CAJ | 학술논문

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。
목적：연구린산이갑배완당장제재중국건강지원자중적단차화련속다차급약약대동역학특정。방법12명건강지원자，남녀각반。단차구복린산이갑배완당장제10，20，40 mg，다차구복린산이갑배완당장제20 mg，매천3차，련속급약4 d。용HPLC－MS／MS법측정혈장중이갑배완적약물농도。결과단차구복린산이갑배완당장제10，20，40 mg 후적주요약대동역학삼수：Cmax위（0．94±0．44），（2．19±1．40），（5．30±4．83）μg ? L－1， AUClast 위（11．06±5．74），（26．41±18．08），（53．78±38．28）μg? L－1? h， AUCinf위（12．14±6．02），（28．46±20．21），（57．26±41．40）μg? L－1? h。다차구복린산이갑배완당장제20 mg 후적주요약대동역학삼수：Cmax위（5．57±3．64）μg? L－1，AUClast위（83．07±62．51）μg? L－1? h， AUCinf위（88．54±68．14）μg? L－1? h。결론단차급약10，20，40 mg후，이갑배완적체내과정부합일급선성동역학과정；련속다차급약20 mg후，이갑배완적축적인자접근3，부합선성루가。
Objective To investigate the pharmacokinetics of dimemor-fan phosphate syrups at single dose or multiple doses in healthy Chinese volunteers.Methods Twelve healthy volunteers were selected, six males and six females.Single doses of dimemorfan phosphate syrups(10, 20, 40 mg) were given, and then multiple doses of 20 mg were given three times a day for four days.The concentrations of dimemorfan in plas-ma were determined by high performance liquid chromatography/tandem mass spectrometry (HPLC-MS/MS).Results The main pharmacoki-netic parameters of dimemorfan after single dose (10, 20, 40 mg) were as follows:Cmaxwas (0.94 ±0.44), (2.19 ±1.40)and (5.30 ±4.83)μg? L-1 , AUClast was ( 11.06 ±5.74 ) , ( 26.41 ±18.08 ) and (53.78 ±38.28)μg? L-1? h, AUCinf was (12.14 ±6.02), (28.46 ± 20.21)and(57.26 ±41.40)μg? L-1? h.The parameters of dimemor-fan after multiple doses 20 mg were as follows:Cmax was (5.57 ±3.64)μg? L-1, AUClast was (83.07 ±62.51)μg? L -1? h, and AUCinf was (88.54 ±68.14)μg? L-1? h.Conclusion After the administration of single dose (10, 20, 40 mg), the pharmacokinetic results show that dimemorfan exhibits first order kinetic characteristics.After administration of multiple doses, the accumulation factor value was nearly three and dimemorfan shows a linear accumulation.