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目的 制备肺靶向汉防己甲素缓释微囊 ,以提高药物降低肺动脉高压的作用并降低其毒性。方法 汉防己甲素用喷雾干燥 热变性微囊化 ,用UV测定汉防己甲素微囊的体外释放特性 ,用反相高效液相测定小鼠体内分布 ,经大鼠肺动脉插管测定其压力。结果 汉防己甲素微囊外观呈圆球形 ,带正电荷 ,载药量 37 88% ,微囊的体外释药规律符合Higuchi方程。小鼠肺部的药物浓度明显提高 ,平均滞留时间延长 ,大鼠肺动脉高压的降压作用从15 7 1h延长到 2 2 3 6h ,体内降压百分数与体外释药百分数之间具有相关性。结论 汉防己甲素经喷雾干燥 热变性微囊化可使其高效、低毒地治疗肺动脉高压
Objective To prepare lung-targeted slow-release microcapsules of tetrandrine in order to increase the effect of drugs on reducing pulmonary hypertension and reduce its toxicity. Methods Tetrandrine was heat-denatured microencapsulated by spray-drying. The in vitro release characteristics of tetrandrine microcapsules were determined by UV. The distribution in mice was determined by RP-HPLC and the pressure was measured by rat pulmonary artery cannulation. Results Tetrandrine microcapsules were spherical in shape and positively charged. The drug loading was 37 88%. The in vitro drug release of microcapsules conformed to the Higuchi equation. The concentration of drug in the lungs of mice was significantly increased, the average residence time was prolonged, and the antihypertensive effect of pulmonary hypertension in rats was prolonged from 157 to 1 2 hours to 2 272 hours. There was a correlation between the percentage of blood pressure in vivo and the percentage of in vitro drug release. Conclusion Tetrandrine is spray-dried by heat-denaturing microencapsulation to make it highly effective and less toxic to treat pulmonary hypertension