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Formulation of controlled-release pelubiprofen tablet using Kollidon(®) SR
Seh Hyon Song1, Bo Ram Chae1, Se Il Sohn1
1Daewon Pharm. Co., Ltd., 520 Cheonhodae-ro, Gwangjin-gu, Seoul 04994, Republic of Korea.
International Journal of Pharmaceutics
|August 6, 2016
Summary
A new controlled-release tablet (K2) of pelubiprofen (PLB) using Kollidon® SR demonstrated stability and effective drug delivery. This formulation enhances patient compliance by allowing twice-daily dosing unaffected by food.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Pharmacokinetics
Background:
- Pelubiprofen (PLB) is a novel non-steroidal anti-inflammatory drug.
- Developing a controlled-release formulation can optimize drug efficacy and patient compliance.
Purpose of the Study:
- To develop and characterize a matrix-type, controlled-release tablet formulation of pelubiprofen (PLB).
- To evaluate the in vitro drug release, stability, and in vivo pharmacokinetic profile of the developed formulation.
Main Methods:
- Screening of polymeric excipients including hypromellose, hydroxypropylcellulose, Eudragit® RS PO, and Kollidon® SR.
- Formulation optimization using Kollidon® SR, followed by accelerated stability testing.
- In vitro drug release studies at different pH values, analyzed using the Hixson-Crowell equation.
- Human pharmacokinetic studies using a randomized, 2-way crossover design and LC-MS/MS assay.
- In vitro-in vivo correlation analysis.
Main Results:
- A formulation with 12.4% w/w Kollidon® SR (K2 tablet) showed promising stability and suitable release characteristics (surface erosion, Hixson-Crowell fit).
- The active metabolite, PLB-transOH, showed significantly higher plasma levels than PLB.
- The K2 tablet exhibited comparable pharmacokinetic profiles to the immediate-release tablet (AUC ratios of 1.02 for PLB and 1.04 for PLB-transOH).
- A Level A in vitro-in vivo correlation was established.
- PLB-transOH's pharmacokinetics were not affected by food, unlike PLB.
Conclusions:
- The developed K2 tablet formulation of pelubiprofen offers stable, controlled release with predictable pharmacokinetics.
- The formulation's independence from food intake for PLB-transOH suggests potential for improved patient compliance with twice-daily dosing.
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