CN1768763A - Compound breviscapine pills - Google Patents
Compound breviscapine pills Download PDFInfo
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- CN1768763A CN1768763A CNA2004100678567A CN200410067856A CN1768763A CN 1768763 A CN1768763 A CN 1768763A CN A2004100678567 A CNA2004100678567 A CN A2004100678567A CN 200410067856 A CN200410067856 A CN 200410067856A CN 1768763 A CN1768763 A CN 1768763A
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Abstract
The invention discloses a compound Chinese medicinal drop pill containing active constituent of Breviscapine, which comprises the following constituents (by weight percentage): Breviscapine active component 1 part, musk 0.5-3 parts, borneol 0.5-5 parts, and pharmaceutically acceptable medicinal carrier or adjuvant.
Description
Technical field
The present invention relates to a kind of Chinese traditional compound medicine for the treatment of cardiovascular and cerebrovascular disease, relate in particular to a kind of compound breviscapine pills.
Background technology
Cardiovascular and cerebrovascular disease is commonly encountered diseases, frequently-occurring disease, is the first human killer.Wherein, the cardiovascular diseases seizes 1,200 ten thousand people's life every year, near 1/4 of the total death of world population, becomes the No.1 formidable enemy of human health.Although the most countries of cardiovascular death rate except that East Bloc all has decline in various degree over nearly 30 years, but still be majority state primary cause of death of male more than 45 years old, in the women then is second cause of the death that is only second to tumor, is having a strong impact on human life expectancy and life quality.Therefore, the medicine of treatment cardiovascular and cerebrovascular disease is human research's a important topic, as Chinese patent application: 01117620.2, its main component comprises: the pharmaceutic adjuvant of the solubilizing composition of breviscapine, blocker and surplus etc., it is good that this Breviscapine slow release preparation has a medicine-releasing performance to the treatment cardiovascular and cerebrovascular disease, and blood drug level is characteristics stably.But its defective is arranged equally, still there is problem such as be absorbed by the body relatively slowly, bioavailability is lower, onset is not fast in effective ingredient breviscapine wherein, this has the disease of sudden characteristic for this class of cardiovascular and cerebrovascular disease, and its curative effect still is unfavorable.
Summary of the invention
For overcoming above-mentioned defective, have according to cardiovascular and cerebrovascular disease chronic, sudden, but characteristics such as causing death when serious need that development is a kind of not only to have can be used for rescuing but also do not influence the daily medicine of taking.The technical issues that need to address of the present invention are: the compound breviscapine pills that a kind of treatment cardiovascular and cerebrovascular disease of quick acting is provided, when strengthening drug effectiveness, promote breviscapine to be absorbed rapidly, improve drug bioavailability, and facilitate patients and carry by human body.
For solving described technical problem, the technical measures that the present invention taked are: a kind of compound breviscapine pills, it is characterized in that forming (weight ratio): 1 part of breviscapine by following drug regimen, 0.5～3 part in Moschus, Borneolum Syntheticum 0.5-5 part, mix with pharmaceutically acceptable pharmaceutical carrier or adjuvant, make compound dripping pill.Breviscapine is the active component of Herba Erigerontis, presses dry product and calculates, and contains lamp-dish flower acetic (C
21H
18O
12) must not be less than 95%, have blood circulation promoting and blood stasis dispelling, the effect of removing obstruction in the collateral to relieve pain.Can be used for treating diseases such as coronary heart disease, angina pectoris, apoplexy sequela.Moschus is the secretions in the male pod of Moschus section animal (glandular sac), have stronger have one's ideas straightened out logically close effect, be applicable to that epidemic febrile disease heat attacking the pericardium coma convulsion faints and the apoplexy syncope due to accumulation of phlegm, excess syndrome of stroke such as infantile convulsion are the key medicine of refreshment analepsia, and can promoting the circulation of blood divide stagnating, blood circulation promoting and dispersing pathogen accumulation is arranged, the effect of reducing swelling and alleviating pain.The compatibility Moschus has utilized this effect of Moschus refreshment analepsia just in compound breviscapine pills, makes acute patient in the very first time " refreshment analepsia ", and the utilize Moschus simultaneously blood circulation promoting and dispersing pathogen accumulation that is had, the effect of reducing swelling and alleviating pain strengthened the effect of drop pill.Borneolum Syntheticum is the processed goods of Dipterocarpaceae aiphyllium XIANGSHU resin, has again with the feverfew Herba Blumeae Balsamiferae to be the Blumeae preparatum Tabellae made of raw material and to be the BORNEOLUM SYNTHETICUM that raw material is made with the Oleum Terebinthinae, contains C
10H
18O should be greater than 55%.Borneolum Syntheticum is a drugs of causing resuscitation by administering aromatic drugs, has the effect of the refreshment of having one's ideas straightened out, clearing away heat to alleviate pain, finds to have the effect of " fragrance is walked to scurry, priming up " after deliberation.Generally speaking, the blood drug level of medicine in cerebral tissue is lower, and this is because due to the blood brain barrier.If medicine can not pass through blood brain barrier, cerebral tissue just is difficult to reach effective blood drug level, thereby can't play a role.Borneolum Syntheticum not only self can pass through blood brain barrier, can also increase blood brain barrier permeability, impel other drug to enter cerebral tissue by blood brain barrier.Compound breviscapine pills has utilized this effect " priming is up " of Borneolum Syntheticum just, impel breviscapine, Moschus to arrive diseased region by blood brain barrier, improved the speed of medicine arrival diseased region, strengthened the curative effect of medicine, this meets the treatment requirement of cardiovascular and cerebrovascular disease fully.Generally speaking, cardiovascular and cerebrovascular disease belongs to chronic disease, has paroxysmal characteristics when only showing effect, and the inducement of its outbreak is more, and happiness, anger, grief and joy are exactly inducement sometimes.And in compound breviscapine pills compatibility Moschus, Borneolum Syntheticum, the people who suffers from cardiovascular and cerebrovascular disease just can be its preventive drug as its seizure of disease of control, utilize the pharmacology synergism of flavour of a drug, prevention and treatment cardiovascular and cerebrovascular disease reduce the chance that cardiovascular and cerebrovascular disease shows effect.Three medicine compatibilities both can remedy single pharmaceutical treatment cardiovascular and cerebrovascular disease effect defect of insufficient, coordinated again medicine between pharmacological action.And, compare relative minimizing dosage with single medicinal material, be to bring out the best in each other.The ingredient that said preparation contained that compound breviscapine pills of the present invention is not only clear and definite gives the proportion compatibility of three kinds of medicines, has solved controllability, safety, the validity problem of medicine preferably.
As preferably, described compound breviscapine pills is characterized in that forming (weight ratio) by following drug regimen: 1 part of breviscapine, 0.8～2 part in Moschus, 0.8～3 part of Borneolum Syntheticum are mixed and made into compound dripping pill with pharmaceutically acceptable pharmaceutical carrier or adjuvant.
As best proportioning, described compound breviscapine pills is characterized in that forming (weight ratio) by following drug regimen: 1 part of breviscapine, 1.2 parts in Moschus, 1.5 parts of Borneolum Syntheticums are mixed and made into compound dripping pill with pharmaceutically acceptable pharmaceutical carrier or adjuvant.
Described pharmaceutical carrier can be Macrogol 4000, polyethylene glycol 6000, poloxamer, sodium stearate, glyceryl monostearate, hydrogenated vegetable oil, glycerin gelatine etc.
On the other hand, according to the animal contrast experiment, its result has dependency, zoopery result such as table 1, Fig. 1.
As can be seen from Table 1, the SD survival of rats rate of irritating stomach water and single breviscapine is similar substantially, P＞0.05, and use the SD survival of rats rate of compound breviscapine pills to compare obvious rising for two groups with the front.
As can be seen from Figure 1, irritate in the mice plasma of stomach single medicinal material breviscapine
14Phase area under a curve and irritating in stomach compound breviscapine pills mice plasma during C concentration
14The ratio of phase area under a curve during C concentration shows that the bioavailability of compound breviscapine pills is obviously higher.
1, randomly draw 450 SD rats through the heart ligation operation and be divided into three groups, wherein 150 as model; Irritate stomach single medicinal material breviscapine, 40mg/kg for 150; Irritate the breviscapine drop pills that stomach grinds, 40mg/kg for other 150.Through behind the fortnight, the survival number (rate) of SD rat sees Table 1
Table 1: different pharmaceutical and SD Rats survival rate
| Group | Medicine (kind) | Example number (n) | Survival number (%) |
| I II III | Water single breviscapine compound breviscapine pills | 150 150 150 | 8(5.33％) 17(11.3％) 103(68.7％) |
Annotate: I group and II group be X relatively
2=0.0026, p＞0.05; I group and III organize the X that compares
2=129.0, p＜0.01; II group and III organize the X that compares
2=102.7, p＜0.01; Illustrate that I group and II group do not have too big difference, between I group and the III group very big difference is arranged, between II group and the III group very big difference is arranged also.
2, randomly draw 200 kunming mices, wherein irritate stomach usefulness for 100
14C is as the single medicinal material breviscapine of tracer labelling, and other 100 irritate stomach uses
14C is as the compound breviscapine pills of tracer labelling.One of the sacrificed by decapitation mice respectively every one hour is collected blood and detects.As shown in Figure 1, with the time as abscissa, map as vertical coordinate with the drug level in the blood plasma.Wherein AUC1 represent measure and irritate in the stomach single medicinal material breviscapine mice plasma
14Phase area under a curve during C concentration, AUC2 represent measure and irritate in the stomach compound breviscapine pills mice plasma
14Phase area under a curve during C concentration, resulting ratio are relative bioavailability between the two.
From above result of the test as can be seen, compound breviscapine pills has pharmacodynamics effect preferably.Therefore, it is clear and definite that the present invention has active constituent content, and pharmaceutical preparation safety, effective, controlled characteristics are that a kind of compatibility is better, can be used for preventing and treating the compound dripping pill of cardiovascular and cerebrovascular disease.
Description of drawings
Accompanying drawing 1 is a blood plasma tracer of the present invention
14Phase area under a curve (AUC) reflection absorbance sketch map during C concentration.
The specific embodiment
Below by embodiment and associative list 2, technical scheme of the present invention is described in further detail.
Table 2: compound breviscapine pills prescription unit: gram
| Prescription | Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Embodiment 5 | Embodiment 6 |
| The fragrant borneol Macrogol 4000 of Breviscapinun She Macrogol 6000 poloxamer odium stearate single stearic acid glycerine | 20 10 100 80 | 20 20 60 50 20 | 20 60 10 60 | 20 16 60 80 | 20 20 40 50 20 | 20 40 16 20 60 |
Embodiment 1:
Prescription: breviscapine 20g
Moschus 10g
Borneolum Syntheticum 100g
Macrogol 4000 80g
Make 5000
Preparation method: get the Macrogol 4000 of recipe quantity, fusion; It is an amount of to get dehydrated alcohol, adds breviscapine, Moschus, Borneolum Syntheticum, and stirring makes molten; With medicinal liquid and fused Macrogol 4000 mixing, continue to stir, fling to ethanol, place the drop pill machine of preheating, 90 ℃ of insulations are dripped as coolant with methyl-silicone oil and to be made ball, promptly.Example 2, example 3 make with method.Every day secondary, 2～4 of each buccal, or take during first aid.
Embodiment 4:
Prescription: breviscapine 20g
Moschus 16
Borneolum Syntheticum 60g
Sodium stearate 80g
Make 5000
Preparation method: get the sodium stearate of recipe quantity, fusion; It is an amount of to get dehydrated alcohol, adds breviscapine, Moschus, Borneolum Syntheticum, and stirring makes molten; With medicinal liquid and stearic acid fusing sodium mixing, continue to stir, fling to ethanol, place the drop pill machine of preheating, 88 ℃ of insulations are dripped as coolant with methyl-silicone oil and to be made ball, promptly.Example 5, example 6 make with method.Every day secondary, 2～4 of each buccal, or take during first aid.
Embodiment 7:
Prescription: breviscapine 20g
Moschus 24g
Borneolum Syntheticum 30g
Macrogol 4000 50g
Poloxamer 20g
Make 5000
Preparation method: get the Macrogol 4000 and the poloxamer of recipe quantity, fusion; It is an amount of to get dehydrated alcohol, adds breviscapine, Moschus, Borneolum Syntheticum, and stirring makes molten; With medicinal liquid and fused Macrogol 4000 and poloxamer mixing, continue to stir, fling to ethanol, place the drop pill machine of preheating, 85 ℃ of insulations are dripped as coolant with methyl-silicone oil and to be made ball, promptly.Every day secondary, 2～4 of each buccal, or take during first aid.
Claims (6)
1, a kind of compound breviscapine pills is characterized in that being formed and being by weight by following drug regimen: 1 part of breviscapine, 0.5～3 part in Moschus, 0.5～5 part of Borneolum Syntheticum, mix with pharmaceutically acceptable pharmaceutical carrier or adjuvant, and make compound dripping pill.
2, compound breviscapine pills according to claim 1, it is characterized in that forming and being by weight: 1 part of breviscapine, 0.8～2 part in Moschus, 0.8～3 part of Borneolum Syntheticum by following drug regimen, mix with pharmaceutically acceptable pharmaceutical carrier or adjuvant, make compound dripping pill.
3, compound breviscapine pills according to claim 1, it is characterized in that forming and being by weight: 1 part of breviscapine, 1.2 parts in Moschus, 1.5 parts of Borneolum Syntheticums by following drug regimen, mix with pharmaceutically acceptable pharmaceutical carrier or adjuvant, make compound dripping pill.
4, compound breviscapine pills according to claim 1 and 2 is characterized in that described pharmaceutical carrier can be one or both in Macrogol 4000, polyethylene glycol 6000, the poloxamer.
5, described compound breviscapine pills according to claim 3 is characterized in that described pharmaceutical carrier can be one or both in Macrogol 4000, polyethylene glycol 6000, the poloxamer.
6,, it is characterized in that described pharmaceutical carrier can be one or both in sodium stearate, glyceryl monostearate, the glycerin gelatine according to claim 1 or 2 or 3 described compound breviscapine pills.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100678567A CN100525780C (en) | 2004-11-02 | 2004-11-02 | Compound breviscapine pills |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100678567A CN100525780C (en) | 2004-11-02 | 2004-11-02 | Compound breviscapine pills |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1768763A true CN1768763A (en) | 2006-05-10 |
| CN100525780C CN100525780C (en) | 2009-08-12 |
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ID=36750468
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2004100678567A Expired - Fee Related CN100525780C (en) | 2004-11-02 | 2004-11-02 | Compound breviscapine pills |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106806581A (en) * | 2015-11-30 | 2017-06-09 | 湖南恒生制药股份有限公司 | A kind of Chinese patent drug containing Breviscapinun |
-
2004
- 2004-11-02 CN CNB2004100678567A patent/CN100525780C/en not_active Expired - Fee Related
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106806581A (en) * | 2015-11-30 | 2017-06-09 | 湖南恒生制药股份有限公司 | A kind of Chinese patent drug containing Breviscapinun |
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| Publication number | Publication date |
|---|---|
| CN100525780C (en) | 2009-08-12 |
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Granted publication date: 20090812 Termination date: 20101102 |