Sustained release phenylpropanolamine hydrochloride from ATO 888 matrix

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Phenylpropanolamine HCl is a drug requiring controlled release for therapeutic efficacy.
• Compritol, a waxy material, is explored as a retardant for sustained drug delivery systems.

Purpose of the Study:

• To develop sustained release phenylpropanolamine HCl tablets using Compritol as a retardant.
• To investigate the impact of Compritol wax concentration and matrix formation method on drug release kinetics.
• To evaluate the compaction properties of the developed tablet formulations.

Main Methods:

• Tablets were formulated with a constant drug concentration (10% w/w) and varying Compritol levels (10-50% w/w).
• Two preparation methods were employed: physical mixture and solid dispersion.
• In vitro drug release studies and compaction profile analysis were conducted.

Main Results:

• Tablets with 10% Compritol prepared via solid dispersion showed 97% drug release in 6 hours.
• Increasing Compritol content to 30% and 50% reduced drug release to 72% and 30%, respectively.
• Physical mixture formulations exhibited higher drug release compared to solid dispersion.
• Compritol incorporation reduced tablet ejection forces, and solid dispersion release followed the Higuchi diffusion model.

Conclusions:

• Compritol is an effective retardant for phenylpropanolamine HCl sustained release tablets.
• Solid dispersion method with optimal Compritol concentration provides predictable controlled release.
• Formulation parameters significantly influence drug release profiles and compaction behavior.