醒鼻微乳温敏凝胶中丹皮酚在大鼠鼻黏膜的吸收研究

Study on Nasal Mucosa Absorption of Paeonol of Xingbi Microemulsion-based Thermosensitive Gel in Rats

目的通过对醒鼻微乳温敏凝胶中丹皮酚的大鼠鼻黏膜吸收进行研究,评价该药的黏膜吸收情况和剂型选择的合理性。方法通过大鼠鼻腔给药试验,对不同时间点丹皮酚的血药浓度进行测定。结果大鼠鼻腔给予醒鼻微乳温敏凝胶后,丹皮酚的生物利用度为78.68%,达到最大浓度(C_(max))0.340 4μg/m L的时间为3 min,平均滞留时间为9.23 h;鼻腔给药的血药浓度达到C_(max)后的变化情况与尾静脉注射丹皮酚类似;丹皮酚的血药浓度数据符合二室模型,权重为W=1。结论醒鼻微乳温敏凝胶经鼻给药生物利用度较高,剂型选择合理。

Objective To study the nasal mucosa absorption of paeonol of Xingbi microemulsion-basedthermo-sensitive gel in rats;To evaluate the nasal mucosa absorption of medicine and the rationality of preparationform.Methods According to the nasal administration method,the blood medicine concentration of paeonol wasdetermined at different time points.Results The nasal administration bioavailability of paeonol in Xingbimicroemulsion-based thermo-sensitive gel was78.68%,the plasma concentration reached the maximum(0.3404μg/mL)after3min of administration,and the average residence time was9.23h.After reaching Cmax,The plasmaconcentration changed similar to intravenous administration of paeonol.The concentration data of paeonol in plasmawas consistent with a two-compartment model,with a weight of1.Conclusion Xingbi microemulsion-based thermosensitivegel has a higher bioavailability,and the preparation form was reasonable.