ENHANCING SOLUBILITY AND DEVELOPING AN ITRACONAZOLE-BETA-CYCLODEXTRIN COMPLEX FOR ANTIFUNGAL THERAPY IN ORALLY DISINTEGRATING TABLETS

Q4 Pharmacology, Toxicology and Pharmaceutics Ankara Universitesi Eczacilik Fakultesi Dergisi Pub Date : 2024-07-01 DOI:10.33483/jfpau.1465360

T. Çomoğlu

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Abstract

Objective: This study aimed to create an orally disintegrating tablet (ODT) formulation using an itraconazole (ITZ)-beta-cyclodextrin (β-CD) complex to enhance itraconazole's solubility, a drug with limited solubility. β-CD was chosen for its compatibility with ITZ. Material and Method: The study prepared equimolar mixtures of ITZ and β-CD through kneading, assessing their solubility and dissolution rates. The inclusion complexes significantly increased ITZ's solubility. This complex was used to develop directly compressed ODTs with a lower ITZ content (25 mg), incorporating D-Mannitol as a bulking agent, sweetener, and to enhance mouthfeel, facilitating rapid disintegration and drug release. Result and Discussion: ODT formulations containing the ITZ-β-CD complex showed a significantly higher dissolution rate of ITZ compared to formulations with pure ITZ. This enhancement in dissolution is expected to significantly improve ITZ's bioavailability, suggesting a potential for reducing ITZ dosage and minimizing adverse effects.

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提高伊曲康唑-β-环糊精复合物的溶解度并开发用于抗真菌治疗的口腔崩解片

研究目的本研究旨在使用伊曲康唑（ITZ）-β-环糊精（β-CD）复合物制成一种口腔崩解片（ODT）制剂，以提高伊曲康唑这种溶解度有限的药物的溶解度。选择 β-CD 是因为它与 ITZ 具有相容性：研究通过捏合法制备了 ITZ 和 β-CD 的等摩尔混合物，评估了它们的溶解度和溶解速率。包合复合物大大提高了 ITZ 的溶解度。这种复合物被用于开发 ITZ 含量较低（25 毫克）的直接压片 ODT，同时加入 D-甘露糖醇作为膨松剂、甜味剂，并增强口感，促进快速崩解和药物释放：与含有纯 ITZ 的制剂相比，含有 ITZ-β-CD 复合物的 ODT 制剂显示 ITZ 的溶出率明显更高。这种溶解度的提高有望显著改善 ITZ 的生物利用度，从而有可能减少 ITZ 的用量并将不良反应降至最低。

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来源期刊

Ankara Universitesi Eczacilik Fakultesi Dergisi Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science

CiteScore

0.80

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