Incorporation of poorly soluble drugs into self emulysifying drug delivery systems,
where the substance is in a solubilized form, is one of the many possibilities for
enhancing solubility.
The aim of the study was to evaluate the possibility of tablet production from dry
microemulsions, produced with spray drying process.
Simvastatin, a HMG CoA reductase inhibitor, was used as a model substance, due to its
poorly aqueous solubility and good permeability. Various solid carriers were used to
produce dry microemulsions, the sample with best results was chosen for further
experiments.
Experimental design was conducted with statistical tool DoE (Design of Experiments).
The aim of the experimental design was to evaluate correlation between composition of
suspension for spray drying and quality of dry emulsions (simvastatin content, granules
flowability and compressibility) or tablets (mass, hardness and disintegration
uniformity). It was impossible to construct a model in most of the cases, but it was
shown, that higher Pharmacoat® 606 content leads to higher efficiency of spray drying
process and lower relative standard deviation in tablets mass uniformity test.
Tablets were compressed from granules with the best characteristics. The dissolution
rate of prepared tablets was higher compared to the original Zocor® tablets, especially
in the first 15 minutes of the dissolution test.
The results of the present work suggest that it is appropriate to incorporate self
microemulsifying drug delivery systems into tablets. Sivastatin, incorporated into tested
self microemulsifying drug delivery systems, is not stable at room temperature, further
methods are needed to enhance its stability.
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