Inclusion Compound of Efavirenz and γ-Cyclodextrin: Solid State Studies and Effect on Solubility
| Autor: | Filipe A. Almeida Paz, Susana S. Braga, Firas El-Saleh, Karyna Lysenko |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Cyclopropanes
Magnetic Resonance Spectroscopy Efavirenz Chemistry Pharmaceutical antiretroviral cyclodextrin inclusion Pharmaceutical Science Article Analytical Chemistry Inclusion compound lcsh:QD241-441 chemistry.chemical_compound X-Ray Diffraction lcsh:Organic chemistry immune system diseases Spectroscopy Fourier Transform Infrared Drug Discovery parasitic diseases Humans Physical and Theoretical Chemistry Solubility Aqueous solution Organic Chemistry virus diseases solid state Benzoxazines Thermogravimetry Freeze Drying chemistry Chemistry (miscellaneous) Alkynes Microscopy Electron Scanning Proton NMR Molecular Medicine solution-phase Powder diffraction Stoichiometry gamma-Cyclodextrins Nuclear chemistry |
| Zdroj: | Molecules Volume 26 Issue 3 Molecules, Vol 26, Iss 519, p 519 (2021) |
| ISSN: | 1420-3049 |
| DOI: | 10.3390/molecules26030519 |
| Popis: | Efavirenz is an antiretroviral drug of widespread use in the management of infections with human immunodeficiency virus type 1 (HIV-1). Efavirenz is also used in paediatrics, but due to its very poor aqueous solubility the liquid formulations available resort to oil-based excipients. In this report we describe the interaction of &gamma cyclodextrin with efavirenz in solution and in the solid state. In aqueous solution, the preferential host&ndash guest stoichiometry was determined by the continuous variation method using 1H NMR, which indicated a 3:2 host-to-guest proportion. Following, the solid inclusion compound was prepared at different stoichiometries by co-dissolution and freeze-drying. Solid-state characterisation of the products using FT-IR, 13C{1H} CP-MAS NMR, thermogravimetry, and X-ray powder diffraction has confirmed that the 3:2 stoichiometry is the adequate starting condition to isolate a solid inclusion compound in the pure form. The effect of &gamma cyclodextrin on the solubility of efavirenz is studied by the isotherm method. |
| Databáze: | OpenAIRE |
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