Abstract

PIPERINE-SACCHARIN COCRYSTAL STUDY: PHYSICOCHEMICAL PROPERTIES AND DISSOLUTION STUDY

Salman Umar, Habibie Ghiffari and Erizal Zaini*

ABSTRACT

The objective of this study was to prepare the crystal of piperine-saccharin in order to increase the solubility, dissolution rate and analgesic activity of piperine. Piperine-saccharin cocrystal was made in the ratio of 1: 2 equimolar with the method of solvents evaporation using ethanol. Characterization of the samples was carried out by X-ray diffraction, Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared (FTIR). The evaluation of cocrystal included a solubility test, dissolution rate test and writhing test. The solubility test and dissolution rate test were carried out using CO2-free distilled water solvents, both tests were measured using a UV-Vis spectrophotometer. The results of X-ray diffraction characterization showed a different diffractogram from the constituent components which indicated the formation of the cocrystal phase. The DSC thermogram results showed a new endothermic peak that was different from the two constituent components. The FT-IR spectrum showed a shift in the wave number in the cocrystal spectrum compared to the piperine and saccharin spectrums. Solubility and dissolution rate of cocrystal increased significantly (P <0.05) 3 times and 8 times compared with pure piperine compounds, analgesic activity of cocrystal has minimal analgesic effect (51,04%). It was concluded that Cocrystal piperine-saccharin can increase solubility, dissolution rate and analgesic activity.

Keywords: piperine; saccharin; cocrystal; solubility; dissolution rate; analgesic activity.