Erizal Zaini

Preparation and characterization of solid dispersion freeze-dried efavirenz – polyvinylpyrrolidone K-30

The aim of this research is to prepare and characterize solid dispersion of efavirenz – polyvinylpyrrolidone (PVP) K-30 by freeze drying to increase its solubility. Solid dispersion of efavirenz – PVP K-30 was prepared by solvent evaporation method with ratio 2:1, 1:1, and 1:2 and dried using a freeze dryer. Characterizations were done by scanning electron microscopy (SEM), powder X-ray diffraction analysis, differential thermal analysis (DTA), and Fourier transform infrared (FT-IR) spectroscopy. Solubility test was carried out in CO2-free distilled water, and efavirenz assay was conducted using high-performance liquid chromatography with acetonitrile:acetic acid (80:20) as the mobile phases. Powder X-ray diffractogram showed a decrease in the peak intensity, which indicated the crystalline altered to amorphous phase. DTA thermal analysis showed a decrease in the melting point of the solid dispersion compared to intact efavirenz. SEM results indicated the changes in the morphology of the crystal into an amorphous form compared to pure components. FT-IR spectroscopy analysis showed a shift wavenumber of the spectrum efavirenz and PVP K-30. The solubility of solid dispersion at ratio 2:1, 1:1, and 1:2 was 6.777 μg/mL, 6.936 μg/mL, and 14,672 μg/mL, respectively, whereas the solubility of intact efavirenz was 0.250 μg/mL. In conclusion, the solubility of solid dispersion increased significantly (P < 0.05).

Cocrystal of Ibuprofen–Nicotinamide: Solid-State Characterization and In Vivo Analgesic Activity Evaluation

Ibuprofen is classified as a BCS class II drug which has low solubility and high permeability. We conducted the formation of the cocrystalline phase of ibuprofen with coformer nicotinamide to increase its solubility. The purpose of this study was to characterize the solid state of cocrystalline phase of ibuprofen-nicotinamide, determine the solubility, and evaluate its in vivo analgesic activity. The cocrystal of ibuprofen-nicotinamide was prepared by a slow evaporation method. The solid-state characterization was conducted by powder X-ray diffraction (PXRD) analysis, differential thermal analysis (DTA), and scanning electron microscopy (SEM). To investigate the in vivo analgesic activity, 28 male Swiss-Webster mice were injected with acetic acid 0.5% following oral administration of intact ibuprofen, physical mixture, and its cocrystalline phase with nicotinamide (equivalent to 26 mg/kg ibuprofen). The number of writhes was counted, and pain inhibition was calculated. All data were analyzed with one-way ANOVA followed by Duncan’s Multiple Range Test (95% confidence interval). The results revealed that a new cocrystalline phase was successfully formed. The solubility testing showed that the cocrystal formation enhanced the solubility significantly as compared with the physical mixture and intact ibuprofen. A significant increase in the analgesic activity of cocrystal ibuprofen-nicotinamide was also confirmed.

Influence of milling process on efavirenz solubility

Introduction: The aim of this study was to investigate the influence of the milling process on the solubility of efavirenz. Materials and Methods: Milling process was done using Nanomilling for 30, 60, and 180 min. Intact and milled efavirenz were characterized by powder X-ray diffraction, scanning electron microscopy (SEM), spectroscopy infrared (IR), differential scanning calorimetry (DSC), and solubility test. Results: The X-ray diffractogram showed a decline on peak intensity of milled efavirenz compared to intact efavirenz. The SEM graph depicted the change from crystalline to amorphous habit after milling process. The IR spectrum showed there was no difference between intact and milled efavirenz. Thermal analysis which performed by DSC showed a reduction on endothermic peak after milling process which related to decreasing of crystallinity. Solubility test of intact and milled efavirenz was conducted in distilled water free CO2with 0.25% sodium lauryl sulfate media and measured using high-performance liquid chromatography method with acetonitrile: distilled water (80:20) as mobile phases. The solubility was significantly increased (P < 0.05) after milling processes, which the intact efavirenz was 27.12 ± 2.05, while the milled efavirenz for 30, 60, and 180 min were 75.53 ± 1.59, 82.34 ± 1.23, and 104.75 ± 0.96 μg/mL, respectively. Conclusions: Based on the results, the solubility of efavirenz improved after milling process.

Crystal structure of olivetolic acid: a natural product from Cetrelia sanguinea (Schaer.)

The packing in olivetolic acid is similar to that in resorcinolic acid.

MANUFACTURE OF PLASTICS FILM CONTAINING OF POLYSTIRENE, POLYCAPROLACTONE, POLY(3-HIDROKSIBUTYRATE-CO-3- HIDROXYVALERATE) AND BIODEGRADATION STUDY IN OCEAN WATER

ABSTRACT The manufacture of a biodegradable plastics film containing of polymer synthetic polystyrene (PS) and biopolymer of polycaprolactone (PCL), poly(3-hydroxybutyrate-co-3-hydroxyvalerate) [P(3HB-ko-3HV)] and biodegradation study in ocean water has been carried out. Plastics film containing of PS/PCL/P(3HB-ko-3HV) produced by blending techniques followed by solvent casting with ratios were of 100/0/0, 95/5/0, 95/0/5, 90/5/5, 85/10/5, 85/5/10. This testing was conducted based on immersion test method recommend by American Society for Testing and Materials. Poly blend plastics film PS/PCL/P(3HB-ko-3HV) were characterized by tensile strength, thermal properties and SEM analysis. The profiles of the rate biodegradation view by weight reduction of the tested plastic film for 1-7 weeks period. Tensile strength analysis showed the decreasing of tensile strength with the addition of P(3HB-ko-3HV). Thermal analysis showed a decreasing in the melting point with the addition of PCL and P(3HB-co- 3HV). SEM micrograph showed the destruction occurred and erosion at surface of plastic film during observation time. The rate of biodegradation showed that increasing of PCL and P (3HBco- 3HV) in a mixture of plastic film, so biodegradation increased. Keywords: polystyrene, polycaprolactone, poly(3-hidroxybutyrate-co-3-hydroxyvalerate), biodegradation, film plastic.