| Objective:1. The optimize the extraction technics of Colchicine, Cassia Angustifolia andAmygdalus communis;2. To compare the different dehydrations on contents of SennosideB in Cassia Angustifolia extracts.3. Study the materials’ nature of prescription to providebase for sustained-release pellet of formula Su Run-jiang;4. Study on preparationtechnique of formula Su Run-jiang pellets.5. To study the preparation of sustained-releasecoated pellets of compound Su Run-jiang and it’s in vitro release mechanism.Methods:1. Used the HPLC, take the Colchicine, Sennoside B and yield rate of paste extracted asthe appraisal target, by single factor and orthogonal testing method optimal extractioncraft parameter respectively. The extraction rate with oil for investigation indexSupercritical CO2extraction technology and orthogonal design were used to investigatethe influence of extraction process for Amygdalus communis Oil.2. Selected the contentof sennoside B as target, reduced pressure condense and vacuum dehydration at differenttemperature effect were investigated by mono-factor experiment; Orthogonal experimentalstudy of inlet temperatures, outlet temperatures and spraying velocity on Cassia Leafextracts of spray drying technology.3. The characteristics of Colchicine includingdissolubility and apparent oil-water partition coefficient were determined by usingmethods such as HPLC and ultrasonic method. Applying modifiers to deal with extractpowder, drawing moisture absorption curve and screening modifier with kind.4. Selectedthe spherical degree and yield of target pellets, the optimal process and formulation wereobtained on the studies of influence factors and Box-behnken design.5. Coated influid-bed with Eudragit NE30D, Using single-factor study on affecting in vitro Colchicinerelease’s each kind of factor by the release measuring method, Carry on the model fittingto its in vitro release data, inspects in vitro to release the medicine mechanism. Results:1.Optimal extraction technology of Colchicum was as followed: extracted coarse powder2times with8times amount of70%ethanol for1h each time. Optimal extractiontechnology of Cassia Leaf was as followed: extracted2times with10times amount of 45%ethanol for15min each time. The optimal preparation condition were that:extractionpressure was35MPa,extraction temperature was70℃,extraction time was1h.2. The bestCassia Leaf extract spray process parameters were determined: inlet air temperature120℃,outlet air temperature55℃,inlet flow rate16ml·min-1.3. The preformation studyshowed that the results of dissolubility and oil-water distribution coefficient were30.5424μg·mL-1and0.5155. Comparing the moisture absorption curve,it shows that stearic acidand lactose have better modified effective.4. The optimal process parameters were asfollows: the ratio of extract and material was1:2.5（w/w）, the MCC and lactose was2:1（w/w）, the adhesive agent was distilled water, Squeeze with27.15Hz and roll5.62minwith the rate39.46Hz.5. A satisfactory sustained release curve can be obtained when thepellets is coated with Eudragit NE30D4.88%, PVP3%,talcum powder40%. The processof drug release from compound Su Run-jiang sustained-release pellets had a goodrelationship to one-order, Higuchi plane-diffusion equation and Ritger-Peppasequation,and the relative coefficients were all more than0.99. Conclusion:1. Thisoptimized extraction process is science,stable and feasible.2. The spray dehydration ismore compatible to drying Cassia leaf extracts.3. The oil-water distribution coefficient ofColchicum in acid solution was higher than in alkaline solution. it showed that the goodmodifier can reduce the extract powder significantly.4. Compound Su Run-jiang pelletswere prepared by extrusion spheronization method and the pellets show a higher yield,better quality and is conducive to the coating process.5. The pellets show an obviouslysustained-release effect. |
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