月桂酸小檗碱肠道给药的相对生物利用度研究  

Relative Bioavailability of Berberine Laurate Following Intestinal Administration

作　　者：田非非[1] 江东波[1] 刘真君[1] 李风云 翁伟宇[1] 

机构地区：[1]华东理工大学药学院,上海200237 [2]湖北省通城县特产局,湖北通城437400

出　　处：《中国现代应用药学》2011年第12期1117-1121,共5页Chinese Journal of Modern Applied Pharmacy

摘　　要：目的以硫酸小檗碱(BS)为参照,研究月桂酸小檗碱(BL)大鼠腹腔注射和肠道给药后的药动学特征和相对生物利用度。方法采用BS与月桂酸钾反应生成BL,用质谱、氢谱等手段确证结构。以高效液相色谱法测定血浆中小檗碱母核的浓度。结果腹腔注射后,BL和BS的体内过程均符合二室模型。以BS为参照,BL肠道给药的相对生物利用度为224.32%;可达腹腔注射的27.66%。结论脂溶性的脂肪酸小檗碱有利于肠道吸收,值得进一步研究。OBJECTIVE To investigate the pharmacokinetic characteristics and relative bioavailability of berberine laurate （BL） following intraperitoneal injection and intestinal administration using berberine sulfate （BS） as a reference. METHODS BL was synthesized by the reaction between BS and potassium laurate. MS and 1H-NMR were used to confirm the structure. The plasma concentrations in rats were measured by HPLC. RESULTS After intraperitoneal injection, the pharmacokinetics of BL and BS in rats were best described by a two-compartment model. After intestinal administration, the relative bioavailability of BL vs BS was 224.32%. Compared with intraperitoneal injection, the relative bioavailability of BL following intestinal administration was 27.66%. CONCLUSION The oral bioavailability of berberine can be increased by improving its lipophilicity. Fatty acid salts of berberine might be potential candidates for further research.

关 键 词：月桂酸小檗碱 肠道给药 相对生物利用度 

分 类 号：R945.1[医药卫生—微生物与生化药学]