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灯盏花素及其β-环糊精包合物在大鼠体内的药代动力学
引用本文:张海燕,平其能,郭健新,操锋.灯盏花素及其β-环糊精包合物在大鼠体内的药代动力学[J].药学学报,2005,40(6):563-567.
作者姓名:张海燕  平其能  郭健新  操锋
作者单位:中国药科大学,药剂教研室,江苏,南京,210038
基金项目:国家自然科学基金重点资助项目 ( 3043790 ),国家自然科学基金青年基金资助项目(30300440).
摘    要:目的建立测定大鼠血浆中灯盏乙素浓度的反相高效液相色谱法,研究灯盏花素及其β-环糊精包合物(灯盏花素-β-CD)大鼠灌胃后体内药代动力学行为。方法以甲醇-水-醋酸盐缓冲液为流动相,Shim-pack C18为固定相;12只大鼠随机均分为2组,分别灌胃灯盏花素及其包合物后,检测血浆药物浓度。药时数据采用3P97药代计算程序处理。结果线性范围10-400 ng·mL-1,方法回收率95.32%-98.81%;灯盏花素和包合物的Cmax分别为(154±18) ng·mL-1和(328±31) ng·mL-1;AUC0-12h分别为(710±126) ng·h·mL-1和(1 093±200)ng·h·mL-1,经t检验两者有极显著性差异(P<0.01)。结论该法准确、灵敏,适用于灯盏乙素血浆浓度的测定;制备的灯盏花素包合物与灯盏花素相比吸收显著增加。

关 键 词:灯盏花素  灯盏花素-β-CD  灯盏乙素  反相高效液相色谱法  药代动力学
收稿时间:2004-10-09

Pharmacokinetics of breviscapine and its β-cyclodextrin complex in rats
ZHANG Hai-yan,PING Qi-Neng,GUO Jian-xin,CAO Feng.Pharmacokinetics of breviscapine and its β-cyclodextrin complex in rats[J].Acta Pharmaceutica Sinica,2005,40(6):563-567.
Authors:ZHANG Hai-yan  PING Qi-Neng  GUO Jian-xin  CAO Feng
Institution:Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210038, China.
Abstract:AIM: To establish RP-HPLC method for determination of plasma scutellarin concentration and study of the pharmacokinetic behavior of scutellarin in rat after ig administration of breviscapine and its beta-cyclodextrin complex (breviscapine-beta-CD). METHODS: Mobile phase composed of methanol and acetate buffer. The column was Shim-pack C18. Twelve rats randomized into 2 groups were separately given breviscapine and breviscapine-beta-CD at single dose of 10.8 mg.kg(-1). Drug in plasma was extracted and determined by HPLC. The pharmacokinetic parameters were calculated by 3P97 software. RESULTS: Linearity was obtained over the range of 10-400 ng.mL(-1). The recovery was 95.32%-98.81%. C(max) and AUC(0-12 h) of breviscapine were (154 +/- 18) ng.mL(-1) and (710 +/- 126) ng.h.mL(-1). For breviscapine-beta-CD, C(max) and AUC(0-12 h) were (328 +/- 31) ng.mL(-1) and (1,093 +/- 200) ng.h.mL(-1), respectively. There were significant differences of AUC(0-12 h) between breviscapine and breviscapine-beta-CD (P < 0.01). CONCLUSION: The assay method was suitable for the determination of scutellarin plasma concentration in rat. Brevescapine-beta-CD showed greater absorption compared with that of brevescapine.
Keywords:breviscapine-β-CD  scutellarin  RP-HPLC  pharmacokinetics  breviscapine
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