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目的:建立HPLC-UV法测定血浆中的美沙酮含量,研究3种给药途径美沙酮在大鼠体内的生物利用度。方法:20只大鼠随机分组,分别采用静注、鼻腔、口服3种给药方式,给予盐酸美沙酮溶液制剂,给药剂量分别为1.4,2.8和5.6 mg.kg-1,通过HPLC法测定血药浓度,计算生物利用度。结果:鼻腔给予盐酸美沙酮起效迅速,与静注相当,Tmax=(2.5±1.2)min,Cmax=(73.48±49.34)μg.L-1,绝对生物利用度为54.50%;口服给药Tmax=(51.0±22.5)min,Cmax=(24.39±9.26)μg.L-1,绝对生物利用度为21.72%。结论:建立的HPLC方法专属性强,适用于美沙酮的药动学研究。将盐酸美沙酮制成鼻用制剂有一定的研究价值和应用前景。
OBJECTIVE: To establish a HPLC-UV method for the determination of methadone in plasma and to study the bioavailability of methadone in rats by three routes of administration. Methods: Twenty rats were randomly divided into three groups: intravenous injection, nasal injection and oral administration respectively. The rats were given methadone hydrochloride solution at dosage of 1.4, 2.8 and 5.6 mg.kg-1, respectively, and the blood samples were determined by HPLC Drug concentration, calculate bioavailability. Results: Nasal administration of methadone hydrochloride had a rapid onset of action comparable to intravenous injection, with Tmax = (2.5 ± 1.2) min and Cmax = (73.48 ± 49.34) μg.L-1, with an absolute bioavailability of 54.50% (51.0 ± 22.5) min, Cmax = (24.39 ± 9.26) μg.L-1, and the absolute bioavailability was 21.72%. Conclusion: The established HPLC method is highly specific and suitable for pharmacokinetic studies of methadone. The methadone hydrochloride nasal preparations have some research value and application prospects.