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Possibility of a patch system as a new oral delivery system
Sudarat Eaimtrakarn1, Y V Rama Prasad, Shivanand P Puthli
1Department of Pharmacokinetics, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8414, Japan. takada@mb.kyoto-phu.ac.jp
International Journal of Pharmaceutics
|December 14, 2002
Summary
A novel oral patch system significantly enhances drug residence time in the gastrointestinal tract. This new delivery system shows potential for improved drug delivery and longer therapeutic effects compared to traditional tablets.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Biopharmaceutics
Background:
- Traditional oral drug delivery systems often face challenges with short gastrointestinal residence times, limiting drug absorption and efficacy.
- Developing novel systems to prolong drug contact with the GI mucosa is crucial for improving therapeutic outcomes, especially for poorly absorbed drugs.
Purpose of the Study:
- To design and evaluate a novel multi-layered oral patch system for increasing the residence time of model drugs in the gastrointestinal tract.
- To compare the in vitro and in vivo performance of the oral patch system against conventional tablets.
Main Methods:
- A three-layered oral patch was fabricated, comprising a water-insoluble backing, a drug-carrying adhesive layer (with fluorescein or fluorescein isothiocyanate-dextran), and a pH-sensitive enteric polymer.
- In vitro dissolution studies were conducted to determine the mean dissolution time (MDT) for both patch and tablet formulations.
- Pharmacokinetic studies in beagle dogs were performed using fluorescein and fluorescein isothiocyanate-dextran to assess plasma drug concentrations, area under the curve (AUC), and mean residence time (MRT).
Main Results:
- The oral patch system demonstrated significantly longer in vitro mean dissolution times for both model drugs compared to tablets.
- In vivo pharmacokinetic analysis in dogs revealed that the oral patch preparation resulted in a greater area under the plasma drug concentration-time curve (AUC) and a longer mean residence time (MRT) for both fluorescein and fluorescein isothiocyanate-dextran compared to tablets.
- Specifically, AUC and MRT values for fluorescein were 2.12 µgh/ml and 4.60 h for the patch versus 1.52 µgh/ml and 3.18 h for the tablet, respectively.
Conclusions:
- The developed three-layered oral patch system effectively increases the residence time of model drugs, including a macromolecular drug, within the gastrointestinal tract.
- This novel oral patch represents a promising new drug delivery system with the potential to enhance drug bioavailability and prolong therapeutic action.