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Essay / Investigation of supersaturation and precipitation kinetics of weakly basic Bcs Ii drugs
Precipitation of solid drug particles in the gastrointestinal tract affects both the rate and extent of intestinal drug absorption , which could be a factor that contributes significantly to the low and highly variable bioavailability observed for some drugs with low solubility. A prerequisite for such precipitation is that a supersaturated solution of the drug is formed in the intestinal lumen. Say no to plagiarism. Get a Custom Essay on “Why Violent Video Games Should Not Be Banned”?Get Original EssayIntestinal precipitation occurs for basic medications, regardless of form or formulation, due to increased 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 intestine. pH and compare the precipitation inhibition capacity of polymers using turbidimetric analysis and particle size analysis. Furthermore, the crystalline state of the precipitates was analyzed by powder X-ray diffractometer to study the changes of the crystals during precipitation in the presence and absence of polymers. The two drugs belonging to BCS class II were selected as model drugs, namely albendazole and itraconazole. Polymers used as precipitation inhibitors, namely HPMC and Eudragit. The capacity of the polymers was determined based on their turbidity profiles and particle size. Supersaturation was induced by the “solvent displacement method” which is a method reported in the literature to study supersaturation and precipitation of drugs. The study was completed by varying the amount of drug and polymer concentration. The effect of changes in drug quantity and precipitation inhibitor concentration was evaluated as a function of time. This attempt will help us select the best possible polymer for drugs with low solubility at an early stage for the development of a supersaturated drug delivery system. such as solid dispersion because many supersaturated systems have failed due to the instability induced by the 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 PXRD study, the precipitate was collected by centrifugation at low speed for 1–2 min and air dried. The study results suggest that supersaturation is a complex process and needs to be further studied at the molecular level to better understand the process. . Variance 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 found to have a significant effect on precipitation inhibition compared to Eudragit. Among the different polymeric concentrations chosen, the inhibitory effect of 0.5 mg/ml of HPMC was found to be the highest for 400 µg of ABZ and of 0.25 mg/ml of HPMC for lower doses ( 200 and 100 µg). On the contrary, for Itraconazole, Eudragit was found to inhibit precipitation significantly compared to HPMC. However, Eudragit shows a good antiprecipitant effect at a higher concentration of 0.5 mg/ml at all doses tested,..