Objective: The goal of this study was to formulate ticagrelor tablets with enhanced dissolution rate using cogrinding technique. However, it belongs to the biopharmaceutical classification system Class IV molecule, poorly soluble, and permeable.Methods: Various ratios (0.2:1–1.67:1) of povidone (PVP)/drug were used in the formulations. Ticagrelor was coground with different percentage of PVP K 25 (carrier) in a mortar with a pestle for 30 min, then mixed with the rest excipients. A high-performance liquid chromatography stability indicating assay was developed to test the stability of ticagrelor in the selected formulae.Results: The results showed that the presence of PVP in relatively high ratios compared to the drug is desirable for enhancing the dissolution rate of ticagrelor. The best-optimized formulae found were that F8 and F9 which showed good disintegration and dissolution rate of ticagrelor more than 92% after 30 min while the dissolution rate for ticagrelor standard was only 22% after 30 min. Stability studies were performed on the selected formulae F8 and F9. Conclusion: The optimized formulae were evaluated for thickness, weight variation, hardness, friability, dissolution, and accelerated stability study for a period of 6 months. Cogrinding using PVP K 25 proved to enhance the dissolution of ticagrelor which may be due to the formation of a soluble complex between ticagrelor and PVP. The selected formulae F8 and F9 showed good stability.
Objective: The scope of this work was to formulate sitagliptin and simvastatin rapidly dissolving tablets. However, simvastatin is practically insoluble in water. For improving its poor oral bioavailability and with the aim of facilitating administration to patients facing problems with swallowing rapidly dissolving tablets were preparedMethods: Tablets were prepared using superdisintegrant addition technique using croscarmellose sodium (Ac-di-sol), sodium starch glycolate (explotab) and crospovidone in different percentages. Evaluation tests such as weight variation, thickness, and content variation, and friability, disintegration, wetting time, in vitro dispersion and in vitro dissolution were carried out.Results: The results showed that the presence of crospovidone could enhance the dissolution rate of simvastatin greatly. The best-optimized formulae found were that F8, F9, and F10 which showed good disintegration and the dissolution rate of simvastatin and sitagliptin was more than 90% after 10 min while the dissolution rate for simvastatin and sitagliptin pure standards was 12% and 30%, respectively after 10 min.Conclusion: Some tablet formulae showed acceptable pharmacotechnical properties and complied with compendium requirements. Results of dissolution studies revealed that F8-F10 showed an increase in the dissolved sitagliptin and simvastatin to be more than 90% after 10 min.
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