甲磺酸二氢麦角毒碱溶液鼻黏膜吸收的研究

Evaluation of nasal absorption for dihydroergotoxine mesylate solution

目的:研究甲磺酸二氢麦角毒碱溶液鼻黏膜吸收规律。方法:考察甲磺酸二氢麦角毒碱在大鼠鼻腔洗出液中的稳定性,在此基础上,以大鼠在体鼻循环为实验模型,研究甲磺酸二氢麦角毒碱溶液的鼻黏膜吸收规律。结果:甲磺酸二氢麦角毒碱在鼻黏膜洗出液中稳定性良好,当循环液体积为5 mL,流速为2．5 mL·min-1时,甲磺酸二氢麦角毒碱溶液鼻黏膜吸收速率常数K不随药物浓度发生变化。结论:甲磺酸二氢麦角毒碱溶液鼻黏膜吸收机制为被动扩散,吸收符合一级动力学,其鼻黏膜平均吸收速率常数K为5．94×10-3min-1。

Objective：To characterize the nasal absorption of dihydroergotoxine mesylate solution. Methods： The stability of dihydroergotoxine mesylate in rats＇nasal lavage was determined. The nasal absorption of dihydroergotoxine mesylate solution was then assessed using a rat nasal recirculation in situ model. Results： Dihydroergotoxine mesylate was stable in rats＇nasal lavage. At the perfusion volume 5 mL and flow rate 2. 5 mL·min^-1, the absorption rate of dihydroergotoxine mesylate remains constant in a dose-independent manner. Dihydroergotoxine mesylate was nasally absorbed by first-order kinetics in a passive diffusion setting. The mean absorption rate constant was 5.94×10^-3min^-1. Conclusion： Dihydroergotoxine mesylate solution had a better bioavailability via nasal distribution.