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Published on: February 3, 2023
Formulation development of a biphasic release tablet-in-tablet system containing ketorolac tromethamine
Ping Zou1,2, Yuan Zeng3, Xiang-Ru Liao3
1Department of Pharmacy, The Central Hospital of Wuhan, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.
Plos One
|July 29, 2026
Summary
This study developed a novel biphasic-release tablet-in-tablet system for ketorolac tromethamine (KT) NSAID, improving pain management by offering immediate and extended drug release for better patient compliance.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Pain Management Therapeutics
Background:
- Ketorolac tromethamine (KT), a potent NSAID, requires frequent dosing due to its short half-life, impacting patient compliance.
- Existing formulations limit sustained pain relief and adherence.
Purpose of the Study:
- To formulate, develop, and optimize a novel biphasic-release tablet-in-tablet (TIT) system for ketorolac tromethamine.
- To achieve both immediate pain relief and extended drug release from a single dosage form.
Main Methods:
- A tablet-in-tablet (TIT) system with immediate-release (IR) outer layer and extended-release (ER) core was designed.
- The ER core was optimized using a 32 full factorial design with HPMC K100M and HPMC K4M as variables.
- Evaluations included pre/post-compression parameters, drug-excipient compatibility, and in vitro drug release kinetics.
Main Results:
- The optimal ER core (F1) showed 4.6% release at 0.5h and 66.1% at 12h (f2=51).
- Release kinetics followed first-order and anomalous non-Fickian diffusion (Korsmeyer-Peppas, n=0.831).
- The TIT formulation (F11) achieved ~30% release in 30 min and >90% over 24 hours with good physicochemical properties.
Conclusions:
- The developed biphasic-release TIT system offers a promising alternative for effective pain management with improved patient compliance.
- This novel formulation provides both rapid onset and prolonged therapeutic effect of ketorolac tromethamine.
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