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Process optimization, characterization and evaluation in vivo of oxymatrine-phospholipid complex
Peng-Fei Yue1, Hai-Long Yuan, Xian-Yi Li
1Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China. ypfpharm@126.com
International Journal of Pharmaceutics
|December 17, 2009
Summary
Researchers developed an oxymatrine-phospholipid complex (OMT-PLC) to improve oxymatrine
Area of Science:
- Pharmacology
- Drug Delivery
- Biochemistry
Background:
- Oxymatrine has limited oral bioavailability.
- Phospholipid complexation is a strategy to enhance drug delivery.
Purpose of the Study:
- To prepare and optimize oxymatrine-phospholipid complex (OMT-PLC).
- To enhance the oral bioavailability and hepatocyte permeability of oxymatrine.
Main Methods:
- Central composite design for process optimization.
- Physicochemical characterization using DSC, XRD, and partition coefficient.
- In vitro hepatocyte permeability and in vivo pharmacokinetic studies in rats using HPCE.
Main Results:
- Optimized OMT-PLC prepared with non-covalent bonds.
- Improved hepatocyte permeability and solubility of OMT-PLC.
- Significantly increased oral bioavailability in rats (p<0.05) with enhanced pharmacokinetic parameters (Tmax, Cmax, AUC).
Conclusions:
- OMT-PLC formation enhances oxymatrine's oral bioavailability.
- Improved solubility and permeability contribute to increased drug absorption.
- OMT-PLC is a promising approach for oral delivery of oxymatrine.
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