大蒜素长循环脂质体的研制及血管刺激性与缓释性研究  

Preparation of allicin long-circulating liposome and research on its vascular stimulation and slow-releasing potential

作　　者：汪燕[1] 史载祥[1] 刘艳[2] 

机构地区：[1]中日友好医院,北京100029 [2]北京大学药学院,北京100083

出　　处：《中华中医药杂志》2015年第7期2615-2617,共3页China Journal of Traditional Chinese Medicine and Pharmacy

摘　　要：目的:制备大蒜素长循环脂质体(ALL),与大蒜素脂质体(AL)和大蒜素注射液在血管刺激性、缓释性方面进行比较。方法:1用反相蒸发法制备ALL,并对其包封率、形态、平均粒径、稳定性进行考察。2通过观察注药后兔耳缘静脉的色泽形态及组织切片判断药物对血管的刺激性。3注药4h后,检测大鼠血浆中大蒜素的浓度判断药物的缓释性。结果:1制备的ALL包封率为(84.57±5.21)%,其平均粒径为103.9nm,电镜下呈圆形或椭圆形,4℃冰箱中放置3个月无沉淀。2ALL对血管的刺激性评分与0.9%氯化钠溶液相当(0分),明显低于大蒜素注射液(4分)。3注药后4h,ALL组大鼠血浆大蒜素浓度是AL组的30倍(P<0.05),是大蒜素注射液组的40倍(P<0.05)。结论:研制的ALL有较高包封率,性质稳定,无血管刺激性,缓释性优于大蒜素其它剂型。Objective： To Prepare allicin long-circulating liposome（ALL）, then compare the liposome with allicin liposome（AL） and garlic injection in the aspect of vascular stimulation, slow-releasing potential. Methods： 1The ALL was prepared by a reverse-phase evaperation technique. The morphology of ALL, the entrapment ratio, the size distribution, and the stability were studied. 2The vascular stimulation caused by drugs was judged by observing the color and lustre of rabbit ear vein and its biopsy. 3Slow-releasing potential of drugs was judged by detecting the allicin concentration in plasma of rat after 4h of injection. Results： 1The entrapment ratio of ALL was（84.57±5.21）%, the mean diameter was 103.9nm, and their sizes were spherical or similar to spherical vesicles, and there was no precipitation occurred when stored in refrigerator of 4℃ for 3 monthes. 2The score of vascular stimulation of ALL was similar with 0.9% of sodium chloride solution（score of 0）, which was far less than that of garlic injection（score of 4）. 3The allicin concentration in plasma of rat in ALL group was 30 times of that in AL group（P〈0.05）, and was 40 times of that in garlic injection group（P〈0.05）. Conclusion： ALL has properties of high entrapment ratio, good stability, and no vascular stimulation, and its slow-releasing potential is superior to other allicin dosage forms.

关 键 词：大蒜素 长循环脂质体 包封率 刺激性 缓释性 

分 类 号：R943[医药卫生—药剂学] R965[医药卫生—药学]