期刊
PHARMACEUTICALS
卷 14, 期 6, 页码 -出版社
MDPI
DOI: 10.3390/ph14060555
关键词
ketoprofen-l-lysine salt; cocrystal; salt; polymorphism; faster-release formulation
资金
- Italian Ministry of Education, University and Research, Research Project AMICO [ARS01_00758]
The study delved into the solid-state characteristics of KLS and identified a new salt/cocrystal polymorphism, with the salt form showing significantly higher absorption and intrinsic dissolution rate, a more bitter taste, and different sensorial kinetics compared to the cocrystal. This discovery may pave the way for the development of a new KET-LYS polymorph drug with enhanced properties for the treatment of acute inflammatory and painful conditions.
Ketoprofen-l-lysine salt (KLS) is a widely used nonsteroidal anti-inflammatory drug. Here, we studied deeply the solid-state characteristics of KLS to possibly identify new polymorphic drugs. Conducting a polymorph screening study and combining conventional techniques with solid-state nuclear magnetic resonance, we identified, for the first time, a salt/cocrystal polymorphism of the ketoprofen (KET)-lysine (LYS) system, with the cocrystal, KET-LYS polymorph 1 (P1), being representative of commercial KLS, and the salt, KET-LYS polymorph 2 (P2), being a new polymorphic form of KLS. Interestingly, in vivo pharmacokinetics showed that the salt polymorph has significantly higher absorption and, thus, different pharmacokinetics compared to commercial KLS (cocrystal), laying the basis for the development of faster-release/acting KLS formulations. Moreover, intrinsic dissolution rate (IDR) and electronic tongue analyses showed that the salt has a higher IDR, a more bitter taste, and a different sensorial kinetics compared to the cocrystal, suggesting that different coating/flavoring processes should be envisioned for the new compound. Thus, the new KLS polymorphic form with its different physicochemical and pharmacokinetic characteristics can open the way to the development of a new KET-LYS polymorph drug that can emphasize the properties of commercial KLS for the treatment of acute inflammatory and painful conditions.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据