CN102552633B - Medicine composition - Google Patents
Medicine composition Download PDFInfo
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- CN102552633B CN102552633B CN201210052421.XA CN201210052421A CN102552633B CN 102552633 B CN102552633 B CN 102552633B CN 201210052421 A CN201210052421 A CN 201210052421A CN 102552633 B CN102552633 B CN 102552633B
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- levamlodipine
- chinese yam
- yam polysaccharide
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Abstract
The invention discloses a medicine composition of amlodipine or medicinal salt thereof and yam polysaccharide and application of the medicine composition in preparing medicine for treating hypertension and diabetes mellitus. The compound medicinal preparation of the amlodipine or medicinal salt thereof and yam polysaccharide provided in the invention is capable of reducing blood pressure and blood sugar; and synergistic effect can be achieved through combining the blood pressure reducing effect with the blood sugar reducing effect, so that the blood pressure and the blood sugar of a sufferer can be effectively controlled.
Description
Technical field
The present invention relates to field of medicaments, relate in particular to the compositions of a kind of Levamlodipine or its officinal salt and Chinese yam polysaccharide and the application in preparation treatment hypertension and diabetes medicament thereof.
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 diabetes has the trend progressively raising.Hypertension and diabetes can say " affluenza " of following the unhealthy life style of economic development, living standard improvement appearance to bring, due to overfeed, eat " very good " (fat with protein too much, vegetable and fruit is few), do not move, energy expenditure must be lacked, and suffers from diabetes and hypertensive patient more and more simultaneously.Doctor often can " search for by following the clues " in the hypertensive process for the treatment of, finds that a lot of hypertensive patients also suffer from diabetes simultaneously, so someone claims that hypertension and diabetes are " twin brothers ".Diabetes and hypertension are close, have data to show, patient of diabetes hyperpietic is ND 1.5～2.5 times, existing hypertension during 30%～50% diabetes diagnosis.Because diabetes and hypertension are usually accompanied, and hypertension complicated with diabetes mellitus is much bigger to the simple hypertension of the damage ratio of the heart, brain, kidney or simple diabetes.More easily there is the serious consequences such as hypertension oculopathy, hypertensive nephropathy, myocardial infarction, cerebrovascular accident in the patient who simultaneously suffers from hypertension and diabetes.Carotid Artery in Hypertension Complicated with Diabetes generation vascular lesion and arteriosclerotic probability are the twices of simple hypertension.Therefore, the control of paying close attention to hypertension, diabetes has very important significance, and the monotherapy that can simultaneously treat these two kinds of diseases can improve patient's compliance.
Levamlodipine is China's the first chiral separation optical voidness medicine, the first chiral separation antihypertensive drug in the Ye Shi world, it is a kind of long-acting, alkaline dihydropyridine calcium ion antagonist, it works by a kind of site being connected with dihydropyridine (N site) on cell, retardance calcium ion cross-film enters cardiac muscle and vascular smooth muscle cell, make smooth muscle loosening, 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, it 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, resist myocardial ischemia, arrhythmia, increase the effects such as insulin sensitivity and certain atherosclerosis.
Rhizoma Dioscoreae is the main medicine of Chinese traditional treatment diabetes, and the blood sugar reducing function of Chinese yam polysaccharide is the focus of Chinese yam polysaccharide research in recent years.Maurica1990 report, Rhizoma Dioscoreae extract has hypoglycemic activity to fasting rat and rabbit, can control the hyperglycemia that alloxan causes.Chinese yam polysaccharide can reduce the blood glucose in diabetic rats of model induced by alloxan, and heavy dose of Chinese yam polysaccharide blood sugar lowering is more obvious, and blood sugar lowering percentage rate increases with dosage.The concrete mechanism of Chinese yam polysaccharide treatment diabetes is also not very clear at present, and think at present, Chinese yam polysaccharide can improve islet cell function, promotes the release of insulin and blood glucose is reduced.Meanwhile, Chinese yam polysaccharide can also reduce blood glucose by reducing the absorption of sugar, and Chinese yam polysaccharide is an a kind of amylase inhibitor to sugar, can reduce blood glucose by reducing sugared absorption.In addition, hematoblastic detection is also found, Chinese yam polysaccharide can reduce hematoblastic quantity, thereby improve microvascular circulation, illustrate that Chinese yam polysaccharide plays an important role in the control of diabetes and the development of prognosis, the minute lesion of body tissue's organ that the early stage blood sugar increasing of energy improvement causes regulates the body of early diabetes to change comprehensively.
Simultaneously, Rhizoma Dioscoreae contains a large amount of mucus albumen, this is a kind of proteinpolysaccharide, and what to cardiovascular disease, can play prevention and auxiliary curative effect is exactly mainly mucus albumen role, because it is after ferment digestion, can form a kind of special dietary fiber, can reduce blood cholesterol concentration, effectively stop the deposition of blood fat in blood vessel wall, keep blood vessel elasticity, the danger that stops atherosclerosis to occur too early, angiocardiopathy preventing.
At present, do not find that Levamlodipine combines the report of use with Chinese yam polysaccharide.
Summary of the invention
One of object of the present invention is to provide a kind of pharmaceutical composition, and this pharmaceutical composition is comprised of Levamlodipine or its officinal salt and Chinese yam polysaccharide.
The officinal salt of wherein said Levamlodipine, includes but not limited to benzene sulfonate, mesylate, acetate, aspat, tartrate, maleate, sulfate, hydrochlorate, hydrobromate.Levamlodipine can make by several different methods, such as CN00102701.8 and CN03821593.4, uses on this basis conventional acid-base neutralization reaction to make stable levo-amlodipine salt.
Wherein said Chinese yam polysaccharide prepares by the following method:
(1) Rhizoma dioscoreae is peeled section, is ground into 200 object Rhizoma Dioscoreae powders after drying;
(2) Rhizoma Dioscoreae powder is soaked in 80% ethanol of 5 times of weight to reflux, extract, 2 hours;
(3) centrifugalize, sediment adds the water of 20 times of weight, 60 ℃ of water bath with thermostatic control heating;
(4) aqueous extract centrifugalize, 60 ℃ of concentrating under reduced pressure of the supernatant, make Baume degrees and are 7 fluid extract;
(5) fluid extract adds 95% ethanol precipitate with ethanol of 5 times of amounts of volume, alcohol deposit fluid centrifugalize;
(6) sediment adds the water stirring and dissolving of 5 times of weight, centrifugalize;
(7) supernatant vacuum lyophilization, obtains Chinese yam polysaccharide.
Wherein the part by weight of Levamlodipine or its officinal salt and Chinese yam polysaccharide is 1: (1/3-1000), and preferably 1: (40-120).
The present invention also provides the method for preparing aforementioned pharmaceutical compositions, and the method is that Levamlodipine or its officinal salt are mixed with Chinese yam polysaccharide.
Aforementioned pharmaceutical compositions can add that pharmaceutically acceptable carrier is prepared into the dosage forms such as tablet, capsule, solution, suspension, pill, powder, also can be prepared into controlled release form as slow release or fast dissolving dosage form, and its preparation method is known to the skilled person.
Pharmaceutical composition of the present invention can also be prepared into new pharmaceutical composition together with pharmaceutically acceptable carrier.
The present invention also provides the medical usage of aforementioned pharmaceutical compositions, and this pharmaceutical composition can be used for treating hypertension and diabetes.
Levamlodipine or its officinal salt and Chinese yam polysaccharide can also be combined the mode of use, are used for the treatment of hypertension and diabetes, and its effect is better than the effect of using separately, can improve patient's compliance simultaneously.
In described pharmaceutical composition, Levamlodipine or its officinal salt (in Levamlodipine) are generally the dosed administrations with 1.0-30mg/ days, are preferably the dosed administration of 2.5-5mg/ days.Chinese yam polysaccharide is generally the dosed administration with 10-1000mg/ days, is preferably the dosed administration of 200-300mg/ days.
The administration in any form of described pharmaceutical composition, as oral administration or injecting drug use.
Positive progressive effect of the present invention is, Levamlodipine or its officinal salt are combined use and are had good synergism with Chinese yam polysaccharide, simultaneously, single survival dose of Levamlodipine and Chinese yam polysaccharide is few, reduced the untoward reaction that single medicine heavy dose causes, can improve patient's compliance simultaneously.
The specific embodiment
In the following example, Levamlodipine besylate is purchased from company limited of Levamlodipine Pharmaceutical group (Jilin), lot number 100805, and Rhizoma dioscoreae is commercially available prod
The Chinese yam polysaccharide that the following example is used prepares by the following method:
By the Rhizoma dioscoreae section of peeling, after drying, be ground into 200 object Rhizoma Dioscoreae powders;
Rhizoma Dioscoreae powder is soaked in 80% ethanol of 5 times of weight to reflux, extract, 2 hours;
Centrifugalize, sediment adds the water of 20 times of weight, 60 ℃ of water bath with thermostatic control heating;
Aqueous extract centrifugalize, 60 ℃ of concentrating under reduced pressure of the supernatant, make Baume degrees and are 7 fluid extract;
Fluid extract adds 95% ethanol precipitate with ethanol of 5 times of amounts of volume, alcohol deposit fluid centrifugalize;
Sediment adds the water stirring and dissolving of 5 times of weight, centrifugalize;
Supernatant vacuum lyophilization, obtains Chinese yam polysaccharide.
Embodiment 1
Take Levamlodipine besylate (in Levamlodipine) 7.5mg, Chinese yam polysaccharide 600mg, mix homogeneously, makes the pharmaceutical composition 1 (compositions of the D in embodiment 5.)
Embodiment 2
Take Levamlodipine besylate (in Levamlodipine) 7.5mg, Chinese yam polysaccharide 900mg, mix homogeneously, makes pharmaceutical composition 2 (compositions of E in embodiment 5)
Embodiment 3
Take Levamlodipine besylate (in Levamlodipine) 15mg, Chinese yam polysaccharide 600mg, mix homogeneously, makes the pharmaceutical composition 3 (compositions of F in embodiment 5.)
Embodiment 4
Take Levamlodipine besylate (in Levamlodipine) 15mg, Chinese yam polysaccharide 900mg, mix homogeneously, makes pharmaceutical composition 4 (G compositions in embodiment 5.)
Embodiment 5
By following animal pharmacodynamics embodiment, the therapeutical effect of pharmaceutical composition of the present invention to hypertension and diabetes is described.
Laboratory animal: SHR rat (source: pharmacology teaching and research room of pharmaceutical college of The 2nd Army Medical College)
Experimental technique: select arteria caudalis blood pressure at 150～180mmHg, 10 week age male SHR rat.Experimental mouse (is called for short: STZ by 1% concentration streptozotocin, Sigma company) be dissolved in 0.1mol/L citrate buffer (pH 4.0), with 60mg/kg STZ dosage, inject rat abdominal cavity rapidly, 48h, 72h measure fasting glucose twice, and being greater than 16.7mmol/L is that model is successfully established.
Experiment grouping: adopt randomized to be divided into 5 groups, comprising: A group model group (gavaging normal saline every day); B group Chinese yam polysaccharide 300mg/kg body weight; C group Levamlodipine besylate (in Levamlodipine) 5mg/kg body weight; D organizes pharmaceutical composition 1,202.5mg/kg body weight; E organizes pharmaceutical composition 2,302.5mg/kg body weight; F organizes pharmaceutical composition 3,205mg/kg body weight; G organizes pharmaceutical composition 4,305mg/kg body weight;
Press above-mentioned dosage gavage every day 1 time, before administration, start Measure blood pressure, and get the eyeground vein blood of experimental rat, with oxidation enzyme process survey blood glucose value, the continuous gavage of each group 15 days, the 16th day measuring blood pressure value, fasting is got the eyeground vein blood of experimental rat for 12 hours again and is surveyed blood glucose value.
Experimental result:
(1) impact on blood pressure:
Experimental result (in Table 1), except A group, B group, every group all has blood pressure lowering in various degree, and successful, and C group, D group, E group, F group, G group blood pressure lowering rate are followed successively by 17.4%, 18.4%, 20.2%, 23.0%, 25.5%.The antihypertensive effect of two kinds of drug regimen mode administration groups is obviously better than single medicine group.
Table 1: the impact (n=10) on rat blood pressure
*with relatively p < 0.01 of A group model group
(2) impact on rat blood sugar:
Experimental result (in Table 2), before and after administration also there is notable difference in each group blood sugar level, has statistical significance (P < 0.01).Except A group, C group, every group of blood glucose value all has reduction in various degree wherein more obvious compared with B group with the hypoglycemic effect of B group Chinese yam polysaccharide same dose E group, G group.
Table 2: the impact (n=10) on rat blood sugar
*with relatively p < 0.01 of A group model group
Conclusion: comprehensive above-mentioned experiment is known, Levamlodipine besylate and the compositions ratio independent use Levamlodipine besylate of Chinese yam polysaccharide and the successful of independent use Chinese yam polysaccharide, illustrate that Levamlodipine besylate combines with Chinese yam polysaccharide to use and have certain synergism, be better than the curative effect of two kinds of medicines when alone.
Claims (2)
1. a pharmaceutical composition, it is characterized in that this pharmaceutical composition is comprised of Levamlodipine or its officinal salt and Chinese yam polysaccharide, wherein, described Levamlodipine officinal salt is benzene sulfonate, mesylate, acetate, aspat, tartrate, maleate, sulfate, hydrochlorate or hydrobromate, and wherein the part by weight of Levamlodipine or its officinal salt and Chinese yam polysaccharide is 1:40-120.
2. the application of pharmaceutical composition claimed in claim 1 in the medicine of preparation treatment hypertension or diabetes.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210052421.XA CN102552633B (en) | 2012-03-02 | 2012-03-02 | Medicine composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210052421.XA CN102552633B (en) | 2012-03-02 | 2012-03-02 | Medicine composition |
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| Publication Number | Publication Date |
|---|---|
| CN102552633A CN102552633A (en) | 2012-07-11 |
| CN102552633B true CN102552633B (en) | 2014-05-07 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201210052421.XA Expired - Fee Related CN102552633B (en) | 2012-03-02 | 2012-03-02 | Medicine composition |
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| CN (1) | CN102552633B (en) |
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2012
- 2012-03-02 CN CN201210052421.XA patent/CN102552633B/en not_active Expired - Fee Related
Non-Patent Citations (4)
| Title |
|---|
| 山药多糖的药理作用;杨宏莉,等;《医学研究与教育》;20100630;第27卷(第3期);80-82 * |
| 文秀英,等.贞清方治疗老年糖尿病肾病50例.《医药导报》.2006,第25卷(第8期),782-784. |
| 杨宏莉,等.山药多糖的药理作用.《医学研究与教育》.2010,第27卷(第3期),80-82. |
| 贞清方治疗老年糖尿病肾病50例;文秀英,等;《医药导报》;20060831;第25卷(第8期);782-784 * |
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| CN102552633A (en) | 2012-07-11 |
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