【作者】 司继刚； 郭瑞臣； 王本杰；

【Author】 Si Jigang, Guo Ruichen, Wang Benjie ( Pharmacy of Zibo Central Hospital, Zibo 255200,China; Institue of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan 250012,China)

【机构】 淄博市中心医院药剂科； 山东大学齐鲁医院临床药理研究所；

【摘要】 目的研究马米酸替加色罗胶囊与其片剂生物等效性。方法20名健康男性受试者随机交叉给药,分别单次口服试验药马米酸替加色罗胶囊和参比药马来酸替加色罗片12mg, 采用LC-MS法测定替加色罗的血浓度。结果替加色罗胶囊与其片剂AUC0-24h分别为(21.436±2.659)、(21.013±2.842)ng.h.mL-1;AUC0-∞为(23.968±2.997)、(23.804±3.404)ng.h.mL-1;cmax为(4.835±1.103)、(4.863±1.164)ng.mL-1;tmax为(1.288±0.383)、(1.250±0.292)h;t1/2为(8.373±1.133)、(8.867±1.052)h。马来酸替加色罗胶囊相对生物利用度为(102.183±2.338)%。方差分析显示制剂间、周期间各参数差异无统计学意义(P>0.05),但个体间存在差异。双单侧t检验和(1-2α)置信区间分析示2制剂符合生物等效的假设。结论马来酸替加色罗胶囊与其片剂为生物等效制剂。更多还原

【Abstract】 AIM To study the bioequivalence of tegaserod maleate capsule and tablet in healthy volunteers. METHODS A single dose 12mg of tegaserod maleate capsule, as test, and tablet, as reference, were oraly given to 20 healthy male volunteers in a randomized cross-over test. The plasma concentrations of tegaserod were determined by LC-MS method and pharmacokinetic parameters were calculated and evaluated. RESULTS The pharmacokinetic parameters of tegaserod capsule and tablet were as follow: AUC0-24 (21.436 ± 2.659) and (21.013 ± 2.842)ng.h.mL-1, AUC0-∞ ( 23.968±2.997) and (23.804±3.404) ng.h.mL-1, Cmax (4.835 ± 1.103) and (4.863 ± 1.164) ng.mL-1; tmax ( 1.288±0.383 ) and (1.250±0.292)h,t1/2 (8.373 ± 1.133) and (8.867 ± 1.052)h, respectively. The relative bioavailability of tegaserod maleate capsule was (102.183 ± 2.338)%. Conclunsion The statistics analysis suggests that the two preparations are bioequivalent.更多还原