| 引用本文: | 田非非，江东波，刘真君，李风云，翁伟宇.月桂酸小檗碱肠道给药的相对生物利用度研究[J].中国现代应用药学,2011,28(12):1117-1121. |
| TIAN Feifei, JIANG Dongbo, LIU Zhenjun, LI Fengyun, WENG Weiyu.Relative Bioavailability of Berberine Laurate Following Intestinal Administration[J].Chin J Mod Appl Pharm(中国现代应用药学),2011,28(12):1117-1121. |
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| 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。 |
| 关键词: 月桂酸小檗碱 肠道给药 相对生物利用度 |
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| Relative Bioavailability of Berberine Laurate Following Intestinal Administration |
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TIAN Feifei, JIANG Dongbo, LIU Zhenjun, LI Fengyun, WENG Weiyu1,2
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1.School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China;2.Tongcheng County Special Products Bureau of Hubei Province, Tongcheng 437400, China
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| Abstract: |
| 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. |
| Key words: berberine laurate intestinal administration relative bioavailability |
