Pharmacokinetics of Single-dose Probucol Tablet in Healthy Volunteers_West China Medical Journal

Authors：

XIANG Jin , XU Nan ,  YU Qin , WANG Ying , LIANG Maozhi , MIAO Jia , NAN Feng , SHEN Qi , QIN Yongping

Institute of Drug Clinical Trial·GCP Center, Department of Clinical Pharmacology, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, P. R. China;

Corresponding author：

YU Qin, Email: xiangjintoday@163.com

Keywords：

普罗布考; 高效液相色谱-质谱联用法; 药物代谢动力学

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目的　采用高效液相色谱-质谱联用法（HPLC-MS/MS）研究普罗布考片的人体药物代谢动力学变化规律。方法　 2010年10月－11月，24例健康男性受试者单次口服普罗布考片0.5 g，采用HPLC-MS/MS法测定给药后不同时间点血浆中普罗布考的经时血药浓度，采用DAS 2.0软件进行药动学参数计算。结果　受试者单次口服普罗布考片，达峰时间为（11.50 ± 6.66）h，峰浓度为（2 894.72 ± 1 320.53）ng/mL，药-时曲线下面积（AUC）0-t为（238 876.96 ± 131 873.67） ng/mL· h，AUC0-∞为（259 989.08 ± 146 112.88）ng/mL· h，半衰期为（278.52 ± 164.72） h。
结论　普罗布考片体内过程符合二室模型，单次口服具有较好的安全性。

Citation： XIANG Jin,XU Nan,YU Qin,WANG Ying,LIANG Maozhi,MIAO Jia,NAN Feng,SHEN Qi,QIN Yongping. Pharmacokinetics of Single-dose Probucol Tablet in Healthy Volunteers. West China Medical Journal, 2012, 27(7): 975-978. doi: Copy

1.	杨玲, 张绍敏, 孙春丽, 等. 普罗布考对老年急性冠脉综合征患者血脂水平、血清高敏CRP和氧化低密度脂蛋白的影响[J]. 四川大学学报: 医学版, 2012, 43(3): 467-469.
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3.	李婷婷, 郭媛. 普罗布考抗动脉粥样硬化作用机制及研究进展[J]. 医学综述, 2009, 15(9): 1390-1392.
4.	Buckley MM, Goa KL, Price AH, et al. Probucol. a reappraisal of its pharmacological properties and therapeutic use in hypercholesterolaemia[J]. Drugs, 1989, 37(6): 761-800.
5.	胡江平. 普罗布考对糖尿病大血管病变患者血清氧化应激水平的干预效果观察[J]. 中国医药导报, 2012, 9(14): 89-90.
6.	朱近悦, 宋娟, 夏娟, 等. 普罗布考治疗早期糖尿病肾病106例观察[J]. 上海预防医学, 2011, 23(2): 88-89.
7.	成西霞, 王金. 抗氧化剂普罗布考的临床应用[J]. 临床合理用药杂志, 2009, 02(13): 125-126.
8.	Jeon H, Lee S, Kim TE, et al. Pharmacokinetics and tolerability of probucol after multiple oral administrations in healthy volunteers[J]. Int J Clin Pharmacol Ther, 2011, 49(11): 688-695.
9.	Kim KP, Kim BH, Lim KS, et al. Potential interactions between cilostazol and probucol: a two-part, single-dose, open-label study in healthy Korean male volunteers[J]. Clin Ther, 2009, 31(10): 2098-2106.
10.	Jiko M, Yano I, Wakasugi H, et al. Evaluation of pharmacokinetic interaction between cyclosporin A and probucol in rats[J]. Pharm Res, 2002, 19(9): 1362-1367.
11.	Reinoehl J, Frankovich D, Machado C, et al. Probucol-associated tachyarrhythmic events and QT prolongation: importance of gender[J]. Am Heart J, 1996, 131(6): 1184-1191.
12.	Merat S, Malekzadeh R, Sohrabi MR, et al. Probucol in the treatment of non-alcoholic steatohepatitis: a double-blind randomized controlled study[J]. J Hepatol, 2003, 38(4): 414-418.

1. 　杨玲, 张绍敏, 孙春丽, 等. 普罗布考对老年急性冠脉综合征患者血脂水平、血清高敏CRP和氧化低密度脂蛋白的影响[J]. 四川大学学报: 医学版, 2012, 43(3): 467-469.
2. 　王哲, 杨向红. 丙丁酚的药理作用及临床应用研究新进展[J]. 实用药物与临床, 2007, 10(1): 46-48.
3. 　李婷婷, 郭媛. 普罗布考抗动脉粥样硬化作用机制及研究进展[J]. 医学综述, 2009, 15(9): 1390-1392.
4. 　Buckley MM, Goa KL, Price AH, et al. Probucol. a reappraisal of its pharmacological properties and therapeutic use in hypercholesterolaemia[J]. Drugs, 1989, 37(6): 761-800.
5. 　胡江平. 普罗布考对糖尿病大血管病变患者血清氧化应激水平的干预效果观察[J]. 中国医药导报, 2012, 9(14): 89-90.
6. 　朱近悦, 宋娟, 夏娟, 等. 普罗布考治疗早期糖尿病肾病106例观察[J]. 上海预防医学, 2011, 23(2): 88-89.
7. 　成西霞, 王金. 抗氧化剂普罗布考的临床应用[J]. 临床合理用药杂志, 2009, 02(13): 125-126.
8. 　Jeon H, Lee S, Kim TE, et al. Pharmacokinetics and tolerability of probucol after multiple oral administrations in healthy volunteers[J]. Int J Clin Pharmacol Ther, 2011, 49(11): 688-695.
9. 　Kim KP, Kim BH, Lim KS, et al. Potential interactions between cilostazol and probucol: a two-part, single-dose, open-label study in healthy Korean male volunteers[J]. Clin Ther, 2009, 31(10): 2098-2106.
10. 　Jiko M, Yano I, Wakasugi H, et al. Evaluation of pharmacokinetic interaction between cyclosporin A and probucol in rats[J]. Pharm Res, 2002, 19(9): 1362-1367.
11. 　Reinoehl J, Frankovich D, Machado C, et al. Probucol-associated tachyarrhythmic events and QT prolongation: importance of gender[J]. Am Heart J, 1996, 131(6): 1184-1191.
12. 　Merat S, Malekzadeh R, Sohrabi MR, et al. Probucol in the treatment of non-alcoholic steatohepatitis: a double-blind randomized controlled study[J]. J Hepatol, 2003, 38(4): 414-418.

West China Medical Journal

Pharmacokinetics of Single-dose Probucol Tablet in Healthy Volunteers

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