Improving solubility and storage stability of rifaximin via solid-state solvation with Transcutol®
| Autor: | Laura Chelazzi, Paola Maffei, Dario Braga, Oleksii Shemchuk, Annalisa Sforzini, Fabrizia Grepioni, Giuseppe Claudio Viscomi |
|---|---|
| Přispěvatelé: | Grepioni F., Braga D., Chelazzi L., Shemchuk O., Maffei P., Sforzini A., Viscomi G.C. |
| Rok vydání: | 2019 |
| Předmět: |
Thermogravimetric analysis
Materials science 02 engineering and technology 010402 general chemistry 01 natural sciences solid-state law.invention solvate Differential scanning calorimetry law General Materials Science Solubility Crystallization Dissolution crystal form solubility Solvation General Chemistry 021001 nanoscience & nanotechnology Condensed Matter Physics X-ray diffraction 0104 chemical sciences rifaximin Solvent Chemical engineering Anhydrous 0210 nano-technology |
| Zdroj: | CrystEngComm. 21:5278-5283 |
| ISSN: | 1466-8033 |
| DOI: | 10.1039/c9ce00567f |
| Popis: | Crystallization of rifaximin from 2-(2-ethoxyethoxy)ethanol (Transcutol®, DEGME or DEGEE), an inactive ingredient approved by the FDA and a solvent commonly used in the pharmaceutical and cosmetic fields, affords a crystalline form of the API with better solubility properties with respect to the known crystalline hydrates, which are characterized by a very low solubility in water and in buffered solutions. The new form, named rifaximin τ, is an anhydrous solvate, fully characterized by single crystal X-ray diffraction, differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA). Solubility properties were also investigated and compared with known forms of rifaximin. Rifaximin τ combines a high dissolution rate, comparable to that of amorphous rifaximin, with a high storage stability, as in its solid form it is not affected by exposure to humidity. |
| Databáze: | OpenAIRE |
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