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Updated: Jan 31, 2026
07:47
ScanLag: High-throughput Quantification of Colony Growth and Lag Time
Published on: July 15, 2014
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Fenofibrate modified-release pellets with lag phase and high oral bioavailability.
Fang Li1, Xin Zheng2, YongChu Bao3
1NHC Key Laboratory of Reproduction Regulation (Shanghai Institute of Planned Parenthood Research), Fudan University, and Shanghai Engineer and Technology Research Center of Reproductive Health Drug and Devices, Shanghai, China, fenglinglinxin@163.com.
Drug Design, Development and Therapy
|January 8, 2019
Summary
A new delayed-release fenofibrate formulation enhances bioavailability and offers potential safety benefits when combined with statins for mixed dyslipidemia treatment. This innovative preparation aims to reduce muscle toxicity risks associated with combination therapy.
Area of Science:
- Pharmacology
- Drug Delivery Systems
- Cardiovascular Medicine
Background:
- Mixed dyslipidemia management often involves combination therapy with fenofibrate and statins.
- Current guidelines recommend fenofibrate-statin combination therapy.
- Simultaneous administration can increase the risk of muscle toxicity.
Purpose of the Study:
- To develop an innovative delayed-release fenofibrate preparation.
- To mitigate muscle toxicity risk by altering fenofibrate's pharmacokinetic profile.
- To enhance the oral bioavailability of the modified-release formulation.
Main Methods:
- Micronized fenofibrate was processed into drug-loaded cores using powder layering.
- Multiparticulate pellets were coated with various formulations (Eudragit®, EC/HPMC) and screened in vitro.
- Optimized formulations were evaluated in beagle dogs against commercial fenofibrate preparations.
Main Results:
- In vivo studies showed a lag phase followed by rapid and complete fenofibrate release from optimized pellets (R1, R2).
- Relative bioavailabilities of R1 and R2 were 100.4% and 201.1%, respectively.
- These bioavailabilities were significantly higher than the commercial sustained-release pellets (Lipilfen® at 67.2%).
Conclusions:
- The developed modified fenofibrate pellets exhibit enhanced bioavailability and delayed-release characteristics.
- This formulation holds potential for improved safety and patient compliance in combination therapy with statins.
- This represents the first reported instance of a delayed-release fenofibrate preparation.
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