Preparation Of Betahistine Mesilate Controlled Porosity Osmotic Pump Tablets And Study On Quality Standard

ObjectiveBetahistine Mesilate is a class of histamine drugs which can play quasi-histamine effects through activating histaminergic(H₁) receptor.It can specifically increase the blood circulation of the cerebrum, brain stem and the micro-circulation of inner ear, eliminate the hydrolabyrinth, and can treat dizziness and giddiness caused by kinds of diseases. But conventional tablet is usually administered three times a day, which would lead to large fluctuation in drug plasma concentration. Betahistine Mesilate controlled porosity osmotic pump tablets can releasing drug at the rate of approximate zero-order, improving compliance of patients, reducing risk of adverse reactions, ensure the safety and efficiency of the medication.MethodsUV-visible spectrophotometry and similarity factor( f₂ ) were used as analytical method; By using single-factor test and orthogonal test, preparation technology was optimized. And MCC, mannitol, CA, PEG-1500, DBP and acetone were respectively used as stuffing bulking agent, penetrating agent, coating material, channeling agent, plasticizer and solvent; Test the stability of Betahistine Mesilate controlled porosity osmotic pump tablets by appearance, content and release in vitro; The quality standard is set up, according to the related requests of the rules of preparation of Chinese Pharmacopoeia (2010 edition,â…¡part). ResultsThe optimized formulation are mannitol: 80mg, PEG-1500: 30%, DBP: 20%, and coating increases 4% on weight,CA: 3%. The drug release profiles in vitro followed zero-order kinetics (r=0.9926).Under strong light, high temperature, the tablets sample had good stability. But at high moisture of air it shows extrence unstable.UV spectrometry was established for assay, and the results revealed that this method had there advantages such as good precision and high recovery rate.ConclusionsBetahistine Mesilate controlled porosity osmotic pump tablets had good effect of controlled release property, and simple in preparation technology, stable in quality,but must store in tight containers.