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Verapamil sustained release: new formulation and convolution.

Chien Nguyen¹, J Mark Christensen, James W Ayres

¹Industrial Department of Pharmacy, Hanoi University of Pharmacy, Hanoi, Vietnam.

Pharmaceutical Development and Technology

|October 21, 2010

Summary

This study introduces a new bead formulation for verapamil hydrochloride, achieving high drug loading and controlled release. The innovative coating technology ensures stable, non-agitation-sensitive, zero-order drug delivery for up to 14 hours.

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Area of Science:

Pharmaceutical Technology
Drug Delivery Systems
Materials Science

Background:

Verapamil hydrochloride is a relatively insoluble drug requiring advanced formulation for optimal delivery.
Achieving zero-order drug release and non-agitation sensitivity is a significant challenge in pharmaceutical development.

Purpose of the Study:

To develop a novel bead formulation of verapamil hydrochloride with high drug load and controlled release characteristics.
To investigate the impact of coating parameters on drug release kinetics and stability.

Main Methods:

Utilized extrusion and spheronization for high drug load bead production.
Applied a coating of ethylcellulose with lactose (channeling agent) to the beads.
Evaluated drug release profiles under various agitation speeds and media conditions (USP basket and paddle methods).

Main Results:

The novel formulation achieved a high drug load and allowed for a uniform, robust coating.
Adjusting coating thickness and ethylcellulose/lactose ratio resulted in approximately zero-order drug release for up to 14 hours.
The formulation demonstrated non-agitation sensitivity across different tested conditions (75-200 rpm, KCl and pH media).

Conclusions:

The developed bead formulation offers a promising approach for sustained and stable verapamil hydrochloride delivery.
The formulation's zero-order release profile and non-agitation sensitivity represent significant advancements in oral drug delivery.
This technology has the potential for application to other relatively insoluble drugs requiring controlled release.