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采用LC-MS／MS研究单次及多次口服给药后磷酸二甲啡烷在中国健康受试者体内药代动力学特征。单剂量试验的12例受试者采用两周期、交叉设计，分别口服本品10 mg、40 mg，以及其余12例受试者单次口服20 mg后的药动学参数：AUC0－48 h（11．81±14．46）、（52．60±96．01）、（34．70±29．59）ng·h／mL；t1／2（12．11±2．54）、（12．16±2．01）、（12．77±1．27）h；cmax（0．9653±0．8178）、（3．150±3．451）、（2．167±1．650）ng／mL。多剂量试验的12例受试者接受单剂量20 mg后，开始每天3次服用磷酸二甲啡烷20 mg，连服至第8天晨采集血样的药代动力学参数：AUC0－48 h（115．9 ±135．2）ng·h／mL；t1／2（11．22±1．61）h；cmax（7．418±7．010）ng／mL；累积常数Rcmax为（3．14±1．34），RAUC为（3．38±1．22）。置信区间法表明磷酸二甲啡烷在10～40 mg范围内，药代动力学参数与剂量无线性关系；多次给药后在体内存在蓄积；磷酸二甲啡烷在中国健康受试者中存在显著的个体差异。“,”An LC-MS/MS method was developed to investigate the pharmacokinetic parameters in healthy Chi-nese volunteers following single and multiple oral administration of dimemorfan phosphate. In the Single-dose study,two-period and crossover study was conducted in 12 healthy volunteers,which were administered with single-dose of 10 mg or 40 mg of dimemorfan phosphate. And another 12 volunteers were administered with 20 mg. The values of AUC0-48 h,t1/2,and cmax were (11. 81 ±14. 46),(52. 60 ±96. 01 )and (34. 70 ±29. 59)ng. h/mL,(12. 11 ±2. 54),(12. 16 ±2. 01)and (12. 77 ±1. 27)h,and (0. 9653 ±0. 8178),(3. 150 ±3. 451)and (2. 167 ±1. 650)ng/mL for 10 mg,40 mg and 20 mg oral administration. The same 12 healthy volunteers as the group of single-dose of 20mg were participated in multiple-dose study,which were administered dimemorfan phos-phate 20 mg,three-time a day until the day-8,showed AUC0-48 h,t1/2,and cmax were (115. 9 ±135. 2)ng.h/mL, (11. 22 ±1. 61)h,and (7. 418 ±7. 010)ng/mL. The accumulation parameter Rcmax and RAUC was (3. 14 ±1. 34) and (3. 38 ±1. 22),respectively. Dose proportional of cmax and AUC was not concluded ranging from 10 mg to 40 mg after confidence interval criteria method. An accumulation was occurred after multiple -dose administra-tion with the consequence. And the results demonstrated significant individual difference.