大蒜素长循环脂质体的研制及血管刺激性与缓释性研究

发布时间：2019-03-17 08:39

【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(P0.05),是大蒜素注射液组的40倍(P0.05)。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。
[Abstract]:Aim: to prepare allitridin long circulating liposomes (ALL),) compared with allicin liposomes (AL) and allicin injection in the aspects of vascular irritation and sustained release. Methods: (1) ALL, was prepared by reverse evaporation and its entrapment efficiency, morphology and average particle size were determined. The stability was investigated. (2) the blood vessel irritation was evaluated by observing the color morphology and tissue sections of the auricular vein of rabbits after injection. (3) after 4 hours of injection, the concentration of allicin in rat plasma was determined to determine the slow-release of the drug. Results: 1 the entrapment efficiency of ALL was (84.57 卤5.21)%, the average particle size was 103.9 nm, and it was round or oval under electron microscope. 2the irritation score of all to blood vessel was equal to 0.9% NaCl solution (0 points), which was significantly lower than that of allicin injection (4 points). 3After injection of allicin, the stimulation score of all was similar to that of 0.9% sodium chloride solution (0 points), significantly lower than that of allicin injection (4 points). The plasma allicin concentration in ALL group was 30 times higher than that in AL group (P0.05) and 40 times as much as that in allicin injection group (P0.05). Conclusion: the prepared ALL has higher entrapment efficiency, stable properties, no vascular irritation and slow release than other forms of allicin.
【作者单位】：中日友好医院;北京大学药学院;
【分类号】：R943;R965

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