Mechanisms underlying changes in indomethacin solubility with local anesthetics and related basic additives
| Autor: | Yohsuke Shimada, Satoru Goto, Ryo Tateuchi, Hitoshi Chatani |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
Nonsteroidal
010304 chemical physics Chemistry Organic Chemistry Intermolecular force 02 engineering and technology biochemical phenomena metabolism and nutrition 021001 nanoscience & nanotechnology 01 natural sciences Analytical Chemistry Bioavailability Inorganic Chemistry chemistry.chemical_compound Differential scanning calorimetry 0103 physical sciences Aqueous solubility Melting point Organic chemistry Solubility 0210 nano-technology Spectroscopy |
| Zdroj: | Journal of Molecular Structure. 1155:165-170 |
| ISSN: | 0022-2860 |
| Popis: | Indomethacin (IND), an acidic nonsteroidal anti-inflammatory drug, and lidocaine (LID), a local anesthetic (LA), form a eutectic complex when mixed, with a lower melting point. The aqueous solubility of the mixture is greater than that of IND or LID alone, improving the bioavailability of IND. Therefore, IND and LID can be used to model changes in efficacy caused by physicochemical interactions between drugs. In this study, the intermolecular interactions between IND and structurally similar LAs were examined by measuring solubility and analyzing thermodynamics using differential scanning calorimetry. The results indicate that the solubility of IND (log S’ IND ) varies with LA hydrophobicity. Reductions in melting point resulting from mixing IND and LAs contributed to changes in IND solubility, attributable to direct intermolecular interactions between IND and the LAs. In addition, binding energy of IND-LA as in water was calculated, and the values were correlating with the solubility of IND in experiments. Understanding these interactions will help address some of the problems encountered in polypharmacy. |
| Databáze: | OpenAIRE |
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