Abstract:

Omeprazole pellets can be made by different methods which are generally time consuming and labor intensive. The current study was carried out to research the feasibility of producing the spherical pellets of Omeprazole using sieving-spheronization. One more optimized formulation was prepared by extrusion-spheronization process to differentiate between the physical parameters of both methods. The omeprazole pellets consisted of sodium lauryl sulphate, microcrystalline cellulose, polyvinylpyrrolidone K 30 and polyethylene glycol 6000. The omeprazole delay release system was established by coating the formulated pellets with aqueous dispersion of Kollicoat 30 DP. The spheronization speed, moisture content and residence time was found to influence the final properties of omeprazole pellets developed by extrusion-spheronization and sieving-spheronization. The Mann-Whitney test discovered that both given methods produced mostly same characteristics of the pellets in terms of, flowability (p=0.677), friability (p=0.553), hardness (p=0.103) and density (bulk, p=0.514, tapped, p=0.149) except the particle size distribution (p=0.004). The percent drug release from the coated formulation prepared using sieving-spheronization and extrusion spheronization was noted to be 84.12 ± 1.10% and 82.67 ± 0.96%, consequently. Termination profiles of both the formulations were same as indicated by the values of f1 and f2, 1.52 and 89.38, respectively. The formulation developed by the sieving-spheronization and the commercial reference product, Zimore also showed similar termination profiles (f1=1.22, f2=91.52). The pellets could be prepared using sieving-spheronization. The process is easy, simple, requires less time, labor-consuming and economical as compared to extrusion-spheronization process.

Introduction:

The main aim of using delayed release products is to protect the drug from gastric fluids, to decrease gastric distress happened due to the drugs that particularly irritate the stomach or making easy the gastrointestinal transit for drugs which are better absorbed from intestine. Enteric polymers are becoming very popular because of their property of intact in the stomach, but will dissolve and release the contents once it arrives at the small intestine, their main focus is to postpone the release of drugs, which are disabled by the stomach contents or may stimulate bleeding or nausea by the irritation of gastric mucosa. Omeprazole is a potent inhibitor of gastric secretion utilized for the cure of acid peptic disease, gastric ulcer, duodenal ulcer, and Zollinger-Ellisonsyndrome and for handling the GastroEsophageal Reflux Disease (GERD). It is highly acid labile and offers many formulation tests to secure it from acidic environment of the stomach; an enteric coated pellets formulation was tried in the present study.

Omeprazole Usage and Dosage

Omeprazole is widely used in treating the peptic ulcers, aspiration problems, gastro-oesophageal reflux disease, dyspepsia and the Zollinger-Ellison syndrome. Omeprazole is a proton pump inhibitor which inhibits emission of gastric acid by absolutely blocking the enzyme system of hydrogen and potassium adenosine triphosphatase, the “proton pump” of the gastric parietal cell. The drug is used in conditions, where the inhibition of gastric acid secretion is beneficial.

Chemically known as 5-methoxy-2-[(RS)-[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]-sulphinyl]-1H-benzimidazole, it is reported in USP, BP of the pharmacopoeias. The product is available in semi-finished formulation in a pelletized structure. The API is made under a strict control with stringent details on the impurity profile and also the molecule size, the utilization of right polymorphs also. The excipients utilized are particularly chosen and are non-encroaching. The product can likewise be offered in a pellet size appropriate for use in a suspension or for compression in tablets.

The dose of Omeprazole may need to be decreased in patients with hepatic impairment. The drug has been determined in formulation and in biological fluids with a variety of methods, like spectrophotometry, HPLC with UV detection, and liquid chromatography merged with tandem mass spectrometry. The overview includes most relevant analytical methodologies used for the resolution of the drug since the origin.