磷酸二甲啡烷糖浆剂在中国健康受试者的药代动力学

发布时间：2019-07-16 18:57

【摘要】：目的研究磷酸二甲啡烷糖浆剂在中国健康志愿者中的单次和连续多次给药药代动力学特征。方法 12名健康志愿者,男女各半。单次口服磷酸二甲啡烷糖浆剂10,20,40 mg,多次口服磷酸二甲啡烷糖浆剂20 mg,每天3次,连续给药4 d。用HPLC-MS/MS法测定血浆中二甲啡烷的药物浓度。结果单次口服磷酸二甲啡烷糖浆剂10,20,40 mg后的主要药代动力学参数:Cmax为(0.94±0.44),(2.19±1.40),(5.30±4.83)μg·L-1,AUClast为(11.06±5.74),(26.41±18.08),(53.78±38.28)μg·L-1·h,AUCinf为(12.14±6.02),(28.46±20.21),(57.26±41.40)μg·L-1·h。多次口服磷酸二甲啡烷糖浆剂20 mg后的主要药代动力学参数:Cmax为(5.57±3.64)μg·L-1,AUClast为(83.07±62.51)μg·L-1·h,AUCinf为(88.54±68.14)μg·L-1·h。结论单次给药10,20,40 mg后,二甲啡烷的体内过程符合一级线性动力学过程;连续多次给药20 mg后,二甲啡烷的蓄积因子接近3,符合线性累加。
[Abstract]:Objective to study the pharmacokinetics of dimethyl phosphate syrup in Chinese healthy volunteers. Methods Twelve healthy volunteers, half male and half male, were enrolled in this study. Single oral administration of dimethyl phosphate slurry 10, 20, 40 mg, multiple oral administration of dimethyl phosphate slurry 20 mg, 3 times a day for 4 days The drug concentration of dimethyl enkephalin in plasma was determined by HPLC-MS/MS. Results the main pharmacokinetics parameters were (0.94 卤0.44), (2.19 卤1.40), (5.30 卤4.83) 渭 g 路L ~ (- 1) and (11.06 卤5.74), (26.41 卤18.08), (53.78 卤38.28) 渭 g 路L ~ (- 1) h, AUCinf after 40 mg, (12.14 卤6.02), (28.46 卤20.21), (57.26 卤41.40) 渭 g 路L ~ (- 1) and (11.06 卤5.74), (26.41 卤18.08), (53.78 卤38.28) 渭 g 路L ~ (- 1). After repeated oral administration of dimethyl phosphate syrup for 20 mg, the main pharmacokinetics parameters were as follows: Cmax was (5.57 卤3.64) 渭 g 路L ~ (- 1), Auclast was (83.07 卤62.51) 渭 g 路L ~ (- 1) 路h, AUCinf, (88.54 卤68.14) 渭 g 路L ~ (- 1), and Auclast was (88.54 卤68.14) 渭 g 路L ~ (- 1) 路h. Conclusion after single administration of 10, 20 and 40 mg, the in vivo process of dimethyl enkephalin accords with the first-order linear kinetic process, and after 20 mg of continuous administration, the accumulation factor of dimethorphan is close to 3, which accords with the linear accumulation.
【作者单位】：中南大学药学院;中南大学湘雅三医院临床药理中心;
【基金】：国家自然科学基金资助项目(81302851,81373476,81301924) 湖南省卫生厅科研基金资助项目(132013-028) 重大疾病新药临床评价研究综合技术平台建设基金资助项目(2012ZX09303014-001)
【分类号】：R969.1

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