CN102048937A - Chinese medicinal composition for treating and resisting platelet aggregation - Google Patents
Chinese medicinal composition for treating and resisting platelet aggregation Download PDFInfo
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- CN102048937A CN102048937A CN2009100711731A CN200910071173A CN102048937A CN 102048937 A CN102048937 A CN 102048937A CN 2009100711731 A CN2009100711731 A CN 2009100711731A CN 200910071173 A CN200910071173 A CN 200910071173A CN 102048937 A CN102048937 A CN 102048937A
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Abstract
The invention discloses a Chinese medicinal composition for treating and resisting platelet aggregation, a medicinal composition taking the compound as an active ingredient, and application of the Chinese medicinal composition and the medicinal composition as medicines for resisting the platelet aggregation, particularly to the preparation of medicines for preventing or treating coronary artery syndrome, myocardial infarction, myocardial ischemia and cardiovascular and cerebrovascular diseases caused by the platelet aggregation.
Description
Technical field
The invention belongs to medical technical field, or rather, relate to a kind of Chinese medicine composition for the treatment of antiplatelet aggregation and preparation method thereof.
Background technology
Along with the problem of an aging population is serious day by day, cardiovascular and cerebrovascular disease has become " the No.1 killer " who has a strong impact on health of people and life.Anticoagulant comprises heparin, vitamin K antagonist warfarin and the direct thrombin inhibitor etc. that suppress IIa and Xa factor by antithrombase indirectly.
Antiplatelet drug mainly contains aspirin, adenosine diphosphate (ADP) (ADP) receptor antagonist thiophene pyridines and glycoprotein (GP) the IIb/IIIa receptor antagonist etc. that suppress thromboxane A2 (TXA2) approach.Blood coagulation is the activatory chain reaction of the proteolysis of a complexity, finally makes the Fibrinogen of solubility become fibrin stable, indissoluble, enlists the services of hemocyte and forms blood clot.The thrombin that participates in comprises with 12 thrombins of Roman number numbering and prekallikrein, kallikrein (kallikrein, Ka), high-molecular-weight kininogen (high molecular weight kininogen, HMWK), platelet phospholipid (PL or PF3) etc.Anticoagulant (anticoagulants) is that a class is disturbed thrombin, stops the medicine of blood coagulation, is mainly used in the prevention and the treatment of thrombotic disease.Platelet aggregation inhibitor claims platelet function inhibitor again, and at that time with such medicine belonged to anticoagulant therapy category in clinical practice the sixties.Along with understanding to the thrombotic disease genesis mechanism, the status of Antiplatelet therapy in clinical is more and more important, new platelet function inhibitor continues to bring out, and medicament for resisting platelet aggregation has become an independent class medicine and has been widely used in thrombotic disease.
Summary of the invention
One object of the present invention is, discloses a kind of Chinese medicine composition another object of the present invention for the treatment of antiplatelet aggregation and has been, discloses the preparation method with the Chinese medicine composition of treatment antiplatelet aggregation.
A further object of the invention is, the application of the Chinese medicine composition of treatment antiplatelet aggregation as the antiplatelet drug aspect disclosed, particularly be used to prepare the coronary syndrome that prevention or treatment cause because of platelet aggregation, myocardial infarction, the purposes of myocardial ischemia, cardiovascular and cerebrovascular diseases medicament aspect.
The preparation of pharmaceutical compositions of The compounds of this invention is as follows: use standard and conventional technology; acceptable solid or liquid-carrier are combined, and make it at random to combine and be prepared into microgranule or microsphere with acceptable adjuvant and excipient on the galenic pharmacy.Solid dosage forms comprises tablet, discrete particles, capsule, slow releasing tablet, slow-release micro-pill or the like.Solid carrier can be at least a material, and it can serve as diluent, flavouring agent, solubilizing agent, lubricant, suspending agent, binding agent, disintegrating agent and coating agent.Inert solid carrier comprises magnesium phosphate, magnesium stearate, smoothers sugar, lactose, pectin, propylene glycol, polyoxyethylene sorbitan monoleate, dextrin, starch, gelatin, cellulose substances for example methylcellulose, microcrystalline Cellulose, low melt point paraffin, Polyethylene Glycol, mannitol, cocoa butter etc.Liquid dosage form comprises solvent, suspension for example injection, powder or the like.
The amount of the active ingredient that contains in pharmaceutical composition and the unit dosage form (The compounds of this invention) can be according to patient's the state of an illness, specific being applied of situation of diagnosis, the amount of used chemical compound or concentration are regulated in the scope of a broad, usually, the weight range of reactive compound is 0.5%～90% (weight) of compositions.Another preferred range is 0.5%-70%.Chemical compound or its pharmaceutically acceptable salt with formula I structure of the present invention has the obvious suppression effect aspect platelet aggregation.Further specify The compounds of this invention to rat platelet aggregation inhibitory action test material below by pharmacodynamic experiment
Medicine and preparation: The compounds of this invention (1-27) is made into suspension with 0.5%CMC and uses for animals administer; Adenosine diphosphate (ADP) (ADP) (SERVA company, lot number 01993)
Animal: male rat, Tianjin Inst. of Materia Medica laboratory animal room provides, the animal quality certification number: No. the 001st, Tianjin animal word.
Instrument: PK121R type centrifuge (Italian ALC International SPL product), SPA-3 type PPP platelet aggregation instrument (Shanghai Kodak test instrunment factory).
Test method:
Male Wistar rat, about body weight 300g, per os is irritated stomach and is given Clopidogrel Hydrogensulfate and analog thereof, and dosage is 10mg/kg, the administration volume is 10ml/kg, behind the 2h, etherization, ventral aorta blood sampling, 3.8% sodium citrate anticoagulant, whole blood is 9: 1 with the ratio of anticoagulant, the centrifugal 7min of 1000rpm, preparation platelet rich plasma (PPP).Transfer PRP with PPP, make its platelet count remain on 2 * 10
6Individual/ml.Get PRP and add in the test cup, 37 ℃ of temperature are incubated 10min.With the PRP zeroing, PPP transfers 100%, is derivant with ADP (final concentration is 5 μ M), measures platelet aggregation percent by turbidimetry with SPA-3 type PPP platelet aggregation instrument, with t-check carrying out statistics relatively.
The specific embodiment
Embodiment 1
Rhizoma Chuanxiong 2-20 part Radix Angelicae Sinensis 2-20 part Radix Salviae Miltiorrhizae (parched with bran) 2-20 part
Herba Erigerontis 1-10 part Bulbus Allii 1-10 part Radix Paeoniae Rubra (Rhizoma Zingiberis Recens is processed) 2-20 part
Herba Agrimoniae 0.1-0.8 part Tremella 1-10 part Fructus Jujubae (enucleation) 10-60 part
Rhizoma Chuanxiong 1-10 part Herba Leonuri 1-10 part.
Take by weighing above-mentioned medical material 200g, decoct with water three times, each 1.0h, collecting decoction filters, and filtrate is concentrated into about 2000ml (0.1MP, 70 ℃).Concentrated solution is by HPD-100 type macroporous adsorptive resins purification, and with 4BV distilled water eluting, reuse 30% ethanol 6BV eluting is collected 30% ethanol elution, and is evaporated to 100mL, gets extract earlier.
Embodiment 2
Rhizoma Chuanxiong 8-11 part Radix Angelicae Sinensis 8-11 part Radix Salviae Miltiorrhizae (parched with bran) 8-11 part
Herba Erigerontis 4-7 part Bulbus Allii 4-7 part Radix Paeoniae Rubra (Rhizoma Zingiberis Recens is processed) 8-11 part
Herba Agrimoniae 0.25-0.35 part Tremella 2-5 part Fructus Jujubae (enucleation) 25-40 part
Rhizoma Chuanxiong 4-7 part Herba Leonuri 3-6 part;
Take by weighing above-mentioned medical material 200g, decoct with water three times, each 1.0h, collecting decoction filters, and filtrate is concentrated into about 2000ml (0.1MP, 70 ℃).Concentrated solution is by HPD-100 type macroporous adsorptive resins purification, and with 4BV distilled water eluting, reuse 30% ethanol 6BV eluting is collected 30% ethanol elution, and is evaporated to 100mL, gets extract earlier.
Embodiment 3
9.94 parts of Rhizoma Chuanxiong 9.94 parts of Radix Salviae Miltiorrhizaes of 9.94 parts of Radix Angelicae Sinensis (parched with bran)
9.94 parts of Herba Erigerontis 5.96 parts of Radix Paeoniae Rubra of 5.96 portions of Bulbus Alliis (Rhizoma Zingiberis Recens is processed)
3.97 parts in 0.3 portion of Tremella of 4.97 parts of Herba Agrimoniaes of Herba Leonuri
5.96 parts of 33.12 parts of Rhizoma Chuanxiongs of Fructus Jujubae (enucleation).
Take by weighing above-mentioned medical material 200g, decoct with water three times, each 1.0h, collecting decoction filters, and filtrate is concentrated into about 2000ml (0.1MP, 70 ℃).Concentrated solution is by HPD-100 type macroporous adsorptive resins purification, and with 4BV distilled water eluting, reuse 30% ethanol 6BV eluting is collected 30% ethanol elution, and is evaporated to 100mL, gets extract earlier.
Embodiment 4
The united extraction thing adds the injection water and makes into 1000mL, ultrafiltration membrance filter (6000 molecular weight) degerming, and under the sterile working, fill is put lyophilizing in the freezer dryer in 5mL sterilization bottle (every bottled 2mL), seal, and promptly gets injectable powder.
Embodiment 5
Extract 10 grams, sorbitol 18 grams, citric acid 0.9 gram, aspartame 0.5 gram, starch 57.6 grams, dextrin 14.4 grams, Rhizoma Coptidis superfine powder 7.2 grams, magnesium stearate 1.5 grams are made 20.
Claims (5)
1. Chinese medicine composition for the treatment of antiplatelet aggregation is characterized in that it is to be made by following materials of weight proportions:
Rhizoma Chuanxiong 2-20 part Radix Angelicae Sinensis 2-20 part Radix Salviae Miltiorrhizae (parched with bran) 2-20 part
Herba Erigerontis 1-10 part Bulbus Allii 1-10 part Radix Paeoniae Rubra (Rhizoma Zingiberis Recens is processed) 2-20 part
Herba Agrimoniae 0.1-0.8 part Tremella 1-10 part Fructus Jujubae (enucleation) 10-60 part
Rhizoma Chuanxiong 1-10 part Herba Leonuri 1-10 part.
2. go the described compositions of claim 1, it is characterized in that it is a medical material by following weight proportion, makes through following method:
Rhizoma Chuanxiong 8-11 part Radix Angelicae Sinensis 8-11 part Radix Salviae Miltiorrhizae (parched with bran) 8-11 part
Herba Erigerontis 4-7 part Bulbus Allii 4-7 part Radix Paeoniae Rubra (Rhizoma Zingiberis Recens is processed) 8-11 part
Herba Agrimoniae 0.25-0.35 part Tremella 2-5 part Fructus Jujubae (enucleation) 25-40 part
Rhizoma Chuanxiong 4-7 part Herba Leonuri 3-6 part.
3. go the described compositions of claim 1, it is characterized in that it is a medical material by following weight proportion, makes through following method:
9.94 parts of Rhizoma Chuanxiong 9.94 parts of Radix Salviae Miltiorrhizaes of 9.94 parts of Radix Angelicae Sinensis (parched with bran)
9.94 parts of Herba Erigerontis 5.96 parts of Radix Paeoniae Rubra of 5.96 portions of Bulbus Alliis (Rhizoma Zingiberis Recens is processed)
3.97 parts in 0.3 portion of Tremella of 4.97 parts of Herba Agrimoniaes of Herba Leonuri
5.96 parts of 33.12 parts of Rhizoma Chuanxiongs of Fructus Jujubae (enucleation).
4. pharmaceutical composition, it comprises each compositions and blended with it one or more pharmaceutically useful excipient of claim 1-3 for the treatment of effective dose.
5. each compositions of claim 1-3 is being used to prepare the coronary syndrome that treatment causes because of platelet aggregation, myocardial infarction, the application of myocardial ischemia, cardiovascular and cerebrovascular diseases medicament aspect.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009100711731A CN102048937A (en) | 2009-11-05 | 2009-11-05 | Chinese medicinal composition for treating and resisting platelet aggregation |
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| Application Number | Priority Date | Filing Date | Title |
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| CN2009100711731A CN102048937A (en) | 2009-11-05 | 2009-11-05 | Chinese medicinal composition for treating and resisting platelet aggregation |
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| CN102048937A true CN102048937A (en) | 2011-05-11 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110522798A (en) * | 2019-09-24 | 2019-12-03 | 新疆华春生物药业股份有限公司 | A kind of compound preparation and preparation method thereof curing mainly coronary heart disease |
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2009
- 2009-11-05 CN CN2009100711731A patent/CN102048937A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110522798A (en) * | 2019-09-24 | 2019-12-03 | 新疆华春生物药业股份有限公司 | A kind of compound preparation and preparation method thereof curing mainly coronary heart disease |
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Application publication date: 20110511 |