Efficacy of super bioavailable itraconazole in the management of dermatophytosis in India

Ramesh M., Dinesh Hawelia, Gayatri Bharadwaj, Gautam Dethe, Biswajit Aich, Krishna C. Veligandla, Rahul Rathod, Bhavesh P. Kotak
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Abstract

Itraconazole (ITZ) is a commonly prescribed oral antifungal agent in India and has a low minimum inhibitory concentration when compared to other oral antifungals. However, clinicians have reported inconsistent clinical responses despite its high skin levels, which may be due to variations in pelletization parameters, which affect its bioavailability and serum levels. Conventional ITZ has a maximum bioavailability of 55%; however, this is unpredictable and inconsistent. In contrast, the novel ITZ formulation, super bioavailable ITZ (ITZ-SB), has targeted drug release in the small intestine, resulting in predictable serum levels with minimal interindividual variability. This makes it a potentially useful drug in treating recalcitrant dermatophytosis. This expert opinion highlights the benefits of novel ITZ-SB with the incorporation of SUBA® technology. The SUBA® technology improves the bioavailability of poorly soluble drugs by ‘solid dispersion’ in polymer to increase drug absorbency. This technology also has potential to reduce variability in absorption and adverse effects. Benefits of this technology include more predictable clinical response and lower drug quantities necessary to achieve therapeutic blood levels, making it a promising treatment option for recalcitrant dermatophytosis. Fixtral SB, which uses this technology, is a novel weapon in the arsenal of treatments for superficial mycoses.
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超生物利用度伊曲康唑在印度治疗皮肤癣的疗效
伊曲康唑(Itraconazole, ITZ)是印度常用的口服抗真菌药物,与其他口服抗真菌药物相比,其最低抑菌浓度较低。然而,临床医生报告了不一致的临床反应,尽管其高皮肤水平,这可能是由于颗粒化参数的变化,影响其生物利用度和血清水平。常规ITZ的最大生物利用度为55%;然而,这是不可预测和不一致的。相比之下,新的ITZ制剂,超生物利用度ITZ (ITZ- sb),具有靶向药物在小肠中的释放,导致可预测的血清水平,个体间差异最小。这使它成为治疗顽固性皮肤癣的潜在有用药物。这一专家意见强调了新型ITZ-SB与SUBA®技术结合的好处。SUBA®技术通过“固体分散”在聚合物中提高药物吸收性,提高了难溶性药物的生物利用度。该技术还具有减少吸收变异性和不良反应的潜力。这项技术的好处包括更可预测的临床反应和达到治疗血液水平所需的更少的药物量,使其成为难治性皮肤真菌病的一个有希望的治疗选择。Fixtral SB使用这种技术,是治疗浅表真菌病的新武器。
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