| To aim directly at the insufficiencies such as it was not clear that what the lipid-lowering material base was,to take the dosage in a big way and so on of Xin-anning tablet and capsule,according to the traditional Chinese medicine modernization mentality, the present paper screened out the lipid-lowering effective parts of Xin-anning compound recipe by inspected lipid-lowering effects,and applied modem methods and technologies to develop a new praeparatum——Fufang lipid-lowering pellets,which the lipid-lowering effects is better than the original praeparatums.The present paper studied the preparation technics,quality standard,preliminary stability,preliminary effectiveness of the pellets,and pharmacokinetics of the primary effective ingredients systematically.The main research contents and conclusions were as follows:1.The lipid-lowering effective parts of Xin-anning compound recipe were screened out by inspected lipid-lowering effects.The effective parts were total flavonoids in Radix Puerariae and Fructus Crataegi,total triterpenic acid in Fructus Crataegi,stilbene glucoside in Radix Polygoni Multiflori Preparata.The lipid-lowering effective parts were purified by modem separation and purification technique.The content of total flavonoids in Radix Puerariae and Fructus Crataegi lipid-lowering effective parts was not less than 50%, and the content of puerarin was not less than 7%.The content of stilbene glucoside(i.e. 2,3,5,4’-tetrahydroxy-stilbene-2-o-β-D-glycoside)in Radix Polygoni Multiflori Preparata lipid-lowering effective parts was not less than 50%.2.It was based on the principles of phannaceutics,the preparation technics of Fufang lipid-lowering pellets were studied.The pellets were prepared by extrusion-spheronization, that was:25%principal agent,65%MCC and 10%Lac.The moistening agent was 50% ethanol,to add 19mL in every 40g sample.The optimized preparation technics was: extrusion speed 25Hz,spheronization speed 40Hz,spheronization time 7min.The pallets were spheral and smooth,the yield was high. 3.The quality standard of Fufang lipid-lowering pellets was established by multi index ingredients control.The Radix Puerariae,Fructus Crataegi,Radix Polygoni Multiflori Preparata were identified by TLC.The primary effective ingredients in the pellets,puerarin and stilbene glucoside were quantitated by HPLC.To define that the content of puerarin and stilbene glucoside could not less than 1.5%and 2.2%.The micromeritics properties and in vitro dissolution of pellets were studied,the results showed that the pellets were spheral and smooth with eligible fluidity and bulk density.The primary effective ingredients in the pellets dissolved completely in about 30min.4.The preliminary stability of pellets was studied.The results showed that the temperature and humidity could affect the appearance of pellets a little,the content of stilbene glucoside in pellets which were exposed in highlight would decrease slowly,and the pellets were stable in accelerating test.The pellets should be closed tightly away from illumination and stored in a cool arid place.5.The preliminary effectiveness of pellets was studied.The results showed that the pellets had better lipid-lowering effects than the Xin-anning capsule.6.The preliminary pharmacokinetics of puerarin and stilbene glucoside was studied. The results showed that the absorption of stilbene glucoside taken orally was not regular and corresponded to any compartment model.The absorption of puerarin taken orally corresponded to two-compartment model.The results of rat intestine perfusion experiment showed that puerarin had a certain extent absorption in the whole intestine,the absorption in ileum was better than others.The sequence of absorption ratio in different intestine section was:Ileum＞Colon＞Jejunum＞Duodenum.It was not clear what status about the absorption of stilbene glucoside in rat intestine was from the experimental data,because it was not stable that stilbene glucoside in Kreb-ringer’s nutrient solution at 37℃. |
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