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(jià)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(yàn)制劑）和埃索美拉唑鎂腸溶片（參比制劑），測定給藥后不同時(shí)間點(diǎn)血漿中埃索美拉唑經(jīng)時(shí)血藥濃度，采用DAS 2.0軟件進(jìn)行藥物代謝動(dòng)力學(xué)參數(shù)計(jì)算和生物等效性評價(jià)。 結(jié)果 受試者單次口服試驗(yàn)制劑與參比制劑后，達(dá)峰時(shí)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(shí)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(yàn)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(jié)論 埃索美拉唑腸溶膠囊與埃索美拉唑鎂腸溶片生物等效。
引用本文： 余勤,向瑾,鄭莉,王穎,梁茂植,苗佳,南峰,沈奇,秦永平. 埃索美拉唑腸溶膠囊人體生物等效性試驗(yàn). 華西醫(yī)學(xué), 2012, 27(7): 971-974. doi: 復(fù)制
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- 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?qū)】抵驹刚咭种莆该谒岬乃幮W(xué)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(xiàn)代生物醫(yī)學(xué)進(jìn)展, 2011, 11(18): 3494-3496.
- 9. 李改芹, 李?？? 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(qū)醫(yī)學(xué)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(zhì)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.