Toxicological Evaluation of Intravenous Formulation of Rifapentine
Rifapentine belongs to the most potent antituberculosis drugs. Nevertheless, there are some limitations for its clinical use because of the low aqueous solubility and side effects. A technological approach to development of rifapentine intravenous formulation based on human serum albumin was describ...
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| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | Russian |
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LLC "Publishing House OKI"
2020-05-01
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| Series: | Антибиотики и Химиотерапия |
| Subjects: | |
| Online Access: | https://www.antibiotics-chemotherapy.ru/jour/article/view/674 |
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| author | K. P. Ostrovskiy E. R. Pereverzeva I. D. Treshchalin N. S. Osipova M. I. Treshchalin E. V. Voznyakovskaya V. Yu. Balabanyan O. O. Maksimenko S. E. Gelperina |
| author_facet | K. P. Ostrovskiy E. R. Pereverzeva I. D. Treshchalin N. S. Osipova M. I. Treshchalin E. V. Voznyakovskaya V. Yu. Balabanyan O. O. Maksimenko S. E. Gelperina |
| author_sort | K. P. Ostrovskiy |
| collection | DOAJ |
| description | Rifapentine belongs to the most potent antituberculosis drugs. Nevertheless, there are some limitations for its clinical use because of the low aqueous solubility and side effects. A technological approach to development of rifapentine intravenous formulation based on human serum albumin was described earlier and its efficacy against experimental tuberculosis was estimated. Toxicological evaluation of that water-compatible form of rifapentine revealed its low acute toxicity (LD50 340 mg/kg). Chronic toxicity tests of both the oral substance and the injectable formulation of rifapentine demonstrated similar adverse effects. However, in contrast to the conventional oral formulations, the intravenous formulation of rifapentine had no gastrointestinal toxic effects or cardiotoxicity, thus suggesting its usefulness for clinical application. |
| format | Article |
| id | doaj-art-8653fe55e53f4f5db7c05759bdb38e7c |
| institution | Kabale University |
| issn | 0235-2990 |
| language | Russian |
| publishDate | 2020-05-01 |
| publisher | LLC "Publishing House OKI" |
| record_format | Article |
| series | Антибиотики и Химиотерапия |
| spelling | doaj-art-8653fe55e53f4f5db7c05759bdb38e7c2025-08-20T03:42:00ZrusLLC "Publishing House OKI"Антибиотики и Химиотерапия0235-29902020-05-01617-81521673Toxicological Evaluation of Intravenous Formulation of RifapentineK. P. Ostrovskiy0E. R. Pereverzeva1I. D. Treshchalin2N. S. Osipova3M. I. Treshchalin4E. V. Voznyakovskaya5V. Yu. Balabanyan6O. O. Maksimenko7S. E. Gelperina8Drugs Technology LLCG.F.Gause Research Institute of New AntibioticsG.F.Gause Research Institute of New AntibioticsDrugs Technology LLCG.F.Gause Research Institute of New AntibioticsG.F.Gause Research Institute of New AntibioticsDrugs Technology LLCDrugs Technology LLCDrugs Technology LLCRifapentine belongs to the most potent antituberculosis drugs. Nevertheless, there are some limitations for its clinical use because of the low aqueous solubility and side effects. A technological approach to development of rifapentine intravenous formulation based on human serum albumin was described earlier and its efficacy against experimental tuberculosis was estimated. Toxicological evaluation of that water-compatible form of rifapentine revealed its low acute toxicity (LD50 340 mg/kg). Chronic toxicity tests of both the oral substance and the injectable formulation of rifapentine demonstrated similar adverse effects. However, in contrast to the conventional oral formulations, the intravenous formulation of rifapentine had no gastrointestinal toxic effects or cardiotoxicity, thus suggesting its usefulness for clinical application.https://www.antibiotics-chemotherapy.ru/jour/article/view/674poor soluble antibioticstuberculosisrifapentineacute toxicitychronic toxicity |
| spellingShingle | K. P. Ostrovskiy E. R. Pereverzeva I. D. Treshchalin N. S. Osipova M. I. Treshchalin E. V. Voznyakovskaya V. Yu. Balabanyan O. O. Maksimenko S. E. Gelperina Toxicological Evaluation of Intravenous Formulation of Rifapentine Антибиотики и Химиотерапия poor soluble antibiotics tuberculosis rifapentine acute toxicity chronic toxicity |
| title | Toxicological Evaluation of Intravenous Formulation of Rifapentine |
| title_full | Toxicological Evaluation of Intravenous Formulation of Rifapentine |
| title_fullStr | Toxicological Evaluation of Intravenous Formulation of Rifapentine |
| title_full_unstemmed | Toxicological Evaluation of Intravenous Formulation of Rifapentine |
| title_short | Toxicological Evaluation of Intravenous Formulation of Rifapentine |
| title_sort | toxicological evaluation of intravenous formulation of rifapentine |
| topic | poor soluble antibiotics tuberculosis rifapentine acute toxicity chronic toxicity |
| url | https://www.antibiotics-chemotherapy.ru/jour/article/view/674 |
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