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Dissolution Performance of High Drug Loading Celecoxib Amorphous Solid Dispersions Formulated with Polymer
1Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana, 47907, USA.
Pharmaceutical Research
|November 14, 2015
Summary
This study demonstrates that combining polymers in celecoxib amorphous solid dispersions (ASDs) enhances drug release and prevents crystallization. Formulating ASDs with a major polymer for release and a minor polymer for stability is a feasible strategy.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Celecoxib, a non-steroidal anti-inflammatory drug, often presents challenges with amorphous solid dispersions (ASDs) due to crystallization.
- Maintaining drug supersaturation is crucial for enhancing oral bioavailability.
Purpose of the Study:
- To assess the efficacy of various polymers in preventing celecoxib solution crystallization.
- To compare the drug release and crystallization behavior of celecoxib ASDs formulated with single or combined polymers.
Main Methods:
- Nucleation induction time measurements were used to evaluate polymer effectiveness in maintaining celecoxib supersaturation.
- Raman spectroscopy monitored crystallization kinetics in ASD suspensions.
- Dissolution studies were conducted under non-sink conditions.
Main Results:
- Pure amorphous celecoxib crystallized rapidly, but polymers inhibited this process, leading to supersaturated solutions.
- Cellulosic polymers (HPMC, HPMCAS) were more effective than polyvinylpyrrolidone (PVP) in maintaining supersaturation.
- Binary polymer combinations, particularly with cellulosic polymers and PVP, improved drug release and crystallization stability.
Conclusions:
- Incorporating a crystallization inhibitor as a minor component in ternary dispersions prolonged supersaturation.
- This research validates formulation strategies for ASDs using distinct polymers for specific functions like release and crystallization inhibition.
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