Fabrication and Evaluation of Oral Multi-Particulate Tablets of Proton Pump Inhibitors: Esomeprazole as a Model

Abstract

Radhwan N. Al-Zidan, Saad M. Majeed, and Mohammed K. Al-Shaheen

Esomeprazole, a proton pump inhibitor, inhibits gastric acid secretion and used to treat many acid-related gastric/duodenal diseases in adults and children. The present article investigated the development of an oral delayed-release multi-particulate tablet of Esomeprazole, which consists of enteric coated pellets of esomeprazole. Such dosage form offers the healthcare providers a higher dosage flexibility to give the appropriate dose regarding the patient age and the disease state of the patient. In addition, the proposed dosage form enhances the physicochemical stability of coated drug by forming multi-unite pellets system (MUPS) ®. Compression of coated pellets is an arduous process and requires the optimization of several formulations and processing variables; among it includes size, nature, and amount of tableting additives as well as the applied compression force. In this study, several trials were executed to prepare a satisfactory product by using the direct compression method with different directly compressible fillers, having suitable cushioning properties, like spray dried lactose, microcrystalline cellulose (MCC), and dibasic calcium phosphate. In this study, it was found that adding up to 49% of (MCC) offered greater protection to the coated pellets, and greatly maintained the integrity of the multi-particulate tablet—even under a compression force of about 3 tons. This research work led to successful formulation of esomeprazole delayed release multi-particulate tablets containing enteric coated pellets equivalent to 20 mg of esomeprazole magnesium trihydrate using the direct compression method.