Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Santa Maria. Santa Maria, Rio Grande do Sul, Brasil.
Departamento de Farmácia Industrial, Universidade Federal de Santa Maria. Santa Maria, Rio Grande do Sul, Brasil.
Eur J Pharm Sci. 2020 Jan 15;142:105141. doi: 10.1016/j.ejps.2019.105141. Epub 2019 Nov 6.
Doxycycline hiclate is a broad spectrum antibiotic widely used in human and veterinary medicine. The inability to perform the parenteral administration of drugs and the lack of oral preparations can be mentioned as difficulties in the treatment of animals in the domestic environment. In this scenario, the aim of this study was to investigate the bioavailability of the drug by rectal route, to propose a potential suppository formulation containing 25 mg of doxycycline as an alternative to the available injectable formulations. Hydrophilic and lipophilic suppositories were prepared, in polyethylene glycol (S-PEG) or cocoa butter (S-CBT), respectively. The suppositories were prepared and evaluated concerning visual characteristics, content, average weight, melting range, content uniformity and in vitro release. A stability study was performed and the two most stable formulations were submitted to a pharmacokinetic study in rabbits. The bioavailability of the suppositories was compared to the data of the intravenous (i.v.) formulation. PEG suppository showed 49.13% bioavailability and CBT 51.43% with C equal to 2.06 ± 2.96 µg.mL and 1.54 ± 0.28 µg.mL, respectively. The data obtained suggest that rectal administration may become another method of administration of doxycycline in the treatment of bacterial infections.
盐酸多西环素是一种广谱抗生素，广泛应用于人类和兽医医学。在家庭环境中治疗动物时，无法进行药物的肠外给药和缺乏口服制剂可被视为困难。在这种情况下，本研究的目的是通过直肠途径研究药物的生物利用度，提出一种含有 25mg 多西环素的潜在栓剂制剂，作为现有注射制剂的替代方案。分别用水溶性和脂溶性基质聚乙二醇（S-PEG）和可可脂（S-CBT）制备栓剂。对栓剂进行了外观特征、含量、平均重量、融距、含量均匀度和体外释放度的评价。进行了稳定性研究，并将两种最稳定的制剂提交给兔的药代动力学研究。将栓剂的生物利用度与静脉注射（i.v.）制剂的数据进行了比较。PEG 栓剂的生物利用度为 49.13%，CBT 为 51.43%，C 分别为 2.06±2.96μg.mL 和 1.54±0.28μg.mL。所得数据表明，直肠给药可能成为治疗细菌感染时多西环素的另一种给药方法。
