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Related Experiment Videos

Percutaneous nitroglycerin absorption in rats.

S T Horhota, H L Fung

    Journal of Pharmaceutical Sciences
    |May 1, 1979
    PubMed
    Summary
    This summary is machine-generated.

    Percutaneous nitroglycerin absorption in rats was surprisingly poor from liquid states compared to ointments. This indicates drug absorption is highly vehicle dependent, not just driven by thermodynamics.

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    Area of Science:

    • Pharmacology
    • Dermatology
    • Drug Delivery Systems

    Background:

    • Percutaneous drug absorption is crucial for topical therapies.
    • Nitroglycerin's efficacy is often limited by inconsistent skin penetration.
    • Drug thermodynamics are typically considered the primary driver of absorption.

    Purpose of the Study:

    • To investigate the absorption of nitroglycerin through rat skin.
    • To evaluate the influence of different formulations on nitroglycerin bioavailability.
    • To determine if drug thermodynamics alone explain percutaneous absorption.

    Main Methods:

    • Studied percutaneous absorption in shaved rats over 4 hours.
    • Monitored unchanged plasma nitroglycerin concentrations.
    • Compared absorption from neat liquid, alcoholic solution, commercial ointment, and experimental polyethylene glycol (PEG) gels.

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    Main Results:

    • Absorption was significantly poorer from neat liquid and alcoholic solutions compared to a commercial ointment.
    • Experimental aqueous gels with PEG 400, even with excess solubilizer, resulted in very low plasma nitroglycerin levels.
    • Investigated and ruled out volatilization, droplet formation, and vehicle occlusion as primary causes.

    Conclusions:

    • Percutaneous nitroglycerin absorption is highly dependent on the vehicle formulation.
    • Simple thermodynamic activity of nitroglycerin does not adequately explain observed absorption differences.
    • Vehicle composition plays a critical, non-thermodynamic role in topical drug delivery.