Formulation and evaluation of metoprolol Extended-Release pellets

Abstract

Introduction: Metoprolol is a beta-1 selective blacker, commonly used in patients with pectoral angina, hypertension, and types of heart failures. It has a half life 3 to 7 hours. When dose is missing it may cause nocturnal attack, so attention was made to develop the extended release of metoprolol. Multi-unit system, the total drug is divided over many units. Failure of a few units may not be as consequential as failure of a single-unit system. Palletization can be defined as an agglomeration process that converts fine powders or particles of bulk drug and excipients into small, free-flowing, more or less spherical units. Pellets offer a great flexibility in pharmaceutical solid dosage from design and development. Aim: Our goal and of the present study is to develop a pharmaceutically stable and quality improved formulation of metoprolol extended release pellets. In addition to profitting the benefits of pellet, by creating the extended release formulation to reduce daily intake, it will increase the patient's acceptance to treatment period (especially in cardiac patients). Methods: In this study, Extrasion-Spheronization has been developed to provide extended release. produced pellets, in the terms of micromeritic properties such as particle size, density, etc, will be checked. And then we will test dissolution on pellets that their mechanical properties are suitable. Results: After several stages of testing and preparation of various formulations, we have obtained a formulation that in addition to its appropriate micromeritic properties, shows acceptable release and dissolution test. Conclusion: According to the studies and tests carried out in this study, we were able to produce an extended release in the metoprolol drug by Stearyl alcohol fatty acid. Based on this research, we found that the production of pellets using by Extruder-spheronizer method depends on a number of factors, such as water, amount and type of excipient, rpm of extruder and spheronizer and so on.