Intragastric positioning of two concurrently ingested pharmaceutical matrix dosage forms

Area of Science:

• Nuclear medicine
• Pharmaceutical sciences
• Gastroenterology

Background:

• Accurate monitoring of drug release and transit within the gastrointestinal tract is crucial for pharmaceutical development.
• Understanding gastric residence time is essential for optimizing oral drug delivery systems.
• Existing methods may lack the precision or duration needed for comprehensive intragastric monitoring.

Purpose of the Study:

• To present a triple nuclide scintigraphic technique for precise, long-term intragastric monitoring of concurrently ingested hydrophilic matrix pharmaceutical forms.
• To validate the technique in healthy volunteers.
• To assess the influence of pharmaceutical and physiological parameters on gastric residence time.

Main Methods:

• Developed a triple nuclide scintigraphic technique using ion exchange resin-coupled 201T1- and 111In-oxinate for drug monitoring.
• Utilized 99mTc-pertechnetate oral solution to delineate the stomach.
• Validated the method in healthy volunteers, evaluating effects of matrix size, density, and subject posture.

Main Results:

• The technique enabled precise and lasting intragastric monitoring of two hydrophilic matrix forms simultaneously.
• Demonstrated the ability to measure the impact of galenic parameters (matrix size, density) on gastric residence time.
• Showed that physiological parameters, such as subject posture, significantly affect gastric residence time.

Conclusions:

• The triple nuclide scintigraphic technique is a validated and effective tool for intragastric drug monitoring.
• This method provides valuable insights into factors influencing oral drug absorption and efficacy.
• The technique facilitates the optimization of pharmaceutical formulations and understanding of drug disposition in vivo.