Abstract
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.
Highlights
Many patients with type 2 diabetes are affected by hypercholesterolemia
The combination of antidiabetic and anti-hypercholesterolemia is appreciated as Juvisync® convenient tablets which are a combination of sitagliptin and simvastatin
Friability of all formulae was less than 1% and the disintegration time of formulae tablets F8-F10 was in the range of 31 to 43 s where crospovidone was in percent of 27-36% of the tablet weight, which may be because crospovidone has been proved to result in fast volume expansion and hydrostatic pressures allowing tablet disintegration [10]
Summary
Many patients with type 2 diabetes are affected by hypercholesterolemia. The combination of antidiabetic and anti-hypercholesterolemia is appreciated as Juvisync® convenient tablets which are a combination of sitagliptin and simvastatin. Sitagliptin and simvastatin rapidly dissolving tablets were formulated to achieve faster release than the convenient tablets and more suitable for elderly patients who face difficulty in swallowing. The literature lacks trials of the formulation of simvastatin and sitagliptin combination in rapidly dissolving tablets dosage form. There are different technologies used for manufacturing fastdissolving tablets, such as freeze-drying, spray-drying, tablet molding, sublimation, sugar-based excipients, tablet compression, and disintegration addition [1, 2]. Simvastatin, and sitagliptin rapidly dissolving tablets were prepared using the easiest technique which is superdisintegrant addition. Sitagliptin phosphate monohydrate is described chemically as 7-[(3R)3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetra-hydro-3(trifluoromethyl)-1,2,4-triazolo[4,3-a] pyrazine phosphate (1:1) monohydrate, with the structural formula shown in fig
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