Itraconazole is the first drug of choice for the treatment of sporotrichosis and it is available at different concentrations for veterinary patients. However, therapeutic failure has been reported, limiting clinical treatment. This study evaluated the in vitro efficacy of brand-name and compounded itraconazole formulations against Sporothrix brasiliensis and estimated the itraconazole content in each tested formulation. Oral capsules were acquired from two brand-name products for human (H-IND) and veterinary (V-IND) uses, and three from compounding pharmacies in Pelotas, RS, for human (H-COMP1/H-COMP2) and veterinary (V-COMP) uses. Capsule purity was analyzed by liquid chromatography-electrospray ionization quadrupole time-of-flight mass spectrometry (LC-ESI-QTOF-MS). Antifungal activity was determined against 29 Sporothrix brasiliensis by the M38-A2 guideline of CLSI. H-IND/H-COMP1/H-COMP2 had high efficacy against S. brasiliensis (approximately 70% of total isolated susceptible), V-COMP showed moderate efficacy (51.7%), and V-IND was the least effective formulation (37.9%). Thirty-four percent of the total isolates were resistant to all formulations. Furthermore, itraconazole content did not match the concentration indicated by the manufacturers, ranging from 387.70 to 7.81 μg/mg (H-COMP2 > V-COMP > H-IND > H-COMP1 > V-IND). Therefore, it is possible that the formulations showed different in vitro efficacy due to the difference in their itraconazole contents. Given the emergence of antifungal resistance for all formulations, the choice product to be used must follow susceptibility testing. Stringent quality control measures are recommended for product manufactures to assure drug content uniformity.

中文翻译：

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巴西孢子丝菌对品牌和复合伊曲康唑制剂的敏感性和抗性

伊曲康唑是治疗孢子丝菌病的首选药物，可用于兽医患者的不同浓度。然而，已经报道了治疗失败，限制了临床治疗。本研究评估了品牌和复方伊曲康唑制剂对巴西孢子丝菌的体外功效，并估计了每个测试制剂中的伊曲康唑含量。口服胶囊来自两种用于人类 (H-IND) 和兽用 (V-IND) 的品牌产品，以及三种来自 RS Pelotas 的复合药房，用于人类 (H-COMP1/H-COMP2) 和兽用 (H-COMP1/H-COMP2) V-COMP) 使用。通过液相色谱-电喷雾电离四极杆飞行时间质谱 (LC-ESI-QTOF-MS) 分析胶囊纯度。根据 CLSI 的 M38-A2 指南确定了对 29 巴西孢子丝菌的抗真菌活性。H-IND/H-COMP1/H-COMP2 对 S. brasiliensis 有很高的疗效（约占总分离出的敏感菌的 70%），V-COMP 表现出中等疗效（51.7%），V-IND 是最不有效的制剂（37.9 %）。34% 的总分离株对所有制剂都具有抗性。此外，伊曲康唑含量与制造商指示的浓度不符，范围为​​ 387.70 至 7.81 μg/mg（H-COMP2 > V-COMP > H-IND > H-COMP1 > V-IND）。因此，由于伊曲康唑含量的差异，这些制剂可能表现出不同的体外功效。鉴于所有配方都出现了抗真菌性，选择使用的产品必须遵循敏感性测试。