3种制剂技术对黄癸素口服生物利用度的影响  

Effects of three preparation technologies on the oral bioavailability of berberineα-hydroxy β-decanoylethyl sulfonate

作　　者：李辉 刘蔓[1] 黄鸿波 丁劲松 

机构地区：[1]中南大学湘雅药学院,湖南长沙410013 [2]湖南中医药高等专科学校,湖南株洲412012

出　　处：《中成药》2018年第2期309-313,共5页Chinese Traditional Patent Medicine

基　　金：湖南省药物制剂优化与早期临床评价工程技术研究中心湖南省科技计划项目(2015TP2005)

摘　　要：目的比较3种制剂技术对黄癸素口服生物利用度的影响。方法制备固体分散体、HP-β-CD包合物、纳米混悬剂冻干粉,SD大鼠分别灌胃给予这3种制剂和原料药的混悬液。HPLC-MS/MS法测定血浆中黄癸素含有量,计算药动学参数。结果与原料药相比,3种制剂技术均能显著提高该成分Cmax(P<0.05),尤其是HP-β-CD包合物(P<0.01);HP-β-CD包合物AUC0~6 h明显高于原料药和其他2种制剂技术(P<0.05)。结论 HP-β-CD包合物能有效提高黄癸素口服生物利用度。AIM To compare the effects of three preparation technologies on the oral bioavailability of HB（ berberine α-hydroxy β-decanoylethyl sulfonate,houttuyn berberine）. METHODS Solid dispersions,HP-β-CD inclusion complexes and nanosuspension freeze-dried powders were prepared. The suspensions of crude drug and these three preparations were intragastrically administered to SD rats,respectively. HPLC-MS/MS was adopted in the content determination of HB in plasma. then pharmacokinetics parameters were calculated. RESULTS Compared with the crude drug,three preparation technologies could significantly increase the Cmaxvalue of this component（ P〈0. 05）,especially for HP-β-CD inclusion complexes（ P〈0. 01）. And HP-β-CD inclusion complexes demonstrated much higher AUC0 ~ 6 hthan the crude drug and the other two preparation technologies（ P〈0. 05）.CONCLUSION HP-β-CD inclusion complexes can effectively increase the oral bioavailability of HB.

关 键 词：黄癸素 固体分散体 HP-β-CD包合物 纳米混悬剂冻干粉 口服生物利用度 HPLC-MS/MS 

分 类 号：R969.1[医药卫生—药理学]