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Published on: July 4, 2014
Characterization of 5-fluorouracil release from hydroxypropylmethylcellulose compression-coated tablets
Baojian Wu1, Ningyun Shun, Xiuli Wei
1Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, China.
Pharmaceutical Development and Technology
|May 19, 2007
Summary
Hydroxypropylmethylcellulose (HPMC) compression-coated tablets offer colon-specific drug delivery. Formulation adjustments, like HPMC viscosity and coating weight, effectively control drug release lag time and rate for targeted 5-fluorouracil delivery.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Materials Science
Background:
- Hydrogel compression-coated tablets enable delayed drug release, crucial for colon-specific delivery.
- Hydroxypropylmethylcellulose (HPMC) is a key polymer for developing such controlled-release systems.
- Understanding formulation variables is essential for optimizing gastrointestinal transit time-based drug delivery.
Purpose of the Study:
- To investigate the impact of formulation parameters on the in vitro release of 5-fluorouracil from HPMC compression-coated tablets.
- To identify key factors influencing release lag time (T(lag)) and zero-order release rate (k).
- To assess the potential for tailoring these tablets for colon-specific drug delivery.
Main Methods:
- Preparation of 5-fluorouracil core tablets using wet granulation and compression.
- Fabrication of HPMC compression-coated tablets with varying HPMC viscosity, lactose content, and coating weight.
- In vitro drug release studies conducted in distilled water using the Chinese Pharmacopoeia rotatable basket method.
Main Results:
- Drug release exhibited a lag time followed by zero-order kinetics for most formulations.
- Higher HPMC viscosity (K4M, K15M) increased T(lag) and decreased release rate (k).
- Increased lactose content in the outer shell reduced T(lag) and increased k; larger coating weight increased T(lag) and decreased k.
Conclusions:
- Release lag time and rate of 5-fluorouracil from HPMC compression-coated tablets can be precisely controlled.
- Formulation variables, including HPMC viscosity, lactose content, and coating weight, are critical for achieving colon-specific delivery.
- These findings support the development of tailored drug delivery systems for targeted colonic therapy.
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