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开发一种测定克霉唑和伊曲康唑含量的方法，并研究其在一种新型治疗孢子丝菌病微乳剂中的稳定性。

Development of a Method for the Quantification of Clotrimazole and Itraconazole and Study of Their Stability in a New Microemulsion for the Treatment of Sporotrichosis.

机构信息

Departamento de Tecnologia Farmacêutica, Faculdade de Farmácia, Universidade Federal Fluminense, Niterói-RJ 24241-000, Brazil.

Departamento de Química Orgânica, Instituto de Química, Universidade Federal Fluminense, Niterói-RJ 24210-141, Brazil.

出版信息

Molecules. 2019 Jun 25;24(12):2333. doi: 10.3390/molecules24122333.

DOI:10.3390/molecules24122333
PMID:31242573
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6630458/
Abstract

Sporotrichosis occurs worldwide and is caused by the fungus . This agent has a high zoonotic potential and is transmitted mainly by bites and scratches from infected felines. A new association between the drugs clotrimazole and itraconazole is shown to be effective against yeasts. This association was formulated as a microemulsion containing benzyl alcohol as oil, Tween 60 and propylene glycol as surfactant and cosurfactant, respectively, and water. Initially, the compatibility between clotrimazole and itraconazole was studied using differential scanning calorimetry (DSC), thermogravimetric analysis (TG), Fourier transform infrared spectroscopy (FTIR), and X-ray powder diffraction (PXRD). Additionally, a simple and efficient analytical HPLC method was developed to simultaneously determine the concentration of clotrimazole and itraconazole in the novel microemulsion. The developed method proved to be efficient, robust, and reproducible for both components of the microemulsion. We also performed an accelerated stability study of this formulation, and the developed analytical method was applied to monitor the content of active ingredients. Interestingly, these investigations led to the detection of a known clotrimazole degradation product whose structure was confirmed using NMR and HRMS, as well as a possible interaction between itraconazole and benzyl alcohol.

摘要

孢子丝菌病分布于世界各地，由真菌引起。这种病原体具有很强的人畜共患潜力，主要通过感染猫科动物的咬伤和抓伤传播。研究表明，克霉唑和伊曲康唑这两种药物的联合具有抗酵母菌的作用。该联合药物被制成含有苯甲醇作为油相、吐温 60 和丙二醇分别作为表面活性剂和助表面活性剂以及水的微乳液。首先，使用差示扫描量热法（DSC）、热重分析（TG）、傅里叶变换红外光谱（FTIR）和 X 射线粉末衍射（PXRD）研究了克霉唑和伊曲康唑之间的相容性。此外，还开发了一种简单高效的 HPLC 分析方法，用于同时测定新型微乳液中克霉唑和伊曲康唑的浓度。该方法对微乳液的两种成分均有效、稳健且重现性良好。我们还对该制剂进行了加速稳定性研究，并应用所开发的分析方法来监测活性成分的含量。有趣的是，这些研究发现了一种已知的克霉唑降解产物，其结构通过 NMR 和高分辨质谱（HRMS）得到了确认，以及伊曲康唑与苯甲醇之间可能存在相互作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/18c02c2a47ef/molecules-24-02333-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/220f26f9d9a6/molecules-24-02333-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/8271a0d0b202/molecules-24-02333-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/461237a41e30/molecules-24-02333-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/14e9e5a243c0/molecules-24-02333-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/7768eb55770c/molecules-24-02333-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/b8493245d59b/molecules-24-02333-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/a3675f968619/molecules-24-02333-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/dc76a2f4cf9b/molecules-24-02333-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/72f7f0351ad3/molecules-24-02333-g009a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/c8aa9218f002/molecules-24-02333-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/18c02c2a47ef/molecules-24-02333-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/220f26f9d9a6/molecules-24-02333-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/8271a0d0b202/molecules-24-02333-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/461237a41e30/molecules-24-02333-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/14e9e5a243c0/molecules-24-02333-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/7768eb55770c/molecules-24-02333-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/b8493245d59b/molecules-24-02333-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/a3675f968619/molecules-24-02333-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/dc76a2f4cf9b/molecules-24-02333-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/72f7f0351ad3/molecules-24-02333-g009a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/c8aa9218f002/molecules-24-02333-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0990/6630458/18c02c2a47ef/molecules-24-02333-g011.jpg

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