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超生物利用度伊曲康唑及其在顽固性皮肤癣菌病中的地位和相关性:重新审视伊曲康唑的皮肤水平和最低抑菌浓度数据。

Super Bioavailable Itraconazole and Its Place and Relevance in Recalcitrant Dermatophytosis: Revisiting Skin Levels of Itraconazole and Minimum Inhibitory Concentration Data.

作者信息

Sardana Kabir, Mathachan Sinu Rose

机构信息

Department of Dermatology, Venereology and Leprosy, Atal Bihari Vajpayee Institute of Medical Sciences and Dr. RML Hospital, New Delhi, India.

出版信息

Indian Dermatol Online J. 2021 Jan 16;12(1):1-5. doi: 10.4103/idoj.IDOJ_618_20. eCollection 2021 Jan-Feb.

Abstract

Itraconazole, is the most commonly prescribed oral antifungal agent in India, and has a low minimum inhibitory concentration as compared to other oral antifungals, and in conjunction with the markedly high skin levels, the drug should have a predictably good clinical response which is not the consistent experience of clinicians. Probably the variation in pelletization parameters might affect the bioavailability of the drug and consequently affect the serum levels. The maximum bioavailability of conventional itraconazole is 55 percent, which is neither consistent nor predictable. However, the novel itraconazole (Super bioavailable Itraconazole) with targeted drug release in the small intestine has predictable serum levels with minimum interindividual variability, which could make it a potentially useful drug in recalcitrant dermatophytosis.

摘要

伊曲康唑是印度最常用的口服抗真菌药,与其他口服抗真菌药相比,其最低抑菌浓度较低,再加上皮肤中的药物水平显著较高,该药理应具有可预见的良好临床反应,但临床医生的实际经验并非如此。颗粒化参数的变化可能会影响药物的生物利用度,进而影响血清水平。传统伊曲康唑的最大生物利用度为55%,既不一致也不可预测。然而,新型伊曲康唑(超生物利用度伊曲康唑)在小肠中靶向释放药物,具有可预测的血清水平,个体间差异最小,这可能使其成为治疗顽固性皮肤癣菌病的潜在有用药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b96/7982045/e728a65b67ea/IDOJ-12-1-g001.jpg

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