CN102716370B - Pharmaceutical composition and application thereof - Google Patents
Pharmaceutical composition and application thereof Download PDFInfo
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- CN102716370B CN102716370B CN201210230643.6A CN201210230643A CN102716370B CN 102716370 B CN102716370 B CN 102716370B CN 201210230643 A CN201210230643 A CN 201210230643A CN 102716370 B CN102716370 B CN 102716370B
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- stigma maydis
- levamlodipine
- pharmaceutical composition
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- hypertension
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Abstract
The invention provides a pharmaceutical composition applied for preparing prevention or treatment of hypertension, which consists of levoamlodipine or medicinal salt thereof and a corn silk extract. The pharmaceutical composition is better in treatment effect on hypertension and is low in side effect.
Description
Technical field
The present invention relates to field of medicaments, relate in particular to a kind of compositions being formed by Levamlodipine or its officinal salt and Stigma Maydis extract, and the application of this compositions in preparation prevention or treatment hypertension drug.
Technical background
Hypertension is common cardiovascular system chronic disease, and at present the whole world there is no effective radical cure method, once ill need take medicine all the life, serious harm human health.Within 2009, chairman professor Liu Lisheng of hypertension alliance of the world points out: " China has 19% adult to suffer from hypertension, and number of patients reaches 2.2 hundred million, still has every year 1000 ten thousand newly-increased patients simultaneously ".Hypertension can cause the infringement of the organs such as the heart, brain, kidney, and has close relationship with sugar, lipid metabolic disorder and diabetes, obviously reduces patient's quality of life, and when serious, even entail dangers to arrives patient's life.And a large amount of internal authority hypertension clinical researches show to strengthen blood pressure lowering dynamics, actively, make enduringly hyperpietic's blood pressure be down to 130/85 millimetres of mercury following (it is following that the best should be down to 120/80 millimetres of mercury), the target organ damages such as the heart and brain kidney that alleviating hypertension causes effectively, reduce or postpone the generation of the complication such as apoplexy, coronary heart diseases and angina pectoris, myocardial infarction, renal failure, atherosclerosis, aneurysm, reduce cardiocerebrovasculaevents events rate, mortality rate and disability rate, improve patients ' life quality, extend patient's life-span.Necrology according to the World Health Organization (WHO) to global various diseases, account for 36% of total death toll ratio take hypertension etc. as the cardiovascular and cerebrovascular disease death toll of representative, therefore improve the understanding of the people to hypertension, early prevention, treatment are in time had to extremely important meaning.
Levamlodipine is China's the first chiral separation optical voidness medicine, and the first chiral separation antihypertensive drug in the Ye Shi world is a kind of long-acting, alkaline dihydropyridine calcium ion antagonist.Can make by several different methods, referring to document CN00102701.8 and CN03821593.4.It works by a kind of site being connected with dihydropyridine (N site) on cell, and retardance calcium ion cross-film enters cardiac muscle and vascular smooth muscle cell, makes smooth muscle loosening, and vascular resistance declines, and reduces blood pressure.The Levamlodipine that at present clinical experiment evidence shows therapeutic dose is atomic or do not have to cardiac contractile force and Atrioventricular Conduction effect, is the medicine to sympathetic activation effect minimum in calcium ion antagonist.It can also treat the hypertension of heart failure; reverse ventricular hypertrophy; improve the lax function of diastole; renal function protecting, prevention coronary heart disease, myocardial infarction and apoplexy, can also partly reverse abnormal blood circadian; slight antiplatelet; resist myocardial ischemia, arrhythmia, increases the effects such as insulin sensitivity and certain atherosclerosis.But Levamlodipine can be because the higher easy initiation retention of sodium and water of using dosage causes edema in blood pressure lowering process, and this is the reason of quite a few patient's drug withdrawal, has been subject to clinically certain restriction.
Stigma Maydis is the zeistic style of grass and stigma, has another name called maize palpus, five chinese sorghum stamens, ear of maize hair.Stigma Maydis fatty oily 2.5%, volatile oil 0.12%, tree gelatinoid 3.8%, resin 2.7%, bitterness glucoside 1.15%, Saponin 3.18%, alkaloid 0.05%, also, containing cryptoxanthine, vitamin C, pantothenic acid, inositol, vitamin K, sitosterol, stigmasterol, malic acid, citric acid, tartaric acid, oxalic acid, potassium nitrate and a-give birth to quinone.The traditional Chinese medical science is thought Stigma Maydis, sweet flat, can inducing diuresis to remove edema, expel the heat-evil, and suppressing the hyperactive liver function of gallbladder promoting, can also antiallergic, treatment nephritis, edema, hepatitis, hypertension, cholecystitis, cholelithiasis, diabetes, sinusitis, mastitis etc.Stigma Maydis has diuresis, can increase chloride output, and its diuresis is the outer property of kidney, so the edema that a variety of causes is caused has certain curative effect, although it can be used for the treatment of chronic nephritis or nephrotic syndrome, effect is not too strong; Stigma Maydis has dilating effect to peripheral vessel, so there is weak hypotensive effect; Stigma Maydis can promote bile excretion, so can be used as choleretic for there is no the chronic cholecystitis of complication or the cholangitis of bile discharge obstacle; Because Stigma Maydis can accelerate Blood Coagulation Process, improve number of platelets, can anti-hemolysis, so can be used as the hemorrhage diuretic of holding concurrently, be applied to bladder and lithangiuria, can also be used for acute hemolytic anemia.Because it has anti-allergic effects, so also can be used for the treatment of urticaria and asthma etc.; Meanwhile, the function of detoxification of Stigma Maydis can also be used to treat mastitis etc.
Summary of the invention
One object of the present invention is to provide a kind of pharmaceutical composition, and this pharmaceutical composition is made up of the Levamlodipine of effective dose or its officinal salt and Stigma Maydis extract; Wherein, the officinal salt of described Levamlodipine is one or more in benzene sulfonate, mesylate, acetate, aspat, tartrate, maleate, sulfate, hydrochlorate or hydrobromate.
Wherein said Stigma Maydis extract is that Stigma Maydis obtains through 50-70% alcohol reflux.
Wherein the weight ratio of Levamlodipine or its officinal salt and Stigma Maydis extract is 1:10/3-4000.
The weight ratio of preferred Levamlodipine or its officinal salt and Stigma Maydis extract is 1:200-1200.
Aforementioned pharmaceutical compositions of the present invention, can be directly mixed by Levamlodipine or its officinal salt and Stigma Maydis extract.
Pharmaceutical composition of the present invention can be used for prevention or treatment hypertension, and the present invention also provides aforementioned pharmaceutical compositions in preparation prevention or treated the application in hypertensive medicine.
Described Levamlodipine can make by several different methods, such as the method for CN00102701.8 and CN03821593.4 record, generating on the basis of Levamlodipine, using conventional acid-base neutralization reaction to make stable Levamlodipine officinal salt; Maybe can obtain by commercially available approach.
Specifically, described Stigma Maydis extract prepares by the following method:
(1) get Stigma Maydis and clean, dry, be ground into 100 object Stigma Maydis powder;
(2) in Stigma Maydis powder, add the alcohol reflux 3 times of the 50-70% weight ratio of 10 times of raw material weights, each 1 hour;
(3) after having extracted, merge extractive liquid,, concentrating under reduced pressure, concentrated solution, through-25 ℃ of vacuum lyophilizations, obtains Stigma Maydis extract.
In aforementioned pharmaceutical compositions per unit preparation, active ingredient content is: take the Levamlodipine of Levamlodipine or its officinal salt content as 1.0-30mg; Stigma Maydis extract content is 100-4000mg.Preferably, take the Levamlodipine of Levamlodipine or its officinal salt content as 2.5-5mg; Stigma Maydis extract content is 1000-3000mg.
Described pharmaceutical composition can add that pharmaceutically acceptable carrier is prepared into required dosage form, and dosage form can be the dosage forms such as tablet, pill, capsule, powder, injection.These dosage forms can be according to well known to a person skilled in the art method preparation.
Described pharmaceutical composition is preferably oral formulations, can also be controlled release form as slow release or fast dissolving dosage form, this controlled release preparation can be according to well known to a person skilled in the art method preparation.
The present invention also provides one to treat hypertensive method, and the method is by Levamlodipine or its officinal salt and Stigma Maydis extract drug combination.
Positive progressive effect of the present invention is: the present invention mixes Levamlodipine or its officinal salt with Stigma Maydis extract, be prepared into required pharmaceutical composition, and two kinds of main components have good Synergistic Hypotensive Effects each other.Moreover, the diuretic properties of Stigma Maydis extract reduces the edema side effect of Levamlodipine initiation retention of sodium and water, single survival dose of both pharmaceutical compositions is few, reduce the untoward reaction that single medicine heavy dose causes, patient's compliance is good, can also reduce the incidence rate of cardiocerebrovasculaevents events, improve patient's quality of life.
The specific embodiment
In the following example, Levamlodipine besylate is purchased from company limited of Levamlodipine Pharmaceutical group (Jilin), lot number 100805, and Stigma Maydis is purchased from rural market.
Stigma Maydis extract used in the following example all prepares by the following method:
Get Stigma Maydis and clean, dry, be ground into 100 object Stigma Maydis powder;
In Stigma Maydis powder, add 60% the alcohol reflux 3 times of 10 times of raw material weights, each 1 hour;
After extraction completes, merge extractive liquid,, concentrating under reduced pressure, concentrated solution, through-25 ℃ of vacuum lyophilizations, obtains Stigma Maydis extract.
Embodiment 1
Take Levamlodipine besylate (in Levamlodipine) 3mg, Stigma Maydis extract 12000mg, mix homogeneously, makes pharmaceutical composition 1.
Embodiment 2
Take Levamlodipine besylate (in Levamlodipine) 90mg, Stigma Maydis extract 300mg, mix homogeneously, makes pharmaceutical composition 2.
Embodiment 3
Take Levamlodipine besylate (in Levamlodipine) 7.5mg, Stigma Maydis extract 9000mg, mix homogeneously, makes pharmaceutical composition 3.
Embodiment 4
Take Levamlodipine besylate (in Levamlodipine) 15mg, Stigma Maydis extract 3000mg, mix homogeneously, makes pharmaceutical composition 4.
Embodiment 5
Take Levamlodipine besylate (in Levamlodipine) 9mg, Stigma Maydis extract 6000mg, mix homogeneously, makes pharmaceutical composition 5.
Embodiment 6
Experimental technique: get 100 of healthy spontaneously hypertensive SHR rats (source: pharmacology teaching and research room of pharmaceutical college of The 2nd Army Medical College), male and female half and half, body weight 200-240g, male and female rat is according to be divided into 10 groups (concrete group technology is in tables 1) of blood pressure height equilibrium, adopt gastric infusion, adopt rat electronic sphygmomanometer for blood pressure, systolic pressure when the clear-headed peace and quiet of tail volumetric method indirect determination rat, before medication, arteria caudalis systolic pressure mensuration is carried out at medication surrounding end respectively.
Table 1: group technology
Note: Levamlodipine besylate weight is in Levamlodipine
Press above-mentioned dosage gavage every day 1 time, before administration, start Measure blood pressure, respectively organize continuous gavage 4 weeks, feed with standard feed for each group.Every morning, 9 employing rat electronic sphygmomanometers were measured rat blood pressure, and calculating mean value, specifically in table 2.
Table 2: the impact (n=10) on blood pressure
A is and relatively p < 0.01 of model group; B is compared with A group, p < 0.01; C is compared with B group, p < 0.05; D is compared with C group, p < 0.01; E is compared with D group, p < 0.01.
Conclusion: to sum up state experiment known, Levamlodipine besylate and the pharmaceutical composition ratio independent use Levamlodipine besylate of Stigma Maydis extract and the successful of Stigma Maydis extract, illustrate that Levamlodipine besylate combines with Stigma Maydis extract to use and have obvious synergism, be better than the curative effect of two kinds of medicines when alone.
Claims (1)
1. prevent or treat a hypertensive pharmaceutical composition, it is characterized in that its Levamlodipine besylate by effective dose and Stigma Maydis extract form, the weight ratio of Levamlodipine besylate and Stigma Maydis extract is 1:200-1200; In above proportioning, the weighing scale that Levamlodipine besylate conversion is Levamlodipine, wherein, described Stigma Maydis extract is that Stigma Maydis obtains through 50-70% alcohol reflux.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210230643.6A CN102716370B (en) | 2012-07-04 | 2012-07-04 | Pharmaceutical composition and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210230643.6A CN102716370B (en) | 2012-07-04 | 2012-07-04 | Pharmaceutical composition and application thereof |
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| Publication Number | Publication Date |
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| CN102716370A CN102716370A (en) | 2012-10-10 |
| CN102716370B true CN102716370B (en) | 2014-07-02 |
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Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20100106145A (en) * | 2009-03-23 | 2010-10-01 | 씨제이제일제당 (주) | Pharmaceutical compositions and formulations containing s-(-)-amlodipine adifate and microcrystalline cellulose |
| KR101085169B1 (en) * | 2009-03-25 | 2011-11-18 | (주)켐트로스 | Process for separating the enantiomers of amlodipine |
| CN102028662B (en) * | 2009-09-30 | 2011-10-19 | 江西施美制药有限公司 | Levamlodipine besylate tablet, preparation process thereof and control method for relevant materials |
| CN101732688B (en) * | 2009-12-30 | 2011-09-14 | 宁波市鄞州奥胜生物科技有限公司 | Amlodipine-containing medicament |
| CN101785781B (en) * | 2010-03-16 | 2012-11-07 | 施慧达药业集团(吉林)有限公司 | Medicine combination of levoamlodipine or medicinal salt of levoamlodipine and auricularia auricula polysaccharide, and application thereof |
| CN101805284B (en) * | 2010-04-19 | 2011-09-28 | 海南美兰史克制药有限公司 | Method for preparing levamlodipine compound |
| EP2575757A1 (en) * | 2010-06-03 | 2013-04-10 | Mahmut Bilgic | Water soluble formulation comprising a combination of amlodipine and a statin |
| CN102048730A (en) * | 2010-12-10 | 2011-05-11 | 浙江昂利康制药有限公司 | Levamlodipine besylate composition and preparation method thereof |
| CN102225083B (en) * | 2011-06-20 | 2013-01-16 | 施慧达药业集团(吉林)有限公司 | Pharmaceutical composition for treating hypertension and hyperlipidemia, and application thereof |
| CN102276516B (en) * | 2011-08-19 | 2013-04-17 | 海南锦瑞制药股份有限公司 | Levamlodipine besylate crystals, preparation method thereof and brand-new medicinal composition containing crystals |
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