Isoniazid-Gentisic acid cocrystallization: Solubility, Stability, Dissolution rate, Antioxidant and Flowability Properties Studies

Mashhadi, Syed Muddassir Ali; Batsanov, Andrei S.; Sajjad, Syed Arslan; Nazir, Yasir; Bhatti, Moazzam Hussain; Yunus, Uzma

Abstract

Isoniazid (INH) is a key antitubercular agent, which exhibits poor chemical stability in the solid state associated with the hydrazide group. Cocrystallization with Gentisic Acid having antioxidant activity, may produce solid forms with improved pharmaceutical properties. The complementary nature of the functional groups of isoniazid and the chosen coformer resulted in success for cocrystal formation. Cocrystal (INH-Gentisic acid) was characterized by solid-state NMR, DSC, PXRD and single crystal-XRD. The synthesized cocrystals were tested for the inhibition of synthetic-free radicals, DPPH. INH-Gentisic acid demonstrated high free radical scavenging activity against DPPH (78.36% for 125µg/ml concentration) which were better than that of ascorbic acid (37.16%) used as standard. Moreover solubility, stability and flowability properties of the synthesized cocrystals are optimized.

Citation

Mashhadi, S. M. A., Batsanov, A. S., Sajjad, S. A., Nazir, Y., Bhatti, M. H., & Yunus, U. (2021). Isoniazid-Gentisic acid cocrystallization: Solubility, Stability, Dissolution rate, Antioxidant and Flowability Properties Studies. Journal of Molecular Structure, 1226, Article 129388. https://doi.org/10.1016/j.molstruc.2020.129388

• Journal Article Type: Article
• Acceptance Date: Oct 1, 2020
• Online Publication Date: Oct 2, 2020
• Publication Date: 2021-02
• Deposit Date: Oct 9, 2020
• Publicly Available Date: Oct 2, 2021
• Journal: Journal of Molecular Structure
• Print ISSN: 0022-2860
• Electronic ISSN: 1872-8014
• Publisher: Elsevier
• Peer Reviewed: Peer Reviewed
• Volume: 1226
• Article Number: 129388
• DOI: https://doi.org/10.1016/j.molstruc.2020.129388
• Public URL: https://durham-repository.worktribe.com/output/1260491