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泮托拉唑肠溶片的研制:制剂的制备、体外和体内评价。

Sustained release enteric coated tablets of pantoprazole: formulation, in vitro and in vivo evaluation.

机构信息

Department of Pharmaceutics Dayananda Sagar College of Pharmacy Kumaraswamy Layout, Bangalore, India.

出版信息

Acta Pharm. 2013 Mar;63(1):131-40. doi: 10.2478/acph-2013-0002.

Abstract

In this study, an attempt was made to deliver pantoprazole in a sustained manner using delayed release tablets. The tablets were prepared by the wet granulation method using HPMC, cassava starch and polyvinyl pyrrolidine as polymers, Avicel PH 102 (MCC) as filler and potato starch as binder. The prepared tablets were evaluated for hardness, mass variation, friability and drug content uniformity, and the results were found to comply with official standards. The prepared tablets were coated using an enteric coating polymer such as cellulose acetate phthalate, Eudragit L100 and drug coat L100 by the dip coating method. The in vitro release was studied using pH 1.2 acidic buffer and pH 6.8 phosphate buffer and the study revealed that the prepared tablets were able to sustain drug release into the intestine. The anti-ulcer activity was evaluated by a water immersion stress induced ulcer model. The enteric coated pantoprazole tablets significantly reduced ulcer formation.

摘要

在这项研究中,尝试使用延迟释放片以持续的方式递送泮托拉唑。这些片剂是通过湿法制粒法制备的,使用 HPMC、木薯淀粉和聚乙烯吡咯烷酮作为聚合物,微晶纤维素(MCC)作为填充剂,马铃薯淀粉作为粘合剂。对制备的片剂进行了硬度、质量变化、脆碎度和药物含量均匀度的评估,结果符合官方标准。通过浸渍涂层法,使用醋酸纤维素酞酸酯、Eudragit L100 和药物涂层 L100 等肠溶聚合物对制备的片剂进行包衣。通过 pH 1.2 酸性缓冲液和 pH 6.8 磷酸盐缓冲液研究了体外释放,研究表明,制备的片剂能够将药物持续释放到肠道中。通过水浸应激诱导溃疡模型评估了抗溃疡活性。肠溶包衣泮托拉唑片剂显著减少了溃疡形成。

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