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Clopidogrel Napadisilate Monohydrate Loaded Surface-Modified Solid Dispersion: Physicochemical Characterization and
Young Hun Kim1, Dong Wuk Kim, Min Seok Kwon
1College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University.
Biological & Pharmaceutical Bulletin
|July 3, 2015
Summary
A novel spray-dried solid dispersion of clopidogrel napadisilate monohydrate (CNM) with hydroxypropylmethyl cellulose (HPMC) and Tween 80 significantly enhances drug solubility, dissolution, and oral bioavailability in rats, while improving stability.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Materials Science
Background:
- Clopidogrel napadisilate monohydrate (CNM) presents challenges in oral bioavailability and stability.
- Existing formulations may not fully address these limitations.
Purpose of the Study:
- To develop a stable, surface-modified solid dispersion of CNM with enhanced oral bioavailability.
- To optimize the formulation using spray-drying with specific excipients.
Main Methods:
- Spray-drying of CNM with hydroxypropylmethyl cellulose (HPMC) and Tween 80 using water as a solvent.
- Solid-state characterization using SEM, PXRD, and DSC.
- In vitro dissolution studies and in vivo oral bioavailability assessment in rats.
Main Results:
- The optimized CNM/HPMC/Tween80 (10/2.5/2.5) solid dispersion exhibited a 4.6-fold increase in drug solubility.
- Significantly improved dissolution profiles compared to CNM and comparable to clopidogrel bisulfate (CB).
- Demonstrated excellent stability and a 4-fold and 1.6-fold increase in AUC compared to CNM and CB, respectively.
Conclusions:
- The developed solid dispersion effectively enhances CNM solubility, dissolution, and oral bioavailability.
- This formulation addresses the stability issues associated with clopidogrel bisulfate.
- Spray-drying with HPMC and Tween 80 offers a promising approach for improving clopidogrel drug delivery.
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