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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

5-Fluorocytosine/5-Fluorouracil Drug-Drug Cocrystal: a New Development Route Based on Mechanochemical Synthesis

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Author(s):
da Silva, Cecilia C. P. [1, 2] ; de Melo, Cristiane C. [1, 3] ; Souza, Matheus S. [1] ; Diniz, Luan F. [1] ; Carneiro, Renato L. [2] ; Ellena, Javier [1]
Total Authors: 6
Affiliation:
[1] Univ Sao Paulo, Inst Fis Sao Carlos, BR-13560970 Sao Carlos, SP - Brazil
[2] Univ Fed Sao Carlos, Dept Quim, BR-13083887 Sao Carlos, SP - Brazil
[3] Univ Fed Alfenas, Fac Ciencias Farmaceut, BR-37130000 Alfenas, MG - Brazil
Total Affiliations: 3
Document type: Journal article
Source: JOURNAL OF PHARMACEUTICAL INNOVATION; v. 14, n. 1, p. 50-56, MAR 2019.
Web of Science Citations: 2
Abstract

Mechanochemistry is addressed here for the green formation of a 1:1 pharmaceutical cocrystal involving the antifungal prodrug 5-Fluorocytosine (5-FC) and the antineoplastic drug 5-Fluorouracil (5-FU). Crystalline material of this drug-drug cocrystal (DDC) was previously obtained by slow evaporation from solution (SES) and was then structurally analyzed. In this paper, neat grinding and solvent-drop grinding (SDG) were applied in an attempt to achieve a route for the supramolecular synthesis of this cocrystal, exhibiting suitable yield and amount for solid characterization, which were not achieved via the SES method. SDG provided the solid drug-drug cocrystal form. The resulting material had its physical stability monitored for 2 years and was then evaluated by a range of analytical technologies: X-ray powder diffraction, differential scanning calorimetry, hot-stage microscopy, thermogravimetric, and spectroscopic analysis. The new cocrystal proved to be stable for 6 months and in environments with high relative humidity. In this sense, it is believed that the new DDC is a potential model system which could be used as a base for further developments in the field, for other molecules or in relation to the feasibility of using this cocrystal therapeutically. (AU)

FAPESP's process: 15/25694-0 - Obtaining, characterization and evaluation of novel crystalline solid forms of drugs used treatment of tuberculosis
Grantee:Luan Farinelli Diniz
Support Opportunities: Scholarships in Brazil - Master