摘要
用乳化法制备盐酸川芎嗪明肢微球，优化了工艺。对微球的外观、粒径与其分布、含量、体外释药、稳定性及体内分布等进行研究。结果表明平均粒径为１２．６５μｍ，粒径范围５．０～２４．９μｍ占总数的８７．５％，球内含药量平均为１６．４９％±０．４９％（ｎ＝３），冰箱或室温放置稳定，体外释药符合一级动力学规律，释药ｔ＿（１／２）比原药延长约５倍。小鼠静注微球后２０ｍｉｎ，在肺内的相对分布百分率明显高于其它组织与血液，与溶液对照组相比，提高近６倍。
The effect of ligustrazine hydrochloride (LTH) on depressing pulmonary arteryhypertension has been proved in recent studies.In an attempt to prepare a lung targeting dosage form,ligustrazine hydrochloride gelatin microspheres (LTH-GMS)were prepared by the method of emulsionprocess,using 2∶1 as the weight ratio of LTH to gelatin. The preparation technique was optimizedand the apl1earance,particle size and size distribution,LTH content,in vitro release,stability,and invivo distribution of LTH-GMS were studied.The results showed that the mean diameter of LTH-GMSmeasured by Coulter counter was 12.65μm,87.5% of the microspheres ranging from 5 to 24.9μm.The average content of LTH in LTHGMS was 16.49%±0.49%(n=3)with an average extent ofentrapment of abOut 89%and the LTH-GMS were stable for three months when stored in refrigeratoror at rcom temperature. The release profile in vitro(pH 7.8～8.0 phosphate buffer)can be describedby first-order kinetic equation. The release t1/2 of LTH when given LTH-GMS was about 6 times asmuch as that of original LTH, The relative distribution percentage of LTH-GMS in lung whendetermined 20 min after iv administration to mice was significantly higher than those of LTH-GMS inother tissues and blood,and was about 6 times as much as that of the LTH solution control group inlung under the same conditions.
出处
《药学学报》
CAS
CSCD
北大核心
1996年第2期132-137,共6页
Acta Pharmaceutica Sinica
基金
卫生部科学基金
关键词
盐酸川芎嗪
明胶微球
肺靶向给药
制备
乳化法
Ligustrazine hydrochloride
Gelatin microspheres
Lung targeting drug deliverysystem
Pulmonary artery hypertension
