CN102552355B - Pharmaceutical composition for treating hypertension - Google Patents
Pharmaceutical composition for treating hypertension Download PDFInfo
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- CN102552355B CN102552355B CN201210052411.6A CN201210052411A CN102552355B CN 102552355 B CN102552355 B CN 102552355B CN 201210052411 A CN201210052411 A CN 201210052411A CN 102552355 B CN102552355 B CN 102552355B
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- levamlodipine
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- officinal salt
- dogbane leaf
- hypertension
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Abstract
The invention discloses a pharmaceutical composition for treating hypertension. The pharmaceutical composition comprises Levoamlodipine or a pharmaceutically-acceptable salt and dogbane leaf extracts. The pharmaceutical composition has a good therapeutic effect on hypertension and has less adverse effects.
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 dogbane leaf extractive, and the application of this compositions in preparation 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 world hypertension alliance 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 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, the cardiovascular and cerebrovascular disease death toll that the hypertension etc. of take is representative accounts for 36% of total death toll ratio, therefore improve the understanding of the people to hypertension, early prevention, treatment are in time had to extremely important meaning.
Levamlodipine is the first chiral separation antihypertensive drug in the first chiral separation optical voidness medicine ，Ye Shi of China 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, slight diuresis; prevention coronary heart disease, myocardial infarction and apoplexy; can also partly reverse abnormal blood circadian, slight antiplatelet, resists myocardial ischemia; arrhythmia, increases insulin sensitivity and certain effects such as 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, also may cause Secondary cases norepinephrine and epinephrine increases and makes increased heart rate and have headache, the untoward reaction such as blush, be the reason of quite a few patient's drug withdrawal, be subject to clinically certain restriction.
Herba Apocyni veneti another name ambary, bluish dogbane, red building, Gaster caprae seu Ovis draw angle etc.Be the most characteristic a kind of fibre plant in the Northwest, be distributed widely in Zhong，Yin Lop Nur, desert, Xinjiang Tianshan south and gain the name, in Chinese Huaihe River, the Qinling Mountains, to the north of Kun Lun Mountain each province (autonomous region) also have distribution.Herba Apocyni veneti has alkalescence, can balance human body acid-base, supplement calcium magnesium plasma trace element, and be the incomparable Chinese herbal medicine of other medicines.Herba Apocyni veneti cold nature, bitter but sweet flavor, can resolving heat and reducing pathogenic fire, and suppressing the hyperactive liver to relieve the wind syndrome cures mainly the diseases such as headache, dizzy, insomnia.In the national antiaging agent seminar that the eighties in last century, Chinese Pharmaceutical Association was held, with regard to the research of Folium Apocyni Veneti, carried out academic exchange, according to Beijing planning commission, two Herba Apocyni veneti research cooperative groups of the leader of Jiangsu Province planning commission, Chinese Pharmaceutical Association, Shanghai Pharmaceutical Inst., Chinese Academy of Sciences, Chinese Academy of Sciences's northwest Institute of Zoology, academy of traditional Chinese medicine institute of materia medica, the units such as institute of Materia Medica,Chinese Academy of Medical Sciences and Shaanxi, Beijing, Shanghai, clinical experimental study and the documents and materials of the medical relevant unit such as Nanjing prove, Folium Apocyni Veneti contains a large amount of flavone, triterpene, organic acid, the chemical analysis such as aminoacid, further studying flavone chemical constitution is Quercetin and isoquercitrin, its pharmacological action has blood pressure lowering, blood fat reducing, increase coronary flow, to hypertension, hyperlipidemia, there is good curative effect, especially to dizzy symptom, improving sleep quality has positive effect, has the immunity of enhancing simultaneously, preventing cold, antiasthmatic-antitussive, eliminate depressed, the skin care of invigorating blood circulation, relieving alcoholism and protecting the liver, degraded tobacco poisoning, vessel softening, the effects such as relieving constipation diuresis, however bradycardic side effect aspect heart, had.
Summary of the invention
One object of the present invention is to provide a kind of hypertensive pharmaceutical composition that is used for the treatment of, and this pharmaceutical composition is comprised of the Levamlodipine of effective dose or its officinal salt and dogbane leaf extractive.
Described Levamlodipine officinal salt is one or more in benzene sulfonate, mesylate, acetate, aspat, tartrate, maleate, sulfate, hydrochlorate or hydrobromate.
Described Levamlodipine can make by several different methods, method such as CN00102701.8 and CN03821593.4 record, generating on the basis of Levamlodipine, using conventional acid-base neutralization reaction to make stable Levamlodipine officinal salt.
Described dogbane leaf extractive prepares by the following method:
(1) Folium Apocyni Veneti is ground into 100 object medicated powder;
(2), in lidded container, Folium Apocyni Veneti medicated powder is soaked in 50% ethanol of 6 times of raw material weights to 2 hours;
(3) after having soaked, reflux, extract, 3 times;
(4) after having extracted, merge extractive liquid,, concentrating under reduced pressure, concentrated solution, through-25 ℃ of vacuum lyophilizations, obtains dogbane leaf extractive.
In described pharmaceutical composition, take the Levamlodipine of Levamlodipine or the weight ratio of its officinal salt and dogbane leaf extractive is 1:(10/3-1000), 1:(80-320 preferably).
The present invention also provides the method for preparing aforementioned pharmaceutical compositions, specifically Levamlodipine or its officinal salt is mixed with dogbane leaf extractive.
In described pharmaceutical composition per unit preparation, active ingredient content is: Levamlodipine or its officinal salt content of Levamlodipine of take is 1.0-30mg; Herba Apocyni veneti extract content is 100-1000mg.Preferably, take Levamlodipine or its officinal salt content of Levamlodipine is 2.5-5mg; Herba Apocyni veneti extract content is 400-800mg.
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.
Pharmaceutical composition of the present invention can be used for treating hypertension.
The present invention also further provides the application of aforementioned pharmaceutical compositions in the hypertensive medicine of preparation treatment.
The present invention also provides a kind of hypertensive method for the treatment of, and the method is by Levamlodipine or its officinal salt and dogbane leaf extractive drug combination.
Positive progressive effect of the present invention is: the present invention, by Levamlodipine or its officinal salt and dogbane leaf extractive drug combination, has good Synergistic Hypotensive Effects each other.Moreover, the diuretic properties of dogbane leaf extractive can reduce the edema side effect that Levamlodipine causes retention of sodium and water, Levamlodipine makes the interaction energy of increased heart rate offset the bradycardic side effect that dogbane leaf extractive causes heart, single survival dose of both pharmaceutical compositions is few, reduced the untoward reaction that single medicine heavy dose causes, patient's compliance is good, can also reduce the incidence rate of cardiocerebrovasculaevents events, improves 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 Folium Apocyni Veneti is purchased from the large pharmacy of Kang Qian.
Dogbane leaf extractive used in the following example all prepares by the following method:
Folium Apocyni Veneti is ground into 100 object medicated powder;
In lidded container, Folium Apocyni Veneti medicated powder is soaked in 50% ethanol of 6 times of raw material weights to 2 hours;
After immersion completes, reflux, extract, 3 times;
After extraction completes, merge extractive liquid,, concentrating under reduced pressure, concentrated solution, through-25 ℃ of vacuum lyophilizations, obtains dogbane leaf extractive.
Embodiment 1
Take Levamlodipine besylate (in Levamlodipine) 3mg, dogbane leaf extractive 3000mg, mix homogeneously, makes pharmaceutical composition 1.
Embodiment 2
Take Levamlodipine besylate (in Levamlodipine) 90mg, Herba Apocyni veneti extract 300mg, mix homogeneously, makes pharmaceutical composition 2.
Embodiment 3
Take Levamlodipine besylate (in Levamlodipine) 7.5mg, Herba Apocyni veneti extract 2400mg, mix homogeneously, makes pharmaceutical composition 3.
Embodiment 4
Take Levamlodipine besylate (in Levamlodipine) 15mg, Herba Apocyni veneti extract 1200mg, mix homogeneously, makes pharmaceutical composition 4.
Embodiment 5
Take Levamlodipine besylate (in Levamlodipine) 12mg, Herba Apocyni veneti extract 1800mg, mix homogeneously, makes pharmaceutical composition 5.
Embodiment 6
Experimental technique: get healthy spontaneously hypertensive SHR rat (source: 100 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 Table 1) of blood pressure height equilibrium, adopt gastric infusion, for blood pressure, adopt rat electronic sphygmomanometer, systolic pressure during the clear-headed peace and quiet of tail volumetric method indirect determination rat, before medication, after medication, arteria caudalis systolic pressure mensuration is carried out at surrounding end respectively.
Table 1: group technology
Note: Levamlodipine besylate weight is in Levamlodipine
Press above-mentioned dosage gavage every day 1 time, start Measure blood pressure before administration, each organizes continuous gavage 4 weeks, and each group is fed with standard feed.Every morning, 9 employing rat electronic sphygmomanometers were measured rat blood pressure, and calculating mean value, specifically in Table 2.
Table 2: on the impact of blood pressure (n=10)
A compares p < 0.01 with model group; B compares with A group, p < 0.01; C compares with B group, p < 0.05; D compares with C group, p < 0.05; E compares with D group, p < 0.01.
Conclusion: to sum up state experiment known, Levamlodipine besylate is used Levamlodipine besylate and uses separately the successful of dogbane leaf extractive than independent with the pharmaceutical composition of dogbane leaf extractive, illustrate that Levamlodipine besylate combines with dogbane leaf extractive to use and have obvious synergism, be better than the curative effect of two kinds of medicines when alone.
Claims (3)
1. one kind is used for the treatment of hypertensive pharmaceutical composition, it is characterized in that it is comprised of Levamlodipine or its officinal salt and dogbane leaf extractive, wherein, described Levamlodipine officinal salt is benzene sulfonate, mesylate, acetate, aspat, tartrate, maleate, sulfate, hydrochlorate or hydrobromate, and the weight ratio of Levamlodipine or its officinal salt and dogbane leaf extractive is 1:10/3-1000.
2. pharmaceutical composition according to claim 1, the weight ratio that it is characterized in that Levamlodipine or its officinal salt and dogbane leaf extractive is 1:80-320.
3. the application of pharmaceutical composition in the hypertensive medicine of preparation treatment described in claim 1-2 any one.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201210052411.6A CN102552355B (en) | 2012-03-02 | 2012-03-02 | Pharmaceutical composition for treating hypertension |
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| CN201210052411.6A CN102552355B (en) | 2012-03-02 | 2012-03-02 | Pharmaceutical composition for treating hypertension |
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| CN102552355B true CN102552355B (en) | 2014-01-29 |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1748723A (en) * | 2004-09-16 | 2006-03-22 | 新疆医科大学 | Poacynum hendersonii woodson leaf extract and blood fat reducing nfunction of two chemical component in it |
| CN102276516A (en) * | 2011-08-19 | 2011-12-14 | 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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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN102217882A (en) * | 2011-03-17 | 2011-10-19 | 上海韬鸿化工科技有限公司 | Chinese medicinal pillow for preventing high blood pressure |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1748723A (en) * | 2004-09-16 | 2006-03-22 | 新疆医科大学 | Poacynum hendersonii woodson leaf extract and blood fat reducing nfunction of two chemical component in it |
| CN102276516A (en) * | 2011-08-19 | 2011-12-14 | 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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| CN102552355A (en) | 2012-07-11 |
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Granted publication date: 20140129 Termination date: 20170302 |