黄芩素纳米混悬液的生物利用度研究

高缘; 江鲲; 李莉; 席一峰

黄芩素纳米混悬液的生物利用度研究

1.
中国药科大学中药制剂教研室
2.
南京医科大学第二附属医院

基金项目: 国家“重大新药创制”科技重大专项资助项目(No.2009ZX09310-004)；中央高校基本科研业务费专项资金资助（No.JKQ2009028）

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- 刊出日期: 2011-08-24

Bioavailability enhancement of baicalein by nanosuspension

摘要

摘要: 采用反溶剂重结晶结合高压均质法制备黄芩素纳米混悬液,并对其在大鼠体内的生物利用度进行研究。对大鼠分别灌胃给予等剂量黄芩素原料和黄芩素纳米混悬液，采用HPLC法测定活性代谢产物黄芩苷在大鼠体内的血药浓度，利用DAS 2.0软件计算药代动力学参数。结果表明，灌胃给予等剂量黄芩素原料和黄芩素纳米混悬液(121 mg/kg)后，大鼠血浆中黄芩苷的血药浓度-时间曲线均呈现双峰现象，c_max分别为7.18和11.12 μg/mL，t_max分别为1.67和0.92 h，AUC_{0-24 h}分别为71.40和118.63μg·h/mL。以黄芩素原料做参比，黄芩素纳米混悬液经口给药后的相对生物利用度为166.1%。黄芩素纳米混悬液可显著提高黄芩素口服给药的生物利用度。
- 黄芩素 /
- 黄芩苷 /
- 纳米混悬液 /
- 生物利用度 /
- 药代动力学
Abstract: Baicalein nanosuspension was prepared by antisolvent recrystalization method combined with subsequent homogenization.The oral bioavailability of baicalein nanosuspension in rats was also studied.The concentration of baicalin in rat plasma was determined by HPLC method.The pharmacokinetic parameters were calculated by DAS 2.0 software.It was found that the plasma drug concentration-time curves of baicalein all showed two peaks after oral administration.The c_max,t_maxand AUC_{0-24 h_{of the raw baicalein and baicalein nanosuspension was 7.18 and 11.12 μg/mL,1.67 and 0.92 h,71.40 and 118.63 μg·h/mL,respectively.Compared with baicalein bulk,the relative bioavailability of baicalein nanosuspension was 166.1%.Nanosuspension could significantly enhance the oral bioavailability of baicalein in rats.}}
- baicalein /
- baicalin /
- nanosuspension /
- bioavailability /
- pharmacokinetics

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文章访问数: 1477
HTML全文浏览量: 0
PDF下载量: 2435
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黄芩素纳米混悬液的生物利用度研究

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Bioavailability enhancement of baicalein by nanosuspension

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出版历程

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