Lukášová Ivana, Muselík Jan, Vetchý David, Gajdziok Jan, Gajdošová Markéta, Juřica Jan, Knotek Zdeněk, Hauptman Karel, Jekl Vladimír
Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackého tř. 1946/1, 612 42 Brno, Czech Republic.
Curr Drug Deliv. 2017;14(1):99-108. doi: 10.2174/1567201813666160502142856.
Prevalence of oral mucosal fungal infections increases with the frequent administration of antibiotics, corticosteroids and immunosuppressive drugs. Therapeutically used antifungals are usually associated with a variety of drug interactions. Furthermore, there has been a noticeable increase in microorganisms resistant to these preparations. Mucoadhesive buccal films represent a modern therapeutic system for the treatment of oral mucosal fungal infection paired with a high degree of patient compliance. Ciclopirox olamine applied directly onto the oral mucosa offers an attractive alternative to treatment with systemic antifungals thanks to its low incidence of resistance and side effects.
The aim of this work was to evaluate the pharmacokinetic parameters of ciclopirox olamine after the buccal application of mucoadhesive film prepared by the solvent casting method.
A chromatographic method using an internal standard was developed and validated for evaluation of ciclopirox olamine plasma concentrations. Method accuracy was 88.5-104.6% and 89.5-99.7% for interday and intraday assays, respectively.
The pharmacokinetic properties of ciclopirox olamine were studied in New Zealand White rabbits. The mucoadhesive films containing ciclopirox olamine in a total dose of 34.4 (33.0; 35.9) mg kg-1 were applied to all the rabbits. Plasma ciclopirox olamine concentrations were determined during the 12 h following application. The time taken to reach maximum plasma concentration was 1.7 (1.1; 2.2) h after the drug administration with cmax 5.73 (4.18; 7.28) μg mL-1. Overall elimination half-life was 3.8 (1.9; 10.8) h.
The experiment suggests that oral mucoadhesive film may be a valuable alternative ciclopirox olamine administration.
随着抗生素、皮质类固醇和免疫抑制药物的频繁使用，口腔黏膜真菌感染的患病率有所增加。治疗用抗真菌药通常会引发多种药物相互作用。此外，对这些制剂耐药的微生物数量显著增加。黏膜黏附性口腔膜是一种现代治疗系统，用于治疗口腔黏膜真菌感染，患者依从性高。直接应用于口腔黏膜的环吡酮胺因其耐药性和副作用发生率低，为全身用抗真菌药治疗提供了一种有吸引力的替代方案。
本研究旨在评估溶剂浇铸法制备的黏膜黏附膜口腔给药后环吡酮胺的药代动力学参数。
建立并验证了一种使用内标物的色谱方法，用于评估环吡酮胺的血浆浓度。日间和日内测定的方法准确度分别为88.5 - 104.6%和89.5 - 99.7%。
在新西兰白兔身上研究了环吡酮胺的药代动力学特性。将总剂量为34.4（33.0；35.9）mg kg-1的含环吡酮胺的黏膜黏附膜应用于所有兔子。给药后12小时内测定血浆中环吡酮胺的浓度。给药后达到最大血浆浓度的时间为1.7（1.1；2.2）小时，cmax为5.73（4.18；7.28）μg mL-1。总体消除半衰期为3.8（1.9；10.8）小时。
该实验表明口腔黏膜黏附膜可能是环吡酮胺给药的一种有价值的替代方式。
