Itraconazole is a drug used in veterinary medicine for the treatment of different varieties of dermatophytosis at doses between 3–5 mg/kg/day in cats. Nevertheless, in Spain, it is only available in the market as a 52 mL suspension at 10 mg/mL. The lack of alternative formulations, which provide sufficient formulation to cover the treatment of large animals or allow the treatment of a group of them, can be overcome with compounding. For this purpose, it has to be considered that itraconazole is a weak base, class II compound, according to the Biopharmaceutics Classification System, that can precipitate when reaching the duodenum. The aim of this work is to develop alternative oral formulations of itraconazole for the treatment of dermatophytosis. Several oral compounds of itraconazole were prepared and compared, in terms of dissolution rate, permeability, and stability, in order to provide alternatives to the medicine commercialized. The most promising formulation contained hydroxypropyl methylcellulose and β-cyclodextrin. This combination of excipients was capable of dissolving the same concentration as the reference product and delaying the precipitation of itraconazole upon leaving the stomach. Moreover, the intestinal permeability of itraconazole was increased more than two-fold.

中文翻译：

---

兽医药物配制：伊曲康唑混悬液

伊曲康唑是一种兽医药物，用于治疗猫的各种皮肤癣菌病，剂量为 3-5 毫克/公斤/天。然而，在西班牙，它仅以 10 mg/mL 的 52 mL 悬浮液形式在市场上出售。替代制剂的缺乏可以通过复配来克服，替代制剂可以提供足够的制剂来治疗大型动物或允许治疗一组动物。为此，必须考虑到，根据生物药剂学分类系统，伊曲康唑是一种弱碱 II 类化合物，在到达十二指肠时会沉淀。这项工作的目的是开发伊曲康唑的替代口服制剂来治疗皮肤癣菌病。制备了几种伊曲康唑口服化合物，并在溶出度、渗透性和稳定性方面进行了比较，以期提供商品化药物的替代品。最有前途的配方含有羟丙基甲基纤维素和β-环糊精。这种赋形剂组合能够以与参比产品相同的浓度溶解，并延迟伊曲康唑离开胃后的沉淀。此外，伊曲康唑的肠道通透性增加了两倍以上。