Yao Chen, Zhou Xiudi, Qu Tao, Wei Dongyu, Mu Hongjie, Liang Rongcai, Wang Aiping, Sun Kaoxiang
School of Pharmacy, Yantai University, Yantai 264005, China.
Zhongguo Zhong Yao Za Zhi. 2011 Aug;36(16):2236-9.
To establish the model of microdialysis, and study the ocular pharmacokinetics of puerarin in anesthetic rabbits.
Implanted the probe into anterior chamber of anesthetic rabbit by surgery. After balanced for 2 h, 1% puerarin eye drop (100 microL) was applied into the cul-de-sac with micropipette. Immediately the dialysate was collected at different time and detected by HPLC with the detection wavelength of 249 nm. The mobile phase was methanol and 0.1% citric acid solution (30:70); the flow rate was 1.0 mL x min(-1).
After the administration, puerarin can be absorbed into aqueous humor quickly. The peak concentration of puerarin appeared at about 1 h and then reduced gradually. The peak concentration(C(max)) is (2.52 +/- 0.31) mg x L(-1). The other lower peak was shown at 3.5 h during the eliminate phase. This might be attributed to the inhibition of aqueous humor production by the puerarin and resulted in a high drug concentration. The area under concentration-time curve (AUC(0-t)) is (5.04 +/- 0.21) mg x h x L(-1) and the eliminate half life (t1/2) is (0.38 +/- 0.13) h.
The microdialysis technique can be used to detect the ocular pharmacokinetics of puerarin, and support the valuable pharmacokinetics parameter for the clinical applications of puerarin eye drop.
建立微透析模型，研究麻醉兔眼内葛根素的药代动力学。
通过手术将探针植入麻醉兔前房。平衡2小时后，用微量移液器将1%葛根素滴眼液（100微升）滴入结膜囊。立即在不同时间收集透析液，采用高效液相色谱法检测，检测波长为249nm。流动相为甲醇和0.1%柠檬酸溶液（30:70）；流速为1.0毫升×分钟-1。
给药后，葛根素能迅速吸收入房水。葛根素的峰值浓度在约1小时出现，然后逐渐降低。峰值浓度（C(max)）为（2.52±0.31）毫克×升-1。在消除相3.5小时出现另一个较低的峰值。这可能归因于葛根素对房水生成的抑制，导致药物浓度升高。浓度-时间曲线下面积（AUC(0-t)）为（5.04±0.21）毫克×小时×升-1，消除半衰期（t1/2）为（0.38±0.13）小时。
微透析技术可用于检测葛根素的眼内药代动力学，为葛根素滴眼液的临床应用提供有价值的药代动力学参数。
