Development of doxycycline hyclate suppositories and pharmacokinetic study in rabbits.

Autor: Christ AP; Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Santa Maria. Santa Maria, Rio Grande do Sul, Brasil., Biscaino PT; Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Santa Maria. Santa Maria, Rio Grande do Sul, Brasil., Lourenço RL; Departamento de Farmácia Industrial, Universidade Federal de Santa Maria. Santa Maria, Rio Grande do Sul, Brasil., de Souza AB; Departamento de Farmácia Industrial, Universidade Federal de Santa Maria. Santa Maria, Rio Grande do Sul, Brasil., Zimmermann ES; Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Santa Maria. Santa Maria, Rio Grande do Sul, Brasil., Adams AIH; 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. Electronic address: andrea.ih.adams@gmail.com.
Jazyk: angličtina
Zdroj: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences [Eur J Pharm Sci] 2020 Jan 15; Vol. 142, pp. 105141. Date of Electronic Publication: 2019 Nov 06.
DOI: 10.1016/j.ejps.2019.105141
Abstrakt: 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 max equal to 2.06 ± 2.96 µg.mL -1 and 1.54 ± 0.28 µg.mL -1 , respectively. The data obtained suggest that rectal administration may become another method of administration of doxycycline in the treatment of bacterial infections.
(Copyright © 2019 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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