Background: Telmisartan (TEL) is an orally active nonpeptide angiotensin II antagonist drug. The drug acts on a subtype of AT1 receptors, which serves to cope with high blood pressure (hypertension). TEL is a class II Biopharmaceutical Classification System (BCS), which is a drug that has low solubility in water and high permeability. Objectives: This study aims to determine the effect of the formation of TEL-PVP K-30 nanoparticles through the solvent drop grinding method on the characteristics of physicochemical properties and the rate of dissolution of TEL. Methods: Nanoparticles are made in 2 formulas, namely formula 1: 1 and formula 1: 2. Results: Characterization of the Particle Size Analyzer (PSA) was performed with the results of the formula 1:1 24nm, and the formula 1:2 35nm. X-ray Diffraction (XRD) analysis resulted from a decrease in the intensity of crystallinity degrees. Fourier Transform Infrared (FT-IR) Spectroscopy occurs wave number shift. Differential Scanning Calorimetry (DSC) decreases in melting point. The dissolution rate was carried out using a pH 7.5 phosphate tart medium. Conclusion: The result of the dissolution rate has increased by 3.3 times for formula 1:1 and 2.9 times for formula 1:2. Keywords: Telmisartan; polyvinylpyrrolidone K-30; nanoparticles; and solvent drop grinding.
Objective: Glibenclamide belongs to the 2nd generation sulfonylurea group as an oral antidiabetic with low solubility in water and high bioavailability in systemic circulation (Biopharmaceutical Classification System class II). This study aimed to increase the solubility and dissolution rate of glibenclamide by preparing an inclusion complex of Glibenclamide and Hydroxypropyl-β-cyclodextrin. Methods: Inclusion complexes were prepared by the co-grinding method in two ratios 1:1 and 1:2 mol. Characterizations of inclusion complex were carried out by Scanning Electron Microscopy (SEM), Fourier Transform Infrared (FT-IR) spectroscopy, Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) analysis. Solubility test was carried out in CO2-free distilled water and dissolution rate was carried out in phosphate buffer pH 7.4. Results: The results of the SEM analysis showed changes in particle morphology. FT-IR spectroscopy shows a shift in wavenumber. DSC analysis showed a decrease in the melting point of the inclusion complex. XRD characterization results showed a decrease in the intensity of the inclusion complex. Solubility of inclusion complex of glibenclamide increased nine times 1:1 mol inclusion complex, twelve times 1:2 mol inclusion complex compared to intact glibenclamide. The dissolution of glibenclamide, inclusion complex 1:1, and inclusion complex 1:2 in phosphate buffer pH 7.4 medium at 60 min was 17.19%, 34.15% and 52.83% respectively. Conclusion: Based on the results of the study, it can be said that the glibenclamide inclusion complex with Hydroxypropyl-β-cyclodextrin successfully increases the solubility and dissolution rate of glibenclamide significantly.
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