[穿琥宁肠溶微丸大鼠肠道吸收及体内药代动力学研究]

[Intestinal absorption of enteric coating potassium sodium dehydroandroan drographolide succinate pellets in rat and in vivo pharmacokinetics study].

作者信息

Gao Yan, Wang Zhong-Lan, Huang Gui-Hua

机构信息

School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.

出版信息

Zhong Yao Cai. 2011 Aug;34(8):1247-50.

PMID:22233041

Abstract

OBJECTIVE

To develop a method for determination the content of Potassium Sodium Dehydroandroan drographolide Succinate (PSDS) in rat intestinal contents and plasma and investigate the intestinal absorption of PSDS pellets in rat and in vivo pharmacokinetics of PSDS pellets.

METHODS

The content of PSDS in rat intestinal contents and plasma was determined by HPLC. In vivo pharmacokinetic properties and intestinal absorption of PSDS pellets in rat were investigated.

RESULTS

Two hours after administration, pellets were not found in the small intestine and large intestine, four hours after administration, the largest number of pellets were found in the small intestine and the concentration of PSDS was the highest in the intestinal contents (3593.13 microg). The characteristics of plasma concentration-time curve was consistent with a single compartment model. The main drug pharmacokinetic parameters were calculated. t1/2, T(max), C(max) and AUC were 2.69 h, 5 h, 3.02 microg/mL and 6.42 microg x h/mL, respectively.

CONCLUSION

PSDS has a good absorption in the rat small intestine and it is feasible to prepare PSDS enteric-coated pellets for oral administration.

摘要

目的

建立大鼠肠内容物及血浆中穿琥宁（PSDS）含量的测定方法，研究穿琥宁微丸在大鼠体内的肠吸收情况及体内药代动力学。

方法

采用高效液相色谱法测定大鼠肠内容物及血浆中PSDS的含量。研究穿琥宁微丸在大鼠体内的药代动力学性质及肠吸收情况。

结果

给药2小时后，在小肠和大肠中未发现微丸；给药4小时后，在小肠中发现的微丸数量最多，肠内容物中PSDS的浓度最高（3593.13μg）。血浆浓度-时间曲线特征符合单室模型。计算了主要药物的药代动力学参数。t1/2、T(max)、C(max)和AUC分别为2.69小时、5小时、3.02μg/mL和6.42μg·h/mL。