Yori YULIANDRA, Erizal ZAINI, Riri IZADIHARI, Henning ROSENAU

Multicomponent crystals of mefenamic acid–tromethamine with improved dissolution rate

Mefenamic acid (MA) is a popular nonsteroidal anti-inflammatory drug classified into BCS class II which has a low solubility and dissolution rate in an aqueous medium. The present study aimed to improve the dissolution rate of MA by preparing multicomponent crystals with tromethamine (TM) through the solvent evaporation technique. The resulting powder was characterized for its solid-state properties and evaluated for the dissolution rate. The results showed that the powder X-ray diffraction pattern of the MA–TM binary system was different from its starting materials, indicating the formation of a new crystalline phase. The differential scanning calorimetry analysis of the MA–TM binary system showed a single and sharp endothermic peak at 110 °C, which was attributed to the melting point of MA–TM multicomponent crystals. The Fourier transform infrared spectroscopy analysis showed the occurrence of solid-state interaction involving proton transfer between MA and TM. The dissolution efficiency of MA–TM multicomponent crystal was 2.5-fold higher than the intact MA. The study concludes that the MA–TM binary system forms a salt-type multicomponent crystal. The multicomponent crystals can significantly increase its dissolution rate and is an alternative technique for modifying the physicochemical properties of active pharmaceutical ingredients.

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