Parameters that determine dissolution and efficacy of itraconazole and its relevance to recalcitrant dermatophytoses.

Parameters that determine dissolution and efficacy of itraconazole and its relevance to recalcitrant dermatophytoses. Expert Rev Clin Pharmacol. 2019 Apr 05;: Authors: Sardana K, Khurana A, Gupta A Abstract INTRODUCTION: Recalcitrant dermatophytoses is on the rise. Though myriad factors may contribute to recalcitrance including terbinafine resistance, itraconazole largely remains sensitive and is increasingly prescribed for dermatophytoses. However, there are increasing instances of patients not responding adequately to itraconazole despite low MICs, probably due to issues plaguing the pelletization process, resulting in suboptimal quality of itraconazole. Data on this topic was searched on pubmed using the search items: itraconazole, MIC, MFC, quality, assay, pharmacokinetics, pharmacodynamics, dermatophytosis and recalcitrance. Areas covered: A detailed analysis of the manufacturing process of itraconazole with emphasis on pelletization and parameters affecting the dissolution and bioavailability is presented. Important formulation factors including drug-polymer ratio, polymer type, coating thickness, bead size and numberare discussed. Also covered is the rationale of dosimetry of itraconazole in tinea infections based on the skin pharmacokinetics and the MIC of the organism. Expert opinion: The process of pelletization has multiple components aiming to achieve maximum dissolution of the drug. Variations in the process, pellet qual...
Source: Expert Review of Clinical Pharmacology - Category: Drugs & Pharmacology Tags: Expert Rev Clin Pharmacol Source Type: research