左旋盐酸苯环壬酯鼻腔喷雾剂的体内评价

In vivo Study on a Nasal Spray Containing L-Phencynonate Hydrochloride

目的对制备的左旋盐酸苯环壬酯鼻腔喷雾剂进行药动学评价,比较鼻喷剂和片剂的生物利用度。方法LC-MS/MS测定给药后2种制剂在比格犬体内的血药浓度,计算药动学参数和相对生物利用度。结果左旋盐酸苯环壬酯鼻腔喷雾剂的tmax实测为(16.6±8.6)min,比片剂约快5倍,ρmax实测为(10.026±4.903)μg·L-1,约是片剂的4倍,对片剂的相对生物利用度为(231±79)%。结论左旋盐酸苯环壬酯鼻喷剂起效迅速,相对生物利用度高,具有很好的应用前景。

OBJECTIVE To study pharmacokinetics of a nasal spray containing L-phencynonate hydrochloride and compared with the tablet. METHODS Six beagle dogs were given L-phencynonate hydrochloride nasal spray and tablets in a randomized cross over desigh.The plasma concentrations of L-phencynonate hydrochloride were determined and the pharmacokinetic parameters of two preparations were calculated. RESULTS The pharmacokinetic parameters of nasal spray were as follow： tmax （16.6±8.6）min and Pmax （10.026±4.903） μg.L^-1, respectively 5 times and 4 folds or so higher than conventional tablets. The relative bioavailability of nasal spray was （231±79）%.CONCLUSIONS The nasal spray of L-phencynonate hydrochloride developed in this study was confirmed with quick absorption and higher relative bioavailability.