Summary of the invention
The object of the present invention is to provide a kind of pharmaceutical composition that contains Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract, this pharmaceutical composition contains multiple medicine or nutritional labeling, as health product or medicine, in use has better effect.
Another object of the present invention provides a kind of preparation of drug combination method that contains Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract.
A further object of the present invention provides a kind of purposes that contains the pharmaceutical composition of Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract at beauty treatment, defying age, antitumor, prevention of arterial sclerosis and treatment cardiac disease.
The consumption of drug component of the present invention is groped to sum up to draw through the inventor in a large number, and each amounts of components all has curative effect preferably in the following weight parts scope:
One, major ingredient
Fructus Vitis viniferae extract 1-700 part
Stem and leaf of Radix Ginseng total saponins 1-100 part
The extract that mixed extract that Fructus Vitis viniferae extract wherein of the present invention is Semen Vitis viniferae and Pericarpium Vitis viniferae or Semen Vitis viniferae, Pericarpium Vitis viniferae extract respectively, usually the mixed extract of Semen Vitis viniferae and Pericarpium Vitis viniferae is the extract behind the Fructus Vitis viniferae fleshing, be generally wine or Sucus Vitis viniferae produce in slag charge preparation after the squeezing, also claim the wine extract; The extract that the present invention preferably adopts Semen Vitis viniferae, Pericarpium Vitis viniferae to extract respectively, its compositions comprises:
Semen Vitis viniferae extract 50-400 part
Pericarpium Vitis viniferae extract 1-300 part
Stem and leaf of Radix Ginseng total saponins 1-100 part
Be preferably:
Semen Vitis viniferae extract 100-300 part
Pericarpium Vitis viniferae extract 50-150 part
Stem and leaf of Radix Ginseng total saponins 10-40 part
The best is:
200 parts of Semen Vitis viniferae extracts
100 parts of Pericarpium Vitis viniferae extract
25 parts of stem and leaf of Radix Ginseng total saponins
Wherein:
Mainly contain procyanidin oligomer (OPC) in the Semen Vitis viniferae extract, its content is 70-99%, is preferably 85-99%; Contain polyphenol and procyanidin in the Pericarpium Vitis viniferae extract, wherein polyphenol content is 30-80%, is preferably 50-70%.Stem and leaf of Radix Ginseng total saponins content is 60-95%, is preferably 80-90%.
Fructus Vitis viniferae extract among the present invention or Semen Vitis viniferae, Pericarpium Vitis viniferae extract can adopt the commercially available prod, also can adopt in the prior art disclosed method preparation, routine GB1, and disclosed method in 541,469, perhaps:
Fructus Vitis viniferae and/or Semen Vitis viniferae extract with the alcohol-water solution of 50-80% extract, centrifugal, merchant's clear liquid concentrates, behind macroporous resin column chromatography, with the aqueous solution gradient elution of alcohol, eluent is through concentrating with concentrated solution, concentrated solution behind macroporous resin column chromatography, is concentrated, is drying to obtain.
Specifically, the preparation method of Semen Vitis viniferae extract is: Semen Vitis viniferae is crushed to the 100-150 order, extract with the 60-80% ethanol water, solid-liquid ratio is 1: 5-8, and lixiviate is 2-4 time on 40-60 ℃ of water-bath rotary shaker, each 20-40 minute, cool off centrifugally, merge supernatant and carry out vacuum concentration, with concentrated solution behind macroporous resin column chromatography, use 20%, 40%, 60% ethanol elution respectively, above-mentioned eluent is carried out vacuum concentration, is drying to obtain.
Or adopt method described in the Chinese patent application 03137933.8 " extracting method of Semen Vitis viniferae Oligomeric Proanthocyanidins " that Semen Vitis viniferae is extracted.
Or adopt U.S. Henlel house journal method in 1997, and from Semen Vitis viniferae, with boiling water extraction, ethyl acetate extraction crude extract, chloroform precipitated product.
Pericarpium Vitis viniferae extract can adopt following method preparation: Pericarpium Vitis viniferae is crushed to the 80-150 order, with 50-70% methanol or ethanol water lixiviate, concentrated filtrate, adsorb through the macroporous resin chromatographic column, adopt 40%, 60% concentration methanol or ethanol liquid to carry out eluting, collect eluent, concentrate and get final product.
Or adopt method described in the application number 01122674.9 " from Pericarpium Vitis viniferae, extracting the method for extractum or oleanolic acid " that Pericarpium Vitis viniferae is extracted.
Or adopt method described in the application number 02118243.4 " alcohol-extracted extract method and grape liver-nourishing capsule thereof from grape skin " that Pericarpium Vitis viniferae is extracted.
Two, adjuvant
Pharmaceutical composition of the present invention can be aided with the various adjuvants on the pharmaceutics, is prepared as various common formulations, as oral liquid, syrup, medicated wine and tincture, injection, capsule, tablet, granule etc.; When being prepared as solid preparations such as capsule, tablet, granule, used adjuvant is as follows:
Beta-schardinger dextrin-0-200 part
Mannitol 0-200 part
Starch 0-300 part
Low-substituted hydroxypropyl cellulose 0-100 part
Hypromellose 2.5% is an amount of
Polyethylene glycol 6000 2.5% is an amount of
EtOH: H
2O=1: 1 is an amount of
Micropowder silica gel 0-80 part
Carboxymethyl starch sodium 0-80 part
Crospolyvinylpyrrolidone 0-20 part
Magnesium stearate 0-20 part
Cross-linking sodium carboxymethyl cellulose 0-20 part
Carboxymethylcellulose calcium 0-20 part
Xylitol 0-200 part
Microcrystalline Cellulose 0-150 part
Honey peach essence 0-20 part
Preferably can be:
100 parts of beta-schardinger dextrin-s
100 parts in mannitol
150 parts of starch
50 parts of low-substituted hydroxypropyl celluloses
Hypromellose 2.5% is an amount of
Polyethylene glycol 6000 2.5% is an amount of
EtOH: H
2O=1: 1 is an amount of
40 parts of micropowder silica gels
40 parts of carboxymethyl starch sodium
10 parts of crospolyvinylpyrrolidone
10 parts of magnesium stearate
10 parts of cross-linking sodium carboxymethyl celluloses
10 parts of carboxymethylcellulose calciums
100 parts of xylitol
80 parts of microcrystalline Cellulose
5 parts in honey peach essence
Pharmaceutical composition of the present invention can adopt following method preparation:
1, main materials and auxiliary materials is accurately weighed up to scale, it is standby to cross the 90-150 mesh sieve respectively, is preferably 100,110,120 orders;
2, Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract are fully mixed earlier with beta-schardinger dextrin-, mannitol, evenly cross twice of 20-50 mesh sieve, be preferably 40 mesh sieves and 28 mesh sieves respectively once, add stem and leaf of Radix Ginseng total saponins and other adjuvant then, mix homogeneously is crossed the 20-50 mesh sieve;
3, add the mixed adhesive for preparing in advance in the material of above mix homogeneously, mix homogeneously sieves;
The preparation of above-mentioned mixed adhesive: 1. weigh up hypromellose, polyethylene glycol 6000 in accordance with regulations, it is an amount of to add medicinal EtOH earlier, makes it to be uniformly dispersed; 2. add 80 ℃ of process waters, making it total concentration is 5%, places preferably after 12 hours that to cross 60 mesh sieves standby.
4, granule is preferably 50 ℃ with 30-80 ℃ of aeration-drying, with the 10-60 mesh sieve, is preferably and adds other adjuvant behind the 16 mesh sieve granulate, promptly can be made into various regular dosage forms.
Pharmaceutical composition of the present invention can also add various conventional adjuvant required when preparing different dosage form, prepare any peroral dosage form commonly used as disintegrating agent, lubricant, binding agent etc. with the method for Chinese medicinal of routine, as the dispersible tablet in pill, powder, capsule or the tablet, oral cavity disintegration tablet, effervescent tablet, general thin coated tablet etc.
Pharmaceutical composition of the present invention has functions such as beauty treatment, defying age, antitumor, prevention of arterial sclerosis and treatment heart disease.
The amount of application of medicine of the present invention can be according to variations such as route of administration, pill taker's age, body weight, and its daily dose can be the 0.01-10mg/kg body weight, and preferred 2-6mg/kg body weight can be used by one or many.
Pharmaceutical composition of the present invention is a Semen Vitis viniferae, the extract of Pericarpium Vitis viniferae and stem and leaf of Radix Ginseng total saponins, adding other adjuvant again forms, because Semen Vitis viniferae, the extract of Pericarpium Vitis viniferae has trophocyte, promote cell metabolism, prevent effects such as skin aging, stem and leaf of Radix Ginseng total saponins extracts from Radix Ginseng, has strengthening by means of tonics, the Fructus Alpiniae Oxyphyllae of calming the nerves, the function of enhancing human body immunity power, energy endocrine regulation and autonomic nervous dysfunction, strengthen myocardial contraction, improve cardiac function and hepatoprotective effect, be mainly used in preparation treatment coronary heart disease, climacteric syndrome, diseases such as weakness due to chronic disease, so its compositions has following several characteristics:
1, pharmaceutical composition of the present invention adopts pure natural substance to extract and makes, and cost is low, green, environmental protection;
2, pharmaceutical composition of the present invention contains a large amount of nutritional labelings, takes for a long time to reach beauty treatment, antidotal purpose, can strengthen body immunity;
3, pharmaceutical composition of the present invention has better curative effect at aspects such as antitumor, prevention of arterial sclerosis and treatment heart diseases;
4, pharmaceutical composition of the present invention, because cost is low, nutritional labeling is many, is the succedaneum of natural sheep placental extract;
5, pharmaceutical composition of the present invention mainly adopts tablet form, and is easy to use, safe, effective, is convenient to storage, transportation.
The specific embodiment:
The following examples can make the professional and technical personnel understand the present invention all sidedly, but cannot any way restriction the present invention.Following examples are except that special description preparation method, Semen Vitis viniferae extract is researched and developed company limited, standing grain field, Hangzhou Bioisystech Co., Ltd, is gone up Haikang nine chemical industry company limited Pericarpium Vitis viniferae extract available from Tianjin spike natural product research and development company limited, Guilin Lay mattress bio tech ltd, Guizhou Dragon Lord health product company limited available from Tianjin spike natural product; Stem and leaf of Radix Ginseng total saponins is available from Jilin Hongjiu Biotech Co., Ltd., Tianjin spike natural product research and development company limited, Tianshan Mountains, Dalian Industrial Co., Ltd..The said goods also can be available from other manufacturing enterprise.
The preparation tablets of embodiment 1 medicine of the present invention
One, major ingredient
200 parts of Semen Vitis viniferae extracts (procyanidin content 99%)
100 parts of Pericarpium Vitis viniferae extract (polyphenol content 30%)
25 parts of stem and leaf of Radix Ginseng total saponins (content 90%)
Two, adjuvant
100 parts of beta-schardinger dextrin-s
100 parts in mannitol
150 parts of starch
50 parts of low-substituted hydroxypropyl celluloses
Hypromellose 2.5% is an amount of
Polyethylene glycol 6000 2.5% is an amount of
EtOH: H
2O=1: 1 is an amount of
40 parts of micropowder silica gels
40 parts of carboxymethyl starch sodium
10 parts of crospolyvinylpyrrolidone
10 parts of magnesium stearate
10 parts of cross-linking sodium carboxymethyl celluloses
10 parts of carboxymethylcellulose calciums
100 parts of xylitol
80 parts of microcrystalline Cellulose
5 parts in honey peach essence
Production method is as follows:
1, main materials and auxiliary materials is accurately weighed up to scale, it is standby to cross 100,120 mesh sieves respectively;
2, Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract are fully mixed with microcrystalline Cellulose, even mistake 40,28 mesh sieves respectively once add stem and leaf of Radix Ginseng total saponins, crospolyvinylpyrrolidone then, and mix homogeneously is crossed 40,28 mesh sieves respectively once;
3, add magnesium stearate, the polyethylene glycol 6000 that weighs up in advance in the material of above mix homogeneously, fully mix homogeneously is crossed 32,20 mesh sieves respectively once, gets final product tabletting;
4, tabletting is with 16 * 7
Special-shaped punch die, the heavy S ' of sheet=800mg, active component content is 40mg.
The preparation tablets of embodiment 2 medicines of the present invention
One, major ingredient
50 parts of Semen Vitis viniferae extracts (procyanidin content 70%)
300 parts of Pericarpium Vitis viniferae extract (polyphenol content 80%)
1 part of stem and leaf of Radix Ginseng total saponins (content 60%)
Two, adjuvant
200 parts of beta-schardinger dextrin-s
200 parts in mannitol
300 parts of starch
100 parts of low-substituted hydroxypropyl celluloses
Hypromellose 2.5% is an amount of
Polyethylene glycol 6000 2.5% is an amount of
EtOH: H
2O=1: 1 is an amount of
80 parts of micropowder silica gels
80 parts of carboxymethyl starch sodium
Production method is as follows:
1, main materials and auxiliary materials is accurately weighed up to scale, it is standby to cross 90,100 mesh sieves respectively;
2, Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract are fully mixed with microcrystalline Cellulose, even mistake 20,40 mesh sieves respectively once add stem and leaf of Radix Ginseng total saponins, crospolyvinylpyrrolidone then, and mix homogeneously is crossed 40,28 mesh sieves respectively once;
3, add the mixed adhesive for preparing in advance in the material of above mix homogeneously, fully mix homogeneously is crossed 32,20 mesh sieves respectively once;
The preparation of above-mentioned mixed adhesive: 1. weigh up hypromellose, polyethylene glycol 6000 in accordance with regulations, it is an amount of to add medicinal EtOH earlier, makes it to be uniformly dispersed; 2. add 80 ℃ of process waters, making it total concentration is 5%, places preferably after 12 hours that to cross 60 mesh sieves standby;
4, tabletting is with 16 * 7
Special-shaped punch die, the heavy S ' of sheet=800mg, active component content is 40mg.The preparation tablets of embodiment 3 medicines of the present invention
One, major ingredient
400 parts of Semen Vitis viniferae extracts (procyanidin content 85%)
1 part of Pericarpium Vitis viniferae extract (polyphenol content 70%)
100 parts of stem and leaf of Radix Ginseng total saponins (content 80%)
Wherein:
Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract are bought from last Haikang nine chemical industry company limiteies; Stem and leaf of Radix Ginseng total saponins, grand biotech inc of a specified duration is bought from Jilin.
Two, adjuvant
Hypromellose 2.5% is an amount of
Polyethylene glycol 6000 2.5% is an amount of
EtOH: H
2O=1: 1 is an amount of
20 parts of crospolyvinylpyrrolidone
20 parts of magnesium stearate
20 parts of cross-linking sodium carboxymethyl celluloses
20 parts of carboxymethylcellulose calciums
200 parts of xylitol
150 parts of microcrystalline Cellulose
20 parts in honey peach essence
Production method is as follows:
1, main materials and auxiliary materials is accurately weighed up to scale, it is standby to cross 110,150 mesh sieves respectively;
2, Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract are fully mixed with microcrystalline Cellulose, even mistake 40,50 mesh sieves respectively once add stem and leaf of Radix Ginseng total saponins, crospolyvinylpyrrolidone then, and mix homogeneously is crossed 40,50 mesh sieves respectively once;
3, add magnesium stearate, the polyethylene glycol 6000 that weighs up in advance in the material of above mix homogeneously, fully mix homogeneously is crossed 32,20 mesh sieves respectively once, gets final product tabletting;
4, tabletting is with 16 * 7
Special-shaped punch die, the heavy S ' of sheet=800mg, active component content is 40mg.
The granule preparation of embodiment 4 medicines of the present invention
One, major ingredient
200 parts of Semen Vitis viniferae extracts (procyanidin content 99%)
100 parts of Pericarpium Vitis viniferae extract (polyphenol content 50%)
25 parts of stem and leaf of Radix Ginseng total saponins (content 90%)
Wherein:
Semen Vitis viniferae extract can adopt following method preparation: Semen Vitis viniferae is crushed to 120 orders, extract with 70% ethanol water, solid-liquid ratio is 1: 6, lixiviate is 3 times on 50 ℃ of water-bath rotary shakers, each 30 minutes, cools off centrifugal, merge supernatant and carry out vacuum concentration, concentrated solution behind the macroporous resin chromatography, is used 20%, 40%, 60% ethanol elution respectively, above-mentioned Xian is taken off liquid carry out vacuum concentration, be drying to obtain.
Pericarpium Vitis viniferae extract can adopt following method preparation: Pericarpium Vitis viniferae is crushed to 80 orders, and with 70% methanol aqueous solution lixiviate, filtrate concentrates, adsorb through the macroporous resin chromatographic column, employing 40%, 60% concentration methanol solution carries out eluting, collects meoh eluate, concentrates to get final product.
Two, adjuvant
100 parts of beta-schardinger dextrin-s
100 parts in mannitol
150 parts of starch
50 parts of low-substituted hydroxypropyl celluloses
Hypromellose 2.5% is an amount of
Polyethylene glycol 6000 2.5% is an amount of
EtOH: H
2O=1: 1 is an amount of
40 parts of micropowder silica gels
40 parts of carboxymethyl starch sodium
10 parts of crospolyvinylpyrrolidone
10 parts of magnesium stearate
10 parts of cross-linking sodium carboxymethyl celluloses
10 parts of carboxymethylcellulose calciums
100 parts of xylitol
80 parts of microcrystalline Cellulose
5 parts in honey peach essence
Production method is as follows:
1, main materials and auxiliary materials is accurately weighed up to scale, it is standby to cross 120,110 mesh sieves respectively;
2, Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract are fully mixed earlier with xylitol, mannitol, even mistake 40,28 mesh sieves respectively once add stem and leaf of Radix Ginseng total saponins, micropowder silica gel, mix homogeneously then;
3, in the material of above mix homogeneously, add hypromellose, the polyethylene glycol 6000 for preparing in advance, mixed adhesive, system soft material------granule;
The preparation of above-mentioned mixed adhesive: 1. weigh up hypromellose, polyethylene glycol 6000 in accordance with regulations, it is an amount of to add medicinal EtOH earlier, makes it to be uniformly dispersed; 2. add 80 ℃ of process waters, making it total concentration is 5%, places preferably after 12 hours that to cross 60 mesh sieves standby;
4, granule always mixes to add micropowder silica gel, magnesium stearate behind the 30 mesh sieve granulate with 48-52 ℃ of aeration-drying, gets final product packing, and 1000mg/ bag, active component content are 50mg.
The granule preparation of embodiment 5 medicines of the present invention
One, major ingredient
350 parts of Fructus Vitis viniferae extract
1 part of stem and leaf of Radix Ginseng total saponins (content 60%)
Wherein:
Fructus Vitis viniferae extract can adopt following method preparation: with the residue after the Fructus Vitis viniferae squeezing, extract with 80% ethanol water, solid-liquid ratio is 1: 5, lixiviate is 2 times on 60 ℃ of water-bath rotary shakers, each 40 minutes, cools off centrifugal, merge supernatant and carry out vacuum concentration, concentrated solution behind the macroporous resin chromatography, is used 20%, 40%, 60% ethanol elution respectively, above-mentioned Xian is taken off liquid carry out vacuum concentration, be drying to obtain.
Two, adjuvant
200 parts of beta-schardinger dextrin-s
200 parts in mannitol
300 parts of starch
100 parts of low-substituted hydroxypropyl celluloses
Hypromellose 2.5% is an amount of
Polyethylene glycol 6000 2.5% is an amount of
EtOH: H
2O=1: 1 is an amount of
80 parts of micropowder silica gels
80 parts of carboxymethyl starch sodium
Production method is as follows:
1, main materials and auxiliary materials is accurately weighed up to scale, it is standby to cross 120,130 mesh sieves respectively;
2, Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract are fully mixed earlier with xylitol, mannitol, even mistake 40,28 mesh sieves respectively once add stem and leaf of Radix Ginseng total saponins, micropowder silica gel, mix homogeneously then;
3, in the material of above mix homogeneously, add hypromellose, the polyethylene glycol 6000 for preparing in advance, mixed adhesive, system soft material------granule;
The preparation of above-mentioned mixed adhesive: 1. weigh up hypromellose, polyethylene glycol 6000 in accordance with regulations, it is an amount of to add medicinal EtOH earlier, makes it to be uniformly dispersed; 2. add 80 ℃ of process waters, making it total concentration is 5%, places preferably after 12 hours that to cross 70 mesh sieves standby;
4, granule always mixes to add micropowder silica gel, magnesium stearate behind the 20 mesh sieve granulate with 50 ℃ of aeration-dryings, gets final product packing, and 1000mg/ bag, active component content are 50mg.
The granule preparation of embodiment 6 medicines of the present invention
One, major ingredient
400 parts of Semen Vitis viniferae extracts (procyanidin content 85%)
1 part of Pericarpium Vitis viniferae extract (polyphenol content 70%)
100 parts of stem and leaf of Radix Ginseng total saponins (content 80%)
Wherein:
Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract are bought from green day Bioisystech Co., Ltd of Zhejiang Hangzhou; Stem and leaf of Radix Ginseng total saponins is bought from the Xi'an prompt biotech development of richness company.
Two, adjuvant
Hypromellose 2.5% is an amount of
Polyethylene glycol 6000 2.5% is an amount of
EtOH: H
2O=1: 1 is an amount of
20 parts of crospolyvinylpyrrolidone
20 parts of magnesium stearate
20 parts of cross-linking sodium carboxymethyl celluloses
20 parts of carboxymethylcellulose calciums
200 parts of xylitol
150 parts of microcrystalline Cellulose
20 parts in honey peach essence
Production method is as follows:
1, main materials and auxiliary materials is accurately weighed up to scale, it is standby to cross 90,110 mesh sieves respectively;
2, Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract are fully mixed earlier with xylitol, mannitol, even mistake 40,28 mesh sieves respectively once add stem and leaf of Radix Ginseng total saponins, micropowder silica gel, mix homogeneously then;
3, in the material of above mix homogeneously, add hypromellose, the polyethylene glycol 6000 for preparing in advance, mixed adhesive, system soft material------granule;
The preparation of above-mentioned mixed adhesive: 1. weigh up hypromellose, polyethylene glycol 6000 in accordance with regulations, it is an amount of to add medicinal EtOH earlier, makes it to be uniformly dispersed; 2. add 80 ℃ of process waters, making it total concentration is 5%, places preferably after 12 hours that to cross 60 mesh sieves standby;
4, granule always mixes to add micropowder silica gel, magnesium stearate behind the 16 mesh sieve granulate with 50 ℃ of aeration-dryings, gets final product packing, and 1000mg/ bag, active component content are 50mg.
The capsule preparation of embodiment 7 medicines of the present invention
One, major ingredient
200 parts of Semen Vitis viniferae extracts (procyanidin content 99%)
100 parts of Pericarpium Vitis viniferae extract (polyphenol content 50%)
25 parts of stem and leaf of Radix Ginseng total saponins (content 90%)
Wherein:
Semen Vitis viniferae extract can adopt following method preparation: Semen Vitis viniferae is crushed to 120 orders, extract with 70% ethanol water, solid-liquid ratio is 1: 6, lixiviate is 3 times on 50 ℃ of water-bath rotary shakers, each 30 minutes, cools off centrifugal, merge supernatant and carry out vacuum concentration, concentrated solution behind the macroporous resin chromatography, is used 20%, 40%, 60% ethanol elution respectively, above-mentioned Xian is taken off liquid carry out vacuum concentration, be drying to obtain.
Pericarpium Vitis viniferae extract can adopt following method preparation: Pericarpium Vitis viniferae is crushed to 80 orders, and 70% methanol aqueous solution lixiviate, filtrate concentrates, adsorb through the macroporous resin chromatographic column, employing 40%, 60% concentration methanol solution carries out eluting, collects meoh eluate, concentrates to get final product.
Two, adjuvant
100 parts of beta-schardinger dextrin-s
100 parts in mannitol
150 parts of starch
50 parts of low-substituted hydroxypropyl celluloses
Hypromellose 2.5% is an amount of
Polyethylene glycol 6000 2.5% is an amount of
EtOH: H
2O=1: 1 is an amount of
40 parts of micropowder silica gels
40 parts of carboxymethyl starch sodium
10 parts of crospolyvinylpyrrolidone
10 parts of magnesium stearate
10 parts of cross-linking sodium carboxymethyl celluloses
10 parts of carboxymethylcellulose calciums
100 parts of xylitol
80 parts of microcrystalline Cellulose
5 parts in honey peach essence
Production method is as follows:
1, main materials and auxiliary materials is accurately weighed up to scale, it is standby to cross 130,80 mesh sieves respectively;
2, Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract are fully mixed with low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, carboxymethyl starch sodium, evenly cross 40,28 mesh sieves respectively once, add stem and leaf of Radix Ginseng total saponins, carboxymethylcellulose calcium, micropowder silica gel, magnesium stearate then, mix homogeneously.Cross 32,28 mesh sieves respectively once, standby;
3, with the above-mentioned mixture for preparing, direct fill capsule, 600mg/ capsule, active component content are 30mg.
The capsule preparation of embodiment 8 medicines of the present invention
One, major ingredient
50 parts of Semen Vitis viniferae extracts (procyanidin content 70%)
300 parts of Pericarpium Vitis viniferae extract (polyphenol content 80%)
1 part of stem and leaf of Radix Ginseng total saponins (content 60%)
Wherein:
Semen Vitis viniferae extract can adopt following method preparation: Semen Vitis viniferae is crushed to 100 orders, extract with 80% ethanol water, solid-liquid ratio is 1: 5, lixiviate is 2 times on 60 ℃ of water-bath rotary shakers, each 40 minutes, cools off centrifugal, merge supernatant and carry out vacuum concentration, concentrated solution behind the macroporous resin chromatography, is used 20%, 40%, 60% ethanol elution respectively, above-mentioned Xian is taken off liquid carry out vacuum concentration, be drying to obtain.
Pericarpium Vitis viniferae extract can adopt following method preparation: Pericarpium Vitis viniferae is crushed to 150 orders, and with 50% methanol aqueous solution lixiviate, filtrate concentrates, adsorb through the macroporous resin chromatographic column, employing 40%, 60% concentration methanol solution carries out eluting, collects meoh eluate, concentrates to get final product.
Two, adjuvant
200 parts of beta-schardinger dextrin-s
200 parts in mannitol
300 parts of starch
100 parts of low-substituted hydroxypropyl celluloses
Hypromellose 2.5% is an amount of
Polyethylene glycol 6000 2.5% is an amount of
EtOH: H
2O=1: 1 is an amount of
80 parts of micropowder silica gels
80 parts of carboxymethyl starch sodium
Production method is as follows:
1, main materials and auxiliary materials is accurately weighed up to scale, it is standby to cross 100,80 mesh sieves respectively;
2, Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract are fully mixed with low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, carboxymethyl starch sodium, evenly cross 40,28 mesh sieves respectively once, add stem and leaf of Radix Ginseng total saponins, carboxymethylcellulose calcium, micropowder silica gel, magnesium stearate then, mix homogeneously.Cross 32,28 mesh sieves respectively once, standby;
3, with the above-mentioned mixture for preparing, direct fill capsule, 600mg/ capsule, active component content are 30mg.
The capsule preparation of embodiment 9 medicines of the present invention
One, major ingredient
400 parts of Semen Vitis viniferae extracts (procyanidin content 85%)
1 part of Pericarpium Vitis viniferae extract (polyphenol content 70%)
100 parts of stem and leaf of Radix Ginseng total saponins (content 80%)
Wherein:
Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract are bought from Shandong Province Marine Organism Co., Ltd., Penglai City; Stem and leaf of Radix Ginseng total saponins is bought from Guangzhou Thailand auspicious chemical industry Advisory Co., Ltd.
Two, adjuvant
Hypromellose 2.5% is an amount of
Polyethylene glycol 6000 2.5% is an amount of
EtOH: H
2O=1: 1 is an amount of
20 parts of crospolyvinylpyrrolidone
20 parts of magnesium stearate
20 parts of cross-linking sodium carboxymethyl celluloses
20 parts of carboxymethylcellulose calciums
200 parts of xylitol
150 parts of microcrystalline Cellulose
20 parts in honey peach essence
Production method is as follows:
1, main materials and auxiliary materials is accurately weighed up to scale, it is standby to cross 100,90 mesh sieves respectively;
2, Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract are fully mixed with low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, carboxymethyl starch sodium, evenly cross 40,28 mesh sieves respectively once, add stem and leaf of Radix Ginseng total saponins, carboxymethylcellulose calcium, micropowder silica gel, magnesium stearate then, mix homogeneously.Cross 32,28 mesh sieves respectively once, standby;
3, with the above-mentioned mixture for preparing, direct fill capsule, 600mg/ capsule, active component content are 30mg.
The preparation tablets of embodiment 10 medicines of the present invention
One, major ingredient
100 parts of Semen Vitis viniferae extracts (procyanidin content 99%)
150 parts of Pericarpium Vitis viniferae extract (polyphenol content 70%)
10 parts of stem and leaf of Radix Ginseng total saponins (content 90%)
Wherein:
Semen Vitis viniferae extract can adopt the solvent extraction method preparation: Semen Vitis viniferae is crushed to 150 orders, extract with 60% ethanol water, solid-liquid ratio is 1: 8, lixiviate is 4 times on 40 ℃ of water-bath rotary shakers, each 20 minutes, cools off centrifugal, merge supernatant and carry out vacuum concentration, concentrated solution behind macroporous resin column chromatography, is used 20%, 40%, 60% ethanol elution respectively, above-mentioned Xian is taken off liquid carry out vacuum concentration, be drying to obtain.
Pericarpium Vitis viniferae extract can adopt following method preparation: Pericarpium Vitis viniferae is crushed to 120 orders, and with 60% methanol aqueous solution lixiviate, filtrate concentrates, adsorb through the macroporous resin chromatographic column, employing 40%, 60% concentration methanol solution carries out eluting, collects meoh eluate, concentrates to get final product.
Two, adjuvant
110 parts of beta-schardinger dextrin-s
120 parts in mannitol
170 parts of starch
40 parts of low-substituted hydroxypropyl celluloses
Hypromellose 2.5% is an amount of
Polyethylene glycol 6000 2.5% is an amount of
EtOH: H
2O=1: 1 is an amount of
30 parts of micropowder silica gels
10 parts of crospolyvinylpyrrolidone
10 parts of magnesium stearate
10 parts of carboxymethylcellulose calciums
90 parts of xylitol
60 parts of microcrystalline Cellulose
10 parts in honey peach essence
Production method is as follows:
1, main materials and auxiliary materials is accurately weighed up to scale, it is standby to cross 100,120 mesh sieves respectively;
2, Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract are fully mixed with microcrystalline Cellulose, even mistake 40,28 mesh sieves respectively once add stem and leaf of Radix Ginseng total saponins, crospolyvinylpyrrolidone then, and mix homogeneously is crossed 40,28 mesh sieves respectively once;
3, add magnesium stearate, the polyethylene glycol 6000 that weighs up in advance in the material of above mix homogeneously, fully mix homogeneously is crossed 32,20 mesh sieves respectively once, gets final product tabletting;
4, tabletting is with 16 * 7
Special-shaped punch die, the heavy S ' of sheet=700mg, active component content is 35mg.
The granule preparation of embodiment 11 medicines of the present invention
One, major ingredient
300 parts of Semen Vitis viniferae extracts
50 parts of Pericarpium Vitis viniferae extract
40 parts of stem and leaf of Radix Ginseng total saponins
Wherein:
Semen Vitis viniferae extract can adopt the solvent extraction method preparation: Semen Vitis viniferae is crushed to 100 orders, extract with 60% alcohol-water solution, solid-liquid ratio is 1: 8, lixiviate is 2 times on 60 ℃ of water-bath rotary shakers, each 20 minutes, cools off centrifugal, merge supernatant and carry out vacuum concentration, concentrated solution behind the macroporous resin chromatography, is used 20%, 40%, 60% ethanol elution respectively, above-mentioned Xian is taken off liquid carry out vacuum concentration, be drying to obtain.
Pericarpium Vitis viniferae extract can adopt following method preparation: Pericarpium Vitis viniferae is crushed to 130 orders, and with 65% methanol aqueous solution lixiviate, filtrate concentrates, adsorb through the macroporous resin chromatographic column, employing 40%, 60% concentration methanol solution carries out eluting, collects meoh eluate, concentrates to get final product.
Two, adjuvant
110 parts of beta-schardinger dextrin-s
90 parts in mannitol
100 parts of starch
70 parts of low-substituted hydroxypropyl celluloses
Hypromellose 2.5% is an amount of
Polyethylene glycol 6000 2.5% is an amount of
EtOH: H
2O=1: 1 is an amount of
50 parts of micropowder silica gels
10 parts of crospolyvinylpyrrolidone
8 parts of magnesium stearate
10 parts of cross-linking sodium carboxymethyl celluloses
15 parts of carboxymethylcellulose calciums
90 parts of microcrystalline Cellulose
Production method is as follows:
1, main materials and auxiliary materials is accurately weighed up to scale, it is standby to cross 120,110 mesh sieves respectively;
2, Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract are fully mixed earlier with xylitol, mannitol, even mistake 40,28 mesh sieves respectively once add stem and leaf of Radix Ginseng total saponins, micropowder silica gel, mix homogeneously then;
3, in the material of above mix homogeneously, add hypromellose, the polyethylene glycol 6000 for preparing in advance, mixed adhesive, system soft material------granule;
The preparation of above-mentioned mixed adhesive: 1. weigh up hypromellose, polyethylene glycol 6000 in accordance with regulations, it is an amount of to add medicinal EtOH earlier, makes it to be uniformly dispersed; 2. add 80 ℃ of process waters, making it total concentration is 5%, places preferably after 12 hours that to cross 60 mesh sieves standby;
4, granule always mixes to add micropowder silica gel, magnesium stearate behind the 30 mesh sieve granulate with 48-52 ℃ of aeration-drying, gets final product packing, and 900mg/ bag, active component content are 45mg.
Be function and the beneficial effect that shows that pharmaceutical composition of the present invention Europe must be believed-be joined, further set forth the beneficial effect of medicine of the present invention below by the test example:
1 beauty treatment of test example, anti-aging effects evaluation test
Test material: get the prepared pharmaceutical composition that contains Fructus Vitis viniferae extract of the embodiment of the invention 1,2,3,800mg/ sheet, active component content are 40mg.
Test method: select 90 ages the facial pigmentation person of increasing between 20-50 year, wherein freckle 29 examples, chloasma 38 examples, exogenous (after the inflammation heavy, the cosmetic dermatitis of color etc.) pigmentation 23 examples; The heavy position of color Jian Yu Zygomatic buccal person 57 examples involve entire face person's 12 examples, are confined to nose or eye socket 21 examples on every side.(2 slices/time) Europe of the present invention that takes night and morning every day must be believed-be joined, and uses for 12 weeks.
Result of the test: cure (facial pigmentation disappears or disappears substantially) 5 examples (5.6%), (pigment obviously disappears more than 50% produce effects, latent see pigmented spots) 28 examples (31.1%), effectively (pigment alleviates before treating, color is thin out) 30 examples (33.3%), invalid 27 examples (30%), total effective rate reaches 70.0%.
Conclusion: medicine of the present invention Europe must believe-join to have beauty treatment, anti-aging effects.
Through comparing with independent use Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract or stem and leaf of Radix Ginseng total saponins, under the same dose, effect obviously is better than using separately Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract, and its result has statistical significance; Use stem and leaf of Radix Ginseng total saponins not have obvious effects separately.
The product that other embodiments of the invention (4-11) obtain, adopt said method to test, obtain essentially identical effect, the effect of embodiment 5 is poor than other embodiment, but still is higher than one of independent employing Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract or stem and leaf of Radix Ginseng total saponins.
Test example 2 anti-cancers, antitumor evaluation test
Test material: get the prepared pharmaceutical composition that contains Fructus Vitis viniferae extract of the embodiment of the invention 4,5,6,1000mg/ bag, active component content are 50mg; White mice (40) only, source The Biochemical Pharmaceutical Factory of Zhuhai SEZ Animal House; Nitrous ammonium (carcinogen), chemical reagent four factories in Beijing provide.
Test method: 40 white mice are divided into two groups at random, every group 20, give to shine every day X ray 5 hours simultaneously and feed for two groups with carcinogen nitrous ammonium, cause the cancer condition of suffering from, wherein first group of feedstuff is the Semen Maydis powder that contains 2% nitrous ammonium, second group of feedstuff is the Ou Bixin-ginseng that contains 2% nitrous ammonium, and test period is 150 days.
Result of the test: first group of white mice amounts to 10 and suffers from cancer, wherein suffers from cardiac cancer for 5, suffers from 1 of the esophageal carcinoma for 3 and gets a cancer of the stomach, and suffers from pulmonary carcinoma for 1; Second group of white mice has only one to suffer from the esophageal carcinoma.See table 1 for details:
Table 1
The white mice number |
Natural law |
Suffer from the cancer number for first group |
Remarks |
Suffer from the cancer number for second group |
Remarks |
20 |
60 |
0 |
0 |
0 |
|
20 |
100 |
4 |
Suffer from cardiac cancer for 2, suffer from the esophageal carcinoma for 2 |
0 |
|
20 |
120 |
8 |
Suffer from cardiac cancer for 5, suffer from the esophageal carcinoma for 3 |
0 |
|
20 |
150 |
10 |
Increase a gastric cancer and a pulmonary carcinoma |
1 |
1 esophageal carcinoma |
Conclusion: medicine of the present invention Europe must believe-join to have anti-cancer, antitumor action.
Through comparing with independent use Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract or stem and leaf of Radix Ginseng total saponins, under the same dose, effect obviously is better than using separately Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract, stem and leaf of Radix Ginseng total saponins, and its result has statistical significance.
Through comparing with independent use Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract or stem and leaf of Radix Ginseng total saponins, under the same dose, effect obviously is better than using separately Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract, and its result has statistical significance.
The product that other embodiments of the invention (4-11) obtain, adopt said method to test, obtain essentially identical effect, the effect of embodiment 5 is poor than other embodiment, but still is higher than one of independent employing Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract or stem and leaf of Radix Ginseng total saponins.
The atherosis evaluation test of test example 3 prevention of arterial
Test material: get the prepared pharmaceutical composition that contains Fructus Vitis viniferae extract of the embodiment of the invention 7,8,9,600mg/ capsule, active component content are 30mg; White mice (48) only, source The Biochemical Pharmaceutical Factory of Zhuhai SEZ Animal House.
Test method: 48 white mice are divided into normal control group (raising normal diet), hyperlipidemia model group (raising high lipid food: contain 2% cholesterol, 0.4% cholate, 10% Adeps Sus domestica), low, the high dose group (when raising high lipid food, adding Ou Bixin-ginseng 0.2,0.6mg/g body weight respectively) of Ou Bixin-ginseng at random.21 weekends of experiment to the, eyeball sacrificed by exsanguination mice, detect serum triglycerides (TG), cholesterol (CHOL), oxidized low-density lipoprotein (OX-LDL) and erythrocyte malonaldehyde (MDA), superoxide dismutase (SOD) activity, get aorta simultaneously and make the pathology morphological observation.
Result of the test: compare with the hyperlipidemia model group, Ou Bixin-ginseng group mice serum TG, CHOL, OX-LDL, MDA content obviously reduce, and active obviously improve (P<0.01) of erythrocyte sod.Simultaneously Europe must believe-ginseng group mouse aorta wall thickness and the obvious higher fat model group of foam cell quantity alleviate.The remarkable P of mouse aorta damage diversity of values<0.01.
Conclusion: medicine of the present invention Europe must believe-join to have the effect that slows down the formation of mice atherosclerosis.
Test example 4 is got the prepared pharmaceutical composition that contains Fructus Vitis viniferae extract of the embodiment of the invention 10, the 700mg/ sheet, active component content is 35mg, carries out the content comparative determination with natural sheep placental extract (the Li Zhuojia sheep placental extract is bought from the family doctor of Zhongshan Medical Univ. scientific and technological development company limited):
|
Natural Foetus Caprae seu Ovis rope |
Ou Bixin-ginseng |
Remarks |
Polyphenols |
20 |
23 |
Content percent |
Vitamin |
11 |
15 |
Content percent |
Trace element |
3 |
2 |
Content percent |
Conclusion: nutritional labeling and natural sheep placental extract that medicine of the present invention Europe must be believed-be joined are basic identical, can be used as its succedaneum.
Among the above-mentioned test example 1-4, no matter Semen Vitis viniferae extract, Pericarpium Vitis viniferae extract, stem and leaf of Radix Ginseng total saponins be to adopt that the inventive method is prepared or other company buys from the market, as long as its content within the scope of the present invention, no matter be to adopt the inventive method to be prepared or the medicine of the present invention that other method is prepared, all have identical purposes and effect.