2023-04-03 アイルランド・リムリック大学(UL)
この研究は、結晶薬剤の性質を改善するための未開発の結晶工学戦略の可能性について調査し、それによって、ヒトの体内で薬物吸収が改善されることが示されました。
この戦略は、世界中で2.5億人以上に影響を与える熱帯病の治療に使用される薬剤に適用されました。この研究は、子供たちにとって薬をより溶解性が高く飲みやすくすることで重要な影響を持つ可能性があります。
<関連情報>
- https://www.ul.ie/news/university-of-limerick-research-could-make-medicine-more-soluble-and-palatable-for-children
- https://pubs.acs.org/doi/full/10.1021/acs.molpharmaceut.2c00984
プラジクアンテルの共結晶固溶体による高溶解性・速吸収性の実現 Co-Crystalline Solid Solution Affords a High-Soluble and Fast-Absorbing Form of Praziquantel
Chiara Cappuccino, Enrico Spoletti, Fiammetta Renni, Elisabetta Muntoni, Jennifer Keiser, Dario Voinovich, Beatrice Perissutti, and Matteo Lusi
Molecular Pharmaceutics Published:March 8, 2023
DOI:https://doi.org/10.1021/acs.molpharmaceut.2c00984
Abstract
Praziquantel (PZQ) is a chiral class-II drug, and it is used as a racemate for the treatment of schistosomiasis. The knowledge of several cocrystals with dicarboxylic acids has prompted the realization of solid solutions of PZQ with both enantiomers of malic acid and tartaric acid. Here, the solid form landscape of such a six-component system has been investigated. In the process, two new cocrystals were structural-characterized and three non-stoichiometric, mixed crystal forms identified and isolated. Thermal and solubility analysis indicates a fourfold solubility advantage for the newly prepared solid solutions over the pure drug. In addition, a pharmacokinetic study was conducted in rats, which involved innovative mini-capsules for the oral administration of the solid samples. The available data indicate that the faster dissolution rate of the solid solutions translates in faster absorption of the drug and helps maintain a constant steady-state concentration.
