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; 高效液相色譜法; 生物等效性

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目的　采用高效液相色譜法測定受試者口服埃索美拉唑腸溶膠囊與埃索美拉唑鎂腸溶片后血藥濃度，評價埃索美拉唑腸溶膠囊的生物等效性。方法　2009年9月－10月，36例健康男性受試者單次交叉口服埃索美拉唑腸溶膠囊（試驗制劑）和埃索美拉唑鎂腸溶片（參比制劑），測定給藥后不同時間點血漿中埃索美拉唑經時血藥濃度，采用DAS 2.0軟件進行藥物代謝動力學參數計算和生物等效性評價。結果　受試者單次口服試驗制劑與參比制劑后，達峰時間分別為（2.19 ± 0.96）、（2.43 ± 0.92） h，峰濃度分別為（1 748.86 ± 615.81）、（1 442.92 ± 476.41） μg/L，藥時曲線下面積（AUC）0-t分別為（3 927.14 ± 1 839.10）、（3 878.79 ± 1 734.84） μg/L·h，AUC0-∞分別為（3 998.36 ± 1 866.22）、（3 918.31 ± 1 773.44） μg/L·h。試驗制劑與參比制劑的生物等效性為94.0%，其90%CI為（82.3%，107.2%）。結論　埃索美拉唑腸溶膠囊與埃索美拉唑鎂腸溶片生物等效。

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.	陳華, 王曉蕙, 金偉華. 耐信[J]. 中國新藥雜志, 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. 埃索美拉唑對健康志愿者抑制胃泌酸的藥效學研究[J]. 中華消化雜志, 2004, 24(12): 711-714.
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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, 許亞平, 姚俊, 等. 埃索美拉唑治療幽門螺桿菌陽性十二指腸球部潰瘍療效觀察[J]. 現代生物醫學進展, 2011, 11(18): 3494-3496.
9.	李改芹, 李福康, 李曉沛. 注射用埃索美拉唑治療消化性潰瘍大出血的療效分析[J]. 社區醫學雜志, 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. 質子泵抑制劑的新成員——埃索美拉唑[J]. 中華消化雜志, 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.	陳剛. 2種埃索美拉唑制劑的人體生物等效性研究[J]. 中國藥房, 2009, 20(2): 116-118.

1. 　陳華, 王曉蕙, 金偉華. 耐信[J]. 中國新藥雜志, 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. 埃索美拉唑對健康志愿者抑制胃泌酸的藥效學研究[J]. 中華消化雜志, 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, 許亞平, 姚俊, 等. 埃索美拉唑治療幽門螺桿菌陽性十二指腸球部潰瘍療效觀察[J]. 現代生物醫學進展, 2011, 11(18): 3494-3496.
9. 　李改芹, 李福康, 李曉沛. 注射用埃索美拉唑治療消化性潰瘍大出血的療效分析[J]. 社區醫學雜志, 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. 質子泵抑制劑的新成員——埃索美拉唑[J]. 中華消化雜志, 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. 　陳剛. 2種埃索美拉唑制劑的人體生物等效性研究[J]. 中國藥房, 2009, 20(2): 116-118.

West China Medical Journal

Pharmacokinetic and Bioavailability of Esomeprazole Enteric Capsule In Healthy Volunteers

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