Effect of Surfactant-Bile Interactions on the Solubility of Hydrophobic Drugs in Biorelevant Dissolution Media
| Autor: | Slavka Tcholakova, Zahari Vinarov, Nikolai D. Denkov, Nikola Burdzhiev, Vladimir Katev |
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| Rok vydání: | 2018 |
| Předmět: |
Drug
Swine media_common.quotation_subject Chemistry Pharmaceutical Proton Magnetic Resonance Spectroscopy Pharmaceutical Science Salt (chemistry) Administration Oral 02 engineering and technology Absorption (skin) 030226 pharmacology & pharmacy Micelle 03 medical and health sciences chemistry.chemical_compound Surface-Active Agents 0302 clinical medicine Pulmonary surfactant Fenofibrate Drug Discovery Animals Solubility Dissolution Micelles Progesterone media_common chemistry.chemical_classification Polysorbate Taurodeoxycholic Acid Chromatography Danazol Water 021001 nanoscience & nanotechnology Drug Liberation chemistry Intestinal Absorption Molecular Medicine 0210 nano-technology Hydrophobic and Hydrophilic Interactions |
| Zdroj: | Molecular pharmaceutics. 15(12) |
| ISSN: | 1543-8392 |
| Popis: | Biorelevant dissolution media (BDM) methods are commonly employed to investigate the oral absorption of poorly water-soluble drugs. Despite the significant progress in this area, the effect of commonly employed pharmaceutical excipients, such as surfactants, on the solubility of drugs in BDM has not been characterized in detail. The aim of this study is to clarify the impact of surfactant–bile interactions on drug solubility by using a set of 12 surfactants, 3 model hydrophobic drugs (fenofibrate, danazol, and progesterone) and two types of BDM (porcine bile extract and sodium taurodeoxycholate). Drug precipitation and sharp nonlinear decrease in the solubility of all studied drugs is observed when drug-loaded ionic surfactant micelles are introduced in solutions of both BDM, whereas the drugs remain solubilized in the mixtures of nonionic polysorbate surfactants + BDM. One-dimensional and diffusion-ordered 1H NMR spectroscopy show that mixed bile salt + surfactant micelles with low drug solubilization ca... |
| Databáze: | OpenAIRE |
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