Non-effervescent Polymeric Floating Tablets of Clarithromycin and Pantoprazole: Preparation and In-Vitro Evaluation for Improved Gastric Drug Retention

IF 2.7 4区医学 Q2 PHARMACOLOGY & PHARMACY

Journal of Pharmaceutical Innovation Pub Date : 2025-01-02 DOI:10.1007/s12247-024-09917-8

Fahad Ashraf, Kifayat Ullah Shah, Muhammad Danish Saeed, Faiqa Falak Naz, Fahad Y. Sabei, Tahseen Ahmed, Syed Shafqat Ali Shah, Amir Badshah, Naeem Ur Rehman, Kausar Ali Mahsud

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引用次数: 0

Abstract

Purpose

The study intended to develop and investigate controlled release non-effervescent floating polymeric tablets of Clarithromycin and Pantoprazole to enhance their bioavailability by prolonging the gastrointestinal transit time of drugs, a system for Helicobacter pylori elimination.

Methods

The gastro-retentive tablets were prepared via direct compression method using different concentrations and combinations of hydroxypropyl methylcellulose (HPMC) K4M, Carbopol and guar gum as hydrophilic polymers and Avicel 102 as a filler. The pre-compression solid mixture was characterized for angle of repose and compressibility index, applying Hausner’s ratio to predict the flowability, as well as fourier transform infrared spectroscopy for drug-excipient interaction evaluation. The prepared tablets were investigated for dimension, hardness and friability, weight variation and content uniformity, swelling index, density, buoyancy and in-vitro drug release.

Results

All the formulations exhibited desired floating and flow attributes. Solid-state characterization revealed no chemical interaction between excipients and the drugs. With reference to in-vitro study results, all formulations, except F7, have displayed slow drug release and reduced burst effect (F6). The lowest lag buoyancy of 5 min was achieved in F2. This study develops a non-effervescent floating system for dual drug delivery to enhance gastric residence time, thereby optimizing local therapeutic effects. This innovative approach aims to reduce dosing frequency and associated side effects, improving patient compliance and treatment efficacy for gastric ulcer. This innovative approach can provide effective ulcer healing with shortened treatment time, reduced side effects and improved patient compliance.

Conclusion

This study also highlights the effectiveness of non-effervescent approach to improve dissolution and bioavailability.

Graphical Abstract

Abstract Image

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克拉霉素和泮托拉唑非泡腾聚合物漂浮片的制备及其改善胃药潴留的体外评价

目的研究克拉霉素和泮托拉唑的非泡腾控释聚合物漂浮片剂，通过延长药物的胃肠道传递时间来提高其生物利用度，建立消除幽门螺杆菌的系统。方法以羟丙基甲基纤维素（HPMC） K4M、卡波波尔和瓜尔胶为亲水性聚合物，以Avicel 102为填料，采用直接压缩法制备不同浓度及组合的胃保留片。采用休止角和可压缩性指数对预压缩固体混合物进行表征，利用Hausner比值预测其流动性，利用傅里叶变换红外光谱评价药物与赋形剂的相互作用。考察了所制片剂的尺寸、硬度和脆性、重量变化和含量均匀性、溶胀指数、密度、浮力和体外释放度。结果各配方均表现出良好的漂浮和流动特性。固态表征表明赋形剂与药物之间没有化学相互作用。参考体外研究结果，除F7外，所有制剂均表现出缓释和减少爆裂效应（F6）。最低滞后浮力在F2达到5分钟。本研究开发了一种非泡腾的双重给药漂浮系统，以延长胃停留时间，从而优化局部治疗效果。这种创新方法旨在减少给药频率和相关副作用，提高患者对胃溃疡的依从性和治疗效果。这种创新的方法可以提供有效的溃疡愈合，缩短治疗时间，减少副作用，提高患者的依从性。结论非泡腾法提高溶出度和生物利用度是有效的。图形抽象

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来源期刊

Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-

CiteScore

3.70

自引率

3.80%

发文量

审稿时长

>12 weeks

期刊介绍： The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.