RT Journal Article
SR Electronic
T1 Solubility and Stability Enhancement of Atorvastatin by Cyclodextrin Complexation
JF PDA Journal of Pharmaceutical Science and Technology
JO PDA J Pharm Sci Technol
FD Parenteral Drug Association (PDA)
SP 217
OP 225
VO 63
IS 3
A1 Chinna Reddy Palem
A1 Shweta Patel
A1 Varsha B. Pokharkar
YR 2009
UL http://journal.pda.org/content/63/3/217.abstract
AB The objective of the study was to increase the solubility, stability, and dissolution rate of atorvastatin calcium (ATN Ca), a poorly water-soluble 3-hydroxy 3-methyl glutaryl CoA (HMG-CoA) reductase inhibitor through inclusion complexation with β-cyclodextrin (β-CD). The phase solubility profile indicated that the solubility of ATN Ca was significantly increased in the presence of β-CD and was classified as AL-type, indicating the 1:1 stoichiometric inclusion complexes. Solid complexes prepared by physical mixing, kneading, co-evaporation, and freeze-drying methods were characterized using differential scanning calorimetry, fourier transform infrared spectroscopy, and powder X-ray diffractometry. In vitro studies showed that the solubility and dissolution rate of ATN Ca were significantly improved by complexation with β-CD with respect to the drug alone. In contrast, freeze-dried product showed higher solubility and dissolution rates than the other complexes. ATN Ca unit dosage form was developed and evaluated for physico-chemical properties, stability, and dissolution rate. The stability of tablets was studied and no significant changes were detected in the dissolution profile of tablets after 1 month.