Edward Widjojokusumo

Physicochemical and mechanical properties of paracetamol cocrystal with 5-nitroisophthalic acid

We report novel pharmaceutical cocrystal of a popular antipyretic drug paracetamol (PCA) with coformer 5-nitroisophhthalic acid (5NIP) to improve its tabletability. The cocrystal (PCA-5NIP at molar ratio of 1:1) was synthesized by solvent evaporation technique using methanol as solvent. The physicochemical properties of cocrystal were characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetry analysis (TGA), fourier transform infrared spectroscopy (FTIR), hot stage polarized microscopy (HSPM) and scanning electron microscopy (SEM). Stability of the cocrystal was assessed by storing them at 40°C/75% RH for one month. Compared to PCA, the cocrystal displayed superior tableting performance. PCA-5NIP cocrystal showed a similar dissolution profile as compared to PCA and exhibited good stability. This study showed the utility of PCA-5NIP cocrystal for improving mechanical properties of PCA.

Supercritical fluid carbon dioxide extraction of Nigella sativa (black cumin) seeds using taguchi method and full factorial design

Abstract Optimum condition for Nigella sativa seeds oil and its bioactive compound, thymoquinone (TQ) using supercritical fluid carbon dioxide extraction (SCFE-CO2), were investigated. The optimization process was

Co-precipitation of loperamide hydrochloride and polyethylene glycol using aerosol solvent extraction system

The co-precipitation of loperamide hydrochloride (LPM) and polyethylene glycol (PEG) using aerosol solvent extraction system (ASES) was examined. Scanning electron microscopy — energy dispersive X-ray spectroscopy (SEM-EDS) analysis showed that the co-precipitation was achieved in various LPM-PEG mass ratios with changes in its morphology. In 10–50% PEG mass ratios, angular-shaped particles were formed, whereas in 65–90% PEG mass ratios, irregular-shaped particles were formed. X-ray diffraction (XRD) analysis of the co-precipitates revealed that the LPM retained amorphous structure, while, on the other hand, the PEG retained crystalline structure. Fourier transform infrared (FT-IR) spectra indicated carbonyl function group of LPM and ether function group of PEG appeared in the co-precipitates. Results of a dissolution test showed that the co-precipitates of LPM-PEG had higher dissolution rate compared to that of the raw material and processed LPM with ASES. Taken together, the co-precipitation of LPMPEG was achieved using ASES and higher in its dissolution rate.

Simultaneous micronization and purification of bioactive fraction by supercritical antisolvent technology

Simultaneous micronization and purification of DLBS3233 bioactive fraction, a combination of two Indonesian herbals Lagerstroemia speciosa and Cinnamomum burmannii has been successfully performed via supercritical anti-solvent (SAS) technology. The objective of the present study was to investigate the effectiveness of SAS technology to micronize and reduce coumarin content of DLBS3233. The effects of four SAS process parameters, i.e. pressure, temperature, concentration and solution flow rate on particle formation were investigated. In SAS process, DLBS3233 was dissolved in dimethylformamide (DMF) as the liquid solvent. The solution was then pumped through a nozzle into a chamber simultaneously with supercritical carbon dioxide (SC-CO2) which acts as the anti-solvent, resulting in DLBS3233 precipitation. Physicochemical properties of unprocessed DLBS3233 and SAS-processed DLBS3233 particles were analyzed using scanning electron microscopy (SEM) and high pressure liquid chromatography (HPLC). Total polyphenol content (TPC) was also analyzed.Particles with mean particle size ranging from 0.107±0.028 μm to 0.298±0.138 μm were obtained by varying the process parameters. SAS-processed DLBS3233 particles showed no coumarin content in all experiments studied in this work. Results of TPC analysis revealed no significant change in SAS-processed DLBS3233 particles compared to unprocessed DLBS3233. Nano-sized DLBS3233 particles with no coumarin content have been successfully produced using SAS process. This study demonstrates the ability of SAS for processing herbal medicine in single step process.