去氧氟尿苷两种片剂与胶囊在恶性肿瘤患者中的药代动力学及生物等效性研究  

Pharmacokinetics and Bioequivalence of 5'-deoxy-5-fluorouridine Two tablets and A Capsule in Volunteers with Cancer

作　　者：冒国光[1] 裘福荣[1] 陈波[1] 戴敏[1] 孙华[1] 孙瑞元[1] 

机构地区：[1]皖南医学院弋矶山医院临床药理研究所,芜湖241000

出　　处：《中国临床药理学杂志》2002年第4期290-293,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：目的:在恶性肿瘤志愿者体内对去氧氟尿苷两种片剂和胶囊的药代动力学和生物等效性研究。方法:24名消化道肿瘤病人受试者按体重分层,随机三交叉口服去氧氟尿苷两种受试片和参比制剂去氧氟尿苷胶囊,剂间间隔为1周,剂量均为600mg。每次服药后180min内多点采集血样,用HPLC法测定血清中药物浓度,药-时数据用3P97拟合,按一室模型计算药物动力学参数。结果:两受试片剂和参比胶囊t1/2ka分别为（11.85±0.90）min,（14.10±7.66）min和（16.64±8.54）min,t1/2ke分别为（23.02±6.58）min,（21.85±4.80）min和（23.28±7.47）min,tmax分别为（41.94±12.62）min,（37.08±11.03）min和（43.33±11.38）min,Cmax分别为（5.27±2.02）mg·L-1,（5.84±2.50）mg·L-1和（5.47±2.25）mg·L-1,AUC0-150分别为（271.77±67.84）mg·min·L-1,（294.71±94.92）mg·min·L-1和（282.55±75.65）mg·min·L-1。和参比胶囊相比,两种受试片剂的相对生物利用度分别为（102.62±12.19）％和（106.46±12.66）％。结论:两受试去氧氟尿苷片剂与参比胶囊具有生物等效性。OBJECTIVE:To study pharmacokinetics and bioequivalence of 5'-deoxy-5-fluorouridine two tablets and a capsule in 24 volunteers with cancer. METHODS: According to the the three-crossover design, each volunteer was orally given 5'-deoxy-5-fluorouridine two tablets or a capsule, the serum concentrations were determined by HPLC. pharmacokinetics parameters were obtained using 3P97 programe ,and were calculated on the basis of one-compartment model .RESULTS: After a single oral dose(600mg), t1/2ka was(l 1.85±5.90)min,(14.10±7.66)min and (16.64±8.54)min,t1/2ke was(23.02±6.58)min,(21.85±4.80)min and(23.28±+7.47)min,Cmax was(5.27±2.02)mg.L-1,(5.84±2.50)mg.L-1 and(5.47±2.25)mg.L-1,tmax was(41.94±12.62) min,(37.08±11.03)min and(43.33±11.38)min,AUC0-150(271.77±67.84)mg.min.L-1, (294.71±94.92)mg.min.L-1 and(282.55±75.65)mg.min.L-1 for two texted tablets and controlled capsule, replectively. Relative bioavailability of two 5'-deoxy-5-fluorouridine tablets were (102.62±12.19)% and (106.46±12.66)%, replectively. CONLUTION: The result shows that three formutions are of bioequivalence.

关 键 词：片剂 胶囊 恶性肿瘤 去氧氟尿苷 药代动力学 生物等效性 血药浓度 

分 类 号：R969.1[医药卫生—药理学] R944[医药卫生—药学]