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Improved Solubility and Dissolution Rates in Novel Multicomponent Crystals of Piperine with Succinic Acid

1
Department of Pharmaceutics, Faculty of Pharmacy, Andalas University, Padang 25163, Indonesia
2
Laboratory of Biota Sumatera and Faculty of Pharmacy, Andalas University, Padang 25163, Indonesia
3
Department of Chemistry, School of Science, Tokyo Institute of Technology, Tokyo 1528551, Japan
*
Author to whom correspondence should be addressed.
Sci. Pharm. 2020, 88(2), 21; https://doi.org/10.3390/scipharm88020021
Received: 18 March 2020 / Revised: 3 April 2020 / Accepted: 9 April 2020 / Published: 13 April 2020
The objectives of this study were to prepare and characterize a novel piperine–succinic acid multicomponent crystal phase and to evaluate the improvement in the solubility and dissolution rate of piperine when prepared in the multicomponent crystal formation. The solid-state characterization of the novel multicomponent crystal was performed by powder X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform-infrared (FT-IR) spectroscopy. Solubility and dissolution rate profiles were evaluated in distilled water. The physical stability was evaluated under high relative humidity (75% and 100% RH). The determination of the single crystal X-ray diffraction structure revealed that this novel multicomponent crystal was a cocrystalline phase of piperine–succinic acid (2:1 molar ratio). The differential scanning calorimetry thermogram of the cocrystal showed a single and sharp endothermic peak at 110.49 °C. The cocrystal resulted in greater solubility and a faster dissolution rate of piperine than intact piperine. This improvement was a result of the formation of a channel structure in the cocrystal. In addition, the cocrystal was stable under a humid condition. View Full-Text
Keywords: piperine; multicomponent crystal; cocrystal; succinic acid; dissolution rate piperine; multicomponent crystal; cocrystal; succinic acid; dissolution rate
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MDPI and ACS Style

Zaini, E.; Afriyani; Fitriani, L.; Ismed, F.; Horikawa, A.; Uekusa, H. Improved Solubility and Dissolution Rates in Novel Multicomponent Crystals of Piperine with Succinic Acid. Sci. Pharm. 2020, 88, 21.

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