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Formulation and evaluation of ketorolac transdermal systems
Jun Shik Choi1, Young Ah Cho, In Koo Chun
1College of Pharmacy, Chosun University, Gwangju, Korea.
Drug Delivery
|March 17, 2007
Summary
This study found that specific pressure-sensitive adhesives and vehicles enhance ketorolac transdermal permeation. These systems offer a prolonged effect with potentially reduced toxicity compared to oral ketorolac.
Area of Science:
- Pharmacology and Pharmaceutics
- Drug Delivery Systems
- Dermatology
Background:
- Ketorolac is a non-steroidal anti-inflammatory drug (NSAID) used for pain management.
- Transdermal drug delivery offers potential advantages over oral administration, including sustained release and reduced systemic side effects.
- Optimizing the formulation of transdermal ketorolac systems is crucial for effective pain relief.
Purpose of the Study:
- To investigate the impact of different pressure-sensitive adhesives and vehicles on the in vitro permeation of ketorolac.
- To evaluate the in vivo pharmacokinetic profiles of optimized ketorolac transdermal systems.
- To establish a correlation between in vitro drug permeation and in vivo drug absorption.
Main Methods:
- In vitro permeation studies using various pressure-sensitive adhesives and vehicle combinations.
- In vivo pharmacokinetic studies in animal models to assess drug absorption and disposition.
- Analysis of key pharmacokinetic parameters such as Cmax, Tmax, and half-life.
- Correlation analysis between in vitro permeation flux and in vivo AUC0-infinity.
Main Results:
- Duro-Tak 87-2196 demonstrated the highest in vitro ketorolac permeation.
- Propylene glycol monolaurate-diethylene glycol monoethyl ether (DGME) (60:40, v/v) and propylene glycol monocaprylate-DGME (60:40, v/v) formulations showed the most favorable in vitro and in vivo results.
- Ketorolac transdermal systems exhibited decreased Cmax, prolonged Tmax, and extended half-life compared to oral administration.
- An excellent correlation was observed between in vitro permeation flux and in vivo AUC0-infinity.
Conclusions:
- Specific pressure-sensitive adhesives and vehicle compositions can significantly enhance ketorolac transdermal permeation.
- Optimized ketorolac transdermal systems may provide a prolonged therapeutic effect with a reduced risk of systemic toxicity.
- In vitro permeation data can reliably predict in vivo drug absorption for ketorolac transdermal systems.
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