|本期目录/Table of Contents|

[1]张天南,欧宁,张宏文.艾普拉唑肠溶片在中国健康人体中药代动力学及绝对生物利用度研究[J].医学研究与战创伤救治(原医学研究生学报),2017,19(04):372-375.[doi:10.3969/j.issn.1672-271X.2017.04.010]
　ZHANG Tian-nan,OU Ning,ZHANG Hong-wen.Pharmacokinetics and absolute bioavailability of ilaprazole enteric-coated tablet in Chinese healthy volunteers[J].JOURNAL OF MEDICALRESEARCH —COMBAT TRAUMA CARE,2017,19(04):372-375.[doi:10.3969/j.issn.1672-271X.2017.04.010]
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艾普拉唑肠溶片在中国健康人体中药代动力学及绝对生物利用度研究()
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《医学研究与战创伤救治》（原医学研究生学报）[ISSN:1672-271X/CN:32-1713/R]

卷:
第19卷
期数:
2017年04期
页码:
372-375
栏目:
出版日期:
2017-08-10

文章信息/Info

Title:
Pharmacokinetics and absolute bioavailability of ilaprazole enteric-coated tablet in Chinese healthy volunteers
作者:
张天南1; 欧宁2; 张宏文2
作者单位：1. 210029南京，江苏省中医院药学部；2. 210029南京，南京医科大学第一附属医院/江苏省人民医院I期临床试验研究室
Author(s):
ZHANG Tian-nan1;  OU Ning 2;  ZHANG Hong-wen2
(1. Department of Pharmacy，Jiangsu Province Hospital of Traditional Chinese Medicine，Nanjing 210029, Jiangsu, China；2. Phase I Clinical Trial Laboratory, the First Affiliated Hospital of Nanjing Medical University, Jiangsu Province Hospital, Nanjing 21002
关键词:
艾普拉唑; 药代动力学; 绝对生物利用度; 液相色谱串联质谱
Keywords:
Ilaprazole;  Pharmacokinetic;  Absolute bioavailability;  LC-MS/MS
分类号:
R969.1
DOI:
10.3969/j.issn.1672-271X.2017.04.010
文献标志码:
A
摘要:
目的 采用液相色谱串联质谱（UPLC-MS/MS）分析方法 研究艾普拉唑肠溶片在中国健康人体中的吸收特性。方法 采用随机交叉自身对照试验设计,16名健康受试者随机等分成4组,先后口服艾普拉唑肠溶片或静脉注射艾普拉唑钠，采用UPLC-MS/MS测定血浆药物浓度。利用WinNonlin（V6.1）软件标准非房室模型方法 进行药代动力学参数的计算。结果 注射用艾普拉唑钠（10mg）的主要药代动力学参数：最大血药浓度（Cmax）为（834.3±101.2）ng/mL，消除半衰期（t1/2）为（3.4±0.9）h，表观分布容积（Vz）为（14.0±2.2）L, 0到t时间药时曲线下面积（AUC0_t）为（3520.9±915.3）ng·h/mL，血浆清除率（CL）为（3.0±0.9）L/h。艾普拉唑肠溶片（10mg）的主要药代动力学参数：Cmax为（347.9±176.3）ng/mL，t1/2为（3.5±0.8）h，Vz为（29.1±12.2）L,AUC0_t为（1970.2±834.7）ng·h/mL，CL为（5.9±2.5）L/h。与静脉给药相比，口服艾普拉唑肠溶片的绝对生物利用度为（55.2±13.9）%。结论 艾普拉唑肠溶片生物利用度良好，适于开发。
Abstract:
Objective To study the absorption of ilaprazole enteric-coated tablet in Chinese healthy volunteer using UPLC-MS/MS.Methods A randomized crossover self-controlled trial was designed, in which sixteen subjects were randomly divided into 4 groups. Then ilaprazole enteric-coated table or ilaprazole sodium were given to each group by oral or intravenous injection. The drug concentrations were determined by UPLC-MS/MS and pharmacokinetic parameters were calculated using WinNonlin (V6.1) software with non-compartmental model.Results The pharmacokinetic parameters of ilaprazole sodium (10 mg) for injection were as follows: Cmax was (834.3±101.2) ng/mL t1/2 was (3.4±0.9) h. Vz was (14.0±2.2) L. AUC0_t was (3520.9±915.3) ng·h/mL. CL was (3.0±0.9) L/h. The pharmacokinetic parameters of ilaprazole enteric-coated table (10 mg) were as follows: Cmax was (347.9±176.3) ng/mL. t1/2 was (3.5±0.8) h. Vz was (29.1±12.2) L. AUC0_t was (1970.2±834.7) ng·h/mL. CL was (5.9±2.5) L/h. Compared with ilaprazole sodium, the mean absolute bioavailability of ilaprazole enteric-coated table was (55.2±13.9)%.Conclusion Ilaprazole enteric-coated tablet has good bioavailability and is suitable for development.

参考文献/References:

[1]Kil BJ, Kim IW, Shin CY, et al. Comparison of IY81149 with omeprazole in rat reflux oesophagitis[J]. J Auton Pharmacol，2000, 20(5-6):291-296.
[2］Kwon D, Chae JB, Park CW, et al. Effects of IY-81149, a newly developed proton pump inhibitor, on gastric acid secretion in vitro and in vivo[J]. Arzneimittelforschung, 2001, 51(3):204-213.
[3］Kim EJ, Lee RK, Lee SM, et al. General pharmacology of IY-81149, a new proton pump inhibitor[J]. Arzneimittelforschung, 2001, 51(1):51-59.
[4］周丽雅, 林三仁, 杨云生,等. 艾普拉唑对十二指肠溃疡患者胃内pH值的影响[J]. 中华内科杂志, 2010, 49(4):290-292.
[5］Wang H, Lang L, Ning O, et al. Pharmacokinetics, pharmacodynamics and safety of multiple-Infusion ilaprazole in healthy Chinese subjects[J]. Clin Drug Invest, 2016, 36(6):463-470.
[6]Ji XQ, Du JF, Chen G, et al. Efficacy of ilaprazole in the treatment of duodenal ulcers:a meta-analysis[J]. World J Gastroenterol, 2014, 20(17):5119-5123.
[7]李志坤, 王福文. 药物治疗应激性胃溃疡的研究进展[J]. 医学研究生学报, 2015，28(1):110-112.
[8］Wang L, Zhou L, Lin S, et al. A new PPI, ilaprazole compared with omeprazole in the treatment of duodenal ulcer: a randomized double-blind multicenter trial[J]. J Clin Gastroenterol, 2011, 45(4):322-329.
[9］Ho KY, Kuan A, Zao F, et al. Randomized, parallel, double-blind comparison of the ulcer-healing effects of ilaprazole and omeprazole in the treatment of gastric and duodenal ulcers[J]. J Gastroenterol, 2009, 44(7):697-707.
[10］刘腾, 常艳璐, 韩容. 艾普拉唑的作用机制与临床评价[J]. 中国医院用药评价与分析, 2009, 9(10):724-725.
[11］Shin JS, Lee JY, Cho KH, et al. The pharmacokinetics, pharmacodynamics and safety of oral doses of ilaprazole 10, 20 and 40 mg and esomeprazole 40 mg in healthy subjects: a randomised, open-label crossover study[J]. Aliment Pharmacol Ther, 2014, 40(5):548-561.
[12］艾普拉唑临床协作组. 艾普拉唑肠溶片治疗十二指肠溃疡的多中心、随机、双盲、阳性平行对照临床研究[J]. 中华消化杂志, 2009, 29(8):542-546.
[13］梁嘉碧, 冯文周, 边壮,等. 液相色谱-串联质谱法测定人血浆中艾普拉唑的浓度[J]. 药物分析杂志, 2013,33(6):935-940.
[14］吴骏, 陈集志, 徐小燕,等. 2011-2013年我院口服抗消化性溃疡药物的用药分析[J]. 东南国防医药, 2014，16(5):502-504.

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备注/Memo

备注/Memo:
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更新日期/Last Update: 2017-07-20