CN101785781A - Medicine combination of levoamlodipine or medicinal salt of levoamlodipine and auricularia auricula polysaccharide, and application thereof - Google Patents
Medicine combination of levoamlodipine or medicinal salt of levoamlodipine and auricularia auricula polysaccharide, and application thereof Download PDFInfo
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- CN101785781A CN101785781A CN 201010125583 CN201010125583A CN101785781A CN 101785781 A CN101785781 A CN 101785781A CN 201010125583 CN201010125583 CN 201010125583 CN 201010125583 A CN201010125583 A CN 201010125583A CN 101785781 A CN101785781 A CN 101785781A
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Abstract
The invention relates to a medicine combination of levoamlodipine or medicinal salt of the levoamlodipine and auricularia auricula polysaccharide, and the application thereof. Active components of the medicine combination include the levoamlodipine or the medicinal salt of the levoamlodipine and the auricularia auricula polysaccharide. The medicine combination of the invention is applicable to treating mixed hypertension and hyperlipidemia.
Description
Technical field
The present invention relates to comprise the compositions of Levamlodipine or its officinal salt and Auricularia polycose, and the application of this compositions in preparation treatment mixed type hypertension and hyperlipidemia medicine.
Technical background
In recent years, along with improving constantly and the change of diet structure, the increase of life stress, the increase of aging population of China's living standards of the people, the sickness rate of hypertension and hyperlipidemia has progressively trend of rising.Hypertension, hyperlipidemia can cause the heart, brain, angiopathys such as atherosclerosis, angina pectoris, myocardial infarction, cerebral infarction, renal damage, lead to grave consequences, so, pay close attention to hypertension, hyperlipidemia, to having very important significance of positive control cardiovascular and cerebrovascular disease, the monotherapy that can treat these two kinds of diseases simultaneously can improve patient's compliance.
Levamlodipine is China's the first chiral separation optical voidness medicine, it also is the first chiral separation antihypertensive drug in the world, it is a kind of long-acting, alkaline dihydropyridine calcium ion antagonist, it works by a kind of site that links to each other with dihydropyridine (N site) on the cell, the retardance calcium ion is striden film and is entered cardiac muscle and vascular smooth muscle cell, make smooth muscle loosening, vascular resistance descends, and brings high blood pressure down.At present the clinical experiment evidence Levamlodipine that shows therapeutic dose is atomic or do not have to cardiac contractile force and chamber conduction; it is to the medicine of sympathetic activation effect minimum in the 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 the unusual circadian rhythm of blood pressure rhythm and pace of moving things, slight antiplatelet resists myocardial ischemia; arrhythmia increases insulin sensitivity and certain effects such as atherosclerosis.
It is Mycophyta Basidiomycetes Auriculariaceae Auricularia plant that Auricularia [Auricularia auricula (L.ex Hook) Under wood] has another name called Auricularia, it is the medicinal and edible colloid fungus of China's preciousness, in the cultivation history in existing more than 1000 year of China, be the traditional health-care good product of China.Modern medicine worker has new discovery to the medical value of Auricularia, shows that as rabbit experiment Auricularia has blood fat reducing, anti-experimental character atherosclerosis and effects such as antithrombotic formation and anticoagulant; The anthroposcopy experiment shows that Auricularia has tangible blood fat reducing and effects such as antithrombotic formation and anticoagulant.Modern medicine study confirms that the important physiological function of Auricularia is all closely related with its polysaccharide component, and (β-LP) content obviously reduces can to make T-CHOL (TC), free cholesterol (FVCC), cholesterol ester (CnE), triglyceride (TG) and the beta lipoprotein of the higher fatty acid cholesterol feed mice of taking food as Auricularia polycose.Edible in addition Auricularia can reduce on an empty stomach and the level of post-prandial glycemia, increases secretion of insulin, and can increase the tolerance of diabetic mice to oral glucose; Wu and hole find that Auricularia polycose can reduce the blood glucose of the inductive diabetic mice of alloxan, and increase secretion of insulin.Auricularia polycose is except there being effects such as blood fat reducing, antithrombotic, anticoagulation, blood sugar lowering, and it also has effects such as the immunologic function of adjusting, defying age, antitumor.At present, do not find that Levamlodipine and Auricularia polycose unite the article and the patent of use.
Summary of the invention
One object of the present invention is to provide a kind of novel treatment mixed type hypertension and the pharmaceutical composition and the application thereof of hyperlipidemia, to reach the purpose that the associating result of use is better than independent result of use, can improve patient's compliance simultaneously.
Pharmaceutical composition of the present invention, its active component contain Levamlodipine or its officinal salt and Auricularia polycose.The molecular formula of described Levamlodipine is:
Described Levamlodipine pharmaceutical salts can be selected from benzene sulfonate, mesylate, acetate, aspat, tartrate, maleate, sulfate, hydrochlorate or the hydrobromate of Levamlodipine.
The molecular formula of the benzene sulfonate-Levamlodipine besylate of described Levamlodipine is:
Levamlodipine can make by several different methods, and such as the method for CN00102701.8 and CN03821593.4 record, on the basis that generates Levamlodipine, stable levo-amlodipine salt is made in the conventional acid-base neutralization reaction of utilization.
Described Auricularia polycose can make by reported method on the document, also can buy via the market approach.Auricularia polycose is that raw material adopts the combinative enzyme hydrolysis method to extract acquisition with Auricularia (Auricularia auricula) sporophore preferably, and combinative enzyme hydrolysis method extractive technique is a known technology, on a lot of documents report is being arranged all.
In the described pharmaceutical composition, be 1 in the Levamlodipine of Levamlodipine or the weight ratio of its officinal salt and Auricularia polycose: (0.2-400), preferred 1: (20-80).
Active ingredient content is in the described pharmaceutical composition per unit preparation: Levamlodipine or its officinal salt content in Levamlodipine are 1.0-30mg; Auricularia polycose content is 5-400mg.Preferably, Levamlodipine or its officinal salt content in Levamlodipine is 2.5-5mg; Auricularia polycose content is 100-200mg.
Also can contain proper quantity of medicinal auxiliary material in the described pharmaceutical composition, adjuvant can be selected from microcrystalline Cellulose, pregelatinized Starch, lactose, Sodium Hydroxymethyl Stalcs, magnesium stearate, Pulvis Talci etc., can also add acceptable diluent, binding agent, disintegrating agent, lubricant, coloring agent, correctives in an amount of other the pharmacy, the addition of pharmaceutic adjuvant is 1 as active component and pharmaceutic adjuvant weight ratio: 0.1-50 routinely.
Preferable, described pharmaceutical composition is an oral formulations, dosage form is optional from dosage forms such as solution, suspension, tablet, pill, capsule, powders.These dosage forms can be according to well known to a person skilled in the art the method preparation.
Described pharmaceutical composition can also be controlled release form such as slow release or fast dissolving dosage form, and this controlled release preparation can be according to well known to a person skilled in the art the method preparation.
The present invention also further discloses the application of aforementioned pharmaceutical compositions in preparation treatment mixed type hypertension and hyperlipidemia medicine.
Pharmaceutical composition of the present invention administration in any form is preferably oral administration, can also be the form administration of controlled release form.
In the described pharmaceutical composition, Levamlodipine or its officinal salt (in Levamlodipine) generally are the dosed administrations with 1.0-30mg/ days, are preferably 2.5-5mg/ days dosed administration.Auricularia polycose generally is the dosed administration with 5-400mg/ days, is preferably 100-200mg/ days dosed administration.
Among the present invention, the use of uniting of Auricularia polycose and Levamlodipine or its officinal salt has good synergism, simultaneously, single survival dose of Levamlodipine and Auricularia polycose is few, reduce the untoward reaction that single medicine heavy dose causes, can be used for treating mixed type hypertension and hyperlipidemia.
The specific embodiment
Embodiment 1-4
As following table formulated pharmaceutical composition:
| Component | Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 |
| Auricularia polycose (g) | ??50 | ??100 | ??150 | ??200 |
| Levamlodipine besylate (g) (in Levamlodipine weight) | ??2.5 | ??2.5 | ??2.5 | ??2.5 |
| Microcrystalline Cellulose (g) | ??30 | ??40 | ??60 | ??80 |
| Pregelatinized Starch (g) | ??27.5 | ??13.5 | ??36.5 | ??59.5 |
| Lactose (g) | ??30 | ??30 | ??30 | ??30 |
| Sodium Hydroxymethyl Stalcs (g) | ??9 | ??12 | ??18 | ??24 |
| Magnesium stearate (g) | ??1 | ??2 | ??3 | ??4 |
| 95% ethanol | In right amount | In right amount | In right amount | In right amount |
| Make (sheet) altogether | ??1000 | ??1000 | ??1000 | ??1000 |
Preparation method: it is even that Levamlodipine besylate, Auricularia polycose, microcrystalline Cellulose, pregelatinized Starch, lactose, Sodium Hydroxymethyl Stalcs are put into the mortar ground and mixed, cross 20 mesh sieves, add an amount of 95% ethanol and make soft material, granulate by 20 mesh sieves, 40 ℃ of aeration-dryings, dry granular adds magnesium stearate with 16 mesh sieve granulate, and tabletting promptly behind the mix homogeneously.
Instructions of taking: oral, once a day, and each 1-2 sheet, take early morning.
Other salt of Levamlodipine or Levamlodipine can be replaced the component Levamlodipine besylate and all the other compositions are configured to capsule or tablet with reference to said method; with reference to above-mentioned preparation technology, the mode of the amount that those skilled in the art also can be by changing corresponding component makes the application and asks for protection other prescription in the scope.
Embodiment 5
By following animal pharmacodynamics embodiment the therapeutical effect of pharmaceutical composition of the present invention to mixed type hypertension and hyperlipidemia is described.
Laboratory animal: SD rat, totally 80
Experimental technique: with two kidneys, one folder type method operation modeling, feed with three week of high lipid food (82% standard feed+10% yolk powder+8% Adeps Sus domestica) back survey the mean arterial pressures of rats, increased blood pressure 2.66Kpa is assessed as hypertension modeling success greater than 15.96Kpa.
Experiment grouping: adopt randomized to be divided into 8 groups, comprising: A group model group (gavaging normal saline every day); B organizes sham operated rats (renal artery not being carried out ligation during operation); C group Auricularia polycose 200mg/kg body weight; D organizes Levamlodipine besylate 5mg/kg body weight (in Levamlodipine); E group Levamlodipine besylate 2.5mg/kg body weight (in Levamlodipine) and Auricularia polycose 100mg/kg body weight; F group Levamlodipine besylate 5mg/kg body weight (in Levamlodipine) and Auricularia polycose 100mg/kg body weight; G group Levamlodipine besylate 2.5mg/kg body weight (in Levamlodipine) and Auricularia polycose 200mg/kg body weight; H group Levamlodipine besylate 5mg/kg body weight (in Levamlodipine) and Auricularia polycose 200mg/kg body weight.
Irritate stomach 1 time every day by above-mentioned dosage, begin to measure blood pressure before administration, each organizes 4 weeks of continuous irrigation stomach, and the B group is fed with standard feed, and other groups continue to raise with high lipid food.Every morning 9 employings rat electronic blood pressure instrument is measured rat blood pressure, calculating mean value.Measure triglyceride (TG), cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), HDL-C (HDL-C) the last time after the administration.
Experimental result:
(1) to the influence of blood pressure:
The result shows (seeing Table 1), and except A group, B group, C group, every group all has blood pressure lowering in various degree, and effect is obvious, and D group, E group, F group, G group, H group blood pressure lowering rate are followed successively by 14.8%, 18.4%, 23.3%, 20.2%, 23.7%.
Table 1: to the influence (n=10) of blood pressure
*Compare p＜0.01 with model group, wherein, # compares p＜0.01 ， ﹠amp with single medicine group C group; Compare p＜0.05 ， ﹠amp with single medicine group D group; ﹠amp; Compare p＜0.01 with single medicine group D group.
(2) to the influence of rat cholesterol, triglyceride, low-density lipoprotein cholesterol, HDL-C:
Experimental result (seeing Table 2) compares with the B group, and the A group has evident difference with the C group, and the modeling success is described.C group, E group, F group, G organize, more all there were significant differences with the hyperlipidemia model group for the H group.
Table 2: to the influence (n=10) of rat TG, TC, LDL-C, HDL-C
*Compare p＜0.05 with model group;
*Compare p＜0.01 with model group
Conclusion: to sum up state experiment as can be known, Levamlodipine is more obvious than using the effect of Levamlodipine and Auricularia polycose separately with the Auricularia polycose coupling, illustrate that Levamlodipine and Auricularia polycose unite to use and have certain synergism, be better than the curative effect of two kinds of medicine list times spent.
Claims (10)
1. pharmaceutical composition, its active component contains Levamlodipine or its officinal salt and Auricularia polycose.
2. pharmaceutical composition according to claim 1, it is characterized in that described Levamlodipine officinal salt is selected from benzene sulfonate, mesylate, acetate, aspat, tartrate, maleate, sulfate, hydrochlorate or the hydrobromate of Levamlodipine.
3. pharmaceutical composition according to claim 1 is characterized in that, in the described pharmaceutical composition, is 1 in the Levamlodipine of Levamlodipine or the weight ratio of its officinal salt and Auricularia polycose: (0.2-400).
4. as pharmaceutical composition as described in the claim 3, it is characterized in that, in the described pharmaceutical composition, is 1 in the Levamlodipine of Levamlodipine or the weight ratio of its officinal salt and Auricularia polycose: (20-80).
5. pharmaceutical composition according to claim 1, it is characterized in that active ingredient content is in the described pharmaceutical composition per unit preparation: Levamlodipine or its officinal salt content in Levamlodipine are 1.0-30mg; Auricularia polycose content is 5-400mg.
6. as pharmaceutical composition as described in the claim 5, it is characterized in that active ingredient content is in the described pharmaceutical composition per unit preparation: Levamlodipine or its officinal salt content in Levamlodipine are 2.5-5mg; Auricularia polycose content is 100-200mg.
7. as pharmaceutical composition as described in arbitrary claim among the claim 1-6, it is characterized in that, also contain pharmaceutic adjuvant in the described pharmaceutical composition.
8. as pharmaceutical composition as described in the claim 7, it is characterized in that described pharmaceutical composition is an oral formulations.
9. as pharmaceutical composition as described in the claim 7, it is characterized in that described pharmaceutical composition is a controlled release form.
10. as the application of pharmaceutical composition as described in arbitrary claim among the claim 1-9 in preparation treatment mixed type hypertension and hyperlipidemia medicine.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010101255832A CN101785781B (en) | 2010-03-16 | 2010-03-16 | Medicine combination of levoamlodipine or medicinal salt of levoamlodipine and auricularia auricula polysaccharide, and application thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010101255832A CN101785781B (en) | 2010-03-16 | 2010-03-16 | Medicine combination of levoamlodipine or medicinal salt of levoamlodipine and auricularia auricula polysaccharide, and application thereof |
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| CN101785781A true CN101785781A (en) | 2010-07-28 |
| CN101785781B CN101785781B (en) | 2012-11-07 |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102225083A (en) * | 2011-06-20 | 2011-10-26 | 施慧达药业集团(吉林)有限公司 | Pharmaceutical composition and application thereof |
| CN102716370A (en) * | 2012-07-04 | 2012-10-10 | 施慧达药业集团(吉林)有限公司 | Pharmaceutical composition and application thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1857726A (en) * | 2005-04-30 | 2006-11-08 | 石家庄制药集团欧意药业有限公司 | Medicine composition for treating hypertension complicated with hyperlipemia and cardiac and cerebral vascular diseases |
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- 2010-03-16 CN CN2010101255832A patent/CN101785781B/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1857726A (en) * | 2005-04-30 | 2006-11-08 | 石家庄制药集团欧意药业有限公司 | Medicine composition for treating hypertension complicated with hyperlipemia and cardiac and cerebral vascular diseases |
Non-Patent Citations (2)
| Title |
|---|
| 《中国煤炭工业医学杂志》 20091031 范永洁 高血压病的防治 1656-1657 1-10 第12卷, 第10期 * |
| 《食品研究与开发》 20050630 张立娟 黑木耳多糖酶法提取条件的研究 89-91 1-10 第26卷, 第3期 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102225083A (en) * | 2011-06-20 | 2011-10-26 | 施慧达药业集团(吉林)有限公司 | Pharmaceutical composition and application 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 |
| CN102716370A (en) * | 2012-07-04 | 2012-10-10 | 施慧达药业集团(吉林)有限公司 | Pharmaceutical composition and application thereof |
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| CN101785781B (en) | 2012-11-07 |
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