Study On Modified Excipientâ…¡

Objective:Explore modified excipient Ⅱpreparation,to clarify the properties、compatibility and stability of modified excipient Ⅱ, to provide the evidence for the development and application of modified excipient Ⅱ.Methods:① Use viscosity as index, compare the different modified excipient Ⅱ samples, choose modified excipient Ⅱ preparate method, and use the orthogonal experimental method to optimize the parameters.② Use solubility, p H, viscosity,, degree of swelling as index to compare the properties change between excipient Ⅱ and modified excipient Ⅱ.③ Use HPLC method,establish modified excipient Ⅱ Chuanping sustained-release tablets release assay methods in vitro,.④Take dissolution test in vitro and HPLC method,use release degree and similarity factor as index to investigate the balance release of complex components from different modified ExcipientⅡcompatibility.⑤ Use humidity,high-temperature, light test, take properties and balance release as indext o investigate the modified excipientⅡ stability.Results:①Hydrolysis alcohol precipitation method is more propriate for modified excipient Ⅱ, the preparation Parameters are: liquid ratio is 1: 4, the basic catalyst is b1, boiling water bath for 0.5h, and alcohol precipitation is e1.RSD is 0.72% between samples.show the process is stable and reliable.② the properties of Excipient Ⅱhas changed:turn acidic to neutral,from very slightly soluble to slightly soluble in water, the degree of swelling near 30 changed to 56,the viscosity changed from 12 m Pa·S to 204 m Pa·S; the result show the properties between excipient Ⅱand modified excipient Ⅱ has changed.③The chromatographic conditions 1 to determine the ephedrine, pseudoephedrine ingredients of modified excipient Ⅱ Chuanping sustained-release tablets : Column is Phenomenex synergi 4u polar-RP 80 A column(250 × 4.6mm,4μm), mobile phase: methanol-0.092% phosphoric acid solution(containing 0.04% triethylamine and 0.02% di-n-butylamine)(1.5: 98.5), the column temperature was 25℃; the flow rate was 1.0m L/min; detection wavelength of 210 nm. accurate and feasible.the chromatographic conditions 2 to determine the ingredient of Scopolamine:ZORBAX SB-C18 column(4.6mm×250mm,5μm). Mobile phase: acetonitrile-0.07mol/L sodium phosphate solution(0.0175mol/L sodium lauryl sulfate,adjusted to p H 6.0 with phosphoric acid)(50:100);detection wavelength:216nm; flow rate is 1ml/min. ④The excipient Ⅱ Chuanping sustained release tablets has 0.5h drug realse time,sustained-release effect is weak, modified excipientⅡChuanping sustained release tablet drug release time up to 12 h, the release time Significantly prolong. the usaget of 23 % modified excipientⅡ,the drug release time was 12 h, the differences of the relese between the various components is clsoe, and can achieve good balance release. Compatible filler are starch filler and 46% starch / dextrin, drug release time for 12h;when match with 46% starch / MCC, 28% starch / MCC,drug release time is10 h,all those fillers can make Chuanping sustained-release tablets Similarity factors more closer,and well-balance release.⑤Modified excipients Ⅱ critical relative moisture(CRH) is near 67%, modified excipients Ⅱ viscosity down with light, high temperature the time prolong, the difference of balanced release increases, and the temperature effect is more obvious than light.Conclusion: ① The modified excipient Ⅱ samples preprated by Hydrolysis alcohol precipitation,its parameters is: solid-liquid ratio of 1: 4, catalyst b1, boiling water bath for 0.5h, alcohol precipitation concentration e1 with stable and relible quality. ②The excipient Ⅱafter modified :turn acid to neutral; the soluble in water、degree of swelling、viscosity all becomes greater. ③ The stained release properties will enhance through modified process; the usage of modified excipient Ⅱ influence drug release time, does not affect the balance release; compatibile with different fillers,drug release time and balance release are different. ④ Modified excipient Ⅱ is vulnerable tolight, humidity, temperature effects,and the effect of light is the more obvious.