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。
Abstract
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 ρmax(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.
关键词
左旋盐酸苯环壬酯 /
鼻腔喷雾剂 /
液相色谱-质谱/质谱 /
药动学 /
相对生物利用度
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Key words
L-phencynonate hydrochloride /
nasal spray /
LC-MS/MS /
pharmacokinetics /
bioavailability
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参考文献
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