Literature DB >> 25010838

Novel pharmaceutical cocrystal consisting of paracetamol and trimethylglycine, a new promising cocrystal former.

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.
Copyright © 2014 Elsevier B.V. All rights reserved.

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


  4 in total

1.  Pharmaceutical Co-Crystals, Salts, and Co-Amorphous Systems: A Novel Opportunity of Hot Melt Extrusion.

Authors:  Sagar Narala; Dinesh Nyavanandi; Priyanka Srinivasan; Preethi Mandati; Suresh Bandari; Michael A Repka
Journal:  J Drug Deliv Sci Technol       Date:  2020-11-09       Impact factor: 3.981

2.  Co-crystals as a new approach to multimodal analgesia and the treatment of pain.

Authors:  Carmen Almansa; Christopher S Frampton; José Miguel Vela; Steve Whitelock; Carlos R Plata-Salamán
Journal:  J Pain Res       Date:  2019-09-04       Impact factor: 3.133

3.  Unexpected Salt/Cocrystal Polymorphism of the Ketoprofen-Lysine System: Discovery of a New Ketoprofen-l-Lysine Salt Polymorph with Different Physicochemical and Pharmacokinetic Properties.

Authors:  Andrea Aramini; Gianluca Bianchini; Samuele Lillini; Simone Bordignon; Mara Tomassetti; Rubina Novelli; Simone Mattioli; Larisa Lvova; Roberto Paolesse; Michele Remo Chierotti; Marcello Allegretti
Journal:  Pharmaceuticals (Basel)       Date:  2021-06-10

4.  Solubility Improvement of Benexate through Salt Formation Using Artificial Sweetener.

Authors:  Okky Dwichandra Putra; Daiki Umeda; Eriko Fujita; Tamami Haraguchi; Takahiro Uchida; Etsuo Yonemochi; Hidehiro Uekusa
Journal:  Pharmaceutics       Date:  2018-05-26       Impact factor: 6.321

  4 in total

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