The present invention seeks to extract a kind of effective site, make pharmaceutical preparation from the root of A.chinensis Planch..Described pharmaceutical preparation have encourage healthy trends, raise immunity; The effect of epidemic disease, enhancing body anti-infective ability and dispersing swelling and dissipating binds, the inhibition tumor of dispelling.
Another object of the present invention provides a kind of method of extracting the effective site with described specific pharmacologic action from the root of A.chinensis Planch..
Another object of the present invention provides a kind of method for preparing medicine with A.chinensis Planch. root effective site.
Pharmaceutical preparation of the present invention contains the A.chinensis Planch. root polysaccharide total extract for the treatment of effective dose, preferably contains the A.chinensis Planch. root polysaccharide total extract of 10-80% weight ratio.
Pharmaceutical preparation of the present invention contains the effective site of extracting from Chinese Radix Actinidiae Chinensis portion with following method of treatment effective dose:
Get the Fructus actinidiae chinensis heel piece, add alcohol dipping 1-3 time that 2-8 doubly measures 20-50%, each 18-30 hour, get supernatant, merge, add ethanol and transfer to that to contain amount of alcohol be 60-95%, leave standstill, centrifugal, precipitate is also respectively washed once with ethanol, dehydrated alcohol that 2-7 doubly measures 50-80%, discards washing liquid, precipitate adds 2-4 again and doubly measures the ether washing once, discard ether solution, the precipitate reduced pressure at room temperature, grind powder.
Pharmaceutical preparation of the present invention preferably contains the effective site of extracting from Chinese Radix Actinidiae Chinensis portion with following method of 20-70% weight ratio:
Get the Fructus actinidiae chinensis heel piece, add alcohol dipping 1-3 time that 3-6 doubly measures 25-40%, each 20-28 hour, get supernatant, merge, add ethanol and transfer to that to contain amount of alcohol be that 65-80% leaves standstill, centrifugal, precipitate is also respectively washed once with ethanol, dehydrated alcohol that 3-6 doubly measures 60-78%, discard washing liquid, precipitate adds 2-4 again and doubly measures the ether washing once, discards ether solution, the precipitate reduced pressure at room temperature, grind powder.
Pharmaceutical preparation of the present invention preferably contains the effective site of extracting from Chinese Radix Actinidiae Chinensis portion with following method of 30-65% weight ratio:
Get the Fructus actinidiae chinensis heel piece, clean, add the alcohol dipping 2 times of 5 times of amounts 30%, each 24 hours, leave standstill, get supernatant, merge, add ethanol and transfer to that to contain amount of alcohol be 72%, left standstill 24 hours, centrifugal, precipitate is also respectively washed once with ethanol, the dehydrated alcohol of 5 times of amounts 72%, discards washing liquid, precipitate adds the washing of 3 times of amount ether once again, discard ether solution, the precipitate reduced pressure at room temperature, grind powder.
Pharmaceutical preparation the best of the present invention contains the above-mentioned A.chinensis Planch. root effective site of 40-60% weight ratio.
Medicine of the present invention also contains conventional medicine excipient except containing described A.chinensis Planch. root effective site, for example, and solvent, filler, binding agent, disintegrating agent, solubilizing agent, thickening agent, correctives, antiseptic, wetting agent, lubricant etc.
The said pharmaceutical preparation of the present invention according to the preparation process of routine, can be made any pharmaceutical dosage form that can use clinically, as, tablet, unguentum, oral liquid, injection, suspensoid, pill, powder, eye drop, spongaion, liniment, cutaneous permeable agent, patch, capsule, granule, suppository etc.
The preparation method of medicine eye drop of the present invention is as follows:
Get the Fructus actinidiae chinensis heel piece, clean, add the alcohol dipping 2 times of 5 times of amounts 30%, each 24 hours, leave standstill, get supernatant, merge, add ethanol and transfer to that to contain amount of alcohol be 72%, left standstill 24 hours, centrifugal, precipitate is also respectively washed once with ethanol, the dehydrated alcohol of 5 times of amounts 72%, discards washing liquid, precipitate adds the washing of 3 times of amount ether once again, discard ether solution, the precipitate reduced pressure at room temperature, grind powder.Coarse powder adds the dissolving of injection water, and is centrifugal, gets supernatant, through the microporous filter membrane classified filtering, get the filtrate under the 0.45 μ filter membrane, add 0.03% ethyl hydroxybenzoate and an amount of sodium chloride, add the injection water and transfer to every milliliter to contain polysaccharide be 1 milligram solution, filter, aseptic potting, promptly.
In the above-mentioned method for making, after coarse powder added the dissolving of injection water, the preferred commentaries on classics with mulser 10000 earlier stirred 3 minutes, with 25000 rev/mins centrifugal 1 hour, incline and get supernatant, the precipitation add again the injection water an amount of, centrifugal again 1 hour, get supernatant and last time supernatant merging, then, through the microporous filter membrane classified filtering, get the filtrate under the 0.45 μ filter membrane again, add 0.03% ethyl hydroxybenzoate and an amount of sodium chloride, adding the injection water transfers to every milliliter to contain polysaccharide is 1 milligram solution, filter, aseptic potting, promptly.
In the above-mentioned method for making, the addition of sodium chloride reaches the required amount of isoosmotic pressure with finished product and is as the criterion.
The drug action of said medicine mainly depends on the effective site of being extracted from Chinese Radix Actinidiae Chinensis portion, because the Fructus actinidiae chinensis root contains plurality of active ingredients, screening a kind of rational extracting method, therefrom obtain to have the effective site of required drug action, is an important content of the present invention.The extracting method of A.chinensis Planch. root effective site of the present invention is as follows:
Get the Fructus actinidiae chinensis heel piece, add alcohol dipping 1-3 time that 2-8 doubly measures 20-50%, each 18-30 hour, get supernatant, merge, add ethanol and transfer to that to contain amount of alcohol be 60-95%, leave standstill, centrifugal, precipitate is also respectively washed once with ethanol, dehydrated alcohol that 2-7 doubly measures 50-80%, discards washing liquid, precipitate adds 2-4 again and doubly measures the ether washing once, discard ether solution, the precipitate reduced pressure at room temperature, grind powder.
The preferred extracting method of A.chinensis Planch. root effective site of the present invention is:
Get the Fructus actinidiae chinensis heel piece, clean, add the alcohol dipping 2 times of 5 times of amounts 30%, each 24 hours, leave standstill, get supernatant, merge, add ethanol and transfer to that to contain amount of alcohol be 72%, left standstill 24 hours, centrifugal, precipitate is also respectively washed once with ethanol, the dehydrated alcohol of 5 times of amounts 72%, discards washing liquid, precipitate adds the washing of 3 times of amount ether once again, discard ether solution, the precipitate reduced pressure at room temperature, grind powder.
The inventive method drug prepared has pharmacological action widely, and its main pharmacodynamics experiment effect is as follows:
One, encourages healthy trends raise immunity
1, promotes that the DNA of mice spleen, thymocyte cell is synthetic.
2, to the influence of human T-cell and subgroup thereof
A.chinensis Planch. root effective site of the present invention can stimulate people's T lymphocyte, and the outer blood T4 cell number that improves hepatitis B patient is had certain effect.
3, induce interleukin-22 (IL-2)
A.chinensis Planch. root effective site of the present invention can make that the IL-2 activity obviously improves than matched group in the spleen cell cultures supernatant.
4, induce M
φProduce interleukin-11 (IL-1)
Experimental result shows that A.chinensis Planch. root effective site of the present invention can significantly promote mice M
φDischarge IL-1.
5, to the effect of NK cell (NK) cell
Experiment shows that A.chinensis Planch. root effective site of the present invention can activate the NK cell activity.
6, the influence that tardy super quick (DTH) reacted
Experiment shows that medicine of the present invention can recover tardy super quick (DTH) reaction that has been suppressed by cyclophosphamide effectively.
7, to special rosette forming cell and antibody forming cell's influence
Experiment shows that medicine of the present invention can obviously increase special rosette forming cell (SRFC) number, has no effect but antagonist forms cell (PFC).
Two, dispel epidemic disease, enhancing body anti-infective ability
Medicine experiment in vitro of the present invention all has inhibitory action to 11 strains (comprising DNA viruses and RNA viruses) of five kinds of viruses such as herpes simplex virus.Then invalid to vesicular stomatitis virus and poliovirus.In the body the deadly of single bleb, influenza infection there is obvious protective effect, and can inducement interferon.Curative effect to rabbit experiment herpes simplex virus keratitis is better than the Western medicine iodouracil desoxyriboside.Therefore, medicine of the present invention also is a kind of anti virus herb preparation, and causing death of pathogenic infection also had obvious protective effect.
Three, dispersing swelling and dissipating binds, inhibition tumor
Medicine vivo medicine-feeding of the present invention has inhibitory action to mice-transplanted tumor EAC, Heps, P388.
The clinical research result of medicine of the present invention is as follows:
1, medicine of the present invention shows that to the I phase experiment of normal volunteer's 40 human eyes medicine of the present invention is to the human eye nonirritant.Observation of curative effect of initial step of II to the herpes simplex keratitis of 46 routine human eyes shows that medicine of the present invention is better than the Western medicine iodouracil desoxyriboside, can shorten healing period, improves cure rate.
2, medicine of the present invention shows the therapeutic outcome of 89 routine HIV sufferers, and long-term (three months) intramuscular injection is except that minority case one is crossed heat pyrexia and the local pain no obvious toxicity.Medicine of the present invention share separately or with Chinese medicine, has obtained the effect that improves symptom and adjust the cellular immune function curative effect, and the cloudy commentaries on classics of HIV serum antibody appears in the minority case.
3, medicine of the present invention shows the preliminary therapeutic outcome of 9 routine hepatitis B patients, to adjusting cellular immune function, improving liver function and symptom has certain effect.
Embodiment 1 extracts the effective site of A.chinensis Planch. root
Get Fructus actinidiae chinensis heel piece 1000 gram, clean, add the alcohol dipping 2 times of 5 times of amounts 30%, each 24 hours, leave standstill, get supernatant, merge, add ethanol and transfer to that to contain amount of alcohol be 72%, left standstill 24 hours, centrifugal, precipitate is also respectively washed once with ethanol, the dehydrated alcohol of 5 times of amounts 72%, discards washing liquid, precipitate adds the washing of 3 times of amount ether once again, discard ether solution, the precipitate reduced pressure at room temperature grinds to such an extent that powder 100 restrains.
Embodiment 2 preparations medicine eye drop of the present invention
Get the coarse powder of embodiment 1 preparation, add the dissolving of injection water, change with mulser 10000 earlier and stirred 3 minutes, centrifugal 1 hour with 25000 rev/mins, incline and get supernatant, precipitation adds centrifugal more in right amount 1 hour of injection water again, get supernatant and last time supernatant merging, then, again through the microporous filter membrane classified filtering, get the filtrate under the 0.45 μ filter membrane, add 0.03% ethyl hydroxybenzoate and an amount of sodium chloride (addition of sodium chloride is that finished product reaches the required amount of isoosmotic pressure), add the injection water and transfer to every milliliter to contain polysaccharide be 1 milligram solution, filter, aseptic potting, promptly.
The preparation of embodiment 3 medicine capsules of the present invention
Get Fructus actinidiae chinensis heel piece 1000 gram, clean, add the alcohol dipping 2 times of 5 times of amounts 30%, each 24 hours, leave standstill, get supernatant, merge, add ethanol and transfer to that to contain amount of alcohol be 72%, leave standstill 24 hours, centrifugal, precipitate is also respectively washed once with ethanol, the dehydrated alcohol of 5 times of amounts 72%, discard washing liquid, precipitate adds the washing of 3 times of amount ether once again, discards ether solution, the precipitate reduced pressure at room temperature, grind, cross 100 mesh sieves, get powder 100 grams, gained medicated powder and starch is even with 1: 1 mixed, encapsulated, every gram pastille 1 gram.
The preparation of embodiment 4 drug injections of the present invention
Get coarse powder 500 grams of embodiment 1 preparation, add the dissolving of injection water, change with mulser 10000 earlier and stirred 3 minutes, centrifugal 1 hour with 25000 rev/mins, incline and get supernatant, precipitation adds centrifugal more in right amount 1 hour of injection water again, get supernatant and last time supernatant merging, then, again through the microporous filter membrane classified filtering, get the filtrate under the 0.45 μ filter membrane, add 0.03% ethyl hydroxybenzoate and an amount of sodium chloride (addition of sodium chloride is that finished product reaches the required amount of isoosmotic pressure), add the injection water and transfer to every milliliter to contain polysaccharide be 1 milligram solution, filter, aseptic potting, promptly.
The preparation of embodiment 5 medicinal tablets of the present invention
Get coarse powder 1000 grams of embodiment 1 preparation, add excipient starch, mix homogeneously, with the ethanol pelletize, granulate as the tablet machine tabletting, makes tablet.