Pharmacokinetic and Bioavailability of Esomeprazole Enteric Capsule In Healthy Volunteers_West China Medical Journal

Authors：

YU Qin , XIANG Jin , ZHENG Li , 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：

LIANG Maozhi, Email: yuqin_GCP@163.com

Keywords：

埃索美拉唑; 高效液相色谱法; 生物等效性

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目的　采用高效液相色谱法测定受试者口服埃索美拉唑肠溶胶囊与埃索美拉唑镁肠溶片后血药浓度，评价埃索美拉唑肠溶胶囊的生物等效性。方法　2009年9月－10月，36例健康男性受试者单次交叉口服埃索美拉唑肠溶胶囊（试验制剂）和埃索美拉唑镁肠溶片（参比制剂），测定给药后不同时间点血浆中埃索美拉唑经时血药浓度，采用DAS 2.0软件进行药物代谢动力学参数计算和生物等效性评价。结果　受试者单次口服试验制剂与参比制剂后，达峰时间分别为（2.19 ± 0.96）、（2.43 ± 0.92） h，峰浓度分别为（1 748.86 ± 615.81）、（1 442.92 ± 476.41） μg/L，药时曲线下面积（AUC）0-t分别为（3 927.14 ± 1 839.10）、（3 878.79 ± 1 734.84） μg/L·h，AUC0-∞分别为（3 998.36 ± 1 866.22）、（3 918.31 ± 1 773.44） μg/L·h。试验制剂与参比制剂的生物等效性为94.0%，其90%CI为（82.3%，107.2%）。结论　埃索美拉唑肠溶胶囊与埃索美拉唑镁肠溶片生物等效。

Citation： YU Qin,XIANG Jin,ZHENG Li,WANG Ying,LIANG Maozhi,MIAO Jia,NAN Feng,SHEN Qi,QIN Yongping. Pharmacokinetic and Bioavailability of Esomeprazole Enteric Capsule In Healthy Volunteers. West China Medical Journal, 2012, 27(7): 971-974. doi: Copy

1.	陈华, 王晓蕙, 金伟华. 耐信[J]. 中国新药杂志, 2003, 12 (6): 478-476.
2.	Hassan-Alin M, Andersson T, Bredberg E, et al. Pharmacokinetics of esomeprazole after oral and intravenous administration of single and repeated doses to healthy subjects[J]. Eur J Clin Pharmacol, 2000, 56(9-10): 665-670.
3.	Lind T, Rydberg L, Kylebäck A, et al. Esomeprazole provides improved acid control vs. omeprazole In patients with symptoms of gastro-oesophageal reflux disease[J]. Aliment Pharmacol Ther, 2000, 14(7): 861-867.
4.	湛先保, 李兆申, 程能能, 等. 埃索美拉唑对健康志愿者抑制胃泌酸的药效学研究[J]. 中华消化杂志, 2004, 24(12): 711-714.
5.	Miner P Jr, Katz PO, Chen Y, et al. Gastric acid control with esomeprazole, lansoprazole, omeprazole, pantoprazole, and rabeprazole: a five-way crossover study[J]. Am J Gastroenterol, 2003, 98(12): 2616-2620.
6.	Richter JE, Kahrilas PJ, Johanson J, et al. Efficacy and safety of esomeprazole compared with omeprazole in GERD patients with erosive esophagitis: a randomized controlled trial[J]. Am J Gastroenterol, 2001, 96(3): 656-665.
7.	Johnson DA, Benjamin SB, Vakil NB, et al. Esomeprazole once daily for 6 months is effective therapy for maintaining healed erosive esophagitis and for controlling gastroesophageal reflux disease symptoms: a randomized, double-blind, placebo-controlled study of efficacy and safety[J]. Am J Gastroenterol, 2001, 96(1): 27-34.
8.	陶立生, 许亚平, 姚俊, 等. 埃索美拉唑治疗幽门螺杆菌阳性十二指肠球部溃疡疗效观察[J]. 现代生物医学进展, 2011, 11(18): 3494-3496.
9.	李改芹, 李福康, 李晓沛. 注射用埃索美拉唑治疗消化性溃疡大出血的疗效分析[J]. 社区医学杂志, 2012, 10(4): 11-13.
10.	Chan FK, Jy C, Hung LC, et al. Clopidogrel versus aspirinand esomeprazole to prevent recurrent ulcer bleeding[J]. N Engl J Med, 2005, 352(3): 238-244.
11.	Zawkey C, Talley NJ, Yeomans ND, et al. Improvements with esomeprazole in patients with upper gastrointestinal symptoms taking non-steroidal antiinflammatory drugs, including selective COX-2 inhibitors[J]. Am J Gastroenterol, 2005, 100(5): 1028-1036.
12.	姚光弼. 质子泵抑制剂的新成员——埃索美拉唑[J]. 中华消化杂志, 2002, 22(4): 233-235.
13.	Hu XP, Xu JM, Hu YM, et al. Effects of CYP2C19 genetic polymorphism on the pharmacokinetics and pharmacodynamics of omeprazole in Chinese people[J]. J Clin Pharm Ther, 2007, 32(5): 517-524.
14.	陈刚. 2种埃索美拉唑制剂的人体生物等效性研究[J]. 中国药房, 2009, 20(2): 116-118.

1. 　陈华, 王晓蕙, 金伟华. 耐信[J]. 中国新药杂志, 2003, 12 (6): 478-476.
2. 　Hassan-Alin M, Andersson T, Bredberg E, et al. Pharmacokinetics of esomeprazole after oral and intravenous administration of single and repeated doses to healthy subjects[J]. Eur J Clin Pharmacol, 2000, 56(9-10): 665-670.
3. 　Lind T, Rydberg L, Kylebäck A, et al. Esomeprazole provides improved acid control vs. omeprazole In patients with symptoms of gastro-oesophageal reflux disease[J]. Aliment Pharmacol Ther, 2000, 14(7): 861-867.
4. 　湛先保, 李兆申, 程能能, 等. 埃索美拉唑对健康志愿者抑制胃泌酸的药效学研究[J]. 中华消化杂志, 2004, 24(12): 711-714.
5. 　Miner P Jr, Katz PO, Chen Y, et al. Gastric acid control with esomeprazole, lansoprazole, omeprazole, pantoprazole, and rabeprazole: a five-way crossover study[J]. Am J Gastroenterol, 2003, 98(12): 2616-2620.
6. 　Richter JE, Kahrilas PJ, Johanson J, et al. Efficacy and safety of esomeprazole compared with omeprazole in GERD patients with erosive esophagitis: a randomized controlled trial[J]. Am J Gastroenterol, 2001, 96(3): 656-665.
7. 　Johnson DA, Benjamin SB, Vakil NB, et al. Esomeprazole once daily for 6 months is effective therapy for maintaining healed erosive esophagitis and for controlling gastroesophageal reflux disease symptoms: a randomized, double-blind, placebo-controlled study of efficacy and safety[J]. Am J Gastroenterol, 2001, 96(1): 27-34.
8. 　陶立生, 许亚平, 姚俊, 等. 埃索美拉唑治疗幽门螺杆菌阳性十二指肠球部溃疡疗效观察[J]. 现代生物医学进展, 2011, 11(18): 3494-3496.
9. 　李改芹, 李福康, 李晓沛. 注射用埃索美拉唑治疗消化性溃疡大出血的疗效分析[J]. 社区医学杂志, 2012, 10(4): 11-13.
10. 　Chan FK, Jy C, Hung LC, et al. Clopidogrel versus aspirinand esomeprazole to prevent recurrent ulcer bleeding[J]. N Engl J Med, 2005, 352(3): 238-244.
11. 　Zawkey C, Talley NJ, Yeomans ND, et al. Improvements with esomeprazole in patients with upper gastrointestinal symptoms taking non-steroidal antiinflammatory drugs, including selective COX-2 inhibitors[J]. Am J Gastroenterol, 2005, 100(5): 1028-1036.
12. 　姚光弼. 质子泵抑制剂的新成员——埃索美拉唑[J]. 中华消化杂志, 2002, 22(4): 233-235.
13. 　Hu XP, Xu JM, Hu YM, et al. Effects of CYP2C19 genetic polymorphism on the pharmacokinetics and pharmacodynamics of omeprazole in Chinese people[J]. J Clin Pharm Ther, 2007, 32(5): 517-524.
14. 　陈刚. 2种埃索美拉唑制剂的人体生物等效性研究[J]. 中国药房, 2009, 20(2): 116-118.

West China Medical Journal

Pharmacokinetic and Bioavailability of Esomeprazole Enteric Capsule In Healthy Volunteers

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