CN107550912A - A kind of drug compound preparation for treating arterial embolism - Google Patents
A kind of drug compound preparation for treating arterial embolism Download PDFInfo
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- CN107550912A CN107550912A CN201710830538.9A CN201710830538A CN107550912A CN 107550912 A CN107550912 A CN 107550912A CN 201710830538 A CN201710830538 A CN 201710830538A CN 107550912 A CN107550912 A CN 107550912A
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- compound preparation
- dipyridamole
- arterial embolism
- hexanicit
- compound
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Abstract
The invention discloses a kind of drug compound preparation for treating arterial embolism, by weight, including 10~300 parts of hexanicits, 10~120 parts of Dipyridamoles and 10~1600 parts of pharmaceutical carriers, the hexanicit mixes with Dipyridamole as drug ingedient with pharmaceutical carrier forms compound preparation.The invention provides a kind of hexanicit convenient to take, safe to use and the drug compound preparation of the treatment arterial embolism of Dipyridamole, its therapeutic effect is notable, and high degree reduces complication, and sequelae is less, typically have no adverse reaction, patient can be made quickly to get well.
Description
Technical field
The present invention relates to drug compound preparation field, in particular to a kind of drug compound preparation for treating arterial embolism.
Background technology
Arterial embolism refers to that the foreign matter in clot or intravasation turns into embolus, and as blood flow is parked on, bore is similar to be moved
In arteries and veins, circulatory disorders are caused.Arterial embolism is mainly caused by thrombus, in addition, the foreign matter such as tumour, air, fat may also turn into
Embolus.
The weight of symptom and the speed of lesion growth, the number of Doppler flow mapping have substantial connection.Early symptom is intermittence
Walk lamely, distal popliteal beating weakens or disappeared, as lesion is located at abdomen master-common iliac artery person.Pain can betide lower waist, stern, ilium, big
On rear side of leg or shank gastrocnemius position is sometimes with impotence；Lesion is in Gu — popliteal artery persons.
Pain betides shank muscle group.During limbs chronic ischemia, atrophoderma is thinning, shinny, osteoporosis, amyotrophia,
Trichomadesis, toenail are thickened and deformed.Later stage may occur in which rest pain, and skin temperature substantially lowers, cyanosis, far-end of limb gangrene and
Ulcer.
Pathogenic factor and mechanism are not fully understood, hyperlipidemia, hypertension, smoking, diabetes, obesity and high density fat
Albumen is low etc., is susceptible factor.
Existing treatment method uses operative treatment, including percutaneous transluminal angio plasty, Endarterectomy art, bypasses turn of tidal stream
Art etc., although therapeutic effect is got instant result, side effect is serious, and patient needs to bear the doctor of larger pain and great number
Treatment expense.
The content of the invention
The technical problems to be solved by the invention are to provide a kind of drug compound preparation for treating arterial embolism.
Technical scheme is used by the present invention solves the above problems：A kind of drug compound preparation for treating arterial embolism,
By weight, including 10~300 parts of hexanicits, 10~120 parts of Dipyridamoles and 10~1600 parts of pharmaceutical carriers,
The hexanicit mixes with Dipyridamole as drug ingedient with pharmaceutical carrier forms compound preparation.
In order to which the present invention is better achieved, further, by weight, the pharmaceutical carrier is that 100~120 inertia are consolidated
Body or 160~1000 parts of inert fluids.
In order to which the present invention is better achieved, further, the inert solid is excipient, disintegrant, lubricant, hydrotropy
One kind or above-mentioned a variety of mixtures formed with arbitrary proportion in agent, flavouring, adhesive.Excipient, disintegrant, lubrication
Agent, cosolvent, flavouring, adhesive include lactose, starch, dextrin, microcrystalline cellulose, PVP, gelatin, superfine silica gel powder,
Polyethylene glycol etc..
In order to which the present invention is better achieved, further, the inert fluid is in diluent, wetting agent, additive
The mixture that a kind of or above two is formed with arbitrary proportion.
In order to which the present invention is better achieved, further, the formulation of the compound preparation include tablet, capsule, granula,
Supensoid agent and syrup.A kind of drug compound preparation for treating arterial embolism, by weight mainly by hexanicit 20~
The mixture of 400 parts and 2~40 parts of Dipyridamole is medicinal component composition.
The drug compound preparation for the treatment of arterial embolism of the present invention can be prepared according to method known in the industry, that is, pass through by
Hexanicit and Dipyridamole are admixed and obtained with appropriate inert solid or liquid pharmaceutical carrier.It can be made and be adapted to orally
Compound preparation, the formulation for being adapted to oral compound preparation can be tablet, granula, capsule, supensoid agent, syrup.Wherein piece
Agent, granula, capsule can contain the carrier and/or assistant agent commonly used in pharmaceuticals industry.Such as Icing Sugar, starch, absorbent (such as
Dextrin), disintegrant (such as Tween-80), lubricant (such as 50% ethanol), magnesium stearate etc..Wherein supensoid agent, syrup
Carrier and/or assistant agent that system is industrially commonly used can be contained.Such as diluent (such as it is water, distilled water, ethanol, polyethylene glycol, sweet
Oil etc.), conventional additive (such as suspending liquid, preservative, flavouring etc.).Tablet, granula can be by dry or wet granulation works
It is prepared by skill.The appropriate mixture of compound can be inserted soft or hard gelatine capsule kind and is made by capsule.Supensoid agent and syrup
The appropriate mixture of compound can be added mixed with the aqueous solution, the diluent is made in the diluent of suspending agent, preservative etc.
Preferably distilled water, suspending agent are preferably tragacanth, and preservative is preferably nipalgin second, the third fat, is preferably added in syrup strong
Taste agent, flavouring are sucrose.
Hexanicit is after intestines and stomach absorption, then slowly metabolism in vivo, is gradually hydrolyzed into nicotinic acid and inositol, then passes through
Both play a role for this.Energy mitigation, enduringly diastole peripheral vascular, improve abnormalities of sugar/lipid metabolism, solution fibrin, dissolve blood
Bolt and anti-freezing.To the same nicotinic acid of idicatio of hyperlipoprotememia, auxiliary treatment can be used as.And it can be used for coronary heart disease and various tips
The auxiliary treatment of vasospasm disease (such as Arteriosclerosis obliterans, Raynaud's disease, antimigraine)
Dipyridamole has anti-thrombosis function.Dipyridamole suppresses platelet aggregation, and high concentration (50 μ g/ml) can press down
Intra platelet free calcium processed.
Mechanism of action may be：
(1) blood platelet intake adenosine is suppressed, and adenosine is a kind of platelet response inhibitor；
(2) suppress phosphodiesterase, increase CAMP in blood platelet (cAMP)；
(3) thromboxane element A2 (TXA2) formation, the robust agonist of TXA2 biologically active pdgfs are suppressed；
(4) endogenous PGI2 is strengthened.
Dipyridamole has dilating effect to blood vessel.Dog gives Dipyridamole 0.5~4.0mg/kg producing agent through duodenum
Measuring correlation body circulation and coronary vascular resistance reduces, and systemic blood pressure reduces and coronary blood flow increase.After administration from 24 minutes
Effect, effect lasts about 3 hours.In people it was observed that identical hemodynamic Effects.But Acute Venous administration can make narrow coronary artery
Distally local heart muscle perfusion is reduced.In mouse 111 weeks and 128~142 weeks oral tests of rat, 8,25 and 75mg/kg (1,
The daily maximum recommended dosage of 3.1 and 9.4 times of people) Dipyridamole do not produce obvious carcinogenic effect.The result of mutagenicity test is
It is negative.Rat reproduction test uses the daily maximum recommended dosage Dipyridamole of 60 times of people, does not show the impaired evidence of reproduction.But
In the daily maximum recommended dosage of 115 times of people, corpus luteum quantity is significantly reduced, and tire plantation living is reduced.Mouse, rat and rabbit experiment
The evidence of Dipyridamole infringement fetus is not shown.Mouse oral LD50 is 2150mg/kg；Single oral lethal dose is in rat
6000mg/kg, it is 350mg/kg in dog.
Dipyridamole injection liquid：Plasma half-life is 2~3 hours.With plasma protein binding rate height.In intrahepatic metabolism, with
Glucuronic acid combines, from bile excretion.
Dipyridamole sustained-release capsules：Plasma concentration peak time about 2 hours after oral, plasma steady state Cmax is 1.98 μ
G/ml (1.01~3.99 μ g/ml), Steady state trough concentration are 0.53 μ g/ml (0.18~1.01 μ g/ml) and plasma protein binding rate
For 99%, half-life period is about 12 hours.In intrahepatic metabolism, from bile excretion after being combined with glucosiduronate.
In summary, the beneficial effects of the invention are as follows：The invention provides a kind of nicotinic acid flesh convenient to take, safe to use
The drug compound preparation of the treatment arterial embolism of alcohol ester and Dipyridamole, its therapeutic effect is notable, and high degree reduces complication,
And sequelae is less, typically have no adverse reaction, patient can be made quickly to get well.
Embodiment
With reference to embodiment, the present invention is described in further detail, but the implementation of the present invention is not limited to this.
Embodiment 1：
The compound oral administration preparation of the present embodiment is prepared using pharmaceuticals industry known method, and the specific dosage of each component is referring to table
One：
The specific dosage of each component of table one
Mixed simultaneously using two kinds of oral drugs of hexanicit and Dipyridamole and take the therapeutic effect of progress and show, made
A kind of alone medicine is superior to the effect of hexanicit and Dipyridamole, so as to answering for two kinds of medicines reasonable 5 of development
Square preparation is laid a good foundation.
Embodiment 2：
The therapeutic effect checking of rat model：
Purpose：The compound preparation of the different ratio of hexanicit joint Dipyridamole is observed to DOCA (acetic acid deoxidation skins
Matter ketone) influence with arterial embolism rat, to inquire into the therapeutic action in compound under various dose collocation.
Method：SD rats 1200, ♂, 180~190g of body weight.It is secondary weekly under germ-free condition after the kidney of excision right side
Give DOCA 5mg/ only, sc, and raise with 1% sodium chloride solution；12 groups are randomly divided into, every group 8, is specifically grouped and disposes feelings
Condition such as table two.
The animal packet of table two and pharmaceutical formulation, medication
| Model group | Physiological saline |
| Hexanicit group | 400 milligrams of hexanicit |
| High group of Dipyridamole | 40 milligrams of Dipyridamole |
| One group of compound | 20 milligrams of hexanicit, 2 milligrams of Dipyridamole |
| Two groups of compound | 20 milligrams of hexanicit, 20 milligrams of Dipyridamole |
| Three groups of compound | 20 milligrams of hexanicit, 40 milligrams of Dipyridamole |
| Four groups of compound | 200 milligrams of hexanicit, 2 milligrams of Dipyridamole |
| Five groups of compound | 200 milligrams of hexanicit, 20 milligrams of Dipyridamole |
| Six groups of compound | 200 milligrams of hexanicit, 40 milligrams of Dipyridamole |
| Seven groups of compound | 400 milligrams of hexanicit, 2 milligrams of Dipyridamole |
| Eight groups of compound | 400 milligrams of hexanicit, 20 milligrams of Dipyridamole |
| Nine groups of compound | 400 milligrams of hexanicit, 40 milligrams of Dipyridamole |
Medication：Compound group medicine is diluted with water to scattered paste shape, daily gastric infusion, po, qd (orally, one day one
It is secondary)；Continuous 5 weeks.
As a result：After 5 weeks, the rehabilitation situation of each group animal is determined, each group animal dead rehabilitation rate and statistical result are shown in Table three.
The each group mortality of animals of table three and rehabilitation rate statistical result
| Group | Death toll (only) | The death rate (%) | Rehabilitation number (only) | Rehabilitation rate (%) |
| Model group | 97 | 97 | 0 | 0 |
| Hexanicit group | 51 | 51 | 49 | 49 |
| Dipyridamole group | 64 | 64 | 36 | 36 |
| One group of compound | 47 | 47 | 53 | 53 |
| Two groups of compound | 40 | 40 | 60 | 60 |
| Three groups of compound | 43 | 43 | 57 | 57 |
| Four groups of compound | 48 | 48 | 52 | 52 |
| Five groups of compound | 30 | 30 | 70 | 70 |
| Six groups of compound | 38 | 38 | 62 | 62 |
| Seven groups of compound | 24 | 24 | 76 | 76 |
| Eight groups of compound | 20 | 20 | 80 | 80 |
| Nine groups of compound | 10 | 10 | 90 | 90 |
It is visible according to the result of table three：
1st, when hexanicit in compound or the one of dose of Dipyridamole are fixed, as another medicine is to medicament
The rising of amount, therapeutic effect are better；
2nd, when the dosage of a composition in compound is identical with the dosage of the alone medicine, the therapeutic effect of compound is always big
In the therapeutic effect of single medicine, especially with (P ＜ 0.05 or P ＜ 0.01) when another Ingredient Amount increases in compound.
3rd, when two medicines take half amount of single pharmaceutical quantities in compound (five groups of compound), its therapeutic effect is better than wherein appointing
Therapeutic effect (hexanicit group or Dipyridamole group, P ＜ 0.01) during one single component full dose
Adverse reaction is observed：Administration group relatively has no obvious animal behavior difference, each master after animal execution with model group
Want the internal organs such as heart, liver, kidney, brain, spleen, lung, testis, intestine and small intestine, stomach etc. to be showed no the acute pathologies such as bleeding, scorching change to change,
The difference on other pathology is had no, does not also observe obvious side effect.
Conclusion：
When hexanicit in compound or the one of dose of Dipyridamole are fixed, with another medicine dosage
Rising, therapeutic effect is better, and either diastolic pressure or systolic pressure is not always the case；When hexanicit is double using maximum dose
The phonetic therapeutic effect up to the compound for not using lowest dose level will be weaker than hexanicit Dipyridamole use using lowest dose level
The compound of maximum dose, show that Ah's Dipyridamole plays bigger therapeutic action in compound；When hexanicit takes maximum
When, with the dosage increase of Dipyridamole, therapeutic effect increase, until hexanicit and Dipyridamole get maximum dose
When, mass effect is best.Vice versa.In terms of comprehensive, this compound maximum therapy effect is more than the treatment of two compositions in compound
Effect sum.
As can be seen here, either hexanicit or Dipyridamole, the two compound formed are equal to treatment arterial embolism
By optimal effectiveness, better than respective single preparations of ephedrine；And compound preparation its will not bring extra side effect or adverse reaction,
The difference in side effect and adverse reaction will not be brought.Show that the compound preparation that hexanicit and Dipyridamole are formed not only has
There is a bigger therapeutic effect, and using being above safe.
As described above, it can preferably realize the present invention.
Claims (5)
- A kind of 1. drug compound preparation for treating arterial embolism, it is characterised in that by weight, including 10~300 parts of nicotinic acid Mesoinositol, 10~120 parts of Dipyridamoles and 10~1600 parts of pharmaceutical carriers, the hexanicit and Dipyridamole conduct Drug ingedient mixes with pharmaceutical carrier forms compound preparation.
- 2. a kind of drug compound preparation for treating arterial embolism according to claim 1, it is characterised in that by weight Meter, the pharmaceutical carrier is 100~120 inert solids or 160~1000 parts of inert fluids.
- 3. a kind of drug compound preparation for treating arterial embolism according to claim 2, it is characterised in that the inertia is consolidated Body is excipient, disintegrant, lubricant, cosolvent, flavouring, one kind in adhesive or above-mentioned a variety of formed with arbitrary proportion Mixture.
- A kind of 4. drug compound preparation for treating arterial embolism according to claim 2, it is characterised in that the inert liquid Body is the mixture that diluent, wetting agent, one kind in additive or above two are formed with arbitrary proportion.
- A kind of 5. drug compound preparation for treating arterial embolism according to any one of Claims 1-4, it is characterised in that The formulation of the compound preparation includes tablet, capsule, granula, supensoid agent and syrup.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710830538.9A CN107550912A (en) | 2017-09-15 | 2017-09-15 | A kind of drug compound preparation for treating arterial embolism |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710830538.9A CN107550912A (en) | 2017-09-15 | 2017-09-15 | A kind of drug compound preparation for treating arterial embolism |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107550912A true CN107550912A (en) | 2018-01-09 |
Family
ID=60981055
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710830538.9A Withdrawn CN107550912A (en) | 2017-09-15 | 2017-09-15 | A kind of drug compound preparation for treating arterial embolism |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107550912A (en) |
-
2017
- 2017-09-15 CN CN201710830538.9A patent/CN107550912A/en not_active Withdrawn
Non-Patent Citations (2)
| Title |
|---|
| 李宏建: "双嘧达莫预防血栓形成的作用——治疗和预防卒中的实际意义", 《国际脑血管病杂志》 * |
| 郁富顺等: "烟酸肌醇酯防治腿抽筋", 《2010年中国药学大会暨第十届中国药师周论文集》 * |
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Application publication date: 20180109 |