| Literature DB >> 25010838 |
Yusuke Maeno1, Toshiro Fukami2, Masatoshi Kawahata3, Kentaro Yamaguchi3, Tatsuaki Tagami4, Tetsuya Ozeki4, Toyofumi Suzuki5, Kazuo Tomono5.
Abstract
Paracetamol (APAP), a frequently used antipyretic drug, has poor compression moldability. In this study, we identified a novel cocrystal consisting of APAP and trimethylglycine (TMG) that exhibits improved tabletability. TMG was used instead of oxalic acid (OXA), which is a coformer reported previously. The cocrystal (APAP-TMG at a molar ratio of 1:1) was characterized by X-ray analysis, infrared spectroscopy, and thermal analysis. The crystal structure of APAP-TMG revealed that it was a cocrystal, since no proton was transferred between the APAP and TMG molecules. The compression and dissolution properties of APAP-TMG were similar to that of the APAP-OXA cocrystal. In addition, taste sensing measurements suggested that TMG has a sweet and umami taste, indicating that TMG should suppress the bitterness of APAP. From these results, TMG could be a safe and promising cocrystal former that could replace OXA, which can irritate tissues.Entities:
Keywords: Cocrystal; Crystal structure; Paracetamol; Tabletability (moldability); Trimethylglycine (betaine)
Mesh:
Substances:
Year: 2014 PMID: 25010838 DOI: 10.1016/j.ijpharm.2014.07.008
Source DB: PubMed Journal: Int J Pharm ISSN: 0378-5173 Impact factor: 5.875