伏立诺他在皮肤 T细胞淋巴瘤患者的药代动力学研究  

Pharmacokinetic study of vorinostat in cutaneous T cell lymphoma patients

作　　者：郑靖[1] 秦永平[1] 苗佳[1] 章丽[1] 刘雯[1] 舒世清[1] 王颖[1] 朱晓红[1] 

机构地区：[1]四川大学华西医院I期临床研究室,成都610041

出　　处：《中国临床药理学杂志》2015年第21期2118-2120,共3页The Chinese Journal of Clinical Pharmacology

摘　　要：目的评价皮肤T细胞淋巴瘤(CTCL)患者口服伏立诺他胶囊的药代动力学特点。方法 2例CTCL患者分别于早餐后单次顿服伏立诺他胶囊200,400mg,于各个时间采集血液,用HPLC-MS/MS法测定人血清中伏立诺他(SHA)、M2代谢物(M2)的浓度,用Win Nonlin 6.1计算药代动力学参数。结果单次口服伏立诺他200,400 mg后,伏立诺他的Cmax分别为262.95,257.46 ng·m L-1;t1/2分别为1.86,2.52 h;tmax分别为3.00,4.00 h;AUC0-t分别为638.13,1503.14ng·m L-1·h。M2的Cmax分别为450.88,652.70 ng·m L-1;t1/2分别为80.21,14.14h,tmax均为4.00 h,AUC0-t分别为2292.03,4848.29 ng·m L-1·h。2例患者均未见不良反应。结论伏立诺他体内过程个体差异较大。Objective To investigate the pharmacokinetic（ PK） charac-teristics of vorinostat in cutaneous T -cell lymphoma （ CTCL ） patients after a single dose.Methods Two cases of CTCL patients were orally administered of vorinostat capsules at 200 mg or 400 mg once after break-fast.The 3 mL blood samples were collected pre-dose and at different time points.Vorinostat （ SHA ） , M2 metabolites （ M2 ） and the internal standard d5-vorinostat（ d5-SHA） in serum were measured by HPLC-MS/MS method.WinNonlin 6.1 software was used to calculate the non-compartment pharmacokinetic parameters.Results After a single dose of oral administration of 200 mg and 400 mg vorinostat capsule, Cmax were 262.95 and 257.46 ng· mL-1 , t1/2 were 1.86 and 2.52 h, tmax were 3.00 and 4.00 h, AUC0-t were 638.13 and 1503.14 ng· mL-1· h for SHA, respectively.Cmax were 450.88 and 652.70 ng· mL-1 , t1/2 were 80.21 and 14.14 h, tmax was 4.00 h, AUC0-t were 2292.03 and 4848.29 ng· mL-1· h for M2, respectively.It was safe for the two patients to use vorinostat capsule, and there was no adverse reactions.Conclusion The individual disposition of vorinostat had a large different.

关 键 词：伏立诺他 皮肤T细胞淋巴瘤 单次给药 药代动力学 

分 类 号：R969.1[医药卫生—药理学] R979.1[医药卫生—药学]