论文部分内容阅读
目的研究多剂量静滴盐酸卡屈沙星葡萄糖注射液的药动学。方法选择10名中国健康成年志愿者,18~40岁,男女各半,静滴盐酸卡屈沙星葡萄糖注射液,每次400mg,每日1次,连续7d。用高效液相色谱法测定血及尿中药物浓度,利用血药浓度,以DAS软件拟合药动学参数;利用尿药浓度计算尿药累计排泄率。结果受试者静滴盐酸卡屈沙星葡萄糖注射液,体内过程符合二室模型。连续给药后,第1天与第7天的主要药动学参数分别是ρmax(7.33±1.67)和(7.91±1.85)mg·L-1,AUC0-24(41.24±8.11)和(44.07±10.72)mg·h·L-1,AUC0-∞(43.04±8.39)和(44.39±10.85)mg·h·L-1,t1/2β(5.3±1.34)和(4.95±0.98)h。经比较差异无统计学意义。平均稳态血药浓度ρav为(0.33±0.10)mg·L-1,稳态血药浓度-时间曲线下面积AUCss为(39.23±12.63)mg·h·L-1,波动度DF为(25.44±9.54)。单次及多次给药400mg后,0~24h内尿药累积排泄率分别为(68.90±5.31)%和(77.27±5.51)%,经t检验差异存在统计学意义。结论本品每天1次给药400mg,连续给药7d,在体内可达有效血浆浓度,体内未见蓄积。
Objective To study the pharmacokinetics of multidose intravenous infusion of capecitabine hydrochloride. Methods Ten healthy adult Chinese volunteers aged 18-40 years and male and female were divided into two groups. Each group received intravenous infusion of carbachofen hydrochloride (400mg, once daily for 7 days). The concentration of drug in blood and urine was determined by HPLC, the pharmacokinetic parameters were fitted by DAS software and the cumulative urinary excretion rate was calculated by urine concentration. Results Subjects intravenous infusion of carbicalcite hydrochloride, in vivo process in line with the two-compartment model. After continuous administration, the main pharmacokinetic parameters of day 1 and day 7 were ρmax (7.33 ± 1.67) and (7.91 ± 1.85) mg · L-1, AUC0-24 (41.24 ± 8.11) and (44.07 ± 10.72) mg · h · L -1, AUC0-∞ (43.04 ± 8.39) and (44.39 ± 10.85) mg · h · L -1, t1 / 2β (5.3 ± 1.34) and (4.95 ± 0.98) h, respectively. The difference was not statistically significant. The mean steady-state plasma concentration ρav was (0.33 ± 0.10) mg · L-1, and the area under steady-state concentration-time curve AUCss was (39.23 ± 12.63) mg · h · L -1. The fluctuation DF was (25.44 ± 9.54). After single and multiple administrations of 400mg, the urinary cumulative excretion rates within 0-24 h were (68.90 ± 5.31)% and (77.27 ± 5.51)%, respectively. There was significant difference by t test. Conclusion This product is administered once a day 400mg, continuous administration of 7d, up to the effective plasma concentration in the body, no accumulation in the body.