Formulation Variables Influencing the Development of Ketoconazole Gastroretentive Drug Delivery System

Moamin Fattah Al Hablawi; Iman Sabah Jaffar

doi:10.54133/ajms.v7i1(Special).867

Authors

Moamin Fattah Al Hablawi Department of Pharmaceutics, College of Pharmacy, Mustansiriyah University, Baghdad, Iraq. https://orcid.org/0000-0002-2652-0229
Iman Sabah Jaffar Department of Pharmaceutics, College of Pharmacy, Mustansiriyah University, Baghdad

DOI:

https://doi.org/10.54133/ajms.v7i1(Special).867

Keywords:

Drug delivery, Gasteroretaintive, Mucoadhesive, Residence time

Abstract

Background: Ketoconazole (KZ) is categorized as class II according to the Biopharmaceutics Classification System (BSC) classification, which shows a strong pH-dependent solubility where its solubility is enhanced under an acidic medium (pH below 3). This strong pH dependence results in unpredictable absorption and a wide range of bioavailabilities. Objective: To prolong the gastric residence time of KZ’s tablet to enhance KZ’s solubility and hence its bioavailability for better therapeutic activity. Methods: To prepare mucoadhesive tablets, we use both direct and wet granulation methods. We employed various evaluation tests to assess the prepared tablets. These tests encompass a range of assessments, including weight variation, hardness, thickness, friability, disintegration test, swelling study, mucoadhesive strength study, and in vitro drug release studies. Results: The study found that polymer viscosity, as well as polymer concentration, have a significant effect on mucoadhesive strength and drug release, whereas diluent type has a non-significant influence on drug release. We selected Formula 7, which employs xanthan gum as a mucoadhesive polymer in a 1:1 drug polymer ratio, as the optimum formula because it provides an accepted physico-mechanical property and releases 87% of the drug over 8 hours. Conclusions: Gastric mucoadhesive tablets may be an effective method of delivering active ingredients, as they provide a favorable environment that enhances their dissolution by extending their duration in the stomach, thereby increasing their bioavailability.

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