Academic Journal
Solubility and Stability Enhanced Oral Formulations for the Anti-Infective Corallopyronin A
| Title: | Solubility and Stability Enhanced Oral Formulations for the Anti-Infective Corallopyronin A |
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| Authors: | Anna K. Krome, Tim Becker, Stefan Kehraus, Andrea Schiefer, Christian Steinebach, Tilman Aden, Stefan J. Frohberger, Álvaro López Mármol, Dnyaneshwar Kapote, Rolf Jansen, Lillibeth Chaverra-Muñoz, Marc P. Hübner, Kenneth Pfarr, Thomas Hesterkamp, Marc Stadler, Michael Gütschow, Gabriele M. König, Achim Hoerauf, Karl G. Wagner |
| Source: | Pharmaceutics, Vol 12, Iss 11, p 1105 (2020) |
| Publisher Information: | MDPI AG, 2020. |
| Publication Year: | 2020 |
| Collection: | LCC:Pharmacy and materia medica |
| Subject Terms: | corallopyronin A (CorA), antibiotic, anthelmintic, povidone (PVP), copovidone (PVP/VA), solubility enhanced formulation, Pharmacy and materia medica, RS1-441 |
| More Details: | Novel-antibiotics are urgently needed to combat an increase in morbidity and mortality due to resistant bacteria. The preclinical candidate corallopyronin A (CorA) is a potent antibiotic against Gram-positive and some Gram-negative pathogens for which a solid oral formulation was needed for further preclinical testing of the active pharmaceutical ingredient (API). The neat API CorA is poorly water-soluble and instable at room temperature, both crucial characteristics to be addressed and overcome for use as an oral antibiotic. Therefore, amorphous solid dispersion (ASD) was chosen as formulation principle. The formulations were prepared by spray-drying, comprising the water-soluble polymers povidone and copovidone. Stability (high-performance liquid chromatography, Fourier-transform-infrared spectroscopy, differential scanning calorimetry), dissolution (biphasic dissolution), and solubility (biphasic dissolution, Pion’s T3 apparatus) properties were analyzed. Pharmacokinetic evaluations after intravenous and oral administration were conducted in BALB/c mice. The results demonstrated that the ASD formulation principle is a suitable stability- and solubility-enhancing oral formulation strategy for the API CorA to be used in preclinical and clinical trials and as a potential market product. |
| Document Type: | article |
| File Description: | electronic resource |
| Language: | English |
| ISSN: | 1999-4923 53658450 |
| Relation: | https://www.mdpi.com/1999-4923/12/11/1105; https://doaj.org/toc/1999-4923 |
| DOI: | 10.3390/pharmaceutics12111105 |
| Access URL: | https://doaj.org/article/e03acd88b74a4c9d8c536584505e42ed |
| Accession Number: | edsdoj.03acd88b74a4c9d8c536584505e42ed |
| Database: | Directory of Open Access Journals |
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| ISSN: | 19994923 53658450 |
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| DOI: | 10.3390/pharmaceutics12111105 |
| Published in: | Pharmaceutics |
| Language: | English |