Improving Dissolution Rate of Piperine by Multicomponent Crystal Formation with Saccharin Zaini Erizal1,*, Riska Delfi2, Oktavia Maria Dona2, Ismed Friardi3, Fitriani Lili1 1Department of Pharmaceutics, Faculty of Pharmacy, Andalas University, Padang, Indonesia 2Sekolah Tinggi Ilmu Farmasi (STIFARM), Padang, Indonesia 3Laboratory of Biota Sumatera and Faculty of Pharmacy, Andalas University, Padang, Indonesia *Corresponding Author E-mail: erizal@phar.unand.ac.id
Online published on 30 April, 2020. Abstract Piperine, a secondary metabolite of Piper nigrum L., has been known for its pharmacological activities. However, the use of piperine is still limited due to the low solubility in water. The aim of this study was to improve the physicochemical properties of piperine by preparing into multicomponent crystal (MC) using saccharin by solvent evaporation method, and ethanol was used as the solvent. The intact materials and MC were characterized by several solid-state instruments. The amount of dissolved piperine was determined by High Performance of Liquid Chromatography (HPLC) using acetonitrile: water (90:10) as the mobile phase. Both morphology of intact piperine and MC showed irregular crystals. The diffractogram showed that MC had new and specific peaks at 2Φ: 12.91, 15.04, 19.54 and 22.40. The thermogram presented melting point for intact piperine, saccharin and MC which were 132.81°C, 230.02°C, 197.09°C, respectively. The infra-red spectrum showed no significant shift of MC which indicated no chemical interaction between piperine and saccharin. The dissolution study pointed higher amount of piperine dissolved in 0.1 N HCl with addition of 0.5% sodium lauryl sulphate. The dissolution piperine in MC after 60 minutes was 81.29±5.91%, while intact piperine was 44.78±1.89%. In conclusion, the formation of multicomponent crystal of piperine-saccharin was able to increase the dissolution of piperine. Top Keywords Piperine, Saccharin, Multicomponent Crystal, Solvent Evaporation, Dissolution. Top |