CN104490857B - Allicin parenteral solution is as the application for preparing treatment myocardial infarction disease medicament - Google Patents

Abstract

The present invention relates to the applied technical field of allicin, is a kind of application of allicin parenteral solution as preparation treatment myocardial infarction disease medicament.The present invention passes through " allicin parenteral solution " intravenous, carry out histopathology, compare the myocardial infarct size of " allicin intravenous injection administration group " and model group, test result indicates that allicin parenteral solution has the drug effect of anti-infarction, illustrate that allicin parenteral solution can effectively prevent myocardial infarction disease, further illustrate that allicin parenteral solution can become a kind of new pharmaceutical formulation of efficiently treatment myocardial infarction disease.

Description

Allicin parenteral solution is as the application for preparing treatment myocardial infarction disease medicament

Technical field

The present invention relates to the applied technical field of allicin, is that a kind of allicin parenteral solution is myocardium as treatment is prepared The application of infarct disease medicament.

Background technology

Since ancient times, garlic (Allium sativum L) is the medicine-food two-purpose that different parts of the world, different nationalities are generally acknowledged Plant.It is B.C., just there is the medicinal note of many garlics in ancient Egypt, ancient Gingko, the archaeological information of ancient Roman and medical literature Carry.Ancient Times in China, garlic are common drugs.《Compendium of Materia Medica》Described in:Garlic " logical the five internal organs, up to all keys, go cold-dampness, and exorcise evil spirits evil, Subduing inflammation ", " only cholera, evil removing is haunt and plague, solves pestilence, removes disease due to noxious agents produced by various parasites, malignant sore, snakeworm, small stream poison ", " journey taken, then scorching wind miasma rain cannot Add, eating brave cured poison cannot do harm to ".Chen Cangqi is said：" garlic just eats unfavorable mesh, and more foods are bright, and long food makes us serum ".Uygur medicine is discussed Write and record：For treating a variety of diseases such as qi and blood stagnation, sphagitis, apoplexy, hemiplegia, convulsions, joint pain.Dimension doctor's ancient books is recorded One method of Garlic in Treatment hemiplegia：Eat 1, garlic raw within 1st day, increase day by day 1,20 were eaten raw to the 20th day.Hereafter day subtract 1, 39 days as a treatment course, there is special effect.

Modern age, garlic are mainly used as Antibiotics usage.During the World War I, garlic is widely used as anti-corrosion And antimicrobial.In generation nineteen thirty, finds that hundred bright more breaths have antibacterial effect, nineteen thirty-seven synthesis sulfapryidine, nineteen thirty-nine synthesis sulfanilamide (SN) thiophene Azoles, nineteen forty-one synthesis sulphadiazine.Nineteen twenty-eight Fleming finds penicillin（MIT bavins grace in 1938, Florey extraction）Come out. Nineteen sixty instead of after, semi-synthetic, synthetic antibiotic is come out one after another.Various infectious diseases are substantially achieved control.The medicine of garlic With drastically reducing.But hereafter find that a variety of bacterial strains produce antibiotic drug resistance, undesirable and a variety of to the effect of fungi The discovery of side effect.Therefore nineteen fifty is among the people to be not off curing the disease using garlic to 1980.Some large hospitals, are steamed using water Steam distillation prepares galic essential oil and parenteral solution, and treatment nosomycosis obtains good efficacy.The discovery of the 1980's, garlic active ingredient pair Morbidity and mortality highest cardiovascular and cerebrovascular disease in the world's has the effect of good.

The botany research of garlic：1st, plant classification belongs to：How to be named in woods for garlic (Allium sativum L.) Age, plant classification method are still incomplete.The morphological feature of garlic with allium, Lycoris, Anemarrhena and lilium relatively, But belong to Liliaceae (Liliaceae) very reluctantly, 1987, the botanist such as Takhtajan was by the green onion in former Liliaceae Belong to independent into green onion section, solve the umbel of green onion section and it is similar to Amaryllidaceae by the involucre that bract forms and in its ovary Position flower and the contradiction identical with liliaceous ovary epigynous flower, and received by each authoritative institution, allium is under the jurisdiction of green onion section (Alliaceae), thus, the ownership of garlic plant classification, should be revised as：" green onion section (Alliaceae) plant garlic (Allium Sativum L.) ", or broad sense Liliaceae；2nd, the kind of garlic：2.1st, the classification of the kind of garlic:Garlic only has one in the whole world A kind " saying of Allium sativum L. " is inaccurate, it was reported that, (1), form whole world garlic has 600 multi items at present, Credit class (morphology, cytology), Regel (1875) and Vedensky (1968) think A.1ongicuspis be garlic ancestral First, Helm (1956) is classified as 3 mutation：Longicuspis (long plush copper), ophioscordon (snake garlic) and sativum, Kazakova (1971 to 1978) and separate two subspecies:Subtropical (subtropical zone) and Pekinense (Beijing) is altogether 5 kinds, the difference caused by varying environment, and produce many novel species.By color of the leather, white skin garlic and purple garlic, white skin can be divided into Garlic cold resistance is strong, and general late fall sowing, principal item has 23 kinds, and purple garlic crust aubergine, valve fertilizer, number are few, generally early to sow in spring Kind, (2), Phytochemistry classification principal item has 26 kinds, and, cysteine derivative is the shared Phytochemistry of different cultivars garlic Component, cysteine-sulfide have important systematics meaning, are divided into three classes：1）, cysteine-sulfide content It is high；2）, cysteine-sulfide content it is low；3）, based on alliin and different alliin (isoalliin), (3), by purposes point Class, Miao Yongxing, a kind of sedge type, head type, seedling a kind of sedge dual-purpose type, the climing dual-purpose type of head a kind of sedge dual-purpose type head seedling, 2.2, molecular biology method Classification (molecular labeling) confirms the original producton location of garlic, and Vavilov (1926), Kazakova (1971) think that the Central Asia is rising for garlic Source center, Etoh (1986), Kotlinska (1991), Kamenetsky (2004) etc. finds that garlic is fertile in Central Asia Tianshan Mountains Archetype, the support Central Asia are the garlic centre of origin, then by the biochemistry and molecule mark such as Pooler (1993) and Hong (1999) Analysis of scoring is verified that the saying that garlic is introduced from foreign countries is inaccurate；3rd, garlic is original, and Wu Zhengyi etc., proposes new plant Resource classification system：Xinjiang has the wild economic plant germ plasm resource of Important Economic potentiality, including：The vegetables such as green onion, garlic, fragrant-flowered garlic are wild Raw sibling species, has the prospect further developed, 1996 to 1998, Xinjiang academy of agricultural sciences Lu Jun Jun etc., collected, investigates, hair Existing a variety of garlics, the display Mountain Ranges of Tian Shan Mountains is the main distributed areas of allium Garlic Germplasm Resources.

The active ingredient of garlic：

1st, garlicin compound：Since some bacterial strains produce antibiotic drug resistance, and the effect to fungi Undesirable, among the people to be not off curing the disease using garlic, some large hospitals, galic essential oil and injection are prepared using steam distillation Liquid, treatment nosomycosis obtain good efficacy, and 1972 to 1976, Shanghai Mr. Lang Yijiang etc. was smart from garlic steam distillation Isolated a kind of oily yellow liquid in oil, physicochemical property is more stable, has strong garlic odour, isolated and purified through GC, HPLC, IR, MS etc. are analyzed and identified, and confirm as trisulfide（Alliitridum）, (Lang Yijiang, etc., garlic active ingredient research, medium-height grass Medicine communicates, and 1981;12(1):4), this achievement in research is in domestic and international advanced level, and pharmacological experiment is shown with similar The pharmacological action of garlic component, is once named as Allicin, standard is named as allicin within 2002；

2nd, after the results of study such as Lang Yijiang deliver 10 years, the state such as moral, U.S., Israel, Japan find, garlic effectively into Divide has the effect of good to the highest cardiovascular and cerebrovascular disease of world's morbidity and mortality, causes world's extensive concern, starts The climax of garlic research, the experimental results show, alliin (Alliin), allinase (Alliinase) and allicin (Allicin) it is that garlic is anti-infective, prevents the main composition of cardio-cerebrovascular diseases, alliin and allicin is beautiful The multinational pharmacopeia such as state, Britain/European Union are confirmed as garlic and its preparation and are differentiated and the leading indicator of assay, and Chinese Pharmacopoeia and Relevant criterion still uses " allicin（Garlicin compound）" index as quality control, thus, formed in the world Two kinds of " medicinal garlic " quality index systems,（1）, alliin（Alliin, CAS：556-27-24）, chemical name:S- allyls Base-L-cysteine sulfoxide (S-Allyl-L-cysteine sulfoxide), mp:163 DEG C to 165 DEG C, [α] D=+ 60o, in vain Color filament crystal.Separated and identified first from garlic by Stoll and Seeback within 1948.It is present in garlic in the form of odorless It is most original in garlic unicorn bud, most important, the highest sulfur-containing amino acid of content in bulbil.Content has very because of kind and the place of production Big difference (0.3-2.5%)（Note:The U.S.《Chemical abstracts, CA》Society, in order to solve, " multiple compounds are of the same name, or same compound It is several " problem, provided to each compound one coding）,（2), alliin lyase (Alliinase, EC 4.4.1.4 ,CAS:9031-77-0) also known as allinase, Alkylcysteine sulfoxide lyase（S-allyl-L- cysteine sulfoxide lyase）. Belong to dimer glycoprotein, two molecular weight subunits are 51.5 KDa.By N- terminal domains (yellow), pyridoxime 5'-phosphate With reference to domain (blueness) and C- terminal domains (red) composition, crystallization is in yellow, odorless, isoelectric pH:4.9, to temperature It is sensitive（EC 4.4.1.4：Coding of the international enzyme committee to allinase.First digit 4 represents that the enzyme belongs to the fourth-largest class and (splits Synthase);Second digit 4 represents to belong to the 4th subclass (Alkylcysteine sulfoxide lyase);Third digit 1 represents to belong to the first group, fourth digit 4 Represent the sequence number of the discovery enzyme）, (3), allicin (Allicin, CAS:539-86-6), chemical name:The thio Asia of diallyl Sulphonic acid ester (Diallyl thiosulfinate), MW:162.3, BP:28 DEG C (decomposition), are slightly soluble in water, there is garlicky, nineteen forty-four Cavallito and Bailey is isolated from the garlic juice pulverized first, is that the production for closing substrate alliin is split in allinase catalysis Thing, is the most important bioactive ingredients of garlic, but unstable chemcial property, a few hours, that is, decomposed metamorphic in room temperature, air.

Allicin (Allitridum, CAS:2050-87-5)：The national drug standards " WS-10001- (HD-0050)- 2002 " are defined as allicin " Ailitridin, containing C₆H₁₀S₃97%-103% " is should be, Ailitridin, was once named as " garlic New element (Allitride).The national drug standards rename as allicin within 2002.National Pharmacopeia（2015 editions）Continue to use.Continue three The content height of two propylene of sulphur, as the standard for directly judging garlic medicinal material and the quality of the pharmaceutical preparations, " Ailitridin " is named as Allicin, from present（After standard formulation 30 years）From the point of view of, there are hurry and easy the defects of misunderstanding, first, at that time not yet The system research of garlic is completed, second, allicin to be regarded as to the principle active component of garlic, experimenter is misled and is tried using chemistry Agent carries out pharmacodynamics test, replaces garlic vegetable drug with chemical reagent, produces garlic pharmaceutical preparation and plurality kinds of health care product, make China broad masses fail to enjoy the real medical and health care effect of plant garlic, the garlic preparation in China is lagged behind the world, Therefore, China garlic relevant criterion should grow with each passing hour, and revise as early as possible.

Allicin, alliin, the chemical constitution of allicin are different：Alliin, allicin and allicin, are chemically tied Structure, chemical abstracts numbering, physicochemical property, bioactivity etc. are three kinds of different compounds, it is necessary to are eliminated the false and retained the true.

Allicin (Allicin, CAS:539-86-6), chemical name:Diallyl thiosulfinates (Diallyl thiosulfinate),MW:162.3, BP:28 DEG C (decomposition), are slightly soluble in water, there is garlicky, nineteen forty-four Cavallito and Bailey It is isolated from the garlic juice pulverized first, it is that the product for closing substrate alliin is split in allinase catalysis, is that garlic is most important Bioactive ingredients, but unstable chemcial property, a few hours, that is, decomposed metamorphic in room temperature, air.

Allicin is that have moderately toxic chemical industry synthesis product：Allicin (Allitridum), alias：Garlicin Ether, trisulfides two propylene, diallyl trisulfide etc.（Allisatin, Allitrid, Diallyl trisulfide）, it is a kind ofization The reagent of synthesis is learned, once as chemical synthesis intermediate, paint thinner.Yellow flammable liquid, purity:50-99%；Allicin Toxicity level:In (Hazard Class:6.1-b, Poisonous/Toxic Materials), acute toxicity:Mouse oral LD50:100 mg/Kg, intravenous LD50:70mg/kg, Oral Administration in Rats LD50:265mg/kg, hazardous materials transportation number:2810[37]； Hunan Jing Tian scientific ＆ technical corporation produces 1000 tons of synthetic allicin per year, and workshop-sink flows to Xiang River with rainwater, and institute is withered to the greatest extent through part vegetation, Ox is because careless and dead near Chi Liao factories, and the fish of neighbouring Xiang River cultivation, all strange death, several millworkers are through the refined doctor in Hunan Institute is diagnosed as caused neuropathy of being poisoned.The bioactivity of allicin does not represent the effect of plant garlic and its preparation, experiment It has been shown that, garlic is known as many drug effects, but cannot represent the drug effect of plant garlic main component alliin and allicin And the effect of clinical practice, due to the misunderstanding formed for a long time, the active ingredient for replacing Natural Garlic with toxic chemical is made Health food and medicine, make China broad masses fail to enjoy the achievement in research of modern age plant garlic, consumer are caused perhaps More infringements.Therefore, document, pharmacology, toxicity and clinical practice of both " Allitridum ", " Allicin " etc. are lumped together, At home and abroad cause many misunderstandings.Also, the active ingredient in the capsulae allitridi or garlicin injection of current clinical practice It is not " Diallytrisin " single component, but one group of mixture.Allicin is free of in fresh garlic, allicin is all people Work synthesizes, and is not the active ingredient of garlic.The chemical constitution of allicin and alliin or allicin is entirely different.By " two Diallyl trisulfide ether " is referred to as " allicin ", is a gross mistake.Make one to take for " active ingredient that allicin is garlic ", Therefore " allicin can be extracted from fresh garlic " be even more it is a kind of do not have it is valid misread, mislead or guess.Wherein, allicin (three Two propylene of sulphur) it is entirely artificial synthesized, and purity is not high.The allicin produced with the alliin in Natural Garlic and enzymolysis Chemical constitution it is different, also, allicin is free of in fresh garlic（Ailitridin）, allicin is that a kind of of allicin decomposes production Thing does not represent the active ingredient of garlic yet.As shown in Figure 2, Figure 3, Figure 4, can be to the change of alliin, allicin and allicin Structure is learned to be compared；Further, as shown in Figure 5, it will be appreciated that alliin, allinase, allicin and diallyl sulfide The relation of (ally sulfides).

Alliin, garlic are the highest plants of sulfur amino acid content in known edible plant, and wherein alliin accounts for whole More than the 70% of sulfur-containing amino acid, it is sulfur-containing amino acid to have 5% to 6% in the essential amino acid of human body.Body cannot synthesize in itself to be contained Sulphur amino acid, it is necessary to from external intake.Alliin is metabolized in vivo, directly participates in the synthesis of glutathione (GSH).Glutathione (GSH) it is a kind of tripeptides, by cysteine (cysteine), glutamic acid (glutamic acid) and glycine (glycine groups Into), there is Immune-enhancing effect (enhancer), removing toxic substances (detoxifier) and anti-oxidant (antioxidant) etc., so as to send out Drug effect is waved, resists the invasion of pathogen, prevents generation and the adjuvant therapy of tumors of cardiovascular and cerebrovascular disease.

Allinase (allinnase), also known as " Alkylcysteine sulfoxide lyase ", there is the catalysis of mild condition to split cooperation use the C-S keys of compound, There is certain effect for prevention " homocysteine hypercalcinuria ".Homocysteine (homocysteine, Hcy) is horizontal in blood Rise, be the morbidity of the vascular conditions such as atherosclerosis a hazards, and with Atheromatosis feelings in bright Aobvious dose-dependence.And blood vessel endothelium dysfunction caused by Hcy mass formed by blood stasis is in atherosclerosis early stage pathogenic process Important initiating link.Allinase is likely to become " future " medicine of prevention homocysteine hypercalcinuria.Unfortunately, current majority is ground " allicin of the person of studying carefully to be not present in fresh garlic（Diallytrisin）" it is used as research object.

American Pharmacopeia and European Union's pharmacopeia confirm that the principle active component of garlic (Alliium sativum L.) is：1., garlic Propylhomoserin (Alliin), chemical name：S-allyl-L-cysteine sulfoxide (S-Allyl-L-cysteine);2., allinase (Alliinase, EC 4.4.1.4), also known as alliin lyase (Alliin lyase)；3., allinase catalytic pyrolysis alliin production Raw allicin (Allicin) chemical name:Diallyl thiosulfinates (Diallyl thiosulfinate), due to The extraction of allicin and preparation technique are very difficult and complicated, therefore research and develop allicin system safely, effectively, quality controllable Agent becomes the research hotspot of pharmacy man of various countries.

After fresh garlic is cut or smashs to pieces, alliin therein meets with allinase, and rapid catalytic reaction is generated allicin, Allicin is unstable with the physicochemical property in air at normal temperatures, therefore alliin, allinase and preparation are extracted from fresh garlic " alliin+allinase " solid pharmaceutical preparation and allicin parenteral solution are very difficult.Allinase catalytic pyrolysis alliin produces allicin Relational expression schematic diagram as shown in Figure 1,

Relation between potential allicin amount and alliin amount is expressed from the next：

Potential allicin amount=alliin amount × C ×（162.3/354.4）

In formula：C represents alliin purity.

The present invention is related to and uses four patent of invention technologies altogether：

（1）, from fresh garlic extract alliin production technology refer to Publication No. 1425650 Chinese patent literature；

（2）, from fresh garlic extract allinase production technology refer to Publication No. 1424397 Chinese patent literature；

（3）, alliin reference substance preparation method refer to Publication No. 101560174 Chinese patent literature；

（4）, a kind of preparation method of allicin parenteral solution refer to the Chinese patent literature of Publication No. 102058527A.

Numerous studies show that allicin plays an important role in the antimicrobial acivity of garlic.To angiocardiopathy In terms of prevention and treatment, garlic has reducing blood lipid, antithrombotic, blood pressure lowering and prevention atherosclerosis and other effects, mechanism of action It is derived from the organic sulfur compound I of garlic）By suppressing a kind of enzyme-HMG-CoA very important during cholesterol biosynthesis also Protoenzyme suppresses cholesterol biosynthesis；ⅱ）It can suppress platelet aggregation；ⅲ）Suppression plays important in angiocardiopathy pathology Effect the enzyme for causing inflammation, i.e. epoxidase and lipoxygenase activity, reduce nitric oxide synthetase（iNOS）Derivant exists Inflammatory leukocytes（Macrophage）In expression；ⅳ）Suppress propagation and the transfer of vascular smooth muscle cells；V）It can synthesize important Vascular cell in antioxidant-glutathione and have antioxidation activity.

Drawn according to France and clap thunder（Rabelais ）University I. Arnault and J. Auger etc. 2004 is to European countries 11 commercialization garlic products using garlic powder as active ingredient（2 × Austria, 1 × Germany, 2 × Italy, 3 × Sweden, 1 × Britain, wherein only German examined product has medicine qualification）The analysis of progress, the results showed that, most of garlic powder products into Divide and greatly differ from each other with what their manufacturers declared.Neither one product stability reaches 90% limit mark of medicine code requirement Standard, most products have dropped to less than the 50% of assessment values.

So in order to prevent critical illness, clinical requirement active ingredient reaches high-content to ensure curative effect.For this reason, beautiful, The scholar of the minority developed country such as moral, Israel, France is starting using cryogenic freezing, vacuum drying, ion exchange, film point From etc. advanced technology, spend great effort research and development " the efficient novel formulation of garlic ".But development phase is still at present, both at home and abroad still Released without " the efficient novel formulation of garlic " product.

The content of the invention

The present invention provides a kind of allicin parenteral solution as the application for preparing treatment myocardial infarction disease medicament, overcome The deficiency of the above-mentioned prior art, it can effectively solve to there is no at present for " the efficient novel formulation of garlic " product in terms of myocardial infarction And the problem of myocardial infarction effect of drugs is not ideal is treated at present.

The technical scheme is that realized by following measures：A kind of allicin parenteral solution is treated as preparation The application of myocardial infarction disease medicament.

Here is the further optimization and/or improvements to foregoing invention technical solution：

Above-mentioned treatment myocardial infarction disease medicament is allicin parenteral solution.

The preparation method of above-mentioned allicin parenteral solution is with reference to the Chinese patent literature that patent publication No. is 102058527A.

The present invention carries out histopathology, compares " allicin vein note by " allicin parenteral solution " intravenous Penetrate administration group " with the myocardial infarct size of model group, test result indicates that allicin parenteral solution has the drug effect of anti-infarction, say Bright allicin parenteral solution can effectively prevent myocardial infarction disease, further illustrate that allicin parenteral solution can become one kind The efficiently new pharmaceutical formulation for the treatment of myocardial infarction disease.

Brief description of the drawings

Fig. 1 is the relational expression schematic diagram that allinase catalytic pyrolysis alliin produces allicin.

Fig. 2 is alliin chemical constitution schematic diagram in the present invention.

Fig. 3 is allicin chemical constitution schematic diagram in the present invention.

Fig. 4 is allicin chemical constitution schematic diagram in the present invention.

Fig. 5 is the pass of alliin in the present invention, allinase, allicin and diallyl sulfide (ally sulfides) It is schematic diagram.

Fig. 6 is to influence schematic diagram to rat model of myocardial infarction myocardial infarct size for reagent product in the present invention.

Embodiment

The present invention from following embodiments limitation, can technique according to the invention scheme and actual conditions determine specifically Embodiment.

With reference to embodiment, the invention will be further described：

Embodiment 1, the allicin parenteral solution is as the application for preparing treatment myocardial infarction disease medicament.Allicin exists To in terms of angiocardiopathy prevention and treatment, garlic has the work(such as reducing blood lipid, antithrombotic, blood pressure lowering and prevention atherosclerosis Effect, mechanism of action are derived from the organic sulfur compound of garlic：（1）By suppress one kind during cholesterol biosynthesis it is very important Enzyme-HMG-CoA reductase suppresses cholesterol biosynthesis；（2）It can suppress platelet aggregation；（3）Suppress in angiocardiopathy disease What is played an important role in reason causes the enzyme of inflammation, the i.e. activity of epoxidase and lipoxygenase, reduces nitric oxide synthetase （iNOS）Derivant is in inflammatory leukocytes（Macrophage）In expression；（4）Suppress propagation and the transfer of vascular smooth muscle cells； （5）Antioxidant-glutathione in important vascular cell can be synthesized and have antioxidation activity.

Can be according to actual needs, to above-mentioned allicin parenteral solution as the application for preparing treatment myocardial infarction disease medicament Make further optimization and/or improvements：

Embodiment 2, as the preferred of above-described embodiment, treatment myocardial infarction disease medicament is allicin parenteral solution.

Embodiment 3, as the preferred of above-described embodiment, the preparation method of allicin parenteral solution is with reference to patent publication No. The Chinese patent literature of 102058527A, prepares according to the method for the Chinese patent literature that patent publication No. is 102058527A Allicin parenteral solution per ml 5mg containing allicin, meet relevant criterion through spectrum and chromatography quality.

Analysis detection is carried out to drug effect of the allicin parenteral solution in terms of myocardial infarction disease is treated:

1st, animal model and packet

Model group：Using male, to 220gwistar rats as experimental animal, 3.5% is injected intraperitoneally with 10mL/kg by 180g again Chloral hydrate anesthesia, lies on the back and is fixed on rat plate；In rats with left the 4th, 5 intercostal incisions, thoracic cavity is opened, tears pericardium, gently Press thorax extrusion heart, with No. 0 surgical thread under left auricle of heart following coronary artery occlusion left anterior descending branch at 2mm, heart is put back to immediately Thoracic cavity, closes notch, skin suture.

Sham-operation group：Only threading does not ligature.Using male, 180g is weighed to 220gwistar rats as experimental animal, with 10mL/ 3.5% chloral hydrate anesthesia is injected intraperitoneally in kg, lies on the back and is fixed on rat plate；In rats with left the 4th, 5 intercostal incisions, chest is opened Chamber, tears pericardium, light to press thorax extrusion heart, is threaded with No. 0 surgical thread under left auricle of heart at 2mm, heart is put back to chest immediately Chamber, closes notch, skin suture.

Allicin is injected intravenously administration group：Using male, 180g is weighed to 220gwistar rats as experimental animal, with 3.5% chloral hydrate anesthesia is injected intraperitoneally in 10mL/kg, lies on the back and is fixed on rat plate；In rats with left the 4th, 5 intercostal incisions, beat Open thoracic cavity, tear pericardium, it is light to press thorax extrusion heart, with No. 0 surgical thread under left auricle of heart the left front drop of following coronary artery occlusion at 2mm Branch, puts back to thoracic cavity by heart immediately, closes notch, skin suture.

2nd, animal model detects

（1）, Electrocardiography：Each group animal postoperative 1 carries out Electrocardiography when small, and ST sections of elevated animals are included reality Test system.Each group animal is administered in next day, and detection electrocardiogram is repeated in the stipulated time.Electrocardiography is used for determining modeling Whether succeed.

（2）, B ultrasound detection：By detecting left ventricular end diastolic anterior wall thickness（LVAWd）With rear wall thickness（LVPWd）, relax Open latter stage（LVIDd）With end-systole left ventricular interior diameter（LVIDs）, diastasis and end-systole bulk of left ventricle（LVEDV, LVESV）, ejection fraction (EF), shortening fraction (FS) and stroke output (SV) are to determine each race's model group animal model No success.

（3）, myocardial infarction area detection：Take out the heart of every group of mouse, normal saline flushing chambers of the heart remained blood, with filter Paper is weighed after blotting surplus liquid；Ventricle, is uniformly cut into uniform thickness 5, weighed respectively by parallel coronary artery ditch under self-ligating line It is placed on room temperature in 0.2% nitro blue tetrazolium and dyes 2-3min, scanner scans five myocardium positive and negative, swept respectively Trace designs picture；With the infarcted region of every myocardium bilateral of multi-media color Pathologic image analysis systematic survey, the ventricle gross area, stalk are calculated Plug area's gross area and infarct area account for ventricle area percentage.

B ultrasound detects and myocardial infarction area testing result is shown, if sham-operation group Non Apparent Abnormality and model group cardiac muscle are thin Born of the same parents' structure disturbance, vacuole deformation, swelling, myocardial fibrosis, inflammatory cell infiltration, show modeling success.

3rd, medication

" the allicin injection that will be prepared according to the method for the Chinese patent literature that patent publication No. is 102058527A Liquid " is diluted to 1mg/ml, after rat revives, carries out tail vein to allicin intravenous injection administration group by 5.2mg/kg and gives Medicine, once a day, continuous 7 days, draws materials when 1 is small after the last administration and checks.

4th, inspection and interpretation of result

Core dirty relevant portion, wash away crimson blood with cold saline, be put in neutral formalin, be dehydrated, embedding, HE dyes Color, carries out histopathology, compares the myocardial infarct size of " allicin intravenous injection administration group " and model group." garlic is peppery Compared with model group, the myocardial infarction area of rat is substantially reduced and declines element intravenous injection administration group "（P＜ 0.01）, Illustrate that allicin parenteral solution has a better effect myocardial infarction.It is shown in Table 1 and Fig. 6.

It can be seen that by above-mentioned experimentation and result：The present invention carries out tissue by " allicin parenteral solution " intravenous Pathology detect, and compare the myocardial infarct size of " allicin intravenous injection administration group " and model group, test result indicates that garlic is peppery Plain parenteral solution has the drug effect of anti-infarction, illustrates that allicin parenteral solution can effectively prevent myocardial infarction disease, into one Step explanation allicin parenteral solution can become a kind of new pharmaceutical formulation of efficiently treatment myocardial infarction disease.

Table 1 is for influence of the reagent product to myocardial infarction model myocardial infarct size（± SD）

Group	Model group	Allicin is injected intravenously administration group
			Every group of animal number of elements	15	18
Infraction/ventricle（%）	26.7±7.1	16.7±5.5**
			Infraction/whole-heartedly（%）	17.7±4.8	9.98±2.8**

Note：Compared with model group, *P<0.05；**P<0.01

Claims (1)

1. a kind of allicin parenteral solution is as the application for preparing treatment myocardial infarction disease medicament, it is characterised in that treatment cardiac muscle Infarct disease medicament is allicin parenteral solution, and the preparation method of the allicin parenteral solution is with reference to patent publication No. The Chinese patent literature of 102058527A.