药学学报, 2012, 47(10): 1363-1369
引用本文:
刘荷英, 丁 黎, 于 勇, 储 妍, 朱 贺. 替吉奥胶囊在晚期胃癌患者体内的药代动力学研究[J]. 药学学报, 2012, 47(10): 1363-1369.
LIU He-ying, DING Li, YU Yong, CHU Yan, ZHU He. Pharmacokinetics of S-1 capsule in patients with advanced gastric cancer[J]. Acta Pharmaceutica Sinica, 2012, 47(10): 1363-1369.

替吉奥胶囊在晚期胃癌患者体内的药代动力学研究
刘荷英1, 2, 丁  黎1*, 于  勇1, 储  妍1, 朱  贺1
(1. 中国药科大学药物分析教研室, 江苏 南京 210009; 2. 江西省食品药品检验所, 江西 南昌 330029)
摘要:

研究单次及多次给药后替吉奥胶囊在晚期胃癌患者体内的药代动力学特征。12名晚期胃癌患者, 次给药时口服60 mg; 多次给药时100 mg·d−1120 mg·d−1, 连续服药28天。单次给药后替加氟、5-氟尿嘧啶、吉美嘧啶、奥替拉西钾和尿嘧啶的Cmax分别为 (2207 ± 545)(220.0 ± 68.2)(374.9 ± 103.0)(110.5 ± 100.8) (831.1 ± 199.9) ng·mL−1; t1/2分别为 (11.8 ± 3.8)(4.4 ± 3.3)(7.8 ± 5.1)(3.1 ± 0.9) (8.8 ± 4.1) h; 多剂量连续给药6天后平均稳态血药浓度 (Cav) 分别为 (2 425 ± 1 172)(73.88 ± 18.88)(162.6 ± 70.8)(36.89 ± 29.35) (435.3 ± 141.0) ng·mL−148 h内替加氟、5-氟尿嘧啶、吉美嘧啶和奥替拉西钾的尿药累积排泄率分别为 (4.2 ± 2.8) %(4.7 ± 1.6) %(18.5 ± 6.0) % (1.7 ± 1.2) % 。多次给药过程中替加氟有一定的蓄积现象, 5-氟尿嘧啶、吉美嘧啶、奥替拉西钾和尿嘧啶均无蓄积现象。

关键词:   
Pharmacokinetics of S-1 capsule in patients with advanced gastric cancer
Abstract:

The study is to investigate the pharmacokinetics of S-1 capsule (tegafur, gimeracil and potassium oxonate capsule) in patients with advanced gastric cancer after single and multiple oral administration.  Twelve patients with advanced gastric cancer were recruited to the study.  The dose of S-1 for each patient was determined according to his/her body surface area (BSA).  The dose for single administration was 60 mg every subject.  The dose for multiple administration for one subject was as follows: 100 mg·d−1 or 120 mg·d−1, 28-days consecutive oral administration.  The pharmacokinetic parameters of tegafur, 5-fluorouracil, gimeracil, potassium oxonate and uracil after single oral administration were as follows: (2 207 ± 545), (220.0 ± 68.2), (374.9 ± 103.0), (110.5 ± 100.8) and (831.1 ± 199.9) ng·mL−1 for Cmax; (11.8 ± 3.8), (4.4 ± 3.3), (7.8 ± 5.1), (3.1 ± 0.9) and (8.8 ± 4.1) h for t1/2, respectively.  After six days oral administration, the average steady state plasma concentrations (Cav) of tegafur, 5-fluorouracil, gimeracil, potassium oxonate and uracil were (2 425 ± 1 172), (73.88 ± 18.88), (162.6 ± 70.8), (36.89 ± 29.35) and (435.3 ± 141.0) ng·mL−1, respectively, and the degree of fluctuation (DF) were (1.0 ± 0.2), (2.5 ± 0.4), (3.1 ± 0.8), (2.4 ± 0.8) and (1.5 ± 0.3), respectively.  The cumulative urine excretion percentage of tegafur, 5-fluorouracil, gimeracil and potassium oxonate in urine within 48 h were (4.2 ± 2.8) %, (4.7 ± 1.6) %, (18.5 ± 6.0) % and (1.7 ± 1.2) %, repectively, after single oral administration of S-1.  The results exhibited that tegafur had some drug accumulation observed, and gimeracil, potassium oxonate, 5-fluorouracil and uracil had no drug accumulation observed.

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