High-Energy Ball Milling as Green Process To Vitrify Tadalafil and Improve Bioavailability
| Autor: | Jean-François willart, Renata Jachowicz, Beata Strach, Anna Krupa, Elżbieta Wyska, Marc Descamps, Florence Danede |
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| Přispěvatelé: | Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Jagiellonian University, Unité Matériaux et Transformations - UMR 8207 (UMET), Institut National de la Recherche Agronomique (INRA)-Ecole Nationale Supérieure de Chimie de Lille (ENSCL)-Université de Lille-Centre National de la Recherche Scientifique (CNRS), Centre National de la Recherche Scientifique (CNRS), Institut National de la Recherche Agronomique (INRA), National Science Centre in Poland [DEC-2012/07/D/NZ7/01673], One-to-One Mentoring Program by Foundation for Polish Science, Institut National de la Recherche Agronomique (INRA)-Ecole Nationale Supérieure de Chimie de Lille (ENSCL)-Institut de Chimie du CNRS (INC)-Université de Lille-Centre National de la Recherche Scientifique (CNRS), Uniwersytet Jagielloński w Krakowie = Jagiellonian University (UJ), Centre National de la Recherche Scientifique (CNRS)-Université de Lille-Ecole Nationale Supérieure de Chimie de Lille (ENSCL)-Institut National de la Recherche Agronomique (INRA) |
| Jazyk: | angličtina |
| Rok vydání: | 2016 |
| Předmět: |
Materials science
[SDV]Life Sciences [q-bio] Analytical chemistry Biological Availability Pharmaceutical Science 02 engineering and technology 030226 pharmacology & pharmacy 03 medical and health sciences 0302 clinical medicine Differential scanning calorimetry X-Ray Diffraction comilling Drug Discovery Ball mill Dissolution solid dispersion Calorimetry Differential Scanning bioavailability improvement dissolution enhancement 021001 nanoscience & nanotechnology vitrification Amorphous solid Bioavailability X-ray crystallography Microscopy Electron Scanning Molecular Medicine 0210 nano-technology Glass transition tadalafil Powder diffraction |
| Zdroj: | Molecular Pharmaceutics Molecular Pharmaceutics, American Chemical Society, 2016, 13 (11), pp.3891-3902. ⟨10.1021/acs.molpharmaceut.6b00688⟩ Molecular Pharmaceutics, 2016, 13 (11), pp.3891-3902. ⟨10.1021/acs.molpharmaceut.6b00688⟩ |
| ISSN: | 1543-8384 1543-8392 |
| DOI: | 10.1021/acs.molpharmaceut.6b00688⟩ |
| Popis: | In this study, the suitability of high-energy ball milling was investigated with the aim to vitrify tadalafil (TD) and improve its bioavailability. To achieve this goal, pure TD as well as binary mixtures composed of the drug and Soluplus (SL) were coprocessed by high-energy ball milling. Modulated differential scanning calorimetry (MDSC) and X-ray powder diffraction (XRD) demonstrated that after such coprocessing, the crystalline form of TD was transformed into an amorphous form. The presence of a single glass transition (T-g) for all the comilled formulations indicated that TD was dispersed into SL at the molecular level, forming amorphous molecular alloys, regardless of the drug concentration. The high values of T-g determined for amorphous formulations, ranging from 70 to 147 degrees C, foreshow their high stability during storage at room temperature, which was verified by XRD and MDSC studies. The stabilizing effect of SL on the amorphous form of TD in comilled formulations was confirmed. Dissolution tests showed immediate drug release with sustained supersaturation in either simulated gastric fluid of pH 1.2 or in phosphate buffer of pH 7.2. The beneficial effect of both amorphization and coamorphization on the bioavailability of TD was found. In comparison to aqueous suspension, the relative bioavailability of TD was only 11% for its crystalline form and 53% for the crystalline physical mixture, whereas the bioavailability of milled amorphous TD and the comilled solid dispersion was 128% and 289%, respectively. Thus, the results provide evidence that not only the presence of polymeric surfactant but also the vitrification of TD is necessary to improve bioavailability. |
| Databáze: | OpenAIRE |
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