| OBJECTIVE: To increase the dissolution rate of rutin solid dispersions,, and enhance bioavailability in vivo.METHODS: rutin solid dispersions(RSD) were prepared respectively with solvent method , evaporation-fusion method and solvent evaporation-fusion method using PEG6000 as carriers, using rutin dissolution in vitro(UV - spect rophotometry) as testing index to study frozen time . RSD were prepared respectively with three methods using PEG6000,PVP,poloxamer 188 (F68), HPMC, beta-cyclodextin, and . measure carrier and method. With the method of orthogonal experiment design , choosing the 15 minute solubility of rutin as the index ,;powder differential scanning calorimetry were used to examine the physical and chemical characteristics of the solid dispersions to provide some reliable and scientific basis for preformulation,determined the optimum extraction process. To established a quality specification. The similarity factor was used to compare the dissolution characteristics of RSD ,Physical mixture and pure drug.Rutin so lubility of RSD with different temperate and consent was studied in order to discuss by the thermodynamic theory. The last to finish the stability experiment .RESULTS: The dissolution of RSD using PEG6000 as carrier, 36h is better than other frozen time . the result show that every method and carrier can enhance the dissolution of RSD ,expecal the PEG6000 as carrier and solvent evaporation-fusion method . The optimized preparation conditions for RSD were obtained as follows Solvent was ethanol, The ratio of rutin to carrier was 1:9, Temperature was 70℃.DSC show that rutin were dispersed in carrier . we have established a accurate and repeatable quality specification.The dissolution of srveral samples arenot similarity. The solution was a spontaneous process according to the thermodynamic theory. RSD was obviously raised and stable , but the solid dispersion was not easy to age.CONCLUSION: PEG6000 is a very useful carrier in improving the solubility of rutin. |
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