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Solubility and stability enhancement of atorvastatin by cyclodextrin complexation
Chinna Reddy Palem1, Shweta Patel, Varsha B Pokharkar
1Department of Pharmaceutics, Bharati Vidyapeeth University, Poona College of Pharmacy, Erandwane, Pune, Maharashtra, India.
PDA Journal of Pharmaceutical Science and Technology
|January 15, 2010
Summary
Complexing atorvastatin calcium (ATN Ca) with beta-cyclodextrin (beta-CD) significantly enhances its solubility and dissolution rate. Freeze-dried complexes demonstrated superior performance, leading to stable tablet formulations.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Atorvastatin calcium (ATN Ca) is a poorly water-soluble HMG-CoA reductase inhibitor.
- Enhancing ATN Ca solubility and dissolution is crucial for improved bioavailability.
Purpose of the Study:
- To improve the solubility, stability, and dissolution rate of ATN Ca.
- To form inclusion complexes of ATN Ca with beta-cyclodextrin (beta-CD).
Main Methods:
- Phase solubility studies to determine ATN Ca-beta-CD stoichiometry.
- Preparation of solid complexes using physical mixing, kneading, co-evaporation, and freeze-drying.
- Characterization using DSC, FTIR, and PXRD.
- In vitro dissolution testing and stability studies of developed tablets.
Main Results:
- Phase solubility indicated an AL-type profile, suggesting 1:1 ATN Ca-beta-CD complexes.
- Complexation significantly increased ATN Ca solubility and dissolution rate compared to the free drug.
- Freeze-dried complexes exhibited the highest solubility and dissolution rates.
- Developed ATN Ca tablets showed good physico-chemical properties and stability over one month.
Conclusions:
- Beta-cyclodextrin inclusion complexation is an effective strategy to enhance ATN Ca solubility and dissolution.
- Freeze-drying is a promising method for preparing high-performance ATN Ca-beta-CD complexes.
- The developed ATN Ca dosage form is stable and exhibits improved dissolution characteristics.
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