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：

普羅布考; 高效液相色譜-質譜聯用法; 藥物代謝動力學

Video：

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目的　采用高效液相色譜-質譜聯用法（HPLC-MS/MS）研究普羅布考片的人體藥物代謝動力學變化規律。方法　 2010年10月－11月，24例健康男性受試者單次口服普羅布考片0.5 g，采用HPLC-MS/MS法測定給藥后不同時間點血漿中普羅布考的經時血藥濃度，采用DAS 2.0軟件進行藥動學參數計算。結果　受試者單次口服普羅布考片，達峰時間為（11.50 ± 6.66）h，峰濃度為（2 894.72 ± 1 320.53）ng/mL，藥-時曲線下面積（AUC）0-t為（238 876.96 ± 131 873.67） ng/mL· h，AUC0-∞為（259 989.08 ± 146 112.88）ng/mL· h，半衰期為（278.52 ± 164.72） h。
結論　普羅布考片體內過程符合二室模型，單次口服具有較好的安全性。

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.	楊玲, 張紹敏, 孫春麗, 等. 普羅布考對老年急性冠脈綜合征患者血脂水平、血清高敏CRP和氧化低密度脂蛋白的影響[J]. 四川大學學報: 醫學版, 2012, 43(3): 467-469.
2.	王哲, 楊向紅. 丙丁酚的藥理作用及臨床應用研究新進展[J]. 實用藥物與臨床, 2007, 10(1): 46-48.
3.	李婷婷, 郭媛. 普羅布考抗動脈粥樣硬化作用機制及研究進展[J]. 醫學綜述, 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. 普羅布考對糖尿病大血管病變患者血清氧化應激水平的干預效果觀察[J]. 中國醫藥導報, 2012, 9(14): 89-90.
6.	朱近悅, 宋娟, 夏娟, 等. 普羅布考治療早期糖尿病腎病106例觀察[J]. 上海預防醫學, 2011, 23(2): 88-89.
7.	成西霞, 王金. 抗氧化劑普羅布考的臨床應用[J]. 臨床合理用藥雜志, 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. 　楊玲, 張紹敏, 孫春麗, 等. 普羅布考對老年急性冠脈綜合征患者血脂水平、血清高敏CRP和氧化低密度脂蛋白的影響[J]. 四川大學學報: 醫學版, 2012, 43(3): 467-469.
2. 　王哲, 楊向紅. 丙丁酚的藥理作用及臨床應用研究新進展[J]. 實用藥物與臨床, 2007, 10(1): 46-48.
3. 　李婷婷, 郭媛. 普羅布考抗動脈粥樣硬化作用機制及研究進展[J]. 醫學綜述, 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. 普羅布考對糖尿病大血管病變患者血清氧化應激水平的干預效果觀察[J]. 中國醫藥導報, 2012, 9(14): 89-90.
6. 　朱近悅, 宋娟, 夏娟, 等. 普羅布考治療早期糖尿病腎病106例觀察[J]. 上海預防醫學, 2011, 23(2): 88-89.
7. 　成西霞, 王金. 抗氧化劑普羅布考的臨床應用[J]. 臨床合理用藥雜志, 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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