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Gastric floating sustained-release tablet for dihydromyricetin: Development, characterization, and pharmacokinetics
Hao Liu1, Wenmei Zhao1, Qi Hu1
1School of Pharmacy, Southwest Medical University, Luzhou City, Sichuan, People's Republic of China.
Summary
Dihydromyricetin (DHM) has poor solubility, but a new gastric floating tablet (DHM-GFT) improves its bioavailability. This sustained-release formulation enhances DHM
Area of Science:
- Pharmacology
- Pharmaceutics
- Drug Delivery
Background:
- Dihydromyricetin (DHM) possesses significant pharmacological properties but suffers from poor aqueous solubility and stability.
- These limitations hinder DHM's efficacy and clinical application.
- Developing advanced drug delivery systems is crucial for overcoming DHM's bioavailability challenges.
Purpose of the Study:
- To develop and optimize a Dihydromyricetin-loaded gastric floating sustained-release tablet (DHM-GFT).
- To enhance the bioavailability and therapeutic potential of DHM through improved formulation.
- To assess the physicochemical properties, drug release profile, and pharmacokinetic behavior of the DHM-GFT.
Main Methods:
- DHM-GFT was prepared using powder direct compression.
- Tablet formulation was optimized for floating characteristics and drug release kinetics.
- In vitro floating lag time, floating duration, and drug release studies were conducted in acidic media.
- Pharmacokinetic studies were performed to evaluate in vivo performance compared to DHM powder.
Main Results:
- The optimized DHM-GFT demonstrated a short floating lag time (<10 s) and extended floating duration (>12 h) in acidic conditions.
- The formulation achieved 12-hour sustained release of DHM, indicating suitability for twice-daily dosing.
- Pharmacokinetic analysis revealed significantly prolonged in vivo drug residence time and enhanced bioavailability of DHM from DHM-GFT compared to DHM powder.
Conclusions:
- DHM-GFT formulation effectively overcomes the solubility and stability issues of DHM.
- The gastric floating and sustained-release properties of DHM-GFT significantly improve DHM bioavailability.
- DHM-GFT shows promising potential for advancing DHM's clinical application and warrants further development.
Keywords:
BioavailabilityDihydromyricetinGastric floating tabletPharmacokineticsStabilitySustained releaseMore Related Videos
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