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采用湿法制粒技术制备雷贝拉唑缓释骨架片及其评价

Formulation and evaluation of sustained release matrix tablet of rabeprazole using wet granulation technique.

作者信息

Khan Ruqaiyah, Ashraf Md Shamim, Afzal Muhammad, Kazmi Imran, Jahangir Mohammed Asadullah, Singh Rajbala, Chandra Ramesh, Anwar Firoz

机构信息

Department of Pharmacology, Siddhartha Institute of Pharmacy, Dehradun, Uttarakhand, India.

Ibne Seena Pharmacy College, Azmi Vidya Nagri, Shahabad Dist. Hardoi, UP, India.

出版信息

J Pharm Bioallied Sci. 2014 Jul;6(3):180-4. doi: 10.4103/0975-7406.130961.

Abstract

INTRODUCTION

Rabeprazole, a member of substituted benzimidazoles, inhibits the final step in gastric acid secretions. This drug claims to cause fastest acid separation (due to higher pKa), and more rapidly converts to the active species to aid gastric mucin synthesis. The most significant pharmacological action of Rabeprazole is dose dependent suppression of gastric acid secretion; without anticholinergic or H2-blocking action. It completely abolishes the hydrochloric acid secretion as it is powerful inhibitor of gastric acid. Rabeprazole is acid labile and hence commonly formulated as an enteric coated tablet. The absorption of rabeprazole occurs rapidly as soon as tablet leaves the stomach.

AIM

In the present study an attempt was made to formulate and evaluate Rabeprazole sustained release matrix tablet using wet granulation technique incorporating various polymers like HPMC-E15, Carbopol934, and sodium carboxymethyl cellulose (CMC).

MATERIALS AND METHODS

The Formulated tablets were evaluated for different physicochemical properties like rheological properties, weight variation, thickness, hardness, % friability, in vitro release studies and drug content.

RESULTS

Studies revealed that all the physicochemical parameters comply with the official standards. The in vitro release studies exhibits the release up to 90%, over a prolonged period of time which confirms the extended release profile of formulation, having better bioavailability as well as decreased dosing frequency with reduced doses.

CONCLUSION

The sustained release matrix tablets of rabiprazole shown better bioavailability, efficacy and potency, when compared with official standards.

摘要

引言

雷贝拉唑是取代苯并咪唑类药物的一种,可抑制胃酸分泌的最后一步。该药物据称能实现最快的酸分离(由于较高的pKa值),并能更快地转化为活性形式以促进胃黏液合成。雷贝拉唑最显著的药理作用是剂量依赖性地抑制胃酸分泌;无抗胆碱能或H2阻断作用。由于它是胃酸的强力抑制剂,能完全消除盐酸分泌。雷贝拉唑对酸不稳定,因此通常制成肠溶衣片。雷贝拉唑片剂一旦离开胃部就能迅速被吸收。

目的

在本研究中,尝试采用湿法制粒技术,加入羟丙甲纤维素E15、卡波姆934和羧甲基纤维素钠(CMC)等多种聚合物,来制备和评价雷贝拉唑缓释骨架片。

材料与方法

对制备的片剂进行不同理化性质的评价,如流变学性质、重量差异、厚度、硬度、脆碎度百分比、体外释放研究和药物含量。

结果

研究表明,所有理化参数均符合官方标准。体外释放研究显示,在较长时间内释放率高达90%,这证实了制剂的缓释特性,具有更好的生物利用度,以及减少给药频率和降低剂量。

结论

与官方标准相比,雷贝拉唑缓释骨架片显示出更好的生物利用度、疗效和效能。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fd6/4097931/a058fe4051c2/JPBS-6-180-g002.jpg

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