Efficacy of an Intravenous Form of Rifapentine in a Model of Experimental Tuberculosis in Mice
| Autor: | I. D. Treshchalin, E. V. Shipulo, Olga Maksimenko, V. D. Potapov, Svetlana Gelperina, K. P. Ostrovskii, Nadezhda Osipova, E. R. Pereverzeva, L. V. Vanchugova |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Pharmacology Chromatography Tuberculosis biology medicine.drug_class Chemistry 030106 microbiology Antibiotics biology.organism_classification medicine.disease Human serum albumin Rifapentine Mycobacterium tuberculosis 03 medical and health sciences Colloid Drug Discovery medicine Particle size Pathogen medicine.drug |
| Zdroj: | Pharmaceutical Chemistry Journal. 51:616-621 |
| ISSN: | 1573-9031 0091-150X |
| DOI: | 10.1007/s11094-017-1663-7 |
| Popis: | Solubilization of rifapentine with human serum albumin (HSA) was used to produce a water-miscible form consisting of a colloidal suspension of particles of size 538 ± 9 nm. Dilution of the suspension more than 20-fold led to dissociation of the aggregates formed during solubilization procedure, producing a transparent solution. This was associated with a reduction in particle size to 10 – 20 nm, corresponding to the particle size in HSA solution at the same concentration. A fluorescence method showed that suspensions contained both free rifapentine and its complex with HSA. Studies of the activity against the pathogen of tuberculosis, Mycobacterium tuberculosis H37Rv, in a model of acute infection in Balb/c mice showed that the water-miscible form of rifapentine given intravenously had high activity against mycobacteria, comparable with the activity of rifapentine substance, decreasing mycobacterial loadings in the parenchymatous organs from 106 – 107 to 102 – 103 cfu/organ. Thus, use of HSA as solubilizer yielded an intravenous form of rifapentine retaining the activity of the antibiotic against Mycobacterium tuberculosis. |
| Databáze: | OpenAIRE |
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