Engineering Active Pharmaceutical Ingredients by Spray Drying: Effects on Physical Properties and In Vitro Dissolution

Active pharmaceutical ingredients have very strict quality requirements; minor changes in the physical and chemical properties of pharmaceuticals can adversely affect the dissolution rate and therefore the bioavailability of a given drug. Accordingly, the aim of the present study was to investigate the effect of spray drying on the physical and in vitro dissolution properties of four different active pharmaceutical ingredients, namely carbamazepine, indomethacin, piroxicam, and nifedipine. Each drug was dispersed in a solution of ethanol and water (70:30) and subjected to single-step spray drying using similar operational conditions. A complete characterization of the spray-dried drugs was performed via differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffraction (XRPD), particle size distribution analysis, solubility analysis, and an in vitro dissolution study. The results from the thermal analysis and X-ray diffraction showed that, except for carbamazepine, no chemical modifications occurred as a result of spray drying. Moreover, the particle size distribution of all the spray-dried drugs significantly decreased. In addition, SEM images showed that most of the particles had an irregular shape. There was no significant improvement in the solubility of the spray-dried drugs compared with the unprocessed compounds; however, in general, the dissolution rates of the spray-dried drugs showed a remarkable improvement over their non-spray-dried counterparts. Therefore, the results from this study demonstrate that a single spray-drying step may lead to changes in the physical properties and dissolution characteristics of drugs and thus improve their therapeutic action.

Physical-chemical, thermal, and functional properties of achira (Canna indica L.) flour and starch from different geographical origin

Achira (Canna indica L.) is a plant native to the Andes in South America, a starchy source, and its cultivation has expanded to different tropical countries, like Brazil. In order to evaluate the potential of this species, starch and flours with different particle size were obtained from Brazilian achira rhizomes. Proximal analyses, size distribution, SEM, swelling power, solubility, DSC, XRD analysis, and FTIR were performed for characterization of these materials. Flours showed high dietary fiber content (16.532.2% db) and high concentration of starch in the case of the smaller particle size fraction. Significant differences in protein and starch content, swelling power, solubility, and thermal properties were observed between the Brazilian and the Colombian starch. All the studied materials displayed the B-type XRD pattern with relative crystallinity of 20.1% for the flour and between 27.0 and 28.0% for the starches. Results showed that the starch and flour produced from achira rhizomes have great technological potential for use as functional ingredient in the food industry.

Physical, chemical and geological properties of sediments from the central equatorial Pacific

The solution rate of biogenic opal in near-surface sediments in the Central Equatorial Pacific is three to eight orders of magnitude lower than similar acid-cleaned samples. Iron, magnesium and calcium aluminosilicates may be the minerals which are forming on the surface of the opal and reducing its solution rate. The scale height of the system studied suggests that diffusive and not advective processes are primarily responsible for the removal of dissolved silica in sediments. Solution budget calculations for this area suggest that 90-99 per cent of the biogenic opal produced in surface waters dissolves before reaching the sediment-water interface; an additional amount dissolves within the sediment and diffuses into bottom waters leaving 0.05-0.15 per cent of the original amount of opal produced by organisms in the sedimentary record. The relative solution potential of the upper 1000 m of the water column varies by more than an order of magnitude from the Antarctic to Equator and may have a pronounced effect on the accumulation rate of biogenic opal in underlying sediments.

Physical, geochemical and magnetic properties of several ODP Leg 192 sites, Ontong Java Plateau

In this manuscript, we present the results of a physical properties investigation carried out on basaltic cores recovered from the four Leg 192 basement sites, focusing on the relationship between physical properties and alteration in basalts. Variations in physical properties in the Leg 192 basement sites closely resemble each other and reflect the amount of alteration and vein formation in the basement basalts. P-wave velocities, magnetic susceptibilities, and densities for the dense massive basalts are higher than those of more altered and heavily veined basalts. Porosity-dependent alteration is observed at Leg 192 basement sites: P-wave velocity displays a general decrease with increasing loss on ignition and potassium content. These trends are consistent with trends documented for typical alteration of oceanic crust and suggest that basalt alteration is largely responsible for the variation of the physical properties exhibited by rocks at Leg 192 basement sites. Our physical property data support the conclusion that only low-temperature seawater-mediated alteration occurred in the lava flows of the Ontong Java Plateau (OJP). This lack of higher-temperature hydrothermal alteration is consistent with the idea that the OJP basement sites are far from their eruptive vents.