The Impact of Co-crystal Formation on the Stability of Camylofin Dihydrochloride Immediate Release Tablets

Year 2024, Volume: 44 Issue: 2, 108 - 123, 01.06.2024

Sanika Kole , Rutuja Vinchurkar , Ashwini Gawade , Ashwin Kuchekar

https://doi.org/10.52794/hujpharm.1331991

Abstract

The objective of this study was to select an appropriate co-former and investigate its impact on the formation of co-crystals involving Camylofin dihydrochloride and Fumaric acid. To determine co-former, a molecular docking study was conducted, and among the compounds evaluated, fumaric acid exhibited the highest number of hydrogen bonds formed with Camylofin dihydrochloride and demonstrated a favorable Glide score of -5.21 kcal/mol. The kneading method was employed after optimizing the molar ratio of Camylofin dihydrochloride to Fumaric acid, which was found to be 1:1, 1:2, and 1:3. The resulting Camylofin dihydrochloride co-crystals underwent various analytical techniques, including Fourier Transform Infrared Spectroscopy, Scanning Electron Microscopy, Powder X-ray Diffraction, and Differential Scanning Calorimetry. The Camylofin dihydrochloride-Fumaric acid co-crystals, immediate-release tablets were formulated. A result of ex-vivo study revealed that Camylofin dihydrochloride-Fumaric acid co-crystals and their immediate release tablets were more potent than plain Camylofin dihydrochloride, with the immediate release tablets being the most potent of all. Stability analysis demonstrated that the final batch F5 remained stable under accelerated ambient stability conditions (40°C±2°C, 75% RH±5%RH) and accelerated stability conditions (25°C±2°C,62% RH±5%RH). The co-crystal technology utilized in this study successfully improved the stability of Camylofin dihydrochloride without altering its chemical composition.

Keywords

Camylofin dihydrochloride, Co-crystals, Immediate release tablets, Stability Drug release, Ex-vivo study

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