盐酸美沙酮3种途径大鼠给药的生物利用度研究  

Bioavailabilities of methadone hydrochloride via three different administrations in rats

作　　者：武炳贤[1] 余琛[2] 吴红兵[1] 蒋新国[1] 

机构地区：[1]复旦大学药学院药剂学教研室,上海201203 [2]上海市徐汇区中心医院药物代谢分析室,上海200031

出　　处：《中国新药杂志》2009年第9期823-826,共4页Chinese Journal of New Drugs

摘　　要：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 investigate the bioavailabilities of methadone via different administrations in rats after establishing a HPLC-UV method for determining methadone in plasma. Methods： Rats（ n = 20） were randomly given methadone hydrochloride solution via intravenous injection, nasal administration or oral administration. The doses were 1.4, 2.8 and 5.6 mg·kg^-1, respectively. The plasma concentration of methadone was determined by an HPLC method, and the bioavailability was calculated. Results： Methadone given via nasal administration indicated a fast effect similar to that of intravenous injection; T C and bioavailability were （2.5 ±1.2） min, （ 73.48 ± 49.34）μg·L^-1 and 51.37% , respectively. T C and bioavailability of methadone via oral adminis- tration were （51.0 ± 22.5） min, （24.39 ± 9.26） mg·L^-1 and 21.72% respectively. Conclusion： The established HPLC method is selective and suitable for the pharmacokinetic study of methadone. It is promising to take methadone via nasal administration.

关 键 词：美沙酮 鼻腔给药 高效液相色谱法 生物利用度 

分 类 号：R971.2[医药卫生—药品] R945.1[医药卫生—药学]