中文摘要：

目的：研究蝙蝠葛碱自微乳化释药系统（SMEDDS）在大鼠体内的相对生物利用度。方法：12只大鼠随机分为蝙蝠葛碱SMEDDS组（20 mg/kg）和蝙蝠葛碱溶液组（50 mg/kg）,每组6只,ig相应药物。分别于给药前和给药后0.167、0.333、0.5、0.75、1、2、4、8、12、24、36 h由眼眶后静脉丛取血约0.3 ml,采用高效液相色谱-串联质谱法测定血浆中蝙蝠葛碱浓度,采用DAS 3.0软件计算药动学参数,评价蝙蝠葛碱SMEDDS给药后蝙蝠葛碱的相对生物利用度。结果：大鼠血浆中蝙蝠葛碱质量浓度的线性范围为2.12-424 ng/ml（r=0.999 9）,日内、日间RSD均小于10%。蝙蝠葛碱溶液和蝙蝠葛碱SMEDDS组大鼠药动学参数cmax分别为（126.3±37.4）、（179.6±51.5）ng/ml,t1/2分别为（11.48±4.58）、（21.79±6.59）h,AUC0-t分别为（1 963.5±638.3）、（2 535.8±739.5）ng·h/ml,AUC（0-∞）分别为（2 256.3±703.5）、（2 854.6±768.7）ng·h/ml;分别以AUC0-t和AUC0-∞计算,蝙蝠葛碱SMEDDS的相对生物利用度分别为323%和316%。结论：ig蝙蝠葛碱SMEDDS后可以显著提高蝙蝠葛碱的相对生物利用度。

英文摘要：

OBJECTIVE：To study relative bioavailability of dauricine self-microemulsifying drug delivery system（SMEDDS）in rats.METHODS：12 rats were randomly divided into dauricine SMEDDS group（20 mg/kg）and dauricine solution group（50mg/kg）,6 rats in each group.They were given relevant medicine intragastrically.Then,0.3 ml plasma was collected from orbital venous plexus before medication and 0.167,0.333,0.5,0.75,1,2,4,8,12,24,36 h after medication.The plasma concentration of da- uricine was determined by HPLC-MS/MS,and DAS 3.0 was used to calculate pharmacokinetic parameters and evaluate the relative bioavailability of dauricine with dauricine SMEDDS.RESULTS：The linear range of dauricine in plasma were 2.12-424 ng/ml（r=0.999 9）;RSDs of intra-day and inter-day were all lower than 10%.Pharmacokinetic parameters of dauricine solution and dauricine SMEDDS were that cmaxwere（126.3±37.4）ng/ml and（179.6±51.5）ng/ml;t1/2were（11.48±4.58）and（21.79±6.59）h;AUC0-twere（1 963.5±638.3）ng·h/ml and（2 535.8±739.5）ng·h/ml;AUC0-∞were（2 256.3±703.5）ng·h/ml and（2 854.6±768.7）ng·h/ml,respectively.The relative bioavailability of dauricine SMEDDS were 323% and 316% by calculating with AUC0-t and AUC0- ∞,respectively.CONCLUSIONS：Intragastric administration of dauricine SMEDDS can improve relative bioavailability of dauricine significantly.