Formulation Development of Generic Omeprazole 20 mg Enteric Coated Tablets

Christopher Oswald Migoha^1,2, Eliangiringa Kaale², Godliver Kagashe³

¹Tanzania Food and Drugs Authority, Dar es Salaam, Tanzania.
²Pharm R&D Lab, School of Pharmacy, Muhimbili University of Health and Allied Sciences, Dar es Salaam, Tanzania.
³Department of Pharmaceutics , School of Pharmacy, Muhimbili University of Health and Allied Sciences, Dar es Salaam, Tanzania.

DOI: 10.4236/pp.2015.67031                

Abstract

Omeprazole is a potent proton pump inhibitor with powerful inhibition of secretion of gastric juice. Oral site-specific drug delivery systems have recently attracted a great interest for the local treatment of bowel disease and for improving systemic absorption of drugs which are unstable in the stomach. However, microenvironment in the gastrointestinal tract and varying absorption mechanisms cause hindrance for the formulation and optimization of oral drug delivery. The objective of the study was to develop and optimize enteric coating process for omeprazole tablets. Different batches of core tablets were sub coated, one set sub coated with opadry and another with a mixture of light magnesium oxide, magnesium stearate and absolute alcohol omeprazole magnesium. Seal coating was applied by using opadry to achieve certain weight gain and to protect omeprazole from acidic coating polymers. A comparative dissolution test was performed. The variation of thickness and diameter were observed to be minimal with a weight gain of 3% - 4% of enteric polymer. Disintegration test showed that in each tested batch the enteric coated layer remained intact in 0.1N HCl for 2 hours and when exposed to alkaline media of phosphate buffer pH 6.8, it dissolved within few minutes. Dissolution release was 98.8% to 102.4% within two hours when the product was exposed to phosphate buffer pH 6.8 after 2 hours. The similarity and dis-similarity factors were calculated and observed to be 54 to 61 and 4 to 5 respectively. Therefore a simple and good enteric coating process was developed and tested with potential for transfer this technology into local pharmaceutical industries using cheap and easily available materials.

Keywords

Omeprazole Magnesium, Enteric Coating, Tablets, Kollicoat (Methacrylic Acid/Ethyl Acrylate Copolymers) (MAE)

Conflicts of Interest

The authors declare no conflicts of interest.

References

[1]	Blanchi, A., Delchier, J.C., Soule, J.C., Payen, D. and Bader, J.P. (1982) Control of Acute Zollinger-Ellison Syndrome with Intravenous Omeprazole. Lancet, 2, 1223-1224.
[2]	Wurster, D.E. (1957) U.S Patent 2,799,241. Wisconsin Almini Research Foundation.
[3]	Wurster, D.E. (1959) Air-Suspension Technique of Coating Drug Particles. A Preliminary Report. Journal of the American Pharmaceutical Association, 48, 451-454. http://dx.doi.org/10.1002/jps.3030480808
[4]	Hardman, J.G., Limburd, L.E., Molinoff, P.B., Ruddon, R.W. and Gilman, A.G. (Eds.) (1996) Goodman & Gilman’s The Pharmacological Basis of Therapeutics. 9th Edition, McGraw-Hill, New York.
[5]	Nair, A.B., Gupta, R., Kumria, R., Jacob, S. and Attimarad, M. (2010) Formulation and Evaluation of Enteric Coated Tablets of Proton Pump Inhibitors. Journal of Basic and Clinical Pharmacy, 1, 215-221.
[6]	Mäder, K., Bräunig, K., Meyer, K. and Kolter, K. (2005) Development and Stability Studies of Enteric Omeprazole Formulations Based on Kollicoat® MAE Polymers. BASF Aktiengesellschaft, Development Pharma Ingredients, Ludwigshafen.
[7]	United States Pharmacopoeia (USP) 30NF25.
[8]	http://www.pharmpedia.com/Tablet:Tablet_coating
[9]	Mukharya, A., Chaudhary, S., Bheda, A., Mulay, A., Mansuri, N. and Laddh, N. (2011) Stable and Bioequivalent Formulation Development of Highly Acid Labile Proton Pump Inhibitor: Rabeprazole. International Journal of Pharmaceutical Research and Innovation, 2, 1-8.
[10]	FDA (2000) Guidance for Industry: Waiver of in Vivo Bioavailability and Bioequivalence Studies for Immediate-Release Solid Oral dosage Forms Based on a Biopharmaceutics Classification System.