Study On The Quality Of Modified Excipient â…  And Its Sustained- Release Properties

Objective: To illuminate the quality and sustained-release performance of modified excipients Ⅰ and to realize the balanced release of compound traditional Chinese preparation and to provide date for declaring a new excipient.Method: ①Using of dilatometry, viscometer, dissolution tester to detect excipient Ⅰand improved excipient Ⅰ about degree of swelling, viscosity,tablets’ morphology differences in the dissolution process, etc.②With double wavelength of UV,contents of amylose and branched polysaccharide of improved excipientⅠwere obtained. ③With morphological differences with tablets dissolution process as an indicator, the compatibility of improved excipientⅠwith other materials were studied, and the impact of viscosity on tablets’ dissolution rate was described. ④With Chuanping extract,different sustained-release tablets were prepared.HPLC was applied to measure the released degree of ephedrine, pseudoephedrine and scopolamine of chuanping sustained-release tablets,the relationship of dissolution rate and the release degrees.was illuminated.The ?2 value was applied to determine the balanced release of different tablets, descriptions were fitted with the different mathematical models. ⑤With moisture rate,swelling degree,viscosity, branched polysaccharide’ content, release degree,ect as an index,the stability of modified excipientⅠand chuanping sustained-release tablets after different influence were studied.Results: ① Improved excipient Ⅰ had significantly greater expantion degree and viscosity.Tablets with material Ⅰdissolved within 0.5 h,while tablets with improved excipient Ⅰ still present within 12 h. ② Branched polysaccharide measured in wavelength of 539 nm,its wavelength in reference was 700 nm and content was 81.6339%. ③ With different dosage of modified accessory I(40%,45%,50%) anddextrin, the prescriptions were obtained.The viscosity of the prescriptions were 105 cp,265cp,540 cp,while their dissolution rate decreased respectively. With 50% of modified accessory I and other accessories(lactose,dextin-sugar(1:1),starch-sugar(1:1),dextrin,microcrystalline cellulose), the prescriptions were prepared. Their viscosity were respectively 400 cp,435cp,475 cp,540cp,808.3cp.The viscosity was : lactose < dextin-sugar(1:1) < starch-sugar(1:1) < dextrin < microcrystalline,while dissolution rate were: microcrystalline > lactose > starch-sugar(1:1)> dextrin > dextin-sugar(1:1). The prescription that obtained 50% modified excipient I, 49% dextin and 1% magnesium stearate(tablers A) and the prescription that obtained 20% modified excipient I, 5%HPMC-K4 M,74% dextrin and 1% magnesium stearate(tablers B)were excellent while screening materials. The viscosity and dissolution rate were :pescription A>B.④The prescription A and B were excellent in sustained release and balanced release. The release degree of the three index components was positively correlated.Under the control of diffusion-dissolution,prescription A and B.released. ⑤ The swelling,viscosity of improved excipientⅠhad no significant effect under different influence,except that improved Ⅰ had moisture absorption under high humidity conditions. Applying improved Ⅰ, Chuanping sustained-release tablets had better release behavior.The release degree of Chuanping sustained-release tablets had no effect under high temperature, light, low temperature, acceleration for a month,while it changed much under humidity, acceleration for six months.Conclusion: Improved accessory I had sustained-release performance. Different accessories after compatibility would affect the balanced release of Chuanping sustained-release tablets.The improved accessory I could meet the demand of balanced release well.