CN102125553A - Antihypertensive medicine - Google Patents
Antihypertensive medicine Download PDFInfo
- Publication number
- CN102125553A CN102125553A CN2011100233277A CN201110023327A CN102125553A CN 102125553 A CN102125553 A CN 102125553A CN 2011100233277 A CN2011100233277 A CN 2011100233277A CN 201110023327 A CN201110023327 A CN 201110023327A CN 102125553 A CN102125553 A CN 102125553A
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- Prior art keywords
- azelnidipine
- telmisartan
- medicine
- compound preparation
- content
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Abstract
The invention relates to a medicine for treating hypertension, which is a compound preparation consisting of telmisartan angiotensin converting enzyme receptor inhibitor and azelnidipine calcium antagonist. When the compound preparation disclosed by the invention is used, the dose and application times of the medicine are reduced, side effects are reduced, the patient compliance is improved and the treatment effect is enhanced.
Description
Technical field
The present invention relates to the hypertensive medicine of a kind of treatment, the compound preparation that it is made up of angiotensin converting enzyme acceptor inhibitor telmisartan and calcium ion antagonist azelnidipine.
Background technology
Peripheral resistance increases, and systolic heart is hyperfunction, the interior water-sodium retention of body is to form hypertensive three main pathological factors.The hypertensive medicine of treatment also has a variety of at present, relatively commonly used have calcium-channel antagonists, beta-blocker, angiotensin-convertion enzyme inhibitor, angiotensin-convertion enzyme inhibitor acceptor inhibitor, diuretic five class medicines, common medicine has nifedipine, nitrendipine, captopril, valsartan, hydrochlorothiazide etc.Though each medicine all has hypotensive effect, 70% hyperpietic needs Long term combined medication, just can obtain good hypotensive effect.
The objective of the invention is to design the high compound medicine of a kind of low dose of long-acting biological availability,, reduce side effect, improve patient's compliance, improve therapeutic effect to reduce dosage and medication number of times.
Summary of the invention
Key of the present invention is it by the high calcium ion antagonist azelnidipine of long-acting biological availability, and the angiotensin converting enzyme acceptor inhibitor telmisartan that long lasting bioavailability is high makes its a kind of new antihypertensive drugs of forming of compound recipe by a certain percentage.
In the compound preparation of the present invention: the content of telmisartan in unit formulation is 20-100mg, and the content of azelnidipine in unit formulation is 1-30mg.
Be preferably in the compound preparation of the present invention: the content of telmisartan in unit formulation is 40-80mg, and the content of azelnidipine in unit formulation is 8-16mg.
Drug action mechanism of the present invention:
Azelnidipine is long-acting calcium ion antagonist, enters excitatory cells by suppressing calcium ion, causes peripheral blood vessel and coronary vasodilator diastole and plays hypotensive effect.Hypotensive effect low and lasting, and is similar to other long-acting calcium ion antagonist antihypertensive effects, but the incidence rate of side effect such as acute vascular expansion, headache and Blushing obviously reduces, and life-time service does not have the reaction (trend that has heart rate to lower) that heart rate increases flesh.Avoiding aspect the syndrome outbreak is very effective.Azelnidipine has selectivity retardance effect to the arterial smooth muscle cell calcium channel, and its energy blood vessel dilating reduces peripheral vascular resistance and arterial pressure, relaxes to reduce coronary resistance and increase coronary sinus flow; Improve the hemodynamics of heart and lung; Hematoblastic activation there is inhibitory action.By expansion periphery small artery, Peripheral resistance is reduced simultaneously, thereby reduce cardiac muscle power consumption and oxygen demand; Coronary artery dilator is removed coronary vasospasm, has the effect of allevating angina pectoris.The azelnidipine oral absorption is good, long half time, and effect is lasting.
Telmisartan is long-acting angiotensin converting enzyme acceptor inhibitor, by with the AT1 receptors bind; the effect of inhibition angiotensin II; the performance hypotensive effect, and can blood fat reducing and blood sugar level, the injury effect of angiotensin can be protected to kidney.In addition telmisartan can be by lax mesangial cell, improve the mesangium permeability and improve effectively that nephron is drained and heavy absorption function.
Azelnidipine and telmisartan compound recipe advantage have:
(1) can bring high blood pressure down enduringly rapidly, even if it is patient's idol misses, also little to the influence of blood pressure.
(2) telmisartan can reduce the first pass effect of azelnidipine at small intestinal and liver by suppressing the P450 enzyme, improves the azelnidipine bioavailability;
(3) can reduce the angioedema side effect that azelnidipine causes.
The specific embodiment
Embodiment 1 compound recipe telmisartan azelnidipine sheet
Every consumption (mg)
Telmisartan 40
Azelnidipine 8
Microcrystalline Cellulose 140
CMS-Na 10
Magnesium stearate 2
Preparation method: with telmisartan, azelnidipine, microcrystalline Cellulose and CMS-Na mixing, purified water system soft material, 20 mesh sieves are granulated, 55 ℃ of dryings, 18 mesh sieve granulate add the magnesium stearate mixing, tabletting.
Embodiment 2 compound recipe telmisartan azelnidipine sheets
Every consumption (mg)
Telmisartan 20
Azelnidipine 30
Microcrystalline Cellulose 100
CMS-Na 10
Magnesium stearate 2
Preparation method: with telmisartan, azelnidipine, microcrystalline Cellulose and CMS-Na mixing, purified water system soft material, 20 mesh sieves are granulated, 55 ℃ of dryings, 18 mesh sieve granulate add the magnesium stearate mixing, tabletting.
Embodiment 3 compound recipe telmisartan azelnidipine sheets
Every consumption (mg)
Telmisartan 80
Azelnidipine 16
Microcrystalline Cellulose 180
L-HPC 20
Magnesium stearate 2
Preparation method: with telmisartan, azelnidipine, microcrystalline Cellulose and L-HPC mixing, purified water system soft material, 20 mesh sieves are granulated, 55 ℃ of dryings, 18 mesh sieve granulate add the magnesium stearate mixing, tabletting.
Embodiment 4 compound recipe telmisartan azelnidipine capsules
Every consumption (mg)
Telmisartan 40
Azelnidipine 16
Microcrystalline Cellulose 150
Polyvinylpolypyrrolidone 10
Magnesium stearate 2
Preparation method: with telmisartan, azelnidipine, microcrystalline Cellulose and polyvinylpolypyrrolidone mixing, purified water system soft material, 20 mesh sieves are granulated, 55 ℃ of dryings, 18 mesh sieve granulate add the magnesium stearate mixing, incapsulate.
Embodiment 5 compound recipe telmisartan azelnidipine capsules
Every consumption (mg)
Telmisartan 80
Azelnidipine 8
Microcrystalline Cellulose 160
L-HPC 20
Magnesium stearate 2
Preparation method: with telmisartan, azelnidipine, microcrystalline Cellulose and L-HPC mixing, purified water system soft material, 20 mesh sieves are granulated, 55 ℃ of dryings, 18 mesh sieve granulate add the magnesium stearate mixing, incapsulate.
Claims (3)
1. an antihypertensive drugs is characterized in that: the compound preparation that it is made up of angiotensin converting enzyme acceptor inhibitor telmisartan and calcium ion antagonist azelnidipine.
2. compound preparation according to claim 1 is characterized in that: the content of telmisartan in unit formulation is 20-100mg, and the content of azelnidipine in unit formulation is 1-30mg.
3. compound preparation according to claim 2 is characterized in that: the content of telmisartan in unit formulation is preferably 40-80mg, and the content of azelnidipine in unit formulation is preferably and is 8-16mg.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011100233277A CN102125553A (en) | 2011-01-21 | 2011-01-21 | Antihypertensive medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011100233277A CN102125553A (en) | 2011-01-21 | 2011-01-21 | Antihypertensive medicine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102125553A true CN102125553A (en) | 2011-07-20 |
Family
ID=44263988
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2011100233277A Pending CN102125553A (en) | 2011-01-21 | 2011-01-21 | Antihypertensive medicine |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102125553A (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1679954A (en) * | 2005-01-18 | 2005-10-12 | 广东省人民医院 | Compound preparation of calcium antagonist and timishatan for reducing blood pressure and its use |
| CN101247832A (en) * | 2005-06-27 | 2008-08-20 | 第一三共株式会社 | Pharmaceutical preparation containing an angiotensin II receptor antagonist and a calcium channel blocker |
-
2011
- 2011-01-21 CN CN2011100233277A patent/CN102125553A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1679954A (en) * | 2005-01-18 | 2005-10-12 | 广东省人民医院 | Compound preparation of calcium antagonist and timishatan for reducing blood pressure and its use |
| CN101247832A (en) * | 2005-06-27 | 2008-08-20 | 第一三共株式会社 | Pharmaceutical preparation containing an angiotensin II receptor antagonist and a calcium channel blocker |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C12 | Rejection of a patent application after its publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20110720 |