银杏黄酮组分自微乳-微丸释药系统的构建  

Construction of ginkgo flavonoids drug release system

作　　者：刘丹[1] 张露[1] 张振海[1] 贾晓斌[1] 

机构地区：[1]江苏省中医药研究院国家中医药管理局中药释药系统重点研究室,江苏南京210028

出　　处：《中草药》2017年第16期3377-3383,共7页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(H2806/81503265)

摘　　要：目的根据银杏黄酮生物药剂学性质及其临床释药行为的特点构建银杏黄酮组分自微乳-微丸释药系统。方法根据溶解度,筛选出合适的油相、乳化剂和助乳化剂;采用水滴定法绘制伪三元相图,筛选出合适的乳化剂与助乳化剂的质量比(Km值);以粒径、Zeta电位和溶液澄明度为指标,在选定的Km值下进行混合乳化剂与油相比例的筛选;采用HPLC法测定自微乳中银杏黄酮的量;根据筛选出的制剂处方制成自微乳,再加入适当的辅料采用挤出滚圆法制成微丸;评价微丸的溶出行为。结果油相、乳化剂和助乳化剂分别为肉豆蔻酸异丙酯(IPM)、聚山梨酯-80和无水乙醇;Km值为3∶1;聚山梨酯-80和无水乙醇总质量与IPM质量比为9∶1,银杏黄酮加药量0.202 5 g,制得的自微乳粒径均小于30 nm;自微乳中银杏黄酮的量为13.32 mg/m L,以自微乳作为自黏合剂制备载药量为25%的自微乳-微丸释药系统,显著提高了银杏黄酮的溶出。结论以自微乳作为前制剂制成的微丸性质较稳定,且银杏黄酮的溶出能力得到改善。Objective To construct ginkgo flavonoids drug release system based on bioavailability of ginkgo flavonoids and its clinical drug delivery behavior. Methods Suitable oil phase, surfactant and cosurfactant were selected according to the solubility; Suitable Kmvalue（ratio of surfactant to cosurfactant） based on the pseudo-ternary phase diagram was selected by water titration; Further prescription studies were performed at the selected Km value; The microemulsion dose was determined by HPLC; The self-microemulsion was made according to the prescription, and then the appropriate materials were added to make pellets; The preparation of pellets was evaluated. Results Isopropyl myristate（IPM）, Tween 80 and anhydrous ethanol were selected as oil phase, surfactant and cosurfactant; The Km value was 3∶1; The ratio of total quality of Tween 80 and absolute ethanol to IPM was 9∶1; The size of particle was less than 30 nm; Drug loading was 13.32 mg/m L. Conclusion The pellets are stable using microemulsion as the former preparation, which improve the bioavailability of flavonoids.

关 键 词：银杏黄酮 溶解度 伪三元相图 自微乳 微丸 溶出 

分 类 号：R283.6[医药卫生—中药学]