The Research Of Compound Pseudoephedrine Hcl Fast Buccal Disintegrating Tablet

The aim of this study was to develop a fast buccal disintegrating tablet with a simple and low cost manufacturing process.The model drugs were Pseudoephedrine Hcl and Diphenhydramine citrate,and they were very water soluable and very bitterJn this case two factors would be clarified.They were how to improve the dissolving rate of the tablets and how to mask efficiently unpleasant taste of the active components.Therefore,thestudies as follows were carried out:First,formulation design including selection of excipients that were fast soluable and had good compactability;Second,selection of optimized preparation conditions;Thirxl,Some taste-masking methods were used to mask their bitter taste.Firstly,in order to prepare intrabuccally disintegrating tablets which quickly disintegrate and dissolve in the buccal cavity and have adequate hardness, several crystalline sugar alcohols were explored . The experimental results showed that sorbitol had excellent solubility and compactability properties and Erythritol had a fast dissolute character,.So,Sorbitol and Erythritol were selected as the basic excipients of buccal disintegrating tablet .In addition, 10% of microcrystalline cellulose was incorporated to improve the mechanical strength of tablets and facilitate the disintegration of tablets. A polynomial regression algorithm was used to relate the controlling factors such as tablet porosity and ratio of SorbitolrErythritol to disintegration time and tensile strength, and the optimum formulation and tableting conditions (expressed by porosity ) could be determined by contrast the contour plot of tensile strength against that of disintegration time , within this commen region ,the disintegration time was lower than 30s.The taste of fast buccal disintegrating tablets is very important to the patient compliance, in order to mask the astringent and bitter taste of active components, Diphenhydramine Hcl was transformed into Diphenhydramine citrate and solid dispersion of Diphenhydramine citrate was prepared by the solvent method with Eudragit El 00 to mask bitter taste. Fluid bed technology is one of the most common and effective methods in producing microcapsule which can mask bitter taste of drug.Spray solution used for coating particles commonly is water or alcohol ,if water soluable drug microparticles are coated in fluid bed ,they will adhere and form large mass,thus the coating process can not be carried out .In order to solve the adherence problem, Pseudoephedrine Hcl were first absorbed by microsphere silica gel ,and the drug laying method was applied to improve drug loading in the microspheres ,then they were coated with aqueous dispersion (Surelease ) as coating material.The effect of process conditions and formulations on coating were investigated. Microcapsules with taste-masked property were successfully prepared.In dissolution test, two active components can release over 90% of total amounts in 20 minutes and the amount of release is higher than conventional tablet, this shows that the taste masking materials can not retard the dissolution of drug. Stability test shows that buccal fast disintegrating tablet was stable under 60C temperatue , 75% humidity and 4000Lx light.