Pharmaceutical development and characteristics of a new glyceryl trinitrate transdermal patch

Area of Science:

• Pharmaceutical Sciences
• Dermatology
• Cardiology

Background:

• Glyceryl trinitrate (GTN) is a key vasodilator for angina pectoris.
• Transdermal drug delivery systems offer advantages in sustained release and patient compliance.
• Development of novel drug delivery systems aims to optimize therapeutic efficacy and patient experience.

Purpose of the Study:

• To describe the pharmaceutical development and characteristics of Epinitril (EPI), a new GTN transdermal patch.
• To evaluate the GTN release rate and skin permeation properties of the EPI patch.
• To assess the patient-friendliness and potential for improved compliance with EPI.

Main Methods:

• Characterization of EPI patch composition, including GTN concentration and matrix properties.
• In vitro evaluation of GTN release using disk assembly dissolution, artificial membrane, and human skin diffusion tests.
• Assessment of patch physical characteristics (size, thinness, flexibility, transparency) and tolerability.

Main Results:

• EPI is a thin, transparent patch with GTN uniformly dissolved in an acrylate copolymer adhesive.
• The patch exhibits a high GTN flux rate (33 micrograms/cm2/h) due to high concentration and thinness.
• EPI was developed in three strengths (5, 10, 15 mg/24h) for dose individualization.
• While in vitro tests did not yield reliable in vitro-in vivo correlations, they aided formulation development.
• EPI demonstrated favorable characteristics including ease of application/removal and good tolerability.

Conclusions:

• Epinitril (EPI) is a well-characterized glyceryl trinitrate transdermal patch designed for enhanced drug delivery.
• The patch's formulation and physical attributes contribute to high GTN flux and absorption.
• EPI's patient-friendly features suggest potential for improved adherence in long-term angina pectoris management.