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New ethenzamide-trimesic acid cocrystal: Equilibrium solubility
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Abstract
To study the influence of drug cocrystal on the solubility of active pharmaceutical ingredients (APIs). The ETZ·2TMA·MeOH cocrystal was obtained by the solution evaporation crystallization method. The cocrystal structure was characterized by Single Crystal X-ray Diffractometer. The single crystal belongs to orthorhombic crystal system with space group P212121(no.19), a = 12.9863(9) Å, b = 16.6603(11) Å, c = 25.9260(16) Å, V = 5609.2(6) Å3, Z = 8, T = 170.00 K. The main forces are the formation of intermolecular hydrogen bonds between the amide groups on ETZ and the carboxyl groups on TMA and the hydroxyl group on methanol. In addition, the solubility of ETZ and ETZ·2TMA·MeOH cocrystal was determined. The results show that, in contrast to most cocrystal systems that improve solubility, the solubility of ETZ·2TMA·MeOH decreased to 19.30 % of pure ETZ.
Research Square Platform LLC
Title: New ethenzamide-trimesic acid cocrystal: Equilibrium solubility
Description:
Abstract
To study the influence of drug cocrystal on the solubility of active pharmaceutical ingredients (APIs).
The ETZ·2TMA·MeOH cocrystal was obtained by the solution evaporation crystallization method.
The cocrystal structure was characterized by Single Crystal X-ray Diffractometer.
The single crystal belongs to orthorhombic crystal system with space group P212121(no.
19), a = 12.
9863(9) Å, b = 16.
6603(11) Å, c = 25.
9260(16) Å, V = 5609.
2(6) Å3, Z = 8, T = 170.
00 K.
The main forces are the formation of intermolecular hydrogen bonds between the amide groups on ETZ and the carboxyl groups on TMA and the hydroxyl group on methanol.
In addition, the solubility of ETZ and ETZ·2TMA·MeOH cocrystal was determined.
The results show that, in contrast to most cocrystal systems that improve solubility, the solubility of ETZ·2TMA·MeOH decreased to 19.
30 % of pure ETZ.
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