CN109420161A - Composition containing SOD - Google Patents

Composition containing SOD Download PDF

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Publication number
CN109420161A
CN109420161A CN201810939321.6A CN201810939321A CN109420161A CN 109420161 A CN109420161 A CN 109420161A CN 201810939321 A CN201810939321 A CN 201810939321A CN 109420161 A CN109420161 A CN 109420161A
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CN
China
Prior art keywords
composition
sod
preparation
phosphatidylserine
dried powder
Prior art date
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Pending
Application number
CN201810939321.6A
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Chinese (zh)
Inventor
倪少伟
徐公勇
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Shijiazhuang Shiqiang Biological Technology Co Ltd
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Shijiazhuang Shiqiang Biological Technology Co Ltd
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    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/115Fatty acids or derivatives thereof; Fats or oils
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/20Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • A61K31/202Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids having three or more double bonds, e.g. linolenic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/683Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43Enzymes; Proenzymes; Derivatives thereof
    • A61K38/44Oxidoreductases (1)
    • A61K38/446Superoxide dismutase (1.15)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/361Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/55Phosphorus compounds
    • A61K8/553Phospholipids, e.g. lecithin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/64Proteins; Peptides; Derivatives or degradation products thereof
    • A61K8/66Enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • A61P39/06Free radical scavengers or antioxidants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/08Anti-ageing preparations
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12YENZYMES
    • C12Y115/00Oxidoreductases acting on superoxide as acceptor (1.15)
    • C12Y115/01Oxidoreductases acting on superoxide as acceptor (1.15) with NAD or NADP as acceptor (1.15.1)
    • C12Y115/01001Superoxide dismutase (1.15.1.1)

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Abstract

The present invention relates to the compositions containing SOD and lipid.The lipid is acylglycerol class, phospholipid, sphingolipid, sterol and fatty acid.For the invention further relates to the preparation methods and purposes of the SOD and the composition of lipid.

Description

Composition containing SOD
Technical field
The present invention relates to compositions and Its Preparation Method And Use containing SOD and lipid, belong to protein bio Learn engineering and field of medicaments.
Background technique
It is described below and is conducive to reader's understanding.Provided information or the bibliography of reference are all not construed as this hair The bright prior art.
SOD is Super Oxide Dismutase abbreviation, and Chinese superoxide dismutase is important in organism Antioxidase, be distributed widely in various organisms, such as plant, microorganism etc..SOD has special physiological activity, is raw The primary substance of free radical is removed in object.The horizontal height of SOD in vivo means aging and dead intuitive finger Mark;Now it has proven convenient that up to more than 60 kinds of disease caused by oxygen radical.It, which can fight and block, makes cell because of oxygen radical At damage, and damaged cell is repaired in time, to cell damage caused by restoring because of free radical.Due to modern life pressure, ring Border pollution, various radiation and excess movement can all cause oxygen radical largely to be formed.SOD is British scientist Mann in 1938 One kind is isolated from ox red blood cell for the first time with Keilin containing copper protein, is initially named as hemocuprein.Britain in 1956 Professor Harman D proposes " free radical causes of senescence ", it is believed that free radical is the final root for causing aging and disease.1969 Year McCord etc. rediscovers this albumen, and it was found that their bioactivity has understood fully that it is catalyzed superoxide anion hair The property of raw disproportionated reaction, so being formally named as superoxide dismutase.Famous doctor of medicine's plumage Jin of Japan in 1980 Negative to point out: arthroneuralgia, cataract, chloasma, cancer etc., a variety of diseases are related with excessive free radical, and SOD can have Effect removes free radical.Hundreds of scientists of more than 100 countries in the whole world in 1985 unanimously generally acknowledge that there is a set of right in human body The mechanism of free radical resisting, this set mechanism are dominated and are regulated and controled by internal SOD, and SOD is the force at the core of confrontation and Trapped free radical, It is in vivo uniquely using free radical as the scavenger of substrate.Three, the U.S. famous scientist Luo Bai, Fei Rui and Luo Yigena in 1998 Promise to the whole world announce: SOD lack and activity reduction be mankind's birth and old age, sickness and death basic reason, supplement SOD can achieve it is pre- Prevent and treat various diseases, the purpose of anti-aging.This discovery of three of them has shocked countries in the world medical field, biology Educational circles.Also 1998 annual Nobel Prize in Physiology or Medicine are therefore obtained.SOD treats and prevents following disease: (1) can inhibit heart and brain Vascular diseases: the generation and accumulation of the aging of body and internal oxygen radical are closely related, and SOD can remove excessive in human body Harmful oxygen is free, is beneficial effect ingredient to health.With adjust blood lipid health-care effect, can prevention of arterial it is athero- Hardening prevents cardiovascular and cerebrovascular disease caused by hyperlipidemia.Reduce the content of lipid peroxide;(2) anti-aging effects: age Growth and certain extrinsic factors to will cause body and skin histology free radical and generate be more than that body normally removes free radical Ability leads to aging so that skin histology be made to damage.Since SOD can remove free radical, thus can delay aging; (3) autoimmune disease: SOD has certain curative effect to all kinds of autoimmune diseases.Such as lupus erythematosus, chorionitis, skin Myositis etc..Rheumatoid arthritis patients should be used before acute stage lesion is not formed, curative effect is preferable;(4) pulmonary emphysema: lung Wind-puff patient also can be used SOD, but should the use when lesion initial stage lung elastance fiber is not yet damaged, curative effect is preferable;(5) Radiation sickness and radiation protection: this product can be used to cystitis caused by treating because of radiotherapy, dermatomyositis, lupus erythematosus and leucocyte and subtract The diseases such as few, to the personnel being possible to by ionising radiation, also injectable SOD is as precautionary measures;(6) cataract of old people: This kind of disease should be started often to take antioxidant before entering the senescence phase, often inject SOD in other words.If once Form cataract, then it is invalid with SOD treatment in addition to extracing.
The SOD of separate sources, content, amino acid composition and activity are all different.Even if same biology, different tissues Or the SOD content of organ is not also identical.In actually prevention and/or treatment pathological symptom relevant to oxyradical or application In the process, the effect of SOD suffers from limitation, relies solely on the single albumen of SOD and tends not to effectively treat and be used to prevent And/or treatment people's oxygen radical increases and causes relevant pathological symptom or disease.Therefore it is badly in need of a kind of can generate with it to cooperate with The compound of effect forms composition.
Based on the inventors' understanding, there is presently no the prior arts that SOD and lipid are formed to composition, more specifically Composition, preparation method and the new application of the composition are all without open.
Summary of the invention
The present invention is to provide a kind of composition, and the composition is the composition containing SOD and lipid, wherein described group The active constituent part for closing object is made of two kinds of active components, and a kind of active constituent is SOD;Another active constituent is rouge Class.
In one aspect of the invention, the SOD derives from animal, plant or bacterium.The animal selects Free nursing dynamic Object, fish, birds, echinoderm, arthropod, reptile or molluscan group are groups of one or more.Described Bacterium is expression engineering bacteria, contains sod gene.
In one aspect of the invention, the SOD is freeze-dried powder, and has 90% or more purity and 3000U/mg or more Activity;Suitably, the freeze-dried powder has 95% or more purity and 5000U/mg or more activity;Desirably, have 96% The above purity and 7500U/mg or more activity;More suitably there is 97% or more purity and 10000U/mg or more activity;It is preferred that Ground has 98% or more purity and 12500U/mg or more activity;More preferably have 98% or more purity and 15000U/mg with Upper activity;More more preferably there is 98% or more purity and 17500U/mg or more activity;It is most preferably pure with 99% or more Degree and 20000U/mg or more activity.
In an additional aspect of the present invention, wherein at least one lipid of the composition be selected from by acylglycerol class, Phospholipid, sphingolipid, sterol and fatty acid composition group it is one or more;Preferably, at least one rouge of the composition Class is selected from the one or more of the group being made of phospholipid and fatty acid, and the phospholipid includes but is not limited to lecithin, brain phosphorus Rouge, phosphatidylserine, phosphatidyl glycerol, cuorin and phosphatidylinositols, sphingomyelins;The fatty acid includes but is not limited to There are linoleic acid, linolenic acid, ARA (arachidonic acid), DHA, EPA.Suitably, at least one lipid of the composition is selected from By lecithin, cephalin, phosphatidylserine, cuorin, ARA (arachidonic acid), DHA, EPA group formed one kind or It is a variety of.Preferably, at least one lipid of the composition is selected from by phosphatidylserine, cuorin, ARA (arachidonic Acid), DHA, EPA composition group it is one or more.It is highly preferred that at least one lipid of the composition is phosphatidyl silk Propylhomoserin and DHA.Most preferably, the composition at least one lipid is phosphatidylserine.
In the specific aspect that we are bright, the composition also contains fruit and/or vegetables and/or teas and/or cream Product and/or cereal and/or nut and seed and/or its extract and converted products and/or nutritional ingredient and/or flavouring One of or it is a variety of.
The composition of the invention be prepared into oral preparation, external preparation, sucking preparation, through nasal preparation, per rectum Preparation, percutaneous preparation or ejection preparation, the oral preparation are capsule, tablet, pulvis, granule, lozenge, effervescent tablet, sugar Slurry, emulsion, the prepared product of controlled release, rapidly-soluble prepared product, oral liquid dosage forms.
In the specific embodiment of the present invention, a kind of composition of tablet is provided, the composition is By
The two kinds of active components weight percent of the composition, wherein SOD (superoxide dismutase) institute accounting Example, by weight, the total weight for accounting for entire composition is 0.1%-98%;Another lipid proportion, by weight, The total weight for accounting for entire composition is 0.1%-98%.Desirably, SOD 5%-90%, lipid 10-95%;It is preferred that Ground, SOD 20%-85%, lipid 15-80%;It is highly preferred that SOD is 25%-75%, lipid 25-75%;It is especially excellent Selection of land, SOD 30%-70%, lipid 30-70%.
It is free for preventing and/or treating people's oxygen in preparation to be to provide the composition for a further object of the present invention Base increases the purposes of the drug for causing relevant pathological symptom or disease, nutrient and healthcare products, food or cosmetics.The disease It manages pathological symptom described in symptom or disease or disease includes but is not limited to different by more pleat Zou of skin aging, freckle and crow's feet Often increase, arthritis, rheumatoid, rheumatoid, intervertebral disk injury, osteoporosis, cardiovascular disease, inferior health Or lipid material deposition, obesity caused by secondary health, myocarditis, hyperlipidemia, hypertension, hyperglycemia, metabolic disturbance, Artery sclerosis, prostatitis, respiratory infectious disease, senile dementia, fatigue, insomnia, amnesia, anorexia, dysphoria, suppression Strongly fragrant or passive, anxious, dizzy, aging, shortness of breath and palpitation, stool and urine exception, hyposexuality, immune function decline are (often Catch a cold or have cold symptoms, throat discomfort, canker sore etc.), diabetes, ageing diseases, coronary heart disease, sexual function be depressed, chronic resistance The compositions such as plug property pulmonary emphysema, hepatitis, apocamnosis, neurasthenia, cerebral infarction, asthma, cough, adult respiratory distress syndrome (ARDS) One or more clinical pathological symptoms or disease of group.
The purposes further includes that the composition of the invention of prevention and/or therapeutically effective amount, the effective quantity are applied to people Composition of the invention including applying about 0.1mg/kg to about 10000mg/kg weight daily to people.A side of the invention Face further relates to SOD in the purposes of food, nutrient and healthcare products, drug and cosmetics.
The advantage of the invention is that used superoxide dismutase activity is high, purity is high.In the world, inventor The various composition five poisonous creatures: scorpion, viper, centipede, house lizard, toad of prepared superoxide dismutase and lipid and without any side effects, effectively (1) enhancing is exempted from Epidemic disease function is antifatigue;(2) promote longevity anti-aging;(3) SOD prepared by is the jinx of oxygen radical, it can be treated by oxygen freedom A variety of diseases caused by base.Experiment shows it to gastrointestinal function imbalance, loss of appetite, insomnia, memory loss, the improvement heart Vascular function has apparent preventive and therapeutic effect.At present prepare again domestic and international application cosmetics, health food such as;Dairy produce, The intermediate products such as candy, fruit juice, beverage, beer, white wine and health-caring capsule (tablet, spray).As the special of health food Functional additive, SOD have a wide range of applications.The immunogenicity to human body is eliminated, really is able to generate anti-oxidant, anti- Aging, anti-radiation, the anti-inflammatory, class's of dispelling beauty, enhancing immunity of organism and other effects.Accomplish Scientific Usage of Drugs, with a definite target in view.Fill up super The manufacture of superoxide dismutase tip and the country using technique, international blank, are conducive to Rehabilitation.
Specific embodiment
In order to provide property understanding for the essence of the present invention, hereinafter described with different the level of detail of the invention Some aspects, mode, embodiment, modification and feature.
In implementing the present invention, it may, used anatomy, materia medica, bromatology, food science, biochemistry, Many traditional technologies such as protein biochemistry, protein biochemistry engineering, pharmaceutical technology, medicine.These technologies are ripe Know.
Term " plant " of the present invention or " plant tissue " or " plant tissue organ " or " plant cell " or " plant " or " plant body a part " or " its primary prepares product " or " in-between product " or " final products " have in some occasions Identical meaning can be used alternatingly.
Plant used in the present invention includes but is not limited to that may originate at any kind of plant, it is including terrestrial or Aquatic, belong to all plants in kind including biological classification Zhong Jiemen detailed outline section.Wherein, the plant is Euglenophyta (Euglenophy-ta), Chlorophyta (Chlorophyta), charophyta (Charophyta), Chrysophyta (Chrysophyta), Pyrrhophyta (Pyrrophyta), Phaeophyta (Phaeophyta), Rhodophyta (Rhodophyta), Cyanophyta (Cyanophyta), Bacteriophyta (Bacteriophyta), myxomycota (Myxomycophyta), Eumycota (Eumycophyta), lichens door (Lichens), Bryophyta (Bryophyta), Pteridophyta (Pteridophyta), Gymnospermae (Gymnospermae), Angiospermae (Angiospermae) is one or more;It is preferred that the plant is angiosperm; Most preferably Rosa roxburghii Tratt.
Term " plant SOD " of the present invention or " plant tissue SOD " or " plant tissue organ SOD " or " plant cell SOD " Or " plant SOD " or " its primary prepares product " or " in-between product " or " final products " has phase in some occasions Same meaning, can be used alternatingly.
In a specific embodiment of the invention, Angiospermae (Angiospermae), dicotyledon have been used Guiding principle, Rosales, rosaceae, Rosa Rosa roxburghii Tratt carried out the extraction and purifying of SOD.
Term " one ", "an" and "the": indicating except non-content understands, otherwise in this explanation and the attached claims The singular " one " used, "an" and "the" include the reference object of plural number.For example, mentioned " a kind of SOD " includes A kind of independent SOD, the combination etc. of two kinds of difference SOD or more SOD.
Term " activating agent ", " active constituent " and " effective component ", some situations herein have the same meaning, It can be used alternatingly.
Term " animal " of the present invention or " animal tissue " or " animal tissue's organ " or " zooblast " or " animal body " or " animal bodies a part " or " its primary prepares product " or " in-between product " or " final products " have in some occasions Identical meaning can be used alternatingly.
Animal used in the present invention includes but is not limited to that may originate at any kind of animal, it is including terrestrial or Aquatic, belong to all animals in kind including biological classification Zhong Jiemen detailed outline section.Such as protozoa (Protozoa), in Lively object door (Mesozoa), placozoan door (Placo-zoa), has Cnidaria at Poritera (Porifera) (Cnidaria), Ctenophoa (Ctenophora), Platyhelminthes (Platyhelminthes), Nemertea (Nemertea), jaw stomach animal door (Gnathostomulida), Rotifera phylum (Rotifera), Gastrotricha phylum (Gastro-tricha), kinorhynch door (Kinorhyncha), Nemathelminthes (Nematoda), Nemathelminthes (Nematomorpha), the gill drags animal door (Priapula), Acanthocephala (Acanthocephala), endoprocta door (Entoprocta), loriciferan door (Loricifera), Annelida (Annelida), Echiuroidea (Echiura), Genus Golfingia (Sipuncula), Pogonophora (Pogonophora), by wrist animal door (Vestimentifera), Tardigrada (Tardigrada), Onychophora (Onychopho-ra), Arthropoda (Arthropoda), Mollusca (Mollusca), Brachiopoda (Brachiopoda), Ectoprocta (Ectoprocta), Phoronida (Phoronida), Chaetognath (Chaetognatha), Echinodermata (Echinoderma-ta), Hemichordata (Hemichordata), Chordata (Chordata).Chordata packet Include Urochordata, Cephalochordata, Vertebrate.Wherein Vertebrate subphylum includes: garden mouthful guiding principle, net-rope, two It dwells guiding principle, Reptilia, Aves, Mammalia etc..The animal can be selected from by mammal, fish, birds, echinoderm, segmental appendage Animal, reptile or molluscan group are groups of one or more.It is only for example, the mammal packet of the terrestrial of this paper Include but be not limited to the mankind, orangutan, monkey, ox, buffalo, wild ox, pig, wild boar, sheep (such as lamb, sheep, goat), donkey, deer, white horse with a black mane Camel, alpaca, muroid, kangaroo, elephant, tiger, leopard, lion, crocodile, snake, horse etc., the aquatic animal of this paper include but is not limited to fish Class, whale, river horse, sea dog etc..SOD can be extracted from animal tissue or organ, such as from spleen, liver, heart etc..
SOD can also derive from engineering bacteria, such as colibacillus engineering etc., in advance by genes such as SOD clone, expression Engineering means obtain the SOD of expression.Such as the source of people SOD of expression, corn SOD etc..
Term " one ", "an" and "the": indicating except non-content understands, otherwise in this explanation and the attached claims The singular " one " used, "an" and "the" include the reference object of plural number.For example, mentioned " a kind of SOD " includes A kind of independent SOD, the combination etc. of two kinds of difference SOD or more SOD.
Term " animal SOD " of the present invention or " animal tissue SOD " or " animal tissue organ SOD " or " zooblast SOD " Or " animal body SOD " or " its primary prepares product " or " in-between product " or " final products " has phase in some occasions Same meaning, can be used alternatingly.
In an embodiment of the invention, superoxide dismutase obtained is detected, qualitatively and quantitatively Analysis.Detection method includes: Van Gieson decoration method, picrosirius-red (sirius red)-polarized light approach, compound Decoration method (including the alkaline product of Ponceau S (ponceau S)-picric acid (picric acid), resorcinol (resorcin)- Red (fuchsine)) composition compound staining.Quantitative analysis includes: Kjeldahl's method, biuret method, ultraviolet absorption method, examines Mas bright blue method, Picro-Sirius red (sirius red) method.Qualitative analysis includes: BioRad 2D PAGE electrophoresis apparatus, BioRad etc. Electricity point electrophoresis apparatus etc..Calorimeter (DSC), sepectrophotofluorometer, ultraviolet point are scanned using Japanese HITACHI circular dichroism, heat differential Light photometer, infrared spectrophotometer, NMR, albumin crystal diffractometer, scanning electron microscope;Common protein amino assays Have the mass spectrometers such as edman method, mass spectrometry have the full-automatic amino-acid analyzer of Britain Biochrom 30+, (HITACHI) the full-automatic amino-acid analyzer L-8900 of Hitachi, Britain amino-acid analyzer AA4300, Germany Man Moboer A300 automatic amino acid analyser, sykam company, Germany be full-automatic and semi-automatic amino-acid analyzer, Germany sykam+ S433D, 491 protein sequencer of American AB I company ProciseTM, Japanese Shimadzu PPSQ-31A albumen automatic sequencer.
It therefore, can be according to purity, activity and actually from raw material to the assessment of method and art methods of the invention Three aspects of protein content (g or mg) of middle extraction carry out comprehensive assessment.
Used superoxide dismutase freeze-dried powder activity of the invention in 5000U/mg or more, such as 6000U/mg, 6500U/mg, 7000U/mg, 7500U/mg, more than.Preferably 10000U/mg or more, more preferably 12500U/mg or more, more More preferably 15000U/mg or more, most preferably 22000U/mg or more.
Used superoxide dismutase freeze-drying powder purity of the invention is proper to exist in purity 85% or more 85% or more, properly 95% or more, preferably 97% or more, more preferably 98 or more, more more preferably 98.5 or more, most It is preferred that 99% or more.
The vigour-testing method of SOD
The assay NBT photoreduction of improvement is simple and easy, more practical.Chemoluminescence method and Nitrite formation method are uncomfortable React extremely sensitive for measuring Mn-SOD, but for Cu/Zn-SOD.Cyte reduction method is steady for Mn-SOD vitality test result It is fixed, it is reproducible.But specificity and sensitivity are not ideal enough, and need specific apparatus, and practical application is restricted.Nitrous Hydrochlorate forms method and combines with CN- inhibitor or SDS processing, is applied to Mn-SOD and measures, remolding sensitivity Cyte reduction method improves Several times, and specificity is strong, it is reproducible, it is easy to operate, specific apparatus and equipment are not needed, practical application and popularization are easy to, It is one of presently preferred measuring method.Under normal conditions, SOD enzyme activity measurement can only apply indirect activity measuring method.Root According to SOD national standard, our company is using improvement Marklund method, i.e. mouse thymus cells method.
1 definition: required SOD amount is a unit of activity when inhibition pyrogallol talks about rate 50% from oxygen at 25 DEG C.
2 principles: under alkaline condition, autoxidation can occur for pyrogallol, can inhibit mouse thymus cells according to SOD Ability measures SOD vigor.
3 reagents: A liquid: tri- rifle aminomethane (Tris) of pH8.20 0.1mol/L-hydrochloride buffer (includes 1mmol/L EDTA.2Na).It weighs 1.214g Tris and 37.2mg EDTA.2Na and is dissolved in 62.4mL 0.1mol/L hydrochloric acid solution In, 100ml is settled to distilled water.B liquid: 4.5mmol/L pyrogallol hydrochloric acid solution.Weigh pyrogallol (A.R) 56.7mg It is dissolved in a small amount of 10mmol/L hydrochloric acid to be dissolved in, and is settled to 100mL.
4 instruments: ultraviolet-visible spectrophotometer, secret acidometer, accuracy 0.01pH, centrifuge, 10mL cuvette, 10mL centrifuge tube, glass mortar.
The preparation of 5 samples:
6 analytical procedures: A is once added in 10mL cuvette at 25 DEG C or so in mouse thymus cells rate determination Liquid 2.35mL, distilled water 2mL, B liquid 0.15mL.B liquid is added and mixes and be poured into cuvette immediately, is measured respectively in 325 wavelength items Light absorption value, the difference between the two, that is, mouse thymus cells rate Δ A after initial and 1min under part325(min-1) the determining Δ of this test of A325(min-1) it is 0.060.It is as follows that SOD determination of activity is loaded program list:
Test solution Blank Sample liquid SOD liquid
A liquid/ml 2.35 2.35 2.35
Distilled water/ml 2 1.8 1.8
Sample liquid or SOD liquid/ul 0 20 20
B liquid/ml 0.15 0.15 0.15
7 results calculate: fluid sample calculates as follows:
In formula:
U/mL:SOD enzyme activity unit
Δ A325: mouse thymus cells rate
Δ A ' 325: sample liquid or SOD enzyme solution inhibit mouse thymus cells rate
V: added enzyme solution or sample liquid volume, unit are milliliter (mL)
D: the extension rate of enzyme solution or sample liquid
4.5: reaction solution total volume, unit are milliliter (mL)
Calculated result retains 3 effective digitals.
Solid sample calculation formula is as follows:
In formula:
U/g:SOD enzyme activity unit
Δ A325: mouse thymus cells rate
Δ A ' 325: sample liquid or SOD enzyme solution inhibit mouse thymus cells rate
V: added enzyme solution or sample liquid volume, unit are milliliter (mL)
V1: sample liquid total volume, unit are milliliter (mL)
D: the extension rate of enzyme solution or sample liquid
M: sample quality, unit are gram (g)
4.5: reaction solution total volume, unit are milliliter (mL)
Calculated result retains three effective digitals.
Prepared superoxide dismutase is in preparation for preventing and/or mitigating and/or treat according to the method for the present invention And/or cure superoxide anion (O2 -) increase drug, food, health care product or the cosmetics of caused pathological symptom or disease In purposes.The pathological symptom or disease includes but is not limited to be increased extremely by more pleat Zou of skin aging, freckle and crow's feet More, arthritis, rheumatoid, rheumatoid, intervertebral disk injury, osteoporosis, cardiovascular disease, inferior health or secondary The deposition of lipid material caused by health, myocarditis, hyperlipidemia, hypertension, hyperglycemia, metabolic disturbance, obesity, artery Hardening, prostatitis, respiratory infectious disease, senile dementia, fatigue, insomnia, amnesia, anorexia, dysphoria, depression or Passive, anxious, dizzy, aging, shortness of breath and palpitation, stool and urine exception, hyposexuality, immune function decline (often flu Or have cold symptoms, throat discomfort, canker sore etc.), diabetes, ageing diseases, coronary heart disease, sexual function be depressed, chronic obstructive The group of the compositions such as pulmonary emphysema, hepatitis, apocamnosis, neurasthenia, cerebral infarction, asthma, cough, adult respiratory distress syndrome (ARDS) One or more clinical pathological symptoms or disease.
Term " treatment " used herein refers to treatment treatment measures and measure that is preventing or preventing, wherein Prevent or slow down the pathological symptom suffered from or the imbalance of (decrease) subject.If received according to method described herein The superoxide dismutase prepared according to the method for the present invention of therapeutic dose, then the symptom of subject succeed " treatment ", Subject shows, it can be observed that and/or being measured to one or more signs of symptom and symptom is reduced and disappeared.Should also Understand, it is described herein treatment or prevent the various modes of medical conditions to be intended to mean that " significant " comprising all treat or Prevent and be less than all treatments or prevention, wherein having reached certain biology correlation or the relevant result of medicine.
In various embodiments, suitable external test or in vivoassay are carried out to measure and be based on specifically according to this Whether the effect of the therapeutic agent of superoxide dismutase prepared by inventive method and administration are suitable for treatment.In various realities Apply in mode, can representativeness cell involved in the illness to subject carry out external test, it is given based on root to measure Whether desired effect is produced to the cell type according to the therapeutic agent of superoxide dismutase prepared by the method for the present invention Fruit.If receiving the superoxide dismutase prepared according to the method for the present invention of the therapeutic dose according to method described herein Enzyme, then the symptom of subject is treated with succeeding, i.e., subject shows, it can be observed that and/or being measured to above-mentioned pathology disease Shape or the one or more signs and symptom of disease are reduced and are disappeared.It is also understood that described herein treat or prevent medical treatment The various modes of situation are intended to mean that " significant " comprising it all treats or prevents and be less than all treatments or prevent, Certain biology correlation or the relevant result of medicine are wherein reached.
In the specific embodiment of the present invention, to subject apply prevention and/or therapeutically effective amount containing with good grounds The drug of superoxide dismutase prepared by the method for the present invention.
Term " effective quantity " used herein refers to being enough to obtain required treatment and/or preventive effect, such as draws It plays prevention or mitigates the amount of the symptom with pathological symptom or disease.The amount for being administered to the composition of subject will depend on disease Type and seriousness and individual property, such as health condition, age, gender, weight and the tolerance to drug usually Power.The amount additionally depends on extent, seriousness and type.Those skilled in the art will be according to these factors and its He is because usually determining suitable dosage.The composition may also be combined with one or more other therapeutic compounds to be administered.? In method described herein, the compound of the present invention can be administered to one or more signs or pathology with pathological symptom The subject of symptom.For example, " therapeutically effective amount " refers to the average level for minimally mitigating the physiological action of symptom.
In general, the dosage will prevent or mitigate the seriousness or extension of institute's treatment situation or indication.Correct agent Amount will depend on environment, for example, the situation treated, administration time table, the compound whether be administered alone or with it is another Kind therapeutic agent is in conjunction with application, the holistic health of the plasma half-life of the compound and subject.
Can be using including oral, external application, sucking, intranasal, per rectum, percutaneously or injection method of application uses subject Medicine.
In the specific embodiment of the present invention, uses composition of the invention to be administered subject, given daily Pharmaceutical quantities scheme be about 0.1mg/kg to about 10000mg/kg weight, be preferably from about 1mg/kg to about 1000mg/kg weight, more Preferably 1mg/kg to about 500mg/kg, most preferably 1mg/kg are to about 200mg/kg weight.It can apply 1 to 6 time daily, it is excellent Select daily administration 2 or 3 times.Interval be also possible to it is irregular, skilled artisans recognize that compound or its can pharmaceutically connect The optimised quantity for the salt received and the interval of single-dose will be by the property and degree of situation to be treated, form, approach and the positions of administration Point and the concrete condition of subject treated and determine, and can determine most preferably scheme with routine techniques.This field skill Art personnel should also be understood that the optimum process for the treatment of, i.e., the compound given daily in given number of days or its pharmaceutically may be used The administration quantity of the salt of receiving can be determined by those skilled in the art using conventional treatment test method.It is answered in treatment In, there is relatively high dosage to be needed in relatively short time interval sometimes, until the process of disease slows down or terminates Until, and preferably up to subject shows partial or fully improve the disease or pathological symptom.Therefore, Huan Zheke With the administration mode to effecting prevention property of patient.It would be recognized by those skilled in the art that certain factors can influence effectively to control Treat dosage and the time of a subject, the including but not limited to severity of disease or imbalance, previous treatment, healthy feelings The age and existing Other diseases of condition and/or subject.Moreover, utilizing the treatment pair of therapeutically effective amount described herein It may include single therapy or a series of treatments that a subject is treated according to composition.
Prepared SOD of the invention can be applied together at least one lipid.The lipid includes mainly having acyl group sweet Oils (neutral fat), phospholipid, sphingolipid, sterol and fatty acid etc..Preferably at least one phospholipid and/or fat Acid is applied together.Phospholipid is mainly phosphoglyceride, mainly includes glycerophosphatide and sphingomyelins, and glycerophosphatide mainly wraps It is sweet to include phosphatidyl choline (lecithin), phosphatidyl-ethanolamine (cephalin), phosphatidylserine, phosphatidyl glycerol, two phosphatidyls Oily (cuorin) and phosphatidylinositols etc..
The compound of the present invention can be applied together with other at least one compounds.Herein only as an example, such as Common compounds with treatment of arthritis include but is not limited to another specific aspect bright in we, and the composition also wraps Include but be not limited to clenobuterol hydrochloride, Ipratropium Bromide, aminophylline, nedocromil, beclomeasone propionate, ranitidine, bromine third Amine too woods, domperidone, magnesium sulfate, Bisacody, sodium glutamate, metadoxine, pepsin, furosemide, Hydrochioro, Spirolactone, ammonium chloride, theophylline, sorbierite, Nieron Capsules, flavoxate hydrochloride, meclofenoxate, Finasteride, oxytocin, fluorine it is light Pine, desoxycortone, Nandrolone Phenylpropionate, estradiol, Medroxyprogesterone, Gonadorelin, thyroid-stimulating hormone, propylthiouracil (PTU), first Phenbutamide, Glipizide, melbine, acarbose, glucagons, penicillin, ampicillin, Amoxicillin, cephalo thiophene Pheno sodium, cefalexin, Cefradine, Su Batan, gentamicin, amikacin, tetracycline, aureomycin, half promise ring element, chlorine are mould Element, erythromycin, medecamycin, roxithromycin, clarithromycin, the inorganic calcium system of captopril, such as calcium chloride, calcium carbonate Agent or organic calcium preparation, the zinc preparation of such as zinc sulfate, clodronic acid disodium, ethoxy diphosphate sodium, ipriflavone, D-Glucosamine Hydrochloride, Salicylic Acid Formulations, brufen, Fenbid, Indomethacin, Osaminethacine, relaxes at chondroitin sulfate Woods acid (Zulida), excellent appropriate, naproxen, celecoxib, rofecoxib, azithromycin, polymyxin e, cyclammonium pyrimidine, furans It is appropriate because, Norfloxacin, metronidazole, Tinidazole, isoniazid, rifampin, dapsone, acyclovir, Ribavirin, Miconazole, blueness Artemisin pentothal, lidocaine, benzocainum, dissolves, is library bromine ammonium, meclofenoxate, aniracetam, pethidine, tramadol, right Paracetamol (paracetamol), Diclofenac, brufen, Allopurinol, ergotamine and caffeine tablet, amobarbital, chlorine west dissolve, Galanthamine, dilantin sodium, carbamazepine, carbidopa, diphenhydramine, Betahistine, Vinpocetine, chlorpromazine, fluorine piperazine Pyridine alcohol, clopenthixol, Clozapine, Pipotiazine Palmitate, nitrazepam, estazolam, imipramine, cyclophosphamide, first ammonia are talked endlessly Purine, mitomycin, taxol, Leuprorelin, cis-platinum, nitroglycerin, Verapamil, nifedipine, prenylamine, quinindium, Esmolol hydrochloride, amiodarone, bepridil, clonidine, Urapidil, sodium nitroprussiate, Nimodipine, enalapril maleate, Foxalin, Amrinone, adrenaline, niacin, ligustrazine, heparin sodium, urokinase, bromhexine hydrochloride, benproperine, thoroughly Bright matter acid sodium (A Erzhi, Hyalgan, Sofast), aulin (happy U.S. power), indocin, aspirin, feldene, fluorine Fenamic acid, gold salt, penicillamine, chloroquine and its derivative, levamisol, Adrenal Glucocorticoid class drug (such as prednisone), ring It is spore rhzomorph, salicylazosulfapyridine, cyclophosphamide, imuran, methopterin, interferon, specific antibody (McAb), big That organizes composed by beans isoflavones is one or more.It will be appreciated by those skilled in the art that being applied together with the compound of the present invention Above compound can make a choice according to the various disease or pathological symptom.
The compound of the present invention can be with other at least one Chinese herbal medicines, the intermediate product of the Chinese herbal medicine and its extraction Liquid is applied together.Chinese ephedra, ramulus cinnamomi, purple perilla, ginger, elscholtiza, schizonepeta, radix saposhnikoviae, Rhizoma Et Radix Notopterygii, the root of Dahurain angelica, asarum, ligusticumic can be selected in Chinese herbal medicine Sheet, the achene of Siberian cocklebur, the flower bud of lily magnolia, Bulbus Allii Fistulosi, Centipeda minima, coriandrum, Chinese tamarisk, peppermint, great burdock achene, cicada slough, mulberry leaf, chrysanthemum, fructus viticis, bavin Recklessly, cimicifugae foetidae, pueraria lobata, flower of kudzuvine, Fermented Soybean, semen sojae germinatum, duckweed, scouring rush, gypsum, gypsum rubrum, rhizoma anemarrhenae, reed root, radices trichosanthis, bamboo Leaf, lophatherum gracile, dayflower, cape jasmine, Prunella vulgaris, cassia seed, bat's faces, pipewort, butterflybush flower, the seed of feather cockscomb, garter snake gall, pig gall Juice, the coptis, Cortex Phellodendri, rough gentian, the bark of ash, kuh-seng, cortex dictamni, Sophora alopecuroide, barberry, manyleaf meadowure rhizome and root, bark of tree of heaven, honeysuckle, is born radix scutellariae Winter rattan, Fructus Forsythiae, Herba Andrographitis, folium isatidis, Radix Isatidis, indigo naturalis, rhizome of cyrtomium, dandelion, viola mandshurica, wild chrysanthemum, Paris polyphylla, adder-wort, leakage Reed, smilax, cordate houttuynia, cymose buckwheat rhizome, sargentodoxa cuneata, Sargent gloryvine, field pennycress, Patrinia heterophylla, blackberry lily, beans root, Lasiosphaera fenzlii, Chinese olive, bright and beautiful lamp Cage, tinosporae, Oroxylum indicum, the Chinese bulbul, purslane, Java brucea, Herba Euphorbiae Humifusae, potentilla chinensis, potentilla discolor, lobelia chinensis, oldenlandia Grass, edible tulip, bear gall, climbing groundsel, radix ampelopsis, Chinese holly, mung bean, paris polyphylla, Verbena officinalis, hymsleya amabilis, evodia lepta merr, cottonrose hibiscus leaf, half Lotus, iron amaranth, olive, emblic, bicolor, achyranthes aspera, Glabrous Sarcandra Herb, radix rehmanniae recen, radix scrophulariae, cortex moutan, radix paeoniae rubra, Asian puccoon, buffalo Angle, rabdosia lophanthide, sweet wormwood, radix cynanchi atrati, the root bark of Chinese wolf-berry, radix stellariae dichotomae, Radix picrorrhizae, rheum officinale, saltcake, folium sennae, aloe, the root of gansui, the root of Beijing euphorbia, Yuan Flower, Phytolacca acinosa, kaladana, crotons, semen euphorbiae, Chinese tallow tree root skin, fructus cannabis, brush-cherry seed, SEMEN PINI KORAIENSIS, Radix Angelicae Pubescentis, the root of Chinese clematis, monkshood, Radix aconiti agrestis, long-nosed pit viper, Bungarus Parvus, zaocys dhumnade, snake slough, pawpaw, silkworm excrement, lycopodium calvatum, berba aristolochiae mollissimae, turpentine, caulis piperis futokadsurae, caulis sinomenii, Erycibe obtusifolia benth, tripterygium hypoglaucum hutcs, Radix Aconiti Brachypodi (Radix Aconiti Szechenyiani), Fructus Liquidambaris, resina liquidamberis, lanatechead saussurea herb with flower, tripterygium wilfordii, paniculate swallowwort, lamiophlomis rotata, noisy sheep Flower, alangium, gentianae macrophyllae, the root of fangji, ramulus mori, Common St.Paulswort Herb, clerodendron trichotomum, erythrina bark, caulis trachelospermi, tripterygium wilfordii, geranium wilfordii, is worn at Radix zanthoxyli Mountain dragon, luffa, cortex acanthopanacis, herba taxilli, rhizoma cibotii, rhizoma homalonemae, lanatechead saussurea herb with flower, pyrola, folium photiniae, wrinkled giant hyssop, eupatorium, rhizoma atractylodis, thickness Piao, fructus amomi, villous amomum pericarp, cardamom, tsaoko, Poria cocos, semen coicis, umbellate pore furgus, rhizoma alismatis, wax gourd, corn stigma, cucurbit, cortex periplocae, trifoliate orange Dulcis Son, wartwort, mole cricket, shepherd's purse, semen plantaginis, talcum, caulis akebiae, the stem pith of the rice-paper plant, dianthus superbus, pivot storage, the fruit of summer cypress, Lygodium japonicum, pyrrosia lingua, chingma abutilon seed, It is rush, Bi Collettii, oriental wormwood, herba lysimachiae, polygonum cuspidate, hypericum japonicum, stringy stonecrop, Canton love-pea vine, Sagina subulata, centella, rabdosia lophanthide, attached Son, rhizoma zingiberis, cortex cinnamomi, evodia rutaecarpa, fennel, cloves, galangal, galanga galangal seed, pepper, Chinese prickly ash, fructus piperis longi, piper cubeba, kaempferia galanga, dried orange peel, Tangerine seed, tangerine pith, tangerine leaf, Exocarpium Citri Grandis, green peel, the dried immature fruit of citron orange, Fructus Aurantii, radix aucklandiae, agalloch eaglewood, santal, Fructus meliae toosendan, the root of three-nerved spicebush, dutchmanspipe root, lichee Core, rhizoma cyperi, fingered citron, citron, rose, armeniaca mume, buckeye, Longstamen Onion Bulb, herba aristolochiae, the shell of areca nut, rhizoma nardostachyos, aspongopus, sword bean, The calyx and receptacle of a persimmon, fiveleaf akebia fruit, hawthorn, Divine Comedy, malt, rice bud, rice sprout, radish seed, endothelium corneum gigeriae galli, fevervine, cynanchum wilfordii, asafoetide, China tree Skin, betel nut, pumpkin seeds, gemma agrimoninae, stone-like omphalia, Lappula echinata, Chinese torreyanut, fructus ulmi, field thistle, setose thistle, garden burnet, Chinese scholartree, cacumen biotae, rhizoma imperatae, ramie Snippings, sheep hoof, aizoon stonecrop, folium artemisiae argyi, baked ginger, humus flava usta, Radix Notoginseng, madder, cattail pollen, marmor serpentinatum, dalbergia wood, carbonized hair, bletilla, Hairyvein agrimony, Callicarpa bodinieri Levl., Plant Soot, crinis trachycarpi, rhizoma nelumbinis, Loropetalum wood, peanut coat, Rhizoma Chuanxiong, rhizoma corydalis, Radix Curcumae, turmeric, olibanum, myrrh, Excrementum pteropi, decumbent corydalis tuber, resina liquidamberis, balsamine, Radix Salviae Miltiorrhizae, safflower, peach kernel, motherwort, Herba Lycopi, radix achyranthis bidentatae, Caulis Spatholobi, the seed of cowherb, China rose, ground bettle, vomiting nut, native copper, bush, the rhizome of davallia, dragon's blood, catechu, Artemisia anomala, fructus polygoni orientalis, is bitten Chinese trumpet creeper Worm, curcuma zedoary, trigone, leech, gadfly, Chinese blister beetle, pangolin, the tuber of pinellia, Southern Star, rhizoma typhonii, semen brassicae, Chinese honey locust, Inula britannica chinensis, gold boiling Grass, Cynanchum glaucescens, radix ranunculi ternati, bulbus fritillariae cirrhosae, fritillaria thunbergii, Snakegourd Fruit, caulis bambusae in taenian, bamboo juice, tabasheer, the root of purple-flowered peucedanum, campanulaceae, the sterculia seed, seaweed, elder brother Cloth, airpotato yam, concha meretricis seu cylinae, bryozoatum, blood clam, chlorite schist, bezoar from monkeys, indian rorippa herb, almond, perilla seed, the tuber of stemona, aster, tussilago, Birthwort, loguat leaf, the root bark of white mulberry, lepidium seed, gingko, ginkgo leaf, ardisia japonica, datura flower, Physochlaina macrophylla, Siraitia grosvenorii, it is Rhododendron dauricum, Thorny elaeagnus leaf, cinnabar, magnetite, keel, amber, pearl, semen ziziphi spinosae, the seed of Oriental arborvitae, ganoderma lucidum, valerian, the vine of multiflower knotweed, cortex albiziae, conjunction Joyous flower, Radix Polygalae, tuber fleeceflower stem, the shell of seaear, mother-of-pearl, oyster, concha mauritiae, raddle, tribulus terrestris, bluish dogbane, pig iron Luo, Lv beans Clothing, antelope's horn, cornu caprae hircus, cow-bezoar, pearl, uncaria, Rhizoma Gastrodiae, close ring bacterium, pheretima, scorpio, centipede, bombyx batryticatus, stiff pupa, male silk moth That organizes Deng composed by is one or more.
It will be appreciated by those skilled in the art that the above compound applied together with the compound of the present invention can be according to institute The various disease or pathological symptom stated make a choice.
The compound or Chinese herbal medicine can be used as individual preparation or combination is administered simultaneously in unit dosage forms, or Person sequentially applies.Under any circumstance, a variety of therapeutic agents can in any order or be even administered simultaneously.If simultaneously, institute State a variety of therapeutic agents can be provided as single, unified form or in the form of multiple (for example, as single tablet or The different preparations of two kinds of tablet or capsule independent).One of therapeutic agent therapeutic agent may be mentioned with multi-dose type For or it is therein two kinds can be used as multi-dose type provide.If not simultaneously, the time interval between multidose Can from be greater than 0 week to be less than about 1 week, be less than about 2 weeks, less than about 4 weeks, less than about 2 months, less than about 4 months or even small Change in the range of about half a year.
Terms used herein " unit dosage forms " refer to be suitable as the unit dose for people and plant subject Physically separated unit, each unit include the compound of individual predetermined amount or combine with other reagents, and amount is computed It is enough to generate desired effects with pharmaceutically acceptable diluent, carrier or media mix.
In a specific embodiment of the invention, preparation contains superoxide dismutase prepared according to the method for the present invention The pharmaceutical composition of enzyme is used to treat and/or prevent to drop collagen by inhibiting human cathepsin K activity to increase Solution obtains improving relevant pathological symptom or disease.It sends out snibject by modes such as oral, external application, inhalations The effect of waving.Therefore pharmaceutical composition of the invention can be prepared into various dosage forms, for example, the composition for oral medication can Think capsule, tablet, pulvis, granule, lozenge, effervescent tablet, syrup, emulsion, the prepared product of controlled release, rapidly-soluble system Standby object, oral liquid dosage forms etc.;Composition for external application medication can be liniment type drug, creme, external application, ointment, outer With liquid medicine, the gentle spray of liquid spray etc..Composition for inhalation administration can be solution, dispersion liquid, dry powder Deng;, the nanometer of liposome is prepared, ejection preparation and extended drug form are prepared into.Described pharmaceutical composition institute accounting Example, by weight, the total weight for accounting for entire preparation is 0.01%-99%, preferably 0.1%-90%, such as 0.1%- 75%, 0.1%-70%, 0.1%-65%, 0.1%-60%, 0.1%-55%, 0.1%-50%, 0.1%-45%, 0.1%-0.1%-40%, 0.1%-35%, 0.1%-30%, 0.1%-25%, 0.1%-20%, 0.1%-15%, 0.1%-10%, 0.1%-5%, 0.1%-2%.
In pharmaceutical preparation of the present invention, by taking oral preparation as an example, pharmaceutically acceptable auxiliary material used includes but does not limit to Lactose, sucrose, mannitol xylitol, erythritol, D-sorbite, magnesium stearate, calcium stearate or zinc stearate, it is stearic Acid, Compritol 888 ATO, sodium stearyl fumarate, talcum, silica gel;Disintegrating agent, as starch, cyclodextrin, microcrystalline cellulose, (hydroxypropyl methyl is fine for methylcellulose, sodium carboxymethylcellulose, ethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose Dimension element), cellulose acetate phthalate, acetic acid hydroxypropyl methylcellulose succinate, polyvinyl acetate phthallate (PVAP), Acrylic resin, polyvinyl alcohol, sodium carboxymethyl starch, crospovidone, low-substituted hydroxypropyl cellulose, carboxymethyl cellulose Element, cross-linked carboxymethyl cellulose, crosslinked polyvinylpyrrolidone, polylactic acid, glycerol (sorbierite), glycerin gelatine, dodecyl Sodium sulphate, polyethylene glycol, strawberry, orange, banana, peppermint, honey.
Carrier granular can be lactose or the crystal or sphere of sucrose;Or composite sphere or particle, such as by being made with starch For adhesive make sucrose granulate to be formed sugar sphere, the carbonic acid calcospherite or malt formed by starch as adhesive Dextrin.Carrier granular is also possible to the particle of any other medical acceptable excipient, such as hydroxypropyl cellulose Grain, guar gum particle, xanthan gum particle.Carrier can be there are many form, and all these selections and the adjustment of amount are obviously at this In the limit of power of field technical staff.
In the specific embodiment of the present invention, there is provided a kind of tablet composition, the composition is by being By D-mannital, D-sorbite, Rosa roxburghii Tratt SOD freeze-dried powder, maltodextrin, magnesium stearate, phosphatidylserine, citric acid, hydroxyl Propyl methocel, essence for food composition.
SOD of the invention can be with fruit and/or vegetables and/or teas and/or dairy products and/or cereal and/or nut Alimentation composition is formed with seed and/or its extract and converted products and/or nutritional ingredient and/or flavouring.Contain this hair The alimentation composition of superoxide dismutase prepared by bright method, which may include, to be dissolved in the liquid of food or health care product , such as it is optionally dissolved in the aqueous liquid or water-alcohol class solution of seasoning.It can be included into edible solid or half In the composition of dry solid, for example, particle form, pill, tablet, enteric coatel tablets form in.It can also be placed on food In liquid in object or health care product.It can be a variety of Orally administered composition embodiments, especially it is possible to be for swallowing The Orally administered composition embodiment of food additives.Enteric coatel tablets, colloid capsule, gel, emulsification are manufactured by conventional method Object, tablet, capsule or solution and preparation.Specifically, activating agent according to the present invention can be included in dietary supplement ingredient or reinforcing Among any other form of food or health care product, such as food or health care product stick, or compression or uncompressed pulvis.This A little pulvis can be diluted with water, and can be diluted with water in soda, salt cheese production or soybean derivatives, or can be included in food In product or health care product.
In yet another embodiment of the present invention, preparation contains superoxides discrimination prepared according to the method for the present invention Change the cosmetics of enzyme, the cosmetics can for liniment type drug, creme, be applied with ointment or plaster, externally used solution, Dispersion liquid, dry powder, dry liquids spray, gas spray or the various preparations for being suitable for injection etc..Pass through injection, external application side Formula reaches treatment or prevention and/or treatment human cathepsin K activity increases and causes collagen degradation to subject's medication The purpose of relevant pathological symptom or disease.
It is recorded by following examples, more fully understands the present invention, but be not limited to the embodiment.
Embodiment
The preparation of 1 Tablets of embodiment
Tablet A preparation
Preparation process: cattle liver SOD freeze-dried powder 100g, lecithin 10g, cephalin 20g, phosphatidylserine are weighed 100g, cuorin 10g, ARA (arachidonic acid) 15g, DHA20g, EPA15g, sieve with 100 mesh sieve, and tapioca, gala is added Sugar, microcrystalline cellulose cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, and 60 DEG C dry Dry, the magnesium stearate of 2g is added in dry particl for 18 mesh integer dry particls.Then using bi-layer tablet press stamping to get every The amount of the piece freeze-dried powder of SOD containing cattle liver is 200mg and various lipid 400mg.
Tablet B preparation
Activating agent Additive amount (g)
Cattle liver SOD freeze-dried powder 100
Phosphatidylserine 100
Cuorin 25
ARA 25
DHA 25
EPA 25
Auxiliary material
Tapioca 100
Galactolipin 35
Microcrystalline cellulose 65
Preparation process: cattle liver SOD freeze-dried powder 100g, phosphatidylserine 100g, cuorin 25g, ARA (peanut are weighed Tetraenoic acid) 25g, DHA25g, EPA25g, it sieves with 100 mesh sieve, tapioca, galactolipin, microcrystalline cellulose is added and crosses 80 meshes, mixes It closes uniformly, the 6%PVP ethanol solution that 100g is added is pelletized in right amount, 60 DEG C of dryings, 18 mesh integer dry particls, dry particl The middle magnesium stearate that 2g is added.Then use bi-layer tablet press stamping to get the every freeze-dried powder of SOD containing cattle liver amount for 200mg and various lipid 400mg.
Tablet C preparation
Preparation process: weighing cattle liver SOD freeze-dried powder 100g, phosphatidylserine 100g, DHA50g, crosses 100 meshes, Tapioca, galactolipin, microcrystalline cellulose is added and crosses 80 meshes, is uniformly mixed, the 6%PVP ethanol solution of 100g is added The magnesium stearate of 2g is added in dry particl for appropriate granulation, 60 DEG C of dryings, 18 mesh integer dry particls.Then Double layer pellet is used Machine stamping is 200mg and various lipid 300mg to get the amount of the every freeze-dried powder of SOD containing cattle liver.
Tablet D preparation
Activating agent Additive amount (g)
Cattle liver SOD freeze-dried powder 100
Phosphatidylserine 200
Auxiliary material
Tapioca 80
Galactolipin 20
Microcrystalline cellulose 100
Preparation process: weighing cattle liver SOD freeze-dried powder 100g, phosphatidylserine 200g, sieve with 100 mesh sieve, and cassava is added Starch, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, the 6%PVP ethanol solution that 100g is added is made in right amount The magnesium stearate of 2g is added in dry particl for grain, 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press punching press is used Piece is 200mg and various lipid 400mg to get the amount of the every freeze-dried powder of SOD containing cattle liver.
Tablet E preparation
Activating agent Additive amount (g)
Cattle liver SOD freeze-dried powder 100
Phosphatidylserine 100
Auxiliary material
Tapioca 80
Galactolipin 50
Microcrystalline cellulose 20
Preparation process: weighing cattle liver SOD freeze-dried powder 100g, phosphatidylserine 100g, sieve with 100 mesh sieve, and cassava is added Starch, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, the 6%PVP ethanol solution that 100g is added is made in right amount The magnesium stearate of 2g is added in dry particl for grain, 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press punching press is used Piece is 200mg and phosphatidylserine 200mg to get the amount of the every freeze-dried powder of SOD containing cattle liver.
Tablet F preparation
Activating agent Additive amount (g)
Cattle liver SOD freeze-dried powder 100
Phosphatidylserine 50
Auxiliary material
Tapioca 80
Galactolipin 50
Microcrystalline cellulose 20
Preparation process: weighing cattle liver SOD freeze-dried powder, phosphatidylserine 50g, sieve with 100 mesh sieve, addition tapioca, Galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, and 60 DEG C It dries, 18 mesh integer dry particls, the magnesium stearate of 2g is added in dry particl.Then using bi-layer tablet press stamping to get The amount of the every freeze-dried powder of SOD containing cattle liver is 200mg and phosphatidylserine 100mg.
Tablet G preparation
Activating agent Additive amount (g)
Cattle liver SOD freeze-dried powder 100
Phosphatidylserine 10
Auxiliary material
Tapioca 65
Galactolipin 25
Microcrystalline cellulose 10
Preparation process: weighing cattle liver SOD freeze-dried powder 100g, phosphatidylserine 10g, sieve with 100 mesh sieve, and cassava is added Starch, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, the 6%PVP ethanol solution that 100g is added is made in right amount The magnesium stearate of 2g is added in dry particl for grain, 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press punching press is used Piece is 200mg and phosphatidylserine 20mg to get the amount of the every freeze-dried powder of SOD containing cattle liver.
Tablet H preparation
Preparation process: weighing cattle liver SOD freeze-dried powder 100g, phosphatidylserine 1g, sieve with 100 mesh sieve, and para arrowroot is added Powder, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, The magnesium stearate of 2g is added in dry particl for 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press stamping is used, Amount up to the every freeze-dried powder of SOD containing cattle liver is 200mg and phosphatidylserine 2mg.
Tablet I preparation
Activating agent Additive amount (g)
Cattle liver SOD freeze-dried powder 1
Phosphatidylserine 100
Auxiliary material
Tapioca 65
Galactolipin 25
Microcrystalline cellulose 10
Preparation process: weighing cattle liver SOD freeze-dried powder 1g, phosphatidylserine 100g, sieve with 100 mesh sieve, and para arrowroot is added Powder, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, The magnesium stearate of 2g is added in dry particl for 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press stamping is used, Amount up to the every freeze-dried powder of SOD containing cattle liver is 2mg and phosphatidylserine 200mg.
Tablet J preparation
Activating agent Additive amount (g)
Cattle liver SOD freeze-dried powder 10
Phosphatidylserine 100
Auxiliary material
Tapioca 65
Galactolipin 25
Microcrystalline cellulose 10
Preparation process: weighing cattle liver SOD freeze-dried powder 10g, phosphatidylserine 100g, sieve with 100 mesh sieve, and cassava is added Starch, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, the 6%PVP ethanol solution that 100g is added is made in right amount The magnesium stearate of 2g is added in dry particl for grain, 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press punching press is used Piece is 20mg and phosphatidylserine 200mg to get the amount of the every freeze-dried powder of SOD containing cattle liver.
Tablet K preparation
Activating agent Additive amount (g)
Cattle liver SOD freeze-dried powder 50
Phosphatidylserine 100
Auxiliary material
Tapioca 80
Galactolipin 50
Microcrystalline cellulose 20
Preparation process: weighing cattle liver SOD freeze-dried powder 50g, phosphatidylserine 100g, sieve with 100 mesh sieve, and cassava is added Starch, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, the 6%PVP ethanol solution that 100g is added is made in right amount The magnesium stearate of 2g is added in dry particl for grain, 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press punching press is used Piece is 100mg and phosphatidylserine 200mg to get the amount of the every freeze-dried powder of SOD containing cattle liver.
Tablet L preparation
Activating agent Additive amount (g)
Source of people SOD freeze-dried powder 100
Phosphatidylserine 100
Auxiliary material
Tapioca 80
Galactolipin 50
Microcrystalline cellulose 20
Preparation process: weighing source of people SOD freeze-dried powder 100g, the phosphatidylserine 100g of expression, sieve with 100 mesh sieve, and is added Tapioca, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, the 6%PVP ethanol solution that 100g is added is appropriate The magnesium stearate of 2g is added in dry particl for granulation, 60 DEG C of dryings, 18 mesh integer dry particls.Then it is rushed using bi-layer tablet press Tabletting is 200mg and phosphatidylserine 200mg to get the amount of the every freeze-dried powder of SOD containing source of people.
Tablet M preparation
Preparation process: weighing Rosa roxburghii Tratt SOD freeze-dried powder 100g, the phosphatidylserine 100g of expression, sieve with 100 mesh sieve, and is added Tapioca, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, the 6%PVP ethanol solution that 100g is added is appropriate The magnesium stearate of 2g is added in dry particl for granulation, 60 DEG C of dryings, 18 mesh integer dry particls.Then it is rushed using bi-layer tablet press Tabletting is 200mg and phosphatidylserine 200mg to get the amount of the every Rosa roxburghii Tratt SOD freeze-dried powder containing expression.
Tablet N preparation
Activating agent Additive amount (g)
Deer heart SOD freeze-dried powder 100
Phosphatidylserine 100
Auxiliary material
Tapioca 80
Galactolipin 50
Microcrystalline cellulose 20
Preparation process: weighing deer heart SOD freeze-dried powder 100g, phosphatidylserine 100g, sieve with 100 mesh sieve, and cassava is added Starch, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, the 6%PVP ethanol solution that 100g is added is made in right amount The magnesium stearate of 2g is added in dry particl for grain, 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press punching press is used Piece is 200mg and phosphatidylserine 200mg to get the amount of the every SOD of heart containing deer.
Tablet O preparation
Preparation process: weighing cattle liver SOD freeze-dried powder 100g, phosphatidylserine 10g, sieve with 100 mesh sieve, and it is sweet that D- is added Reveal sugar alcohol, D-sorbite, Rosa roxburghii Tratt SOD freeze-dried powder, maltodextrin, magnesium stearate, phosphatidylserine, citric acid, hydroxypropyl first Base cellulose, essence for food cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, and 60 The magnesium stearate of 2g is added in dry particl for DEG C drying, 18 mesh integer dry particls.Then bi-layer tablet press stamping is used, i.e., The amount for obtaining the every freeze-dried powder of SOD containing cattle liver is 200mg and phosphatidylserine 20mg.
Tablet P preparation
Activating agent Additive amount (g)
Cattle liver SOD freeze-dried powder 10
Phosphatidylserine 100
Auxiliary material
D-mannital 25
D-sorbite 25
Maltodextrin 10
Magnesium stearate 5
Citric acid 5
Hydroxypropyl methyl cellulose 5
Essence for food 2
Preparation process: weighing cattle liver SOD freeze-dried powder 10g, phosphatidylserine 100g, sieve with 100 mesh sieve, and it is sweet that D- is added Reveal sugar alcohol, D-sorbite, Rosa roxburghii Tratt SOD freeze-dried powder, maltodextrin, magnesium stearate, phosphatidylserine, citric acid, hydroxypropyl first Base cellulose, essence for food cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, and 60 The magnesium stearate of 2g is added in dry particl for DEG C drying, 18 mesh integer dry particls.Then bi-layer tablet press stamping is used, i.e., The amount for obtaining the every freeze-dried powder of SOD containing cattle liver is 200mg and phosphatidylserine 20mg.
The preparation of the Dospan of the present invention of embodiment 2
a、
Preparation process: pig heart SOD freeze-dried powder 100g and phosphatidylserine 100g are weighed, is sieved with 100 mesh sieve, para arrowroot Powder, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, The magnesium stearate of 2g is added in dry particl for 60 DEG C of dryings, 18 mesh integer dry particls.
B, the preparation of coating
In room temperature, in a fluidized bed, it is dissolved to acetone/isopropanol/aqueous mixtures (54/36/10, weight percent) 90g methacrylic acid and acetate copolymer, 135g methacrylic acid and methylmethacrylate copolymer, 180g ethyl Cellulose and the dissolution of 45g triethyl citrate, while particulate obtained in a of 450g is coated with the mixture.After injection To the particle of cladding.Average diameter is 270 μm.In order to obtain the coating of multilayer, on the basis of original coating, carry out again Injection, above-mentioned steps, which are repeated, can be obtained by required multilayer controlled release layer.
C, by above-mentioned a, two kinds of components of b are using bi-layer tablet press stamping up to double-layer tablets, every pig heart SOD freeze-drying Powder 0.5g.
Extended release tablet of the invention uses swellable and some erosion polymer substrate.Based on the assumption that base Matter, release profiles can square root about temporally the extracorporeal releasing characteristic of sample described.Obtain the body not influenced by pH value Outer release profiles then are conducive to avoid because gastrointestinal tract pH value is different when body absorption then than less being influenced by gastrointestinal tract pH value And bring individual absorption difference.It constitutes extended release matrix to polymer of the invention, and slowly release is used as active constituent Pig heart SOD and its derivative object in combination.After administration, after preparation and liquid, aqueous contact, polymer swelling is formed The gel layer of viscosity adjusts drug release.The viscosity preferred scope of polymer is from 180 to 110,000mPa.s (at 20 DEG C The apparent viscosity of lower 2% aqueous solution).
Controlled release sample prepared by the embodiment of the present invention 6 or 7 is carried out dissolution test simultaneously at various ph values by us, And depicting release test curve according to release experiment data can be seen that the sample of the preparation of embodiment 7 in each pH value medium There are consistent release profiles, release is hardly influenced by PH values.
Embodiment 3: capsule-type preparation
Cor bovinum SOD for the embodiment of the present invention can be the cor bovinum SOD freeze-dried powder of drug purchase, cor bovinum SOD Freeze-dried powder 100g and phosphatidylserine 100g, is ground into fine powder.The component is crossed into 120 meshes, is weighed, is added in above-mentioned table The starch and magnesium stearate of amount are mixed, and are subsequently poured into lower hopper.Granulation coating machine is opened, enters wind pressure O.6bar, inlet air 30 DEG C of temperature, spray gun pressure (CYL) 3b cylinder, atomizing pressure (CAP1) 0.8bar pours into 250g blank capsule core, is granulated, and is granulated speed It spends 4rpm, compacted pump 12%, rotary speed 145rpm, sprays the 7%PVP solution of 200g (solvent is 90% ethyl alcohol).Granulation terminates Afterwards, 50 DEG C of drying, discharging.
By piller obtained using ebonite medicine capsule filling machine according to the freeze-dried powder of SOD containing cor bovinum in every two capsules Amount is respectively that 100mg and phosphatidylserine 100mg is filled capsule of the preparation containing cor bovinum SOD freeze-dried powder.
4. mixed type capsule-type controlled release preparation of embodiment
The controlled release preparation for designing oral administration according to the present invention needs to select and evaluate the extracorporeal releasing characteristic of preparation and determines Shi Xing makes it be most suitable for obtaining desired internal plasma profile, preferably by daily single.Therefore, single list is had studied Several different formulation principles of position matrix tablet, that is, providing has different release formulation types.
A, the preparation of active medicine core
Activating agent Additive amount (g)
Cattle liver SOD freeze-dried powder 100
Phosphatidylserine 100
Auxiliary material
Starch 200
Magnesium stearate 3
Binder
Glucose 2
Maltodextrin 3
Villyl acetate copolymer 1.5
Powder component is lyophilized by cattle liver SOD for the embodiment of the present invention or cattle liver SOD freeze-dried powder can be purchase medicine Product weigh cattle liver SOD freeze-dried powder 100g and phosphatidylserine 100g, are ground into fine powder.The component is crossed into 120 meshes, is claimed It takes, the starch measured in above-mentioned table, magnesium stearate, glucose, maltodextrin and villyl acetate copolymer is added and is mixed It closes, crosses 250 meshes, be subsequently poured into lower hopper.Granulation coating machine is opened, enters wind pressure O.6bar, 30 DEG C of inlet air temperatures, spray gun Pressure (CYL) 3b cylinder, atomizing pressure (CAP1) 0.8bar, pours into 250g blank capsule core, is granulated, and is granulated speed 4rpm, compacted pump 12%, rotary speed 145rpm spray the 7%PVP solution of 200g (solvent is 90% ethyl alcohol).After granulation, 50 DEG C of drying, Discharging.
B, the preparation of coating
In room temperature, in a fluidized bed, 90g is dissolved with acetone/isopropanol/aqueous mixtures (54/36/10, weight percent) Methacrylic acid and acetate copolymer, 135g methacrylic acid and methylmethacrylate copolymer, 180g ethyl cellulose Element and the dissolution of 45g triethyl citrate, while particulate obtained in a of 450g is coated with the mixture.It is wrapped after injection The particle covered.Average diameter is 270 μm.
C, piller made from a and b is filled using ebonite medicine capsule filling machine according to the particulate coated and prepares glue Capsule to get arrive the mixed type controlled release capsule preparation of the invention containing 0.5g cattle liver SOD freeze-dried powder.
The preparation of the injection type of 5 present composition of embodiment
Formula: 10g cattle liver SOD freeze-dried powder
10g phosphatidylserine
20g mannitol
Cattle liver SOD freeze-dried powder 5g and phosphatidylserine 5g are weighed, is configured to 1000ml solution, nothing with water for injection Bacterium filtering, filling by every 1ml, freeze-drying, tamponade rolls lid and obtains finished product injection.
Embodiment 6: coating agent preparation
Preparation process: weighing cattle liver SOD freeze-dried powder 50g, phosphatidylserine 100g, sieve with 100 mesh sieve, and is added stearic Sour magnesium, colloidal silica anhydrous, microcrystalline cellulose cross 80 meshes, are uniformly mixed, the 6%PVP dehydrated alcohol that 100g is added is molten Liquid is pelletized in right amount, 60 DEG C of dryings, 18 mesh integer dry particls, dried lacquer, talcum, the sucrose, N- vinyl fourth being added in dry particl Lactams, titanium dioxide and colorant ground and mixed form the liniment with certain viscosity.
Embodiment 7: the preparation of liquid beverage
Liquid beverage A preparation
Activating agent Additive amount (g)
Cattle liver SOD freeze-dried powder 500
Phosphatidylserine 500
Preparation process: cattle liver SOD freeze-dried powder 500g, phosphatidylserine 500g are weighed, adds certain proportion water, passes through Blender is stirred, filtering, canned, and high temperature (120 °) autoclave sterilization or magnetic wave, microwave uperization is sent to be made.
Liquid beverage B preparation
Activating agent Additive amount (g)
Cattle liver SOD freeze-dried powder 1000
Phosphatidylserine 100
Preparation process: cattle liver SOD freeze-dried powder 500g, phosphatidylserine 500g are weighed, adds certain proportion water, passes through Blender is stirred, filtering, canned, and high temperature (120 °) autoclave sterilization or magnetic wave, microwave uperization is sent to be made.
Liquid beverage C preparation
Activating agent Additive amount (g)
Cattle liver SOD freeze-dried powder 100
Phosphatidylserine 1000
Preparation process: cattle liver SOD freeze-dried powder 500g, phosphatidylserine 500g are weighed, adds certain proportion water, passes through Blender is stirred, filtering, canned, and high temperature (120 °) autoclave sterilization or magnetic wave, microwave uperization is sent to be made.
Liquid beverage D preparation
Activating agent Additive amount (g)
Cattle liver SOD freeze-dried powder 500
Phosphatidylserine 100
Preparation process: cattle liver SOD freeze-dried powder 500g, phosphatidylserine 500g are weighed, adds certain proportion water, passes through Blender is stirred, filtering, canned, and high temperature (120 °) autoclave sterilization or magnetic wave, microwave uperization is sent to be made.
Liquid beverage E preparation
Activating agent Additive amount (g)
Cattle liver SOD freeze-dried powder 100
Phosphatidylserine 500
Preparation process: cattle liver SOD freeze-dried powder 500g, phosphatidylserine 500g are weighed, adds certain proportion water, passes through Blender is stirred, filtering, canned, and high temperature (120 °) autoclave sterilization or magnetic wave, microwave uperization is sent to be made.
The preparation of 8 Tablets of embodiment
Tablet A preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 100
Lecithin 10
Cephalin 20
Phosphatidylserine 100
Cuorin 10
ARA 20
DHA 20
EPA 10
Auxiliary material
Tapioca 50
Galactolipin 80
Microcrystalline cellulose 60
Preparation process: weigh Rosa roxburghii Tratt SOD freeze-dried powder 100g, lecithin 10g, cephalin 20g, phosphatidylserine 100g, Cuorin 10g, ARA (arachidonic acid) 15g, DHA20g, EPA15g, sieves with 100 mesh sieve, and tapioca, galactolipin, micro- is added Crystalline cellulose crosses 80 meshes, is uniformly mixed, the 6%PVP ethanol solution that 100g is added is pelletized in right amount, 60 DEG C of dryings, 18 mesh Integer dry particl is sieved, the magnesium stearate of 2g is added in dry particl.Then thorn is contained to get every using bi-layer tablet press stamping The amount of pears SOD freeze-dried powder is 200mg and various lipid 400mg.
Tablet B preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 100
Phosphatidylserine 100
Cuorin 25
ARA 25
DHA 25
EPA 25
Auxiliary material
Tapioca 80
Galactolipin 20
Microcrystalline cellulose 100
Preparation process: Rosa roxburghii Tratt SOD freeze-dried powder 100g, phosphatidylserine 100g, cuorin 25g, ARA (peanut four are weighed Olefin(e) acid) 25g, DHA25g, EPA25g, it sieves with 100 mesh sieve, tapioca, galactolipin, microcrystalline cellulose is added and crosses 80 meshes, mixes Uniformly, the 6%PVP ethanol solution that 100g is added is pelletized in right amount, 60 DEG C of dryings, 18 mesh integer dry particls, in dry particl The magnesium stearate of 2g is added.Then use bi-layer tablet press stamping to get the amount of the every freeze-dried powder of SOD containing Rosa roxburghii Tratt for 200mg With various lipid 400mg.
Tablet C preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 100
Phosphatidylserine 100
DHA 50
Auxiliary material
Tapioca 80
Galactolipin 20
Microcrystalline cellulose 100
Preparation process: weighing Rosa roxburghii Tratt SOD freeze-dried powder 100g, phosphatidylserine 100g, DHA50g, crosses 100 meshes, adds Enter tapioca, galactolipin, microcrystalline cellulose and cross 80 meshes, be uniformly mixed, the 6%PVP ethanol solution that 100g is added is suitable Amount is pelletized, 60 DEG C of dryings, 18 mesh integer dry particls, and the magnesium stearate of 2g is added in dry particl.Then bi-layer tablet press is used Stamping is 200mg and various lipid 300mg to get the amount of the every freeze-dried powder of SOD containing Rosa roxburghii Tratt.
Tablet D preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 100
Phosphatidylserine 200
Auxiliary material
Tapioca 80
Galactolipin 20
Microcrystalline cellulose 100
Preparation process: weighing Rosa roxburghii Tratt SOD freeze-dried powder 100g, phosphatidylserine 200g, sieve with 100 mesh sieve, and para arrowroot is added Powder, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, The magnesium stearate of 2g is added in dry particl for 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press stamping is used, Amount up to the every freeze-dried powder of SOD containing Rosa roxburghii Tratt is 200mg and various lipid 400mg.
Tablet E preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 100
Phosphatidylserine 100
Auxiliary material
Tapioca 80
Galactolipin 50
Microcrystalline cellulose 20
Preparation process: weighing Rosa roxburghii Tratt SOD freeze-dried powder 100g, phosphatidylserine 100g, sieve with 100 mesh sieve, and para arrowroot is added Powder, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, The magnesium stearate of 2g is added in dry particl for 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press stamping is used, Amount up to the every freeze-dried powder of SOD containing Rosa roxburghii Tratt is 200mg and phosphatidylserine 200mg.
Tablet F preparation
Preparation process: weighing Rosa roxburghii Tratt SOD freeze-dried powder 100g, phosphatidylserine 50g, sieve with 100 mesh sieve, and para arrowroot is added Powder, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, The magnesium stearate of 2g is added in dry particl for 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press stamping is used, Amount up to the every freeze-dried powder of SOD containing Rosa roxburghii Tratt is 200mg and phosphatidylserine 100mg.
Tablet G preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 100
Phosphatidylserine 10
Auxiliary material
Tapioca 65
Galactolipin 25
Microcrystalline cellulose 10
Preparation process: weighing Rosa roxburghii Tratt SOD freeze-dried powder 100g, phosphatidylserine 10g, sieve with 100 mesh sieve, and para arrowroot is added Powder, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, The magnesium stearate of 2g is added in dry particl for 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press stamping is used, Amount up to the every freeze-dried powder of SOD containing Rosa roxburghii Tratt is 200mg and phosphatidylserine 20mg.
Tablet H preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 100
Phosphatidylserine 1
Auxiliary material
Tapioca 65
Galactolipin 25
Microcrystalline cellulose 10
Preparation process: weighing Rosa roxburghii Tratt SOD freeze-dried powder 100g, phosphatidylserine 1g, sieve with 100 mesh sieve, and para arrowroot is added Powder, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, The magnesium stearate of 2g is added in dry particl for 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press stamping is used, Amount up to the every freeze-dried powder of SOD containing Rosa roxburghii Tratt is 200mg and phosphatidylserine 2mg.
Tablet I preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 1
Phosphatidylserine 100
Auxiliary material
Tapioca 65
Galactolipin 25
Microcrystalline cellulose 10
Preparation process: weighing Rosa roxburghii Tratt SOD freeze-dried powder 1g, phosphatidylserine 100g, sieve with 100 mesh sieve, and para arrowroot is added Powder, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, The magnesium stearate of 2g is added in dry particl for 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press stamping is used, Amount up to the every freeze-dried powder of SOD containing Rosa roxburghii Tratt is 2mg and phosphatidylserine 200mg.
Tablet J preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 10
Phosphatidylserine 100
Auxiliary material
Tapioca 65
Galactolipin 25
Microcrystalline cellulose 10
Preparation process: weighing Rosa roxburghii Tratt SOD freeze-dried powder 10g, phosphatidylserine 100g, sieve with 100 mesh sieve, and para arrowroot is added Powder, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, The magnesium stearate of 2g is added in dry particl for 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press stamping is used, Amount up to the every freeze-dried powder of SOD containing Rosa roxburghii Tratt is 20mg and phosphatidylserine 200mg.
Tablet K preparation
Preparation process: weighing Rosa roxburghii Tratt SOD freeze-dried powder 50g, phosphatidylserine 100g, sieve with 100 mesh sieve, and para arrowroot is added Powder, galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, The magnesium stearate of 2g is added in dry particl for 60 DEG C of dryings, 18 mesh integer dry particls.Then bi-layer tablet press stamping is used, Amount up to the every freeze-dried powder of SOD containing Rosa roxburghii Tratt is 100mg and phosphatidylserine 200mg.
Tablet L preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 100
Phosphatidylserine 10
Auxiliary material
D-mannital 25
D-sorbite 25
Maltodextrin 10
Magnesium stearate 5
Citric acid 5
Hydroxypropyl methyl cellulose 5
Essence for food 2
Preparation process: weighing Rosa roxburghii Tratt SOD freeze-dried powder 100g, phosphatidylserine 10g, sieve with 100 mesh sieve, and D- sweet dew is added Sugar alcohol, D-sorbite, Rosa roxburghii Tratt SOD freeze-dried powder, maltodextrin, magnesium stearate, phosphatidylserine, citric acid, hydroxypropyl methyl Cellulose, essence for food cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, and 60 DEG C It dries, 18 mesh integer dry particls, the magnesium stearate of 2g is added in dry particl.Then using bi-layer tablet press stamping to get The amount of the every freeze-dried powder of SOD containing cattle liver is 200mg and phosphatidylserine 20mg.
Tablet M preparation
Preparation process: weighing Rosa roxburghii Tratt SOD freeze-dried powder 10g, phosphatidylserine 100g, sieve with 100 mesh sieve, and D- sweet dew is added Sugar alcohol, D-sorbite, Rosa roxburghii Tratt SOD freeze-dried powder, maltodextrin, magnesium stearate, phosphatidylserine, citric acid, hydroxypropyl methyl Cellulose, essence for food cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, and 60 DEG C It dries, 18 mesh integer dry particls, the magnesium stearate of 2g is added in dry particl.Then using bi-layer tablet press stamping to get The amount of the every freeze-dried powder of SOD containing cattle liver is 200mg and phosphatidylserine 20mg.
The preparation of the Dospan of the present invention of embodiment 9
a、
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 100
Phosphatidylserine 100
Auxiliary material
Tapioca 60
Galactolipin 40
Microcrystalline cellulose 60
Preparation process: weighing Rosa roxburghii Tratt SOD freeze-dried powder 100g and phosphatidylserine 100g, sieve with 100 mesh sieve, tapioca, Galactolipin, microcrystalline cellulose cross 80 meshes, are uniformly mixed, and the 6%PVP ethanol solution that 100g is added is pelletized in right amount, and 60 DEG C It dries, 18 mesh integer dry particls, the magnesium stearate of 2g is added in dry particl.
B, the preparation of coating
In room temperature, in a fluidized bed, it is dissolved to acetone/isopropanol/aqueous mixtures (54/36/10, weight percent) 90g methacrylic acid and acetate copolymer, 135g methacrylic acid and methylmethacrylate copolymer, 180g ethyl Cellulose and the dissolution of 45g triethyl citrate, while particulate obtained in a of 450g is coated with the mixture.After injection To the particle of cladding.Average diameter is 270 μm.In order to obtain the coating of multilayer, on the basis of original coating, carry out again Injection, above-mentioned steps, which are repeated, can be obtained by required multilayer controlled release layer.
C, by above-mentioned a, two kinds of components of b are using bi-layer tablet press stamping up to double-layer tablets, every Rosa roxburghii Tratt SOD freeze-dried powder 0.5g。
Extended release tablet of the invention uses swellable and some erosion polymer substrate.Based on the assumption that base Matter, release profiles can square root about temporally the extracorporeal releasing characteristic of sample described.Obtain the body not influenced by pH value Outer release profiles then are conducive to avoid because gastrointestinal tract pH value is different when body absorption then than less being influenced by gastrointestinal tract pH value And bring individual absorption difference.It constitutes extended release matrix to polymer of the invention, and slowly release is used as active constituent Rosa roxburghii Tratt SOD freeze-dried powder and its derivative object in combination.After administration, after preparation and liquid, aqueous contact, polymer swelling, The gel layer of viscosity is formed to adjust drug release.The viscosity preferred scope of polymer be from 180 to 110,000mPa.s ( The apparent viscosity of 2% aqueous solution at 20 DEG C).
Controlled release sample prepared by the embodiment of the present invention 7 or 8 is carried out dissolution test simultaneously at various ph values by us, And depicting release test curve according to release experiment data can be seen that the sample of the preparation of embodiment 7 in each pH value medium There are consistent release profiles, release is hardly influenced by PH values.
Embodiment 10: capsule-type preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 100
Phosphatidylserine 100
Auxiliary material
Starch 200
Magnesium stearate 3
Composition for the embodiment of the present invention can be the Rosa roxburghii Tratt SOD freeze-dried powder of drug purchase, Rosa roxburghii Tratt SOD freeze-dried powder 100g and phosphatidylserine 100g, is ground into fine powder.The component is crossed into 120 meshes, is weighed, the shallow lake measured in above-mentioned table is added Powder and magnesium stearate are mixed, and are subsequently poured into lower hopper.Granulation coating machine is opened, enters wind pressure O.6bar, inlet air temperatures 30 DEG C, spray gun pressure (CYL) 3b cylinder, atomizing pressure (CAP1) 0.8bar pours into 250g blank capsule core, is granulated, and is granulated speed 4rpm, compacted pump 12%, rotary speed 145rpm spray the 7%PVP solution of 200g (solvent is 90% ethyl alcohol).After granulation, 50 DEG C of drying, discharging.
By piller obtained using ebonite medicine capsule filling machine according to the amount of the freeze-dried powder of SOD containing Rosa roxburghii Tratt in every two capsules Respectively 100mg and phosphatidylserine 100mg is filled capsule of the preparation containing Rosa roxburghii Tratt SOD freeze-dried powder.
11. mixed type capsule-type controlled release preparation of embodiment
The controlled release preparation for designing oral administration according to the present invention needs to select and evaluate the extracorporeal releasing characteristic of preparation and determines Shi Xing makes it be most suitable for obtaining desired internal plasma profile, preferably by daily single.Therefore, single list is had studied Several different formulation principles of position matrix tablet, that is, providing has different release formulation types.
A, the preparation of active medicine core
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 100
Phosphatidylserine 100
Auxiliary material
Starch 200
Magnesium stearate 3
Binder
Glucose 2
Maltodextrin 3
Villyl acetate copolymer 1.5
Powder component is lyophilized by Rosa roxburghii Tratt SOD for the embodiment of the present invention or Rosa roxburghii Tratt SOD freeze-dried powder can be drug purchase, claims Rosa roxburghii Tratt SOD freeze-dried powder 100g and phosphatidylserine 100g are taken, fine powder is ground into.The component is crossed into 120 meshes, is weighed, is added Starch, magnesium stearate, glucose, maltodextrin and the villyl acetate copolymer measured in above-mentioned table are mixed, and cross 250 Mesh is subsequently poured into lower hopper.Granulation coating machine is opened, enters wind pressure O.6bar, 30 DEG C of inlet air temperatures, spray gun pressure (CYL) 3b cylinder, atomizing pressure (CAP1) 0.8bar, pours into 250g blank capsule core, is granulated, and is granulated speed 4rpm, compacted pump 12%, and turntable turns Fast 145rpm sprays the 7%PVP solution of 200g (solvent is 90% ethyl alcohol).After granulation, 50 DEG C of drying, discharging.
B, the preparation of coating
In room temperature, in a fluidized bed, 90g is dissolved with acetone/isopropanol/aqueous mixtures (54/36/10, weight percent) Methacrylic acid and acetate copolymer, 135g methacrylic acid and methylmethacrylate copolymer, 180g ethyl cellulose Element and the dissolution of 45g triethyl citrate, while particulate obtained in a of 450g is coated with the mixture.It is wrapped after injection The particle covered.Average diameter is 270 μm.
C, piller made from a and b is filled using ebonite medicine capsule filling machine according to the particulate coated and prepares glue Capsule to get arrive the mixed type controlled release capsule preparation of the invention containing 0.5g Rosa roxburghii Tratt SOD freeze-dried powder.
The preparation of the injection type of 12 present composition of embodiment
Formula: 10g Rosa roxburghii Tratt SOD freeze-dried powder
10g phosphatidylserine
20g mannitol
Rosa roxburghii Tratt SOD freeze-dried powder 5g and phosphatidylserine 5g are weighed, is configured to 1000ml solution with water for injection, it is sterile Filtering, filling by every 1ml, freeze-drying, tamponade rolls lid and obtains finished product injection.
Embodiment 13: coating agent preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 150
Phosphatidylserine 150
Auxiliary material
Microcrystalline cellulose 70
Coating 60
Magnesium stearate 3
Colloidal silica anhydrous 1
Coating agent
Dried lacquer 5
Talcum 60
Sucrose 50
N- vinyl butyrate lactam 6
Titanium dioxide 0.3
Colorant 5
Preparation process: weighing Rosa roxburghii Tratt SOD freeze-dried powder 50g, phosphatidylserine 100g, sieve with 100 mesh sieve, and stearic acid is added Magnesium, colloidal silica anhydrous, microcrystalline cellulose cross 80 meshes, are uniformly mixed, the 6%PVP ethanol solution of 100g is added Appropriate granulation, 60 DEG C of dryings, 18 mesh integer dry particls, the dried lacquer being added in dry particl, talcum, sucrose, in N- vinyl fourth Amide, titanium dioxide and colorant ground and mixed form the liniment with certain viscosity.
Embodiment 14: the preparation of liquid beverage
Liquid beverage A preparation
Preparation process: Rosa roxburghii Tratt SOD freeze-dried powder 500g, phosphatidylserine 500g are weighed, adds certain proportion water, by stirring The machine of mixing is stirred, filtering, canned, and high temperature (120 °) autoclave sterilization or magnetic wave, microwave uperization is sent to be made.
Liquid beverage B preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 1000
Phosphatidylserine 100
Preparation process: Rosa roxburghii Tratt SOD freeze-dried powder 500g, phosphatidylserine 500g are weighed, adds certain proportion water, by stirring The machine of mixing is stirred, filtering, canned, and high temperature (120 °) autoclave sterilization or magnetic wave, microwave uperization is sent to be made.
Liquid beverage C preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 100
Phosphatidylserine 1000
Preparation process: Rosa roxburghii Tratt SOD freeze-dried powder 500g, phosphatidylserine 500g are weighed, adds certain proportion water, by stirring The machine of mixing is stirred, filtering, canned, and high temperature (120 °) autoclave sterilization or magnetic wave, microwave uperization is sent to be made.
Liquid beverage D preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 500
Phosphatidylserine 100
Preparation process: Rosa roxburghii Tratt SOD freeze-dried powder 500g, phosphatidylserine 500g are weighed, adds certain proportion water, by stirring The machine of mixing is stirred, filtering, canned, and high temperature (120 °) autoclave sterilization or magnetic wave, microwave uperization is sent to be made.
Liquid beverage E preparation
Activating agent Additive amount (g)
Rosa roxburghii Tratt SOD freeze-dried powder 100
Phosphatidylserine 500
Preparation process: Rosa roxburghii Tratt SOD freeze-dried powder 500g, phosphatidylserine 500g are weighed, adds certain proportion water, by stirring The machine of mixing is stirred, filtering, canned, and high temperature (120 °) autoclave sterilization or magnetic wave, microwave uperization is sent to be made.
The advantage of the invention is that used superoxide dismutase activity is high, purity is high.In the world, inventor The various composition five poisonous creatures: scorpion, viper, centipede, house lizard, toad of prepared superoxide dismutase and lipid and without any side effects, effectively (1) enhancing is exempted from Epidemic disease function is antifatigue;(2) promote longevity anti-aging;(3) SOD prepared by is the jinx of oxygen radical, it can be treated by oxygen freedom A variety of diseases caused by base.Experiment shows it to gastrointestinal function imbalance, loss of appetite, insomnia, memory loss, the improvement heart Vascular function has apparent preventive and therapeutic effect.At present prepare again domestic and international application cosmetics, health food such as;Dairy produce, The intermediate products such as candy, fruit juice, beverage, beer, white wine and health-caring capsule (tablet, spray).As the special of health food Functional additive, SOD have a wide range of applications.The immunogenicity to human body is eliminated, really is able to generate anti-oxidant, anti- Aging, anti-radiation, the anti-inflammatory, class's of dispelling beauty, enhancing immunity of organism and other effects.Accomplish Scientific Usage of Drugs, with a definite target in view.Fill up super The manufacture of superoxide dismutase tip and the country using technique, international blank, are conducive to Rehabilitation.
The present invention is not limited to particular implementation described in this application, the list as individual aspect of the invention One explanation.It will be understood by those skilled in the art that being carry out various modifications in the case where spirit and scope can not departed from And change.As described above, the functionally equivalent purposes pair other than enumerating herein, in the scope of the present disclosure It is apparent for those skilled in the art of this field.Such change and modification are intended to fall in appended claims In range.The disclosure is only limited by appended claims and the full scope being equal with the range of such claim System.It should be appreciated that the disclosure is not limited to specific method, reagent, composition and biosystem, and certainly, the method, examination Agent, composition and biosystem can change.It can also be appreciated that term used herein is only used for describing specific embodiment party Formula is not used to be restrictive.
All patents, patent application, earlier application and publication referred herein or reference pass through reference full text It is incorporated herein, including all tables, so that they are not contradicted with the clearly teaching of this specification.In scope of the claims The other embodiments of interior proposition.Superoxide dismutase manufacturing process of the invention at home, international unprecedented, benefit In Rehabilitation.

Claims (15)

1. the composition containing SOD and lipid, it is characterised in that: the active constituent part of the composition is by two kinds of active components Composition, a kind of active constituent are SOD;Another active constituent is lipid.
2. composition as described in claim 1, it is characterised in that: at least one lipid of the composition is selected from sweet by acyl group Oils, phospholipid, sphingolipid, sterol and fatty acid composition group it is one or more.
3. composition as claimed in claim 2, it is characterised in that: at least one lipid of the composition is selected from by phospholipid With fatty acid composition group it is one or more, the phospholipid includes but is not limited to lecithin, cephalin, phosphatidyl silk ammonia Acid, phosphatidyl glycerol, cuorin and phosphatidylinositols, sphingomyelins;The fatty acid includes but is not limited to have linoleic acid, flax Acid, ARA (arachidonic acid), DHA, EPA.
4. composition as claimed in claim 3, it is characterised in that: at least one lipid of the composition is selected from by lecithin Rouge, cephalin, phosphatidylserine, cuorin, ARA (arachidonic acid), DHA, EPA composition group it is one or more.
5. composition as claimed in claim 4, it is characterised in that: at least one lipid of the composition is phosphatidyl silk ammonia Acid and DHA.
6. composition as claimed in claim 5, it is characterised in that: the composition at least one lipid is phosphatidyl silk ammonia Acid.
7. the composition as described in claim 1-6, it is characterised in that: the composition is oral preparation, external preparation, sucking Preparation, through nasal preparation, per rectum preparation, percutaneous preparation or ejection preparation.
8. composition as claimed in claim 7, it is characterised in that: the oral preparation be capsule, tablet, pulvis, granule, Lozenge, effervescent tablet, syrup, emulsion, the prepared product of controlled release, rapidly-soluble prepared product, oral liquid dosage forms.
9. composition as claimed in claim 8, it is characterised in that: the tablet is by D-mannital, D-sorbite, Rosa roxburghii Tratt SOD freeze-dried powder, maltodextrin, magnesium stearate, phosphatidylserine, citric acid, hydroxypropyl methyl cellulose, essence for food group At.
10. composition as claimed in claims 1-9, it is characterised in that: superoxide dismutase proportion, by weight, The total weight for accounting for entire preparation is 0.01%-98%.
11. the composition as described in claim 1-10, it is characterised in that: at least one lipid proportion accounts for by weight The total weight of entire composition is 0.01%-98%.
12. composition as described in claim 1-11, which increases in preparation for preventing and/or treat people's oxygen radical, causes phase The purposes of the pathological symptom of pass or the drug of disease, nutrient and healthcare products, food or cosmetics.
13. purposes as claimed in claim 12, it is characterised in that: pathological symptom described in the pathological symptom or disease or Disease includes but is not limited to by more pleat Zou of skin aging, freckle and crow's feet abnormal increase, arthritis, rheumatoid, rheumatoid Spondylitis, intervertebral disk injury, osteoporosis, cardiovascular disease, inferior health or secondary health, myocarditis, hyperlipidemia, hypertension, The deposition of lipid material caused by hyperglycemia, metabolic disturbance, obesity, artery sclerosis, prostatitis, respiratory infectious disease, Senile dementia, fatigue, insomnia, amnesia, anorexia, dysphoria, depression or passiveness, anxious, dizzy, aging, palpitaition Shortness of breath, stool and urine exception, hyposexuality, immune function decline (often catch a cold or have cold symptoms, throat discomfort, a canker sore Deng), diabetes, ageing diseases, coronary heart disease, sexual function be depressed, chronic obstructive emphysema, hepatitis, apocamnosis, neurasthenia, brain One or more clinical pathological symptoms or disease of the group of the compositions such as infarct, asthma, cough, adult respiratory distress syndrome (ARDS).
14. purposes as described in claim 12 or 13, it is characterised in that: the purposes further include to people apply prevention and/or Composition described in the claim 1-11 of therapeutically effective amount.
15. purposes as claimed in claim 14, it is characterised in that: the effective quantity includes applying about 0.1mg/kg daily to people Composition described in claim 1-28 to about 10000mg/kg weight.
CN201810939321.6A 2017-08-25 2018-08-13 Composition containing SOD Pending CN109420161A (en)

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111450013A (en) * 2020-05-12 2020-07-28 广州怡嘉生物科技有限公司 Repairing stock solution
CN112094817A (en) * 2020-09-23 2020-12-18 绿城农科检测技术有限公司 Hybridoma cell strain secreting thiouracil monoclonal antibody, monoclonal antibody and application
CN117643588A (en) * 2023-11-13 2024-03-05 山东天宏生物医药有限公司 Application of nitrofurantoin in preparation of anti-rheumatoid arthritis drugs

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111450013A (en) * 2020-05-12 2020-07-28 广州怡嘉生物科技有限公司 Repairing stock solution
CN112094817A (en) * 2020-09-23 2020-12-18 绿城农科检测技术有限公司 Hybridoma cell strain secreting thiouracil monoclonal antibody, monoclonal antibody and application
CN112094817B (en) * 2020-09-23 2021-06-04 绿城农科检测技术有限公司 Hybridoma cell strain secreting thiouracil monoclonal antibody, monoclonal antibody and application
CN117643588A (en) * 2023-11-13 2024-03-05 山东天宏生物医药有限公司 Application of nitrofurantoin in preparation of anti-rheumatoid arthritis drugs

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Application publication date: 20190305