Development of doxycycline hyclate suppositories and pharmacokinetic study in rabbits
Autor: | Andréa Inês Horn Adams, Rebeca Lino Lourenço, Pauline Trindade Biscaino, Ana Paula Guarnieri Christ, Alieni Bitencourt de Souza, Estevan Sonego Zimmermann |
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Rok vydání: | 2019 |
Předmět: |
Male
Chemistry Pharmaceutical Cmax Pharmaceutical Science Biological Availability 02 engineering and technology Polyethylene glycol Suppository Pharmacology 030226 pharmacology & pharmacy Doxycycline Hyclate Polyethylene Glycols 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Pharmacokinetics Administration Rectal medicine Animals Doxycycline business.industry Bacterial Infections 021001 nanoscience & nanotechnology Bioavailability Anti-Bacterial Agents chemistry Rectal administration Rabbits 0210 nano-technology business medicine.drug |
Zdroj: | European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 142 |
ISSN: | 1879-0720 |
Popis: | 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 Cmax 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. |
Databáze: | OpenAIRE |
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