4.7 Article

Exploring solid forms of oxytetracycline hydrochloride

Journal

INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 585, Issue -, Pages -

Publisher

ELSEVIER
DOI: 10.1016/j.ijpharm.2020.119496

Keywords

Oxytetracycline hydrochloride; Polymorphism; Solid-state nuclear magnetic resonance; X-ray diffraction; Solubility; Antimicrobial activity

Funding

  1. Consejo Nacional de Investigaciones Cientificas y Tecnicas (CONICET)
  2. Universidad Nacional de Cordoba

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Oxytetracycline hydrochloride, an antibiotic of the tetracycline family, is a polymorphic drug that evidences erratic absorption in oral administration. Additionally, poor solid state characterization of the polymorphs and diversity in the existing nomenclature impede the correct identification of the raw materials. In this work, oxytetracycline hydrochloride solid forms were prepared from isopropyl alcohol, ethanol and methanol through different crystallization techniques, and then their physicochemical and microbiological properties were eval- uated. A combination of advanced techniques such as solid state nuclear magnetic resonance, powder X-ray diffraction, infrared spectroscopy, thermal analysis, scanning electron microscopy and energy -dispersive X-ray spectroscopy were used in the characterization of solid samples giving clear evidence of the existence of three stable and one metastable solid forms of the oxytetracycline hydrochloride. Solubility was determined in aqu- eous solution, simulated gastric fluid, and simulated intestinal fluid. In addition, microbiological studies were performed. The polymorphs showed similar antimicrobial activity against Escherichia coli and Staphylococcus aureus. Therefore, these solid forms of oxytetracycline hydrochloride constitute promising candidates to en- courage studies for repositioning old and known antibiotic drugs in the developing strategies for new therapeutic alternatives.

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