"DESIGN AND EVALUATION OF BUOYANT ROXATIDINE ACETATE TABLETS FOR ENHANCED GASTRIC RETENTION"

ABSTRACTFloating drug delivery systems (FDDS) present a promising technique for increasing the residency periodof medications in the stomach, hence improving their therapeutic benefits, particularly forpharmaceuticals that are absorbed there. Roxatidine acetate, a histamine H2-receptor antagonist with ashort half-life and site-specific absorption in the stomach, is an excellent option for increasing FDDSbioavailability. The purpose of this study was to develop and evaluate floating tablets of Roxatidineacetate in order to increase gastrointestinal residence frequency and control drug release, hence improvingtherapeutic efficacy. The floating tablets were created utilizing the direct compression method, usingRoxatidine acetate as the active pharmaceutical ingredient (API) and a combination of HPMC K15M,Eduragit L 100, and Carbopol 934 as release-retarding polymers. Nine different formulations (F1-F9)were developed and tested for physical attributes such as hardness, friability, content homogeneity, andfloating ability. All of the formulations demonstrated the ability to float and remain buoyant for at least 12hours. In vitro disintegrating experiments revealed that formulation F2 performed the best, releasing 85%of the medication cumulatively. Kinetic study demonstrated that the improved formulation's releasemechanism followed a zero-order release profile, indicating that the medication was released underregulated conditions. The in vitro drug release profile demonstrated a longer release duration than typicalRoxatidine acetate tablets. The study indicated that FDDS of Roxatidine acetate greatly improves thedrug's therapeutic efficacy by increasing its stomach residence period and allowing for regulated release.This makes it a promising formulation for improving the bioavailability and clinical outcomes ofRoxatidine acetate therapy.

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Publication Details

Journal
Zenodo (CERN European Organization for Nuclear Research)
Published
2025-06-21
DOI
https://doi.org/10.5281/zenodo.15710091
Primary Topic
Drug Solubulity and Delivery Systems
Type
article
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article

"DESIGN AND EVALUATION OF BUOYANT ROXATIDINE ACETATE TABLETS FOR ENHANCED GASTRIC RETENTION"

Zenodo (CERN European Organization for Nuclear Research)
Drug Solubulity and Delivery Systems
article

"DESIGN AND EVALUATION OF BUOYANT ROXATIDINE ACETATE TABLETS FOR ENHANCED GASTRIC RETENTION"

article en

Abstract

ABSTRACTFloating drug delivery systems (FDDS) present a promising technique for increasing the residency periodof medications in the stomach, hence improving their therapeutic benefits, particularly forpharmaceuticals that are absorbed there. Roxatidine acetate, a histamine H2-receptor antagonist with ashort half-life and site-specific absorption in the stomach, is an excellent option for increasing FDDSbioavailability. The purpose of this study was to develop and evaluate floating tablets of Roxatidineacetate in order to increase gastrointestinal residence frequency and control drug release, hence improvingtherapeutic efficacy. The floating tablets were created utilizing the direct compression method, usingRoxatidine acetate as the active pharmaceutical ingredient (API) and a combination of HPMC K15M,Eduragit L 100, and Carbopol 934 as release-retarding polymers. Nine different formulations (F1-F9)were developed and tested for physical attributes such as hardness, friability, content homogeneity, andfloating ability. All of the formulations demonstrated the ability to float and remain buoyant for at least 12hours. In vitro disintegrating experiments revealed that formulation F2 performed the best, releasing 85%of the medication cumulatively. Kinetic study demonstrated that the improved formulation's releasemechanism followed a zero-order release profile, indicating that the medication was released underregulated conditions. The in vitro drug release profile demonstrated a longer release duration than typicalRoxatidine acetate tablets. The study indicated that FDDS of Roxatidine acetate greatly improves thedrug's therapeutic efficacy by increasing its stomach residence period and allowing for regulated release.This makes it a promising formulation for improving the bioavailability and clinical outcomes ofRoxatidine acetate therapy.

Zenodo (CERN European Organization for Nuclear Research)
Atma Jaya Catholic University of Indonesia (ID)
Good health and well-being
Openalex Percentile: Top 59%
Drug Solubulity and Delivery Systems
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