A kind of oleanane type triterpene saponin compound and its preparation method and application
A technology of triterpene saponins and oleanane type, which is applied in the application field of pentacyclic triterpene compounds in the preparation of drugs for the treatment of inflammatory vascular diseases, and can solve the anti-inflammatory activity of oleanane type triterpene saponin compounds Unsatisfactory and other issues
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example 1
[0038] 1. Preparation of compounds
[0039] (1) Get the roots of Ilex pubescens, reflux extraction with 12, 10 and 8 times of 70% ethanol successively for 2 hours, combine the ethanol extracts, recycle the ethanol after filtration and concentrate under reduced pressure until there is no alcohol smell, to obtain the total extract 2.2 kg;
[0040] (2) Dissolve the total extract in water, pass through a D-101 macroporous resin column, and elute successively with 30% ethanol, 60% ethanol and 95% ethanol; the collection concentration is 60% % ethanol eluent was recovered under reduced pressure to obtain 566g thick extract, which was passed through a 200-300 mesh silica gel column, and carried out with chloroform-methanol as the solvent according to the gradient of 100:1-0:1 in chloroform:methanol Elution; collect the eluate with chloroform:methanol ratio of 9:1, concentrate and pass through Sephadex LH-20 column, use methanol as the eluent for elution, collect the eluate and conce...
example 2
[0049] Example 2: (injection)
[0050] Take 1000 mg of the compound obtained by the method described in Example 1 above, add 1000 ml of water for injection, adjust the pH value to 7-7.5 with sodium carbonate, stir to dissolve, sterilize and filter, potting, and circulate steam at 100 ° C for 15 minutes Sterilize and make each 2mg / 2ml injection for injection.
example 3
[0051] Example 3: (capsules)
[0052] Take the compound 5000mg obtained by the method described in the above-mentioned Example 1 and fully mix with auxiliary materials such as 4000mg microcrystalline cellulose, 500mg sodium carboxymethyl starch, 400mg sodium lauryl sulfate, and carry out dry granulation by roller compaction, and then mix with An appropriate amount of magnesium stearate is mixed, filled into 3# hollow capsules, and made into capsules with a specification of 100 mg / grain for oral use.
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Abstract
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