Formulation and Evaluation of Pulsatile Drug Delivery System of Metoprolol Tatrate

Abstract

Background: Hypertension exhibits marked circadian variations, with an increased risk of cardiovascular events during the early morning hours. Conventional dosage forms fail to synchronize drug release with these biological rhythms, highlighting the need for chronotherapeutic drug delivery systems. Pulsatile drug delivery offers a promising strategy by providing a programmed lag phase followed by rapid drug release at the desired therapeutic time.

Objective: The present study aimed to develop and evaluate a compression-coated pulsatile drug delivery system of Metoprolol Tartrate for chronotherapeutic management of hypertension.

Materials and Methods: Metoprolol Tartrate core tablets were prepared by direct compression and enteric coated using Eudragit L100. The coated core tablets were subsequently compression coated with optimized immediate-release and sustained-release layers. The formulations were evaluated for pre- and post-compression parameters, FTIR drug–excipient compatibility, acid uptake, drug content, and in vitro dissolution studies.

Results: FTIR analysis confirmed the compatibility of Metoprolol Tartrate with the selected excipients. The optimized formulation exhibited satisfactory physicochemical properties and complied with pharmacopeial specifications. The enteric coating provided effective gastric protection, while the compression-coated system produced a distinct lag phase followed by controlled drug release, achieving 81.85% cumulative drug release within 8 hrs.

Conclusion: The developed compression-coated pulsatile tablet successfully achieved time-dependent release of Metoprolol Tartrate and demonstrated its potential as a chronotherapeutic drug delivery system for hypertension. The formulation may improve therapeutic efficacy by synchronizing drug release with the circadian pattern of cardiovascular events.