Polymeric Matrix Mini-Tablets Based on Eudragit® S 100 and HPMC for Controlled Release of Pantoprazole

<b>Background:</b> Pantoprazole is a widely used proton pump inhibitor that is highly unstable under acidic conditions. This limits the performance of conventional formulations and typically requires enteric-coated dosage forms or alternative modified-release approaches. This study reports the development of polymeric matrix mini-tablets designed to protect pantoprazole during gastric exposure and to enable pH-dependent release under intestinal conditions. The formulations combine Eudragit<sup>®</sup> S 100, a pH-dependent polymer, with HPMC, a hydrophilic matrix former that modulates drug release through hydration and swelling. <b>Methods:</b> Matrix mini-tablets were prepared by blending pantoprazole with selected excipients at optimised proportions and compressing the blends by direct compression using an eccentric tablet press. Powder blends and mini-tablets were characterised according to pharmacopoeial specifications. Analytical techniques-including High-Performance Liquid Chromatography (HPLC), Differential Scanning Calorimetry (DSC), Fourier-Transform Infrared Absorption Spectroscopy (FT-IR), Powder X-Ray Diffraction (PXRD), and Scanning Electron Microscopy (SEM)-were employed to evaluate drug content uniformity, thermal behaviour, and potential drug-excipient interactions. In vitro dissolution studies were performed under sequential pH conditions, and the release kinetics were analysed using mathematical models. <b>Results:</b> Dissolution testing identified formulations F2 and F6 as providing the most suitable gastro-resistant performance in the acidic stage, together with sustained release up to 24 h. Kinetic modelling supported formulation-dependent release mechanisms, and multivariate analysis (PCA) highlighted relationships between physico-mechanical attributes and drug-release behaviour. <b>Conclusions:</b> The proposed matrix system shows potential as a robust, coating-free platform for the modified delivery of acid-labile drugs using direct compression, simplifying manufacturing. These findings support the rational design of oral modified-release formulations based on polymeric matrices.

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Publication Details

Journal
Pharmaceutics
Published
2026-03-05
DOI
https://doi.org/10.3390/pharmaceutics18030327
Primary Topic
Drug Solubulity and Delivery Systems
Type
article
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article

Polymeric Matrix Mini-Tablets Based on Eudragit® S 100 and HPMC for Controlled Release of Pantoprazole

Carlos Torrado‐Salmerón, Víctor Guarnizo-Herrero, Borja Martínez-Alonso, Hugo Pardo et al.
Pharmaceutics
Drug Solubulity and Delivery Systems
article

Polymeric Matrix Mini-Tablets Based on Eudragit® S 100 and HPMC for Controlled Release of Pantoprazole

Carlos Torrado‐Salmerón, Víctor Guarnizo-Herrero, Borja Martínez-Alonso, Hugo Pardo, M. Ángeles Peña
article en

Abstract

<b>Background:</b> Pantoprazole is a widely used proton pump inhibitor that is highly unstable under acidic conditions. This limits the performance of conventional formulations and typically requires enteric-coated dosage forms or alternative modified-release approaches. This study reports the development of polymeric matrix mini-tablets designed to protect pantoprazole during gastric exposure and to enable pH-dependent release under intestinal conditions. The formulations combine Eudragit<sup>®</sup> S 100, a pH-dependent polymer, with HPMC, a hydrophilic matrix former that modulates drug release through hydration and swelling. <b>Methods:</b> Matrix mini-tablets were prepared by blending pantoprazole with selected excipients at optimised proportions and compressing the blends by direct compression using an eccentric tablet press. Powder blends and mini-tablets were characterised according to pharmacopoeial specifications. Analytical techniques-including High-Performance Liquid Chromatography (HPLC), Differential Scanning Calorimetry (DSC), Fourier-Transform Infrared Absorption Spectroscopy (FT-IR), Powder X-Ray Diffraction (PXRD), and Scanning Electron Microscopy (SEM)-were employed to evaluate drug content uniformity, thermal behaviour, and potential drug-excipient interactions. In vitro dissolution studies were performed under sequential pH conditions, and the release kinetics were analysed using mathematical models. <b>Results:</b> Dissolution testing identified formulations F2 and F6 as providing the most suitable gastro-resistant performance in the acidic stage, together with sustained release up to 24 h. Kinetic modelling supported formulation-dependent release mechanisms, and multivariate analysis (PCA) highlighted relationships between physico-mechanical attributes and drug-release behaviour. <b>Conclusions:</b> The proposed matrix system shows potential as a robust, coating-free platform for the modified delivery of acid-labile drugs using direct compression, simplifying manufacturing. These findings support the rational design of oral modified-release formulations based on polymeric matrices.

PharmaceuticsVol. 18(3)
Universidad Complutense de Madrid (ES), Universidad de Alcalá (ES)
Openalex Percentile: Top 33%
Drug Solubulity and Delivery Systems
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