Genotoxicity Evaluation of (R)-(+)-Rabeprazole Sodium for Injection

doi:10.19803/j.1672-8629.2020.09.03

Abstract

Abstract: Objective To evaluate the genotoxicity of (R)-(+)-rabeprazole sodium for injection in order to provide reference for clinical rational drug use. Methods The genotoxicity of (R)-(+)-rabeprazole sodium for injection was evaluated via three experiments, including bacterial reverse mutation test, Chinese hamster lung cell (CHL) chromosome aberration test in vitro and mouse erythrocyte micronucleus test. Results The results of the bacterial reverse mutation test showed that the number of bacterial colonies in each dose group of (R)-(+)-rabeprazole sodium for injection did not increase significantly compared with the solvent control group. In the In vitro chromosome aberration test of CHL cells, the chromosome aberration rate of each dose group was not statistically significant compared with the solvent control group. The In vivo micronucleus test of mice suggested that the micronucleus rate of each dose group was not statistically significant compared with the solvent control group. All the three tests were negative. Conclusion Under the same conditions as in this study, no genotoxicity is detected in (R)-(+)-rabeprazole sodium for injection.

Key words: (R)-(+)-rabeprazole sodium for injection, genotoxicity, bacterial reverse mutation test, chromosome aberration assay, mouse micronucleus test

CLC Number:

R994.1
R975

GAO Mei, MA Hui, CHEN Kai, ZHANG Daizhou. Genotoxicity Evaluation of (R)-(+)-Rabeprazole Sodium for Injection[J]. Chinese Journal of Pharmacovigilance, 2020, 17(9): 559-563.

References

[1] Maradey-Romero C, Fass R.New and future drug development for gastroesophageal reflux disease[J]. J Neurogastroenterol Motil, 2014, 20(1):6-16.
[2] Targownik L.Discontinuing Long-Term PPI Therapy: Why, With Whom, and How[J]. Am J Gastroenterol, 2018, 113(4):519-528.
[3] Bhargava A, Faiz SM, Srivastava MR, et al.Role of Proton Pump Inhibitors in Laryngopharyngeal Reflux: Clinical Evaluation in a North Indian Population[J].Indian J Otolaryngol Head Neck Surg, 2019, 71(3):371-377.
[4] Hunt RH, Xiao SD, Megraud F, et al.World Gastroenterology Organisation Global Guideline: Helicobacter pylori in developing countries[J]. J Clin Gastroenterol, 2011, 45(5):383-388.
[5] Park JH, Park H, Lee DH, et al.A randomized, double blinded, clinical trial to assess the efficacy and cost effectiveness of omeprazole compared to rabeprazole in the maintenance therapy of patients with gastroesophageal reflux disease[J]. J Neurogastroenterol Motil, 2013, 19(2):219-226.
[6] Hashimoto N.Rabeprazole is effective for bile reflux oesophagitis after total gastrectomy in a rat model[J]. World J Gastrointest Pathophysiol, 2015, 6(1):23-28.
[7] Gu L, Li S, He Y, et al.Bismuth, rabeprazole, amoxicillin, and doxycycline as first-line Helicobacter pylori therapy in clinical practice: A pilot study[J]. Helicobacter, 2019, 4(4):e12594.
[8] 林晓冬,刘娜,刘纯,等.右旋雷贝拉唑钠对大鼠消化性溃疡的药效研究[J].食品与药品,2018,20(5):362-366.
[9] 桂元,王砾,詹继东,等.右旋雷贝拉唑钠对反流性食管炎模型大鼠炎性因子及血管活性肠肽的影响[J]. 胃肠病学和肝病学杂志,2017,26(5):539-542.
[10] 国家食品药品监督管理局.药物遗传毒性研究技术指导原则[S].国家食品药品监督管理总局,2018:4,22-26,31-33.
[11] 中华人民共和国卫生部.保健食品检验与评价技术规范[S].2003:189-199.
[12] 袁伯俊,廖明阳,李波.药物毒理学实验方法与技术[M].北京:化学工业出版社,2007:268-271.
[13] Hori H, Takayanagi T, Kamada Y, et al.Genotoxicity evaluation of sesamin and episesamin[J]. Mutat Res, 2011, 719(1-2):21-28.
[14] Shimoyama T, Chinda D, Sawada Y, et al.Randomized Trial Comparing Esomeprazole and Rabeprazole in First-line Eradication Therapy for Helicobacter pylori Infection based on the Serum Levels of Pepsinogens[J]. Intern Med, 2017, 56(13):1621-1627.
[15] 戴晓莉,戴学栋,郭峰,等.注射用右旋雷贝拉唑钠大鼠13周重复给药毒性研究[J].中国药物警戒,2016,13(7):389-393.
[16] 刘翠玲,戴晓莉,马玉奎,等.注射用右旋雷贝拉唑钠Beagle犬13周重复给药毒性实验研究[J].中国药物警戒,2017,14(8):453-456.
[17] Gao YH, Xu JX, Su ZX, et al.The chiral bioconversion and preclinical pharmacokinetic analysis of (R)-(+)-rabeprazole in beagle dogs by HPLC and HPLC-MS/MS[J]. Biomed Chromatog, 2013, 27(11):1380-1386.
[18] Toda R, Shiramoto M, Komai E, et al.Pharmacokinetics and Pharmacodynamics of Azeloprazole Sodium, a Novel Proton Pump Inhibitor, in Healthy Japanese Volunteers[J]. J Clin Pharmacol, 2018, 58(4):425-433.
[19] Patel H, Desai N, Patel P, et al.Pharmacokinetic evaluation of differential drug release formulations of rabeprazole in dogs[J]. Drug Dev Ind Pharm, 2019, 45(9):1459-1467.
[20] 张海艇,齐霞.右旋雷贝拉唑钠对动物体内染色体损伤的影响实验研究[J].药学研究,2014,33(7):384-405.
[21] 苏军,齐霞,张海艇.右旋雷贝拉唑钠对CHL细胞染色体畸变的影响实验研究[J].中国药事, 2015,29(8):865-869.
[22] 贾庆文,英永,马会,等.体外染色体畸变试验染色体标本制备的质量控制[J].中国比较医学杂志. 2018,28(4):108-112.
[23] 刘泳廷,刘佳,高敏,等.贵州鲜铁皮石斛粉小鼠急性经口毒性和骨髓红细胞微核试验研究[J].中国卫生工程学, 2019,18(2):182-184.
[24] 彭双清,郝卫东.药物安全性评价关键计数[M].北京:军事医学科学出版社, 2013:236-237.