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Tanshinol sustained-release pellets with absorption enhancer: optimization, characterization, pharmacokinetics and
Panpan Yu1, Shuangshuang Zhang1, Wenli Zhang1
1a Department of Pharmaceutics , China Pharmaceutical University , Nanjing , PR China.
Drug Development and Industrial Pharmacy
|February 7, 2017
Summary
Tanshinol sustained-release pellets (TS-SRPs) with sodium caprate (SC) absorption enhancer improved bioavailability and efficacy for angina treatment. This novel approach offers a promising strategy for hydrophilic drugs with poor absorption.
Area of Science:
- Pharmacology
- Drug Delivery Systems
- Materials Science
Background:
- Tanshinol (TS) exhibits poor intestinal absorption, limiting its therapeutic efficacy for angina.
- Developing effective drug delivery systems is crucial to enhance the bioavailability and therapeutic outcomes of poorly absorbed drugs.
Purpose of the Study:
- To develop tanshinol sustained-release pellets (TS-SRPs) incorporating sodium caprate (SC) as an absorption enhancer.
- To evaluate the in vitro release, stability, pharmacokinetic, and pharmacodynamic properties of the optimized TS-SRPs.
Main Methods:
- Single-pass intestinal perfusion in rats to determine optimal TS:SC ratio for enhanced permeability.
- Extrusion-spheronization to prepare pellet cores, followed by Eudragit coating.
- In vitro drug release studies, stability testing, pharmacokinetic analysis in rabbits, and pharmacodynamic evaluation in a rabbit angina model.
Main Results:
- A TS:SC weight ratio of 1:3 significantly enhanced TS permeability.
- Optimized TS-SRPs exhibited non-Fickian diffusion release kinetics and remained stable for three months.
- Pharmacokinetic studies showed a 1.97-fold increase in AUC0-24 and prolonged MRT compared to immediate-release pellets.
- Pharmacodynamic studies demonstrated steady and improved efficacy with synchronous drug concentration-efficacy.
Conclusions:
- Sustained-release pellets incorporating an absorption enhancer provide a viable strategy to improve the release and efficacy of hydrophilic drugs with poor intestinal absorption.
- The developed TS-SRPs offer a promising therapeutic option for angina treatment, enhancing both drug bioavailability and therapeutic effect.
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