Development and quality evalution of prolonged release tablet contained chlorpheniramine maleate

Abstract

Background: Chlorpheniramine maleate is widely used in the treatment of allergic diseases. Chlorpheniramine maleate reduces the symptoms of allergic reactions caused by histamine, such as nasal congestion, sneezing, tearing, itchy eyes, and redness. The drug is well absorbed from the gastrointestinal tract when taken orally, and after 30-60 minutes after use, the concentration in the blood plasma reaches a maximum, which leads to side effects such as drowsiness and blurred vision. We decided to develop matrix tablets with extended release to to improve the therapeutic effect and reduce the side effects of drugs and suitable for use. Aim: Development for the production of prolonged release chlorpheniramine maleate tablets in the country and quality evaluation. Materials and Methods: Four design tablets were obtained by wet granulation method and estimated each tablet contains 12 mg of chlorpheniramine maleate. Hydroxypropyl methylcellulose k4M, E5M were used as matrix former, microcrystalline cellulose and sodium dihydrogen phosphate (2 molecules of water) as diluents, purified water as a binder, talc and magnesium stearate as a lubricant in different ratios. The quality of the tablets was determined by criterias such as appearance the average weight, amount of active ingredient, hardness, disintegration, dissolution and bacterial contamination according to the National Pharmacopoeia of Mongolia (NPM) and the United States Pharmacopoeia (USP). Results: The design C2 and C4 tablets met the pharmacopoeial requirements. Drug release were determined in vitro and design C4 released 45.3%, 66.3%, and 96.2% after 3, 6 and 12 hours. Therefore, C4 tablets were the most suitable. Discussion: As a result of our research on the production of prolonged release matrix tablets containing chlorpheniramine maleate, we found that it is suitable to produce matrix tablets based on wet granulation technology, this is similar to the technology used by researchers D.Otgonsuren, D.Jambaninj and D.Davaadagva to produce matrix tablets from Glycyrrhiza uralensis fisch by wet granulation of matrix tablets. Our drug C4 matrix tablet drug release is 45.3% at 3 hours, 66.3% at 6 hours, and 96.2% at 12 hours, which is in line with US pharmacopoeia requirements. Conclusion: Matrix tablets with prolonged release of chlorpheniramine maleate were found to be suitable for C4 formulation and wet granulation. Design C4 with prolonged release of chlorpheniramine maleate meets the quality requirements in terms of appearance, average weight, hardness, assay, drug release and microbiological parameters.