CN1583011A - Plant extracts for preventing eye from fatigue and their preparation and preparing method - Google Patents
Plant extracts for preventing eye from fatigue and their preparation and preparing method Download PDFInfo
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- CN1583011A CN1583011A CN 200410020680 CN200410020680A CN1583011A CN 1583011 A CN1583011 A CN 1583011A CN 200410020680 CN200410020680 CN 200410020680 CN 200410020680 A CN200410020680 A CN 200410020680A CN 1583011 A CN1583011 A CN 1583011A
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- vitis viniferae
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Abstract
A Chinese medicine for preventing and treating visual fatigue is prepared from the seed, peel and stem of grape through pulverizing, extracting in water and then in alcohol, and purifying by macroreticular resin.
Description
Technical field:
The present invention relates to a kind of plant extract and preparation and preparation method, particularly a kind of control asthenopic Fructus Vitis viniferae waste residue extract and preparation and preparation method.
Technical background:
Asthenopia is to produce because of autonomous effort that visual organ attempts to obtain with insufficient adjusting clear vision, as syndromes such as blurred vision, ophthalmic bloated, ophthalmalgia, headache, aching shoulder and back and mental weariness.Along with the high speed development of information age and the quickening of rhythm of life, especially video display terminal (vdt)s (VDT) such as computer, TV, game machine, monitor incorporate in people's work, study and the family life gradually, asthenopia has become present ophthalmology common disease, has seriously influenced people's life.It is not a disease independently, but because one group of fatigue syndrome that a variety of causes causes claims eyestrain's syndrome again.At present, the physiotherapy of treatment has prism rectification, operative treatment, acupuncture etc.; Chemicals adopts neostigmine such as beta-blocker, vancomin etc. more, and neurotrophic agents and tranquilizer etc.But above treatment is all carried out at symptom, does not reach basic therapeutic purposes.Modern study finds, natural drug and Chinese medicine are should disease evident in efficacy, just progressively becomes patient's first-selected medicine.
The Oligomeric Proanthocyanidins that is rich in the Fructus Vitis viniferae (Oligomeric Proanthocyanidins, be called for short OPCs) is the polyphenols that monomer, dimer, the trimer by catechin is formed by combining.As far back as the seventies French scientist just find that Semen Vitis viniferae is a best resource of extracting procyanidin, procyanidin content can be up to 95% in its extract.The grape resource of China is abundant, leftover bits and pieces Fructus Vitis viniferae waste residue after the annual only brew wine is about 8000t just, and in recent years the cultivated area of Fructus Vitis viniferae also in a large amount of increases, yet domestic only with it as simple Oleum Vitis viniferae, feedstuff, fertilizer and the polyphenol raw material of extracting.Discover and have significant non-oxidizability by OPCs (its oxidation resistance is V
C20 times, V
E50 times), remove interior free yl ability, improve unique effects such as microcirculation in human body obstacle, fields such as health care have been applied at present, especially can reduce retinopathy, control capillary hemorrhage aspect the eye health, it is the asthenopic desirable natural drug of treatment, its product is owing to meet the hope and the requirement of modern people's back to nature, and market prospect is very wide.
The method that is used to extract Fructus Vitis viniferae Central Plains anthocyan material at present has: the one, and chemical solvent method, the 2nd, supercritical fluid extraction, the 3rd, microwave extraction method.
Chinese patent such as CN03137933.8 adopt ethyl acetate, petroleum ether or the chloroform organic solvent method as the extraction solvent of Semen Vitis viniferae; CN00134314.9 is that procyanidolic oligomers has been invented a kind of water in the Semen Vitis viniferae, alcohol extraction is followed the example of; CN99111574.0 is raw material with the Semen Vitis viniferae, uses supercritical fluid method extraction of oil from grape seeds and procyanidolic oligomers; CN00120353.3 discloses a kind of new method that adopts microwave method to extract the anthocyan material in the Semen Vitis viniferae.
Said extracted method or technology make moderate progress to the traditional preparation process method, but remaining in the improved problem that needs to be resolved hurrily aspect method of quality control and the preparation technology, as exist impurity many, contain a large amount of saccharides and contain moisture absorption compositions such as a certain amount of inorganic salt and phlegmatic temperament; Organic solvents such as the acetone that uses in the leaching process, ethyl acetate, petroleum ether, not only cost height, dangerous big, contaminated environment, and cause the organic solvent residual excess, influence product quality and drug effect.Though CN00134314.9 has adopted free of contamination water and alcohol, effective site is indeterminate, and yield is lower; And supercritical fluid method cost is higher, and treatment step is also comparatively loaded down with trivial details.
OPCs improves microcirculation in human body, removes free radical, antioxidation is the material base of its disease-prevention health effect, has been widely used in every field as the product that has much DEVELOPMENT PROSPECT.Chinese patent such as CN00121388.1 disclose a kind of grape seed extract OPC s strong anti-oxidative composite capsule and manufacture method thereof, are the complex health care products that has slow down aging, regulates body's immunity; CN02159540.2 is to be being used for defying age, anticancer, antioxidation, improving the patent of the capsule of aspects such as cardiovascular and cerebrovascular vessel of raw material with the Semen Vitis viniferae extract, does not have clear and definite single-minded therapeutic purposes.As seen, also do not use modern extraction technique and method of quality control at present and the Fructus Vitis viniferae waste residue is made the patented invention that is used to prevent and treat (standard extract) pharmaceutical preparation of asthenopic modern times.
Summary of the invention:
The objective of the invention is, shortcoming such as effective site indeterminate and mechanism unclear, no crude drug, intermediate and end product quality control method big, a kind of control asthenopic Fructus Vitis viniferae waste residue extract and preparation and preparation method are provided at the taking dose that exists in the above-mentioned technology.Is standard extract with OPCs content in the Fructus Vitis viniferae waste residue greater than 50% effective site, and make and be used to prevent and treat asthenopic modern preparation, it can solve the medium-term and long-term insoluble technical field problem of Fructus Vitis viniferae waste residue preparation technology, has filled up that Fructus Vitis viniferae waste residue extract OPC s is developed to the domestic blank that is used for the treatment of asthenopic preparation.
The object of the present invention is achieved like this: the effective site of Fructus Vitis viniferae waste residue extract is the flavone of Fructus Vitis viniferae waste residue and Polyphenols composition through the effect experiment screening, oligomer comprising flavanol compound and procyanidin, total content is at 50%-99%, through the further preferred effective site of effect experiment is OPCs, and its content is at 50%-99%.Through the preferred effective ingredient of effect experiment is wherein catechin, and its content is in the 0.5-20% scope.
The technical problem to be solved in the present invention provides a kind of employing resin absorption technology, extracts the OPCs method from the Fructus Vitis viniferae waste residue.
The preparation method of effective site of the present invention, step is as follows:
(1) with Fructus Vitis viniferae waste residue extracting in water 1-10 time, the 2-20 that each consumption is respectively medical material weight doubly, extraction time is 0.5-10 hour, extracting temperature is 10-100 ℃, merge extractive liquid.
(2) with the Fructus Vitis viniferae waste residue with 5-95% alcohol reflux 1-10 time, the 2-20 that each consumption is respectively medical material weight doubly, extraction time is 0.5-10 hour, merge extractive liquid, filters, and reclaims ethanol, concentrated extractum.
(3) with the extracting solution of (1) or (2) extractum after adding water 1-200 and doubly diluting, last resin column absorption, the volume ratio of raw material weight and resin is 1: 0.5-10, resin column footpath is 1 with the post height ratio: 1-30, with pH value be water washing, the concentration of 2-8 be 5-95% alcoholic solution eluting, flow velocity be 0.5-3.5 column volume/hour.
(4) collect ethanol elution, in the ratio adding depigmenting agent of effluent volume 1-30%, reflux 0.1-10 hour, filter, concentrating under reduced pressure, vacuum drying, promptly.OPCs content can reach more than 50% in employing this law Fructus Vitis viniferae waste residue.
OPCs resin extraction process of the present invention is compared with traditional handicraft, and following 3 advantages are arranged:
1. dwindle dosage, improve crude drug inherent quality and preparation level.The refining thing that obtains after RAT handles can make active ingredient highly enriched, and impurity is few, and extraction ratio only is the 2-5% of crude drug in whole (decocting method is about 20-30%, and alcohol deposition method is about 15%), helps making the Chinese medicine of modern formulation, also is convenient to quality control.This technology has once been finished remove impurity and concentrated two procedures.
2. reduce the moisture absorption of product.The medicine major part of traditional handicraft preparation has stronger moisture absorption, is the medium-term and long-term difficult problem that exists of production and storage.And after RAT handles, can remove moisture absorption compositions such as saccharides a large amount of in the decocting liquid, inorganic salt, lymphatic temperament effectively, and help the production of multiple dosage form, strengthen the stability of product.
3.RAT can shorten the production cycle, equipment needed thereby is simple, has removed many operations consuming time such as staticly settling, concentrate from.Not only saved packing, reduced cost, also created condition for Chinese medicine enters the international market.
The present invention compares with traditional solvent extraction, supercritical fluid method, technology is simple, do not use the volatile organic solvent of toxicity in the technological process, safe and reliable, production cost is low, environmentally safe.
Standard extract of the present invention is to make medicinal various clinical acceptable forms, comprise capsule, tablet, powder, granule, oral liquid, medicated wine, pill, pellet, soft gelatin capsule, ointment, mixture, tincture, injection etc., wherein preparations such as soft capsule, drop pill, oral liquid, eye drop preferably.
The standard extract that Fructus Vitis viniferae waste residue of the present invention obtains according to its preparation method can directly be made preparation or be mixed and made into preparation with the medicine acceptable carrier.Described medicine acceptable carrier can be: starch, sucrose, lactose, mannitol, silicon derivative, cellulose family and derivant, alginate, gelatin, polyvinylpyrrolidone, glycerol, tween 80, agar, calcium carbonate, calcium bicarbonate, surfactant, Polyethylene Glycol, cyclodextrin, dextrin, phospholipid material, kaolin, Pulvis Talci, calcium stearate, magnesium stearate etc.
Standard extract of the present invention and compositions are to have functions such as microcirculation improvement, non-oxidizability, elimination interior free yl, enhancing human body immunity power, are applied in preparation asthenopic medicine of control and health product.
The specific embodiment:
The present invention will be further described below in conjunction with embodiment
Embodiment 1: a kind of RAT preparation method of Fructus Vitis viniferae waste residue
Raw material adopts the Fructus Vitis viniferae waste residue, and with 50% alcohol reflux 2 times, each consumption is 7,5 times of crude drug weight, and extraction time is 2,1 hours, and merge extractive liquid, filters, and reclaims ethanol, concentrated extractum.Extractum is added 120 times of dilutions of water, the absorption of last resin column, the volume ratio of raw material weight and resin is 1: 3, resin column footpath and post height ratio are 1: 15, water washing, the 50% alcoholic solution eluting of usefulness pH=6, flow velocity be 1 column volume/hour.
Collect ethanol elution, press effluent volume 5% and add depigmenting agent, reflux 3 hours filters, concentrating under reduced pressure, and vacuum drying, promptly.OPCs content can reach more than 50% in employing this law Fructus Vitis viniferae waste residue.
Embodiment 2: a kind of RAT preparation method of Fructus Vitis viniferae waste residue
Raw material adopts the Fructus Vitis viniferae waste residue, and with 60% alcohol reflux 3 times, each consumption is 8,6,4 times of raw medicinal herbs weight, and extraction time is 60,45,30min, and merge extractive liquid, filters, and reclaims ethanol, concentrated extractum.Extractum is added 150 times of dilutions of water, the absorption of last resin column, raw material heavy with volume ratio resin be 1: 5, resin column through with the post height ratio be 1: 20, with water washing, the 60% alcoholic solution eluting of pH=8, flow velocity be 2 column volumes/hour.Eluent is through concentrating under reduced pressure, vacuum drying, promptly.OPCs content can reach more than 50% in employing this law Fructus Vitis viniferae waste residue.
Embodiment 3:OPCs is greater than 50% Fructus Vitis viniferae waste residue extract (standard extract) soft capsule and the preparation of drop pill
Get OPCs greater than the capsule material that 50% Fructus Vitis viniferae waste residue extract and gelatin make, adopt pressing pill, typing, drying, select ball, wash ball, make soft capsule; Adopt the dropping preparation method pill, through typing, dry, select ball, wash ball, make drop pill.Soft capsule that makes and dropping pill formulation OPCs content should be more than 50%.
The toxicity clinical trial
Below further prove the curative effect and the safety of standard extract of the present invention and compositions by clinical and toxicological test.
The experimental drug thing: standard extract of the present invention does not add the preparation that adjuvant directly makes and is called in test OPCs.
Test example 1: the asthenopic clinical observation I of the treatment of pharmaceutical composition of the present invention
Treatment is divided into 2 groups owing to accommodative asthenopia patient 156 examples of long-term close eye, each 78 people.One winding is subjected to the OPCs Drug therapy, a course of treatment (one month); Another group only adopts composite treatment such as correction of refractive errors, the treatment of Pilocarpin eye drop eye dripping etc. for matched group, and effective percentage is respectively 92%, 36%.
Test example 2: the asthenopic clinical observation II of the treatment of pharmaceutical composition of the present invention
Treatment is engaged in computer operation, is surfed the Net, sees TV for a long time, VDT asthenopia disease patient 90 examples such as play games, and is equally divided into 2 groups, and a winding is subjected to the treatment of OPCs, and another group is matched group, adopts general treatement.After 60 days, the contrast sensitivity of 45 patient's eyes of treatment group has clear improvement than matched group, cures 42 examples, 3 examples that take a turn for the better, effective percentage 93%.
Test example 3: the safety evaluatio of pharmaceutical composition of the present invention
Get 42 of Wistar kind rat, mices respectively, body weight 85-120g, oral OPCs50mg/kgd, continuous 6 months.Observe general drug reaction, detect indexs such as hematology, blood biochemical and histopathology.After 6 months, compare through every inspection and physiology and to have no significant change, without any side effects, and toleration is good, no teratogenesis, mutagenic action, LD
50All more than 4500.
The result of the standard extract of Fructus Vitis viniferae waste residue and clinical observation of composition for preventing and controlling asthenopia and safety evaluatio shows, standard extract of the present invention and preparation determined curative effect, mechanism is clear, have no adverse reaction, and proves that standard extract and preparation that the present invention makes are effective, safe and reliable.
Claims (8)
1. one kind is used to prevent and treat asthenopic plant extract and preparation and preparation method, it is characterized in that it is the effective site procyanidolic oligomers that extracts from the Fructus Vitis viniferae waste residue, can be mixed and made into preparation with arbitrary proportion separately or with adjuvant.
2. a kind of be used to prevent and treat asthenopic plant extract and preparation and preparation method according to claim 1, it is characterized in that, flavone and Polyphenols composition from the extraction of Fructus Vitis viniferae waste residue, oligomer comprising flavanol compound and procyanidin, total content is at 50%-99%, and wherein the content of effective ingredient catechin is in the 0.5-20% scope.
3. a kind of be used to prevent and treat asthenopic plant extract and preparation and preparation method according to claim 1 is characterized in that, with the extraction of Fructus Vitis viniferae waste residue water, alcohol extraction, purification by macroporous resin.
4. a kind of be used to prevent and treat asthenopic plant extract and preparation and preparation method according to claim 3, it is characterized in that: this method step is as follows:
(1) with Fructus Vitis viniferae waste residue extracting in water 1-10 time, the 2-20 that each consumption is respectively medical material weight doubly, extraction time is 0.5-10 hour, extracting temperature is 10-100 ℃, merge extractive liquid.
(2) with the Fructus Vitis viniferae waste residue with 5-95% alcohol reflux 1-10 time, the 2-20 that each consumption is respectively medical material weight doubly, extraction time is 0.5-10 hour, merge extractive liquid, filters, and reclaims ethanol, concentrated extractum.
(3) with the extracting solution of (1) or (2) extractum after adding water 1-200 and doubly diluting, last resin column absorption, the volume ratio of raw material weight and resin is 1: 0.5-10, resin column footpath is 1 with the post height ratio: 1-30, with pH value be water washing, the concentration of 2-8 be 5-95% alcoholic solution eluting, flow velocity be 0.5-3.5 column volume/hour.
(4) collect ethanol elution, in the ratio adding depigmenting agent of effluent volume 1-30%, reflux 0.1-10 hour, filter, concentrating under reduced pressure, vacuum drying, promptly.OPCs content can reach more than 50% in employing this law Fructus Vitis viniferae waste residue.
5. according to claim 3 or 4 described a kind of be used to prevent and treat asthenopic plant extract and preparation and preparation methoies, it is characterized in that described is by the resin of the polystyrene series of polystyrene series, modification and the synthetic opposed polarity of isobutene. series, different model and various concentration ethanol eluent and usage, consumption.
6. a kind of be used to prevent and treat asthenopic plant extract and preparation and preparation method according to claim 1 is characterized in that the standard extract that makes by claim 4 can directly make preparation or be mixed and made into preparation with its acceptable carrier.
7. a kind of be used to prevent and treat asthenopic plant extract and preparation and preparation method according to claim 1, prepared preparation is capsule, tablet, powder, granule, oral liquid, medicated wine, pill, pellet, soft gelatin capsule, ointment, mixture, tincture, injection etc.
8. a kind of be used to prevent and treat asthenopic plant extract and preparation and preparation method according to claim 1 is characterized in that, can be used for preventing and treating the asthenopia disease that a variety of causes causes.
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|---|---|---|---|
| CNB200410020680XA CN100560578C (en) | 2004-06-07 | 2004-06-07 | A kind ofly be used to prevent and treat asthenopic plant milk extract and preparation and preparation method |
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| CNB200410020680XA CN100560578C (en) | 2004-06-07 | 2004-06-07 | A kind ofly be used to prevent and treat asthenopic plant milk extract and preparation and preparation method |
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| CN1583011A true CN1583011A (en) | 2005-02-23 |
| CN100560578C CN100560578C (en) | 2009-11-18 |
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Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101999493A (en) * | 2010-12-08 | 2011-04-06 | 费维来 | Preparation method of plant health-care cool tea |
| CN101703635B (en) * | 2009-12-03 | 2012-08-08 | 应维强 | Production technology of grape pip and grape skin extract |
| CN102086185B (en) * | 2009-12-02 | 2013-05-08 | 中国科学院生物物理研究所 | Oligomeric proanthocyanidins and method for extracting same |
| CN105669780A (en) * | 2016-01-14 | 2016-06-15 | 张敬明 | Method for raising polyphenol content and water-solubility of grape seed extract |
| CN108618137A (en) * | 2018-07-18 | 2018-10-09 | 深圳极醇健康产业股份有限公司 | A kind of lycopene capsules and preparation method thereof |
| CN108887678A (en) * | 2018-07-18 | 2018-11-27 | 深圳极醇健康产业股份有限公司 | A kind of tomato red plain piece and preparation method thereof |
| CN113712957A (en) * | 2021-08-19 | 2021-11-30 | 温州医科大学附属眼视光医院 | Preparation method and application of oligomeric proanthocyanidins ophthalmic product |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1212320C (en) * | 2002-12-06 | 2005-07-27 | 沈阳中科药业公司 | Resin process of extracting proanthocyanidin from graup seed |
-
2004
- 2004-06-07 CN CNB200410020680XA patent/CN100560578C/en not_active Expired - Fee Related
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102086185B (en) * | 2009-12-02 | 2013-05-08 | 中国科学院生物物理研究所 | Oligomeric proanthocyanidins and method for extracting same |
| CN101703635B (en) * | 2009-12-03 | 2012-08-08 | 应维强 | Production technology of grape pip and grape skin extract |
| CN101999493A (en) * | 2010-12-08 | 2011-04-06 | 费维来 | Preparation method of plant health-care cool tea |
| CN105669780A (en) * | 2016-01-14 | 2016-06-15 | 张敬明 | Method for raising polyphenol content and water-solubility of grape seed extract |
| CN108618137A (en) * | 2018-07-18 | 2018-10-09 | 深圳极醇健康产业股份有限公司 | A kind of lycopene capsules and preparation method thereof |
| CN108887678A (en) * | 2018-07-18 | 2018-11-27 | 深圳极醇健康产业股份有限公司 | A kind of tomato red plain piece and preparation method thereof |
| CN113712957A (en) * | 2021-08-19 | 2021-11-30 | 温州医科大学附属眼视光医院 | Preparation method and application of oligomeric proanthocyanidins ophthalmic product |
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| Publication number | Publication date |
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| CN100560578C (en) | 2009-11-18 |
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