Formulation and Characterization of Ketoconazole Incorporated in Tablet With Composite Matrix Alginate - Acacia Gum for Enhancing Solubility

Abstract

Background: Ketoconazole is a BCS class II drug with low solubility and high permeability. This study employed a cross-linked hydrogel tablet as a drug delivery approach to enhance ketoconazole solubility. Objective: This study aims to formulate and characterize the physical properties and analysis of the ketoconazole tablet matrix composite. Methods: The manufacture of ketoconazole beads using alginate polymer and gum acacia to increase solubility of ketoconazole. Tablet manufacturing using the direct compression method. Additionally, the characterization includes hardness, friability, disintegration, and weight uniformity, dissolution, solubility, SEM, XRD, and FTIR. Results: The characterization results of ketoconazole tablet beads include FTIR obtained OH group (3400 cm1), COO-(1654 cm1), C-N (1200 cm31), C-Cl (814 cm 1). SEM results show a crystal that is less clear compared to pure ketoconazole, indicating the presence of networking between the polymer and ketoconazole. The XRD result obtained an amorphous shape, indicating great solubility. The results of the physical test obtained hardness test 7.4 Kgf, friability 0.02%, and disintegration 8 minutes, which indicates all physical tests meet the criteria. The analysis obtained from the solubility test was 37 mg of pure ketoconazole, 120 mg of beads, and 130 tablet beads of ketoconazole; this means the tablet beads of ketoconazole have higher solubility. The percentage of dissolution reached 87% at 30 minutes. The kinetics model included the Korsmeyer model because the highest R2 value was 0.299. Conclusion: The results of the solubility test successfully higher solubility at alkaline pH, with significant results with p-value <0.5.