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Enhanced Bioavailability and Dissolution of Atorvastatin Calcium from Floating Microcapsules using Minimum Additives
Furquan Nazimuddin Khan1, Mohamed Hassan G Dehghan
1Y. B. Chavan College of Pharmacy, Department of Pharmaceutics, Dr. Rafiq Zakaria Campus, Rauza Bagh, Aurangabad-431001, India.
Scientia Pharmaceutica
|March 8, 2012
Summary
Floating microcapsules improved atorvastatin calcium (ATC) bioavailability by enhancing gastric residence time. The developed microcapsules significantly increased drug dissolution and absorption compared to conventional formulations.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Biopharmaceutics
Background:
- Atorvastatin calcium (ATC) exhibits poor bioavailability due to low solubility in acidic environments.
- Optimal absorption of ATC occurs in the upper gastrointestinal (GI) tract.
- Extended gastric residence time is crucial for enhancing ATC bioavailability.
Purpose of the Study:
- To develop multiple-unit floating microcapsules of atorvastatin calcium (ATC).
- To improve the gastric residence time and bioavailability of ATC.
- To enhance the dissolution rate of ATC using dioctyl sodium sulphosuccinate (DSS).
Main Methods:
- Floating microcapsules were prepared using the emulsion-solvent evaporation technique.
- Dioctyl sodium sulphosuccinate (DSS) was incorporated as a dissolution enhancer.
- Characterization included SEM, DSC, PXRD, particle size, drug entrapment, stability, and in-vitro dissolution studies.
Main Results:
- Spherical ATC-loaded floating microcapsules with high drug loading (96.55%) and optimal particle size (~28.10 μm) were successfully prepared.
- Microcapsules formulated with DSS demonstrated significantly higher in-vitro drug dissolution rates.
- The optimized formulation (AT4) achieved 97.86% drug dissolution, markedly exceeding the reference product (54%) over 12 hours.
- Pharmacokinetic studies in rabbits showed a 1.7-fold increase in ATC bioavailability with AT4 microcapsules.
Conclusions:
- Multi-unit floating microcapsules are an effective strategy for improving the bioavailability of atorvastatin calcium.
- The incorporation of DSS as a dissolution enhancer significantly boosts ATC release from floating microcapsules.
- This novel drug delivery system holds promise for enhancing the therapeutic efficacy of atorvastatin calcium.
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