银杏酮酯自微乳化渗透泵控释给药系统的研究  

Study on self-microemulsification delivery system osmotic pump controlled release drug delivery system of Ginkgo biloba extract

作　　者：万芳[1] WAN Fang(School of Chemical Engineering and Pharmacy,Jingchu University of Technology,Jingmen 448000,Hubei Province,China)

机构地区：[1]荆楚理工学院化工与药学院,湖北荆门448000

出　　处：《中国临床药理学杂志》2020年第9期1149-1152,共4页The Chinese Journal of Clinical Pharmacology

基　　金：湖北省教育厅科学技术研究项目资助项目(Q20174302)。

摘　　要：目的研究银杏酮酯(GBE50)自微乳化(SMEDDS)渗透泵控释给药系统。方法用聚氧乙烯蓖麻油、聚乙二醇、中链油和GBE50制备SMEDDS-GBE50。建立SMEDDS-GBE50的高效液相检测方法,评估方法的回收率和日间相对标准偏差。将SMEDDS-GBE50与促渗剂混合测定药物体外累积释放度,评估不同促渗剂(氯化钠、甘露醇、蔗糖和乳糖)、不同促渗剂比例(氯化钠与SMEDDS-GBE50自微乳化的比例分别为3;1、2;1、3;2和1;1)和不同孔径大小(0.3,0.5和0.7 nm)对SMEDDS-GBE50渗透泵控释给药系统释放度的影响。结果高效液相色谱显示,槲皮素、山柰素、异鼠李素峰的平均回收率分别为(86.79±5.87)%,(85.80±5.04)%和(87.36±5.43)%,日间相对标准偏差分别为6.76%,5.87%和6.21%。释放12 h时,促渗剂为氯化钠的药物累积释放度显著高于促渗剂为甘露醇、蔗糖、乳糖时的物累积释放度,氯化钠与SMEDDS-GBE50比例为1;1时的药物释放度明显高于比例为3;1、2;1和3;2的药物释放度,释药孔的孔径大小为0.5和0.7 nm时的药物累积释放度无明显差异,但显著高于孔径大小为0.3 nm时的药物累积释放度。结论SMEDDSGBE50渗透泵控释系统选择50%的氯化钠作为促渗剂,释药孔为0.5 nm的包衣膜,可以有效提高药物的累积释放度。Objective To study self-microemulsification delivery system(SMEDDS)osmotic pump controlled release drug delivery system of Ginkgo biloba extract(GBE50).Methods SMEDDS-GBE50 was prepared by cremophor EL,polyethylene glycol,medium chain oil and GBE50.The high performance liquid chromatography(HPLC)detection method of SMEDDS-GBE50 was established.The recovery rate and diurnal relative standard deviation of method were evaluated.SMEDDS-GBE50 and penetration enhancers were mixed to measure accumulative releasing out of drugs.The effects of different penetration enhancers(sodium chloride,mannitol,sucrose and lactose),different penetration enhancer ratios(sodium chloride/SMEDDS-GBE50 self-microemulsificatio n=3∶1,2∶1,3∶2 and 1∶1)and different aperture sizes(0.3,0.5 and 0.7 nm)on release degree of SMEDDS-GBE50 osmotic pump controlled release drug delivery system were evaluated.Results HPLC showed that average recovery rates of quercetin,kaempferol and isorhamnetin peak were(86.79±5.87)%,(85.80±5.04)%and(87.36±5.43)%,and their diurnal relative standard deviations were 6.76%,5.87%and 6.21%,respectively.After releasing for 12 h,the drug accumulative releasing of sodium chloride was significantly higher than that of mannitol,sucrose and lactose.The drug release degree of sodium/SMEDDS-GBE50 with 1∶1 was significantly higher than that with 3∶1,2∶1 and 3∶2.There was no significant difference in drug cumulative release degree between 0.5 nm and 0.7 nm drug releasing aperture,which was significantly higher of 0.3 nm drug releasing aperture.Conclusion SMEDDS-GBE50 osmotic pump controlled release system with 50%sodium chloride as penetration enhancer and coating film of 0.5 nm drug releasing aperture can effectively improve drug accumulative releasing degree.

关 键 词：银杏酮酯 自微乳化系统 渗透泵控释给药系统 

分 类 号：R28[医药卫生—中药学]