ENHANCEMENT OF SOLUBILITY AND
DISSOLUTION RATE OF DIFFERENT FORMS OF
ATORVASTATIN CALCIUM IN DIRECT
COMPRESSION TABLET FORMULAS.
SALAM W. AHJEL1, DUMITRU LUPULEASA2
1University of Baghdad, Faculty of Pharmacy
2University of Medicine and Pharmacy “Carol Davila”, Faculty of
Pharmacy, 6th Traian Vuia str, Bucharest 2, 020956
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Abstract:
Atorvastatin, as a synthetic lipid-lowering agent, is an inhibitor of 3-hydroxy-3-
methyl-glutaryl-coenzyme A (HMG - CoA) reductase which catalyzes the conversion of
HMG-Co A to mevalonate, an early rate-limiting step in cholesterol biosynthesis. The
bioavailability of atorvastatin is one of the key parameters for its therapeutic use and is
dependent on the form of the atorvastatin calcium to be used in the pharmaceutical
formulation (amorphous, crystalline or a mixture of both). The patient should take a
constant therapeutic daily dose, regardless to the pharmaceutical formulation of the
atorvastatin calcium. The major finding of this study was that the addition of buffering and
/or alkalizing agent will dramatically increase both, the solubility and dissolution rate of
atorvastatin calcium regardless to the form (crystalline , amorphous or a mixture of both)
used in the preparation of the direct compression formulas. The results also showed that it
was possible to provide therapeutic equivalence of atorvastatin calcium in the
pharmaceutical formulation regardless to the form used in the preparation of the direct
compression formulas since it was observed that addition of a buffering or alkalizing agent
that can provide a pH equal to or greater than (pKa +1), i.e. (pH ≥ 6) can enhance both
solubility and dissolution rate of atorvastatin calcium different forms.
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