the capsule wall material. Methods The factors,such as the amount ratio of drug to materials （A）,the concentration of materials （B）,pH value （C） and the amount of glutaraldehyde （D）,were chosen to design orthogonal test with accumulation release rate as index.The pharmacokinetics of Silybin Sustained-release Microcapsules in vivo was studied under the optimal prescription ratio and the mechanism of the sustained-release microcapsules was explored. Results The factors of B,A,D and C showed a great effect on accumulation release rate and the optimal formula were A 2B 3C 1D 2,i.e .,the ratio of drug to glue was 1∶5 and the mass concentration of glue was 〈50.0 g·L^-1,the pH was 3.0 and the glutaraldehyde mass concentration was 0.01g·mL^-1.After intravenous administration,the elimination half-life of Silybin Sustained-release Microcapsules in rats was about 18 h,which was significantly longer than the elimination half-life of the control group.In drug release mechanism,it was found that osmotic pressure,diffusion effect and release power source had an effect on the release of Silybin Sustained-release Microcapsules,but the pH of drug-releasing medium has no effect. Conclusion The prepared Silybin Sustained-release Microcapsules showed a fine profile of sustained-release.
作者
王峰
WANG Feng(Department of Pharmacy,Nanjing University of Chinese Medicine Affiliated Hospital,Jiangyin 214400,China)
出处
《西北药学杂志》
CAS
2018年第5期645-651,共7页
Northwest Pharmaceutical Journal
关键词
水飞蓟宾
微囊
药动学
缓释
体外释放
释药机制
silybin；microcapsule；pharmacokinetics
sustained-release
in vitro release；release mechanism
