CN105412090A - Application of Daphenylline in preparing anti-platelet aggregation drugs - Google Patents
Application of Daphenylline in preparing anti-platelet aggregation drugs Download PDFInfo
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- CN105412090A CN105412090A CN201510901666.9A CN201510901666A CN105412090A CN 105412090 A CN105412090 A CN 105412090A CN 201510901666 A CN201510901666 A CN 201510901666A CN 105412090 A CN105412090 A CN 105412090A
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- daphenylline
- platelet aggregation
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention relates to the application of Daphenylline in preparing anti-platelet aggregation drugs. The application of Daphenylline in preparing anti-platelet aggregation drugs is disclosed for the first time, a novel framework type is adopted, anti-platelet aggregation activity is surprisingly high, the possibility of inspiration of other compounds is completely avoided, prominent substantive features are realized, and remarkable progress is made in terms of the application in resisting platelet aggregation.
Description
Technical field
The present invention relates to the novelty teabag of Compound D aphenylline, particularly relate to Daphenylline and preparing the application in medicament for resisting platelet aggregation.
Background technology
Hematoblastic basic physiological function is sticked, assembles, discharges and secretory granule content (as ATP, 5-hydroxy tryptamine), and the platelet of quiescent condition changes states of physiologic function into and is hematoblastic activation.Can phospholipid surface be provided after platelet activation, promote the carrying out of blood coagulation, be formed and hold by fibrin the thrombosis that platelet forms.Therefore platelet is as a kind of visible component of blood, in the thrombosis of physiological hemostasis and pathology, plays a very important role.Clinical research shows, cardiovascular and cerebrovascular disease common is clinically as basic in hypertension, angina pectoris myocardial infarction, cerebral infarction and cerebral hemorrhage etc., all changes relevant with Abnormal Blood Rheology with platelet function.Antiplatelet drug conventional at present has heavier untoward reaction, therefore develops novel effective, that untoward reaction is little treatment very urgent with the medicine of prevention platelet aggregation.The present inventor studies by experiment, finds that Daphenylline has the effect of antiplatelet aggregation.
The Compound D aphenylline that the present invention relates to is one and delivers (QiangZhang in 2014, etal., Daphenylline, aNewAlkaloidwithanUnusualSkeleton, fromDaphniphyllumlongeracemosum.ORGANICLETTERS.2009, 11 (11), noval chemical compound 2357-2359.), this compound has brand-new framework types (QiangZhang, etal., Daphenylline, aNewAlkaloidwithanUnusualSkeleton, fromDaphniphyllumlongeracemosum.ORGANICLETTERS.2009, 11 (11), 2357-2359.), the Daphenylline that the present invention relates to is belonged to first public preparing the purposes in medicament for resisting platelet aggregation, owing to belonging to brand-new structure type, and its platelet aggregation inhibitory activity is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, the effect of antiplatelet aggregation simultaneously obviously has significant progress.
Summary of the invention
The invention provides Daphenylline and prepare the application in medicament for resisting platelet aggregation.
The present invention, using aspirin and clopidogrel as positive drug, proves by experiment, and Daphenylline can obvious anticoagulant, and index all significantly reduces, and maintains an equal level with positive drug.
Described Compound D aphenylline structure is as shown in formula I:
Described Daphenylline is preparing the application in medicament for resisting platelet aggregation, is derivant with ADP in anticoagulant experiment.
A kind of medicament for resisting platelet aggregation, be that active component interpolation adjuvant is prepared from by Daphenylline, preparation method, for getting 5 g of compound Daphenylline, adds 195 grams, dextrin, and mixing, conventional tablet presses makes 1000.
A kind of medicament for resisting platelet aggregation, be that active component adds adjuvant and is prepared from by Daphenylline, preparation method, for getting 5 g of compound Daphenylline, adds starch 195 grams, mixing, encapsulatedly makes 1000.
The Daphenylline that the present invention relates to belongs to first public preparing the purposes in medicament for resisting platelet aggregation, because framework types belongs to brand-new framework types, and its platelet aggregation inhibitory activity is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, for antiplatelet aggregation, obviously there is significant progress simultaneously.
Detailed description of the invention
The preparation method of Compound D aphenylline involved in the present invention is see document (QiangZhang, etal., Daphenylline, aNewAlkaloidwithanUnusualSkeleton, fromDaphniphyllumlongeracemosum.ORGANICLETTERS.2009,11 (11), 2357-2359.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of Compound D aphenylline tablet involved in the present invention:
Get 5 g of compound Daphenylline, add 195 grams, dextrin, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of Compound D aphenylline capsule involved in the present invention:
Get 5 g of compound Daphenylline, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Test example 1:Daphenylline is on the impact of rat platelet aggregation function
1. animal: cleaning grade Sprague-Dawley rat, male, body weight 200g-250g.
2. method and result
Animal is divided into blank group (waiting capacity solvent), aspirin group (ASA at random, 50mg/kg), clopidogrel group (7mg/kg), Daphenylline0.625mg/kg group, Daphenylline1.25mg/kg group, Daphenylline2.5mg/kg group, often organize 8, gastric infusion, 1 time/d, continuous 5d.1h after last administration, with 3% pentobarbital sodium anesthetized rat (30mg/kg) respectively, take a blood sample through ventral aorta, with 3.8% liquor sodii citratis anticoagulant (blood: anticoagulant=9:1), 1000r/min, be separated platelet rich plasma (PRP), remainder is again with the centrifugal 15min of 3000r/min, be separated platelet poor plasma (PPP), by turbidimetry with ADP (252umol/L) for derivant, platelet aggregation rate in 5min is measured with LBY-NJ blood pool instrument, and calculate platelet aggregation inhibition rate as follows, data % represents, statistical procedures is carried out with t inspection between group, the results are shown in Table 1.
Platelet aggregation inhibition rate=(blank platelet aggregation rate %-delivery tube platelet aggregation rate %)/blank platelet aggregation rate %*100%
Experimentally result is known, and each dosage group of Daphenylline can obviously suppress platelet aggregation in body, and drug effect and positive drug aspirin and clopidogrel maintain an equal level.
Table 1Daphenylline is to hematoblastic gathering suppression ratio (, n=8)
Compare with blank group, * * P<0.001*P<0.01
Conclusion: using aspirin and clopidogrel as positive drug, prove by experiment, Daphenylline can obvious anticoagulant, maintains an equal level, can be used for preparing medicament for resisting platelet aggregation with positive drug.
Claims (4)
- The application of 1.Daphenylline in medicament for resisting platelet aggregation, described Compound D aphenylline structure is as shown in formula I:
- 2. the application of Daphenylline in medicament for resisting platelet aggregation as claimed in claim 1, is characterized in that in anticoagulant experiment be derivant with ADP.
- 3. a medicament for resisting platelet aggregation, it is characterized in that by Daphenylline described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound Daphenylline, adds 195 grams, dextrin, mixing, conventional tablet presses makes 1000.
- 4. a medicament for resisting platelet aggregation, it is characterized in that by Daphenylline described in claim 1 being that active component adds adjuvant and is prepared from, preparation method, for getting 5 g of compound Daphenylline, adds starch 195 grams, and mixing, encapsulatedly makes 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510901666.9A CN105412090A (en) | 2015-12-08 | 2015-12-08 | Application of Daphenylline in preparing anti-platelet aggregation drugs |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510901666.9A CN105412090A (en) | 2015-12-08 | 2015-12-08 | Application of Daphenylline in preparing anti-platelet aggregation drugs |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105412090A true CN105412090A (en) | 2016-03-23 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510901666.9A Pending CN105412090A (en) | 2015-12-08 | 2015-12-08 | Application of Daphenylline in preparing anti-platelet aggregation drugs |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107088945A (en) * | 2017-05-02 | 2017-08-25 | 长乐净能新材料科技有限公司 | A kind of timber preservative containing compound Daphenylline |
-
2015
- 2015-12-08 CN CN201510901666.9A patent/CN105412090A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107088945A (en) * | 2017-05-02 | 2017-08-25 | 长乐净能新材料科技有限公司 | A kind of timber preservative containing compound Daphenylline |
| CN107088945B (en) * | 2017-05-02 | 2018-05-08 | 长乐净能新材料科技有限公司 | A kind of timber preservative containing compound Daphenylline |
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| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160323 |
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| WD01 | Invention patent application deemed withdrawn after publication |