Topic > Investigation of the supersaturation and precipitation kinetics of weakly basic Bcs Ii drugs

Precipitation of solid drug particles in the gastrointestinal tract influences both the rate and extent of intestinal drug absorption could be a major contributing factor significant to low and highly variable bioavailability observed for some low solubility drugs. The prerequisite for such precipitation is that a supersaturated solution of the drug is formed inside the intestinal lumen. Say no to plagiarism. Get a tailor-made essay on "Why Violent Video Games Shouldn't Be Banned"? Get an original essay Intestinal precipitation occurs for basic drugs, regardless of the form or formulation of the drug, due to the increase in pH from acidic in the stomach to basic in the small intestine. To prevent this precipitation, the best way is to use polymers as precipitation inhibitors which will help prevent precipitation from the supersaturated state and increase its bioavailability. The aim of the project work was to study the phenomenon of supersaturation in the gut pH and compare the precipitation inhibition capacity of polymers with the help of turbidimetric analysis and particle size analysis. Furthermore, the crystalline state of the precipitates was analyzed by powder X-ray diffractometer to study the changes in the crystals during precipitation in the presence and absence of polymers. The two drugs belonging to the BCS II class were selected as model drugs, namely albendazole and itraconazole. Polymers used as precipitation inhibitors i.e. HPMC and Eudragit. The capacity of the polymers was determined based on their turbidity profiles and particle sizes. Supersaturation was induced by the “Solvent Shift method”, which is a method reported in the literature to study supersaturation and precipitation of drugs. The study was covered by varying the amount of drug and the concentration of the polymer. The effect of changes in the amount of drug and concentration of precipitation inhibitors was evaluated with respect to time. This attempt will help us to select the best possible polymer for drugs with low solubility in the early stage for the development of supersaturated drug delivery system such as solid dispersion since many supersaturated systems have failed due to instability induced by crystallization phenomenon. Turbidity was analyzed at different time points (2,4,8,12,16,20 min) and particle size was analyzed at two time points (0 and 20 min). For the PXRD study, the precipitate was collected by low-speed centrifugation for 1–2 minutes and air-dried. The results of the study suggested that supersaturation is a complex process and needs to be studied more at the molecular level to better understand the process. A variation was observed for both drugs at different polymer concentrations in the presence of the polymers. After turbidity analysis, it can be clearly stated that for albendazole, HPMC was shown to have a significant effect on precipitation inhibition compared to Eudragit. Among the different polymer concentrations chosen, the inhibitory effect of 0.5 mg/ml HPMC was found to be the highest for 400 µg of ABZ and 0.25 mg/ml HPMC for the lower doses (200 and 100 µg). In contrast, for Itraconazole, Eudragit was found to significantly inhibit precipitation compared to HPMC. However, Eudragit shows a good antiprecipitating effect at concentrations higher than 0.5 mg/ml at all doses tested, i.e. 400 µg, 200 µg and 100 µg. Please note: this is just a sample..