摘要
目的:考察银杏叶提取物类脂质体(GbEN)的体外释放度和体内药效学。方法:采用透析-HPLC法,分别考察温度为(37±1)℃,转速为75r/min时,在3种不同释放介质,磷酸盐缓冲液(pH=6.8)、醋酸缓冲液(pH=4.0)和HCl溶液(9→1 000)黄酮醇苷的释放情况。采用高脂血症大鼠模型,以血液生化指标和血液流变学为考察指标,分别灌胃给予60只大鼠GbEN冻干粉末和银杏叶片(GbE),比较GbEN冻干粉末和银杏叶片的药效学作用。结果:GbEN在PBS(pH6.8)中的释放度较好,在48 h内累计释放率达到80%以上,在HCl溶液(9→1 000)和醋酸缓冲液(pH 4.0)中释放48 h其累计释放率在20%左右。GbEN和银杏叶片均提高血浆高密度脂蛋白胆固醇(HDL-C)含量,降低总甘油三酯(TG)、总胆固醇(TC)、低密度脂蛋白胆固醇(LDL-C)含量、动脉硬化指数AI及LDL-C/HDL-C的比值。结论:本法操作简单,且重现性好。GbEN和银杏叶片均可改善高脂血大鼠的血脂代谢紊乱,并可以降低高脂血大鼠的全血及血浆黏度。
AIM：To optimize release in vitro of Ginkgo biloba extract niosome（GbEN） and pharmacodynamics in vivo.METHODS：The analysis was carried out on Dialysis-HPLC method,under the conditions of temperature of（37 ± 1） ℃ and rotation rate of 75 r/min.We studied the release condition of flavonol glycosides in three kinds of different media;including phosphate buffer solution（pH = 6.8）,acetate buffer（pH = 4.0） and HCl solution（9→1 000）.Sixty experimental hyperlipemia rats were used in the study and then fed with GbEN freeze-dried powder and Ginkgo respectively.Blood biochemical levels and hemorheology were compared between rats.RESULTS：GbEN had satisfactory release behavior in pH 6.8 phosphate buffer solution.,as cumulative release of drug reached up to 80% in 48 h.However cumulative release of drug in HCl solution（9→1000） and acetate buffer were（pH 4.0） only 20% in 48 h.GbEN and GbE tablets could enhance the level of high density lipoprotein cho-lesterol（HDL-C）,decrease the levels of total cholestero（TG）,triglycerid（TC）,low density lipoprotein cholestero（LDL-C）、AI and the ratio of LDL-C/HDL-C.CONCLUSION：This method is simple,and reproducible.GbEN and GbE tablets both have the capability to improve the disorder of blood-fat metabolism of hyperlipoproteinemia rats.They also can decrease the viscosity of whole blood and plasma of hyperlipoproteinemia rats.
出处
《中成药》
CAS
CSCD
北大核心
2010年第11期1877-1882,共6页
Chinese Traditional Patent Medicine
基金
吉林省科技发展计划项目(200705486)
吉林省教育厅"十一五"科学技术项目([2007]第78号)
关键词
银杏叶提取物类脂质体
体外释放度
体内药效学
大鼠
Ginkgo biloba extract niosomes （GbEN）
release in vitro
pharmacodynamic in vivo
rat
