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连续口服盐酸噻氯匹定片在健康人体的药代动力学

Pharmacokinetics of ticlopidine hydrochloride in healthy human subjects after continuous oral administration
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摘要 目的研究连续口服盐酸噻氯匹定片(抗血栓药)在健康人体的药代动力学。方法12名男性健康志愿者连续口服噻氯匹定片,每次250mg,每日2次。第11日按照预定时间点采血,用LC-MS-MS方法测定血浆稳态血药浓度,并求算其药代动力学参数。结果t1/2为(115±13.8)h,AUC0-21d为(24.48±10.02)μg.h.mL-1,tmax为(1.8±0.6)h,Cmax为(1303±428)ng.mL-1,Cmin为(235±107)ng.mL-1,Cav为(541±194)ng.mL-1,AUCss为(6.49±2.32)μg.h.mL-1,CLss为(48.1±33.7)L.h-1。结论连续口服盐酸噻氯匹定,吸收迅速,消除半衰期较单剂量大大延长;个体变异小。 Objective To evaluate the phannacokinetics profile of ticlopidine hydrochloride after continuous oral administration in healthy volunteers. Methods Twelve male healthy volunteers were administrated orally with ticlopidine tablets 250 mg twice daily continuously for 11 days. The plasma concentration of ticlopidine was determined by LC - MS - MS and pharmacokinetic parameters were calculated with winnonlin software. Results The pharmacokinetic parameters of ticlopidine hydrochloride were as follows : t1/2 was ( 115 ± 13.8 ) h, AUC0-21d was ( 24. 48 ± 10.02) μg· h· mL^-1^,tmax was( 1.8 ±0.6 )h,Cm= was( 1303 ±428) ng· mL^-1, CmlnWas(235±107) ng-mL^-1, Cavwas( 541 ±194 )ng ·mL^-1,AUC was (6.49±2.32)μg·h - mL^-1,CLss was (48.1± 33.7) L· h^-1. Conclusion Ticlopidine hydrochloride was absorbed rapidly, and the elimination half life of repeated dosages was much longer than single dose. The pharmacokinetics profile between indiviculs was similar.
机构地区 中国医学科学院
出处 《中国临床药理学杂志》 CAS CSCD 北大核心 2007年第4期264-267,共4页 The Chinese Journal of Clinical Pharmacology
关键词 盐酸噻氯匹定片 药代动力学 液相色谱-串联质普 ticlopidine hydrochloride tablets pharmacokinetics LC -MS - MS
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