CN103566372A - Pharmaceutical composition for lowering blood pressure - Google Patents
Pharmaceutical composition for lowering blood pressure Download PDFInfo
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- CN103566372A CN103566372A CN201210281577.5A CN201210281577A CN103566372A CN 103566372 A CN103566372 A CN 103566372A CN 201210281577 A CN201210281577 A CN 201210281577A CN 103566372 A CN103566372 A CN 103566372A
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- pharmaceutical composition
- ramipril
- pharmaceutical compositions
- azilsartan
- diuretic
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Abstract
The invention relates to a pharmaceutical composition containing azilsartan. The pharmaceutical composition particularly comprises azilsartan and at least one other antihypertensive medicine. The collaborative antihypertensive effect can be effectively played. The pharmaceutical composition for lowering blood pressure, which has a good antihypertensive effect, stable pressure reduction, and good tolerance, is provided.
Description
Technical field
The present invention relates to a kind of hypotensor composition that contains Azilsartan, belong to medical technical field.
Background technology
Hypertension is modal a kind of cardiovascular and cerebrovascular disease in the world at present, it is reported that global hypertensive patient has surpassed 1,000,000,000.The hypertensive patient of China has surpassed 1.6 at present, and hypertensive patient has increasing trend.The hypertensive cause of disease is very complicated, also cannot determine concrete pathogenic factors completely at present, and general hypertensive patient needs treatment throughout one's life to maintain blood pressure stabilization.Follow in addition a series of that hypertension brings to make hypertension become a big factors of harm humans health as the complication of the organs such as heart, brain, kidney, had a strong impact on the mankind's living standard.
Treat clinically at present hypertension drug more, have the various Altace Ramiprils such as calcium antagonist, diuretic, angiotensin-convertion enzyme inhibitor (ACE), angiotensin receptor inhibitor (AT), beta-blocker.But a comprehensive multifactorial process during due to hypertension, the application of these medicines often has its limitation, does not often also reach expected effect in the time for the treatment of clinically.All in the process of clinical use, stable curative effect, the compound hypertension medicine of better tolerance becomes doctor and patient's needs, has also received widely and has paid close attention to.
Azilsartan (Azilsartan), for a kind of novel non-peptide class angiotensin receptor II inhibitor, can optionally block AT1 receptor.Obtain and examine in January, 2012 in Japan, chemical name: 2-ethyoxyl-1-[[2 '-(4,5-dihydro-5-oxo-1,2,4-oxadiazoles-3-yl) biphenyl-4-yl] methyl] benzimidazole-7-carboxylic acid, No. CAS: 147403-03-0.Chemical formula is as follows:
As ABR class medicine of new generation; steadily effectively blood pressure lowering of Azilsartan; improve blood pressure and blood lipoid metabolism; the target organs such as heart and brain kidney are had to protective effect; and it is synthetic not affect Kallidin I degraded and prostaglandin; thereby not causing dry cough and vasodilation, is the important drugs of a class Cardiovarscular.But use separately a hypotensor thing often can not play stable effect in blood pressure lowering, and toleration is poor.Low dose of antihypertensive drugs of combining other is used and tends to reach reasonable effect.
About sartans and calcium antagonist, the existing of the Drug combinations such as diuretic reported widely, and shown clinically reasonable effect at present.The pharmaceutical composition of a Chinese patent CN201110208064.7 Hypertension; CN201110178307.7 Pharmaceutical composition for reducing blood pressure; Medicine hydrochlorothiazide, calcium ion antagonist, angiotensin-convertion enzyme inhibitor that two pieces of patents disclose Azilsartan and blood pressure lowering share and reduce blood pressure.But do not make referrals to the application of this independent chemical composition of Azilsartan in combining with Altace Ramipril.Mono-kind of Chinese patent CN201210072267.2, containing the pharmaceutical composition of Azilsartan, has introduced Azilsartan and has had the effect of combining blood pressure with share of diuretic, has still only related to this diuretic of indapamide, for other medicine, does not explain.
Summary of the invention
During object of the present invention, provide a kind of to treat hypertensive pharmaceutical composition, it is characterized in that being formed by Azilsartan and at least one other Altace Ramipril.Can effectively reduce blood pressure, good stability, can reduce complication and better tolerance.
Technology path
Pharmaceutical composition that can blood pressure lowering, for the one or more combination in Azilsartan and other Altace Ramipril beta-blocker, calcium antagonist, ACE inhibitor, diuretic forms.Beta-blocker is wherein selected from nebivolol, practolol, arotinolol, atenolol, celiprolol, carvedilol, labetalol, bisoprolol.Be preferably in nebivolol, atenolol, arotinolol; Calcium antagonist is wherein selected from nifedipine, amlodipine, Levamlodipine, draws card Horizon, felodipine, nilvadipine, lacidipine, nisoldipine, preferably amlodipine, Levamlodipine, felodipine; ACE inhibitor is wherein selected from alacepril, benazepril, captopril, ceronapril, cilazapril, delapril, enalapril, enalaprilat, fosinopril, lisinopril, ramipril, ramiprilat, perindopril, quinapril, spirapril, temocapril, trandolapril, is preferably enalapril, ramipril, captopril; Diuretic is wherein selected from hydrochlorothiazide, the preferred hydrochlorothiazide of trichlormethiazide.
In this compositions, the unit consumption of Azilsartan is 10-150mg, preferably 20-80mg.
The unit consumption of beta receptor antagonist is:
Nebivolol 1-40mg, preferably 2-10mg
Atenolol 20-500mg, preferably 20-200mg
Arotinolol 1-50mg, preferably 1-20mg
The unit consumption that calcium antagonism connects is:
Amlodipine 1-50mg, preferably 1-20mg
Levamlodipine 1-40mg, preferably 1-20mg
Felodipine 2-60mg, preferably 10-20mg
The consumption of ACE inhibitor is:
Enalapril 1-60mg, preferably 5-20mg
Ramipril 0.5-10mg, preferably 1-2.5mg
Captopril 10-200mg, preferably 10-50mg
The consumption of diuretic is:
Hydrochlorothiazide 20-200mg, preferably 20-100mg
The conventional formulation method that above-mentioned pharmaceutical composition was adopted to this area, is prepared into the oral formulations such as tablet, capsule, granule.
The specific embodiment
Embodiment is only for the present invention is described below, but do not limit the scope of the invention.
Embodiment 1 Azilsartan hydrochlorothiazide tablet
Prescription:
Technique: by Azilsartan, hydrochlorothiazide, microcrystalline Cellulose, pregelatinized Starch and hydroxypropyl methylcellulose mix homogeneously, make binding agent granulate with 5%PVP dehydrated alcohol, 40 ℃ of dry granulate, add magnesium stearate mix tabletting and get final product.
Embodiment 2 Azilsartan nebivolol sheets
Prescription
Technique: by Azilsartan, nebivolol, microcrystalline Cellulose, pregelatinized Starch and hydroxypropyl methylcellulose mix homogeneously, make binding agent granulate with 5%PVP dehydrated alcohol, 40 ℃ of dry granulate, add magnesium stearate mix tabletting and get final product.
Embodiment 3 Azilsartan amlodipines
Prescription
Technique: by Azilsartan, amlodipine, microcrystalline Cellulose, pregelatinized Starch and hydroxypropyl methylcellulose mix homogeneously, make binding agent granulate with 5%PVP dehydrated alcohol, 40 ℃ of dry granulate, add magnesium stearate mix tabletting and get final product.
Embodiment 4 Azilsartan enalapril tablets
Prescription
Technique: by Azilsartan, enalapril, micro-product cellulose, pregelatinized Starch profit hydroxypropyl methylcellulose mix homogeneously, make binding agent granulate with 5%PVP dehydrated alcohol, 40 ℃ of dry granulate, add magnesium stearate mix tabletting and get final product.
Embodiment 5 Azilsartan nebivolol levo-amlodipines
Prescription
Technique: by Azilsartan, nebivolol, Levamlodipine, microcrystalline Cellulose, pregelatinized Starch and hydroxypropyl methylcellulose mix homogeneously, make binding agent granulate with 5%PVP dehydrated alcohol, 40 ℃ of dry granulate, add magnesium stearate mix tabletting and get final product.
Embodiment 6 Azilsartan Ramipril Capsules
Prescription
Technique: Azilsartan, ramipril profit beta-schardinger dextrin-is evenly mixed, add successively microcrystalline Cellulose and micropowder silica gel mixed pelletization encapsulated and get final product.
Embodiment 7 impacts of hypertension agents compositions on spontaneous hypertensive rat blood pressure
Method: get spontaneous hypertensive rat, body weight 3000 ± 20g, after adaptability is fed one week, is divided into animal 8 groups, 10 every group at random.Supply respectively reagent thing, be administered once every day, and gastric infusion is 4 weeks continuously, detects weekly the blood pressure of rat.Rat is fixed in the calorstat of 38 ℃, preheating 10 minutes, detects blood pressure by tail pulses method.
Administration group:
A Azilsartan 5mg/kg
B Azilsartan 2mg/kg+ nebivolol 0.5mg/kg
C Azilsartan 2mg/kg+ Levamlodipine 0.5mg/kg
D Azilsartan 2mg/kg+ hydrochlorothiazide 5mg/kg
E Azilsartan 2mg/kg+ captopril 2mg/kg
F Azilsartan 2mg/kg+ Levamlodipine 0.5mg/kg+ hydrochlorothiazide 5mg/kg
Result of the test:
Hypertension agents compositions is on the impact of spontaneous hypertensive rat blood pressure (n=10)
* compare P < 0.05 with model group, * * and model group be P < 0.01 relatively
By experimental result, can be found out, each administration group shows reasonable blood pressure lowering effect to rat spongtangeous hypertension model.With the simple husky smooth comparison of administration Archie, revealed better effect respectively to compositions medicine group.
Claims (22)
1. a hypotensor composition, is characterized by and contain Azilsartan and at least one other active component.
2. pharmaceutical composition as claimed in claim 1, wherein at least one other active component is Altace Ramipril.
3. pharmaceutical composition as claimed in claim 2, Altace Ramipril is wherein selected from one or more in beta-blocker, calcium antagonist, ACE inhibitor, diuretic.
4. pharmaceutical composition as claimed in claim 2, Altace Ramipril is wherein beta-blocker.
5. pharmaceutical composition as claimed in claim 4, beta-blocker is wherein selected from nebivolol, practolol, arotinolol, atenolol, celiprolol, carvedilol, labetalol, bisoprolol.
6. pharmaceutical composition as claimed in claim 5, beta-blocker is wherein in nebivolol, atenolol, arotinolol.
7. pharmaceutical composition as claimed in claim 2, Altace Ramipril is wherein calcium antagonist.
8. pharmaceutical composition as claimed in claim 6, calcium antagonist is wherein selected from nifedipine, amlodipine, Levamlodipine, draws card Horizon, felodipine, nilvadipine, lacidipine, nisoldipine.
9. pharmaceutical composition as claimed in claim 8, calcium antagonist is wherein amlodipine, Levamlodipine, felodipine.
10. pharmaceutical composition as claimed in claim 2, Altace Ramipril is wherein ACE inhibitor.
11. pharmaceutical composition as claimed in claim 8, ACE inhibitor is wherein selected from alacepril, benazepril, captopril, ceronapril, cilazapril, delapril, enalapril, enalaprilat, fosinopril, lisinopril, ramipril, ramiprilat, perindopril, quinapril, spirapril, temocapril, trandolapril.
12. pharmaceutical compositions as claimed in claim 11, ACE inhibitor be wherein enalapril, ramipril, captopril and.
13. pharmaceutical compositions as claimed in claim 2, Altace Ramipril is wherein diuretic.
14. pharmaceutical compositions as claimed in claim 10, diuretic is wherein selected from hydrochlorothiazide, trichlormethiazide.
15. pharmaceutical compositions as claimed in claim 14, diuretic is wherein hydrochlorothiazide.
16. pharmaceutical compositions as claimed in claim 2, wherein Altace Ramipril is Levamlodipine, hydrochlorothiazide mixture or nebivolol, Levamlodipine mixture.
17. pharmaceutical compositions as claimed in claim 1, the unit consumption that it is characterized in that Azilsartan is 10-150mg, preferably 20-80mg.
The thin compound of 18. medicine as claimed in claim 3, is characterized in that wherein the unit consumption of beta receptor antagonist is nebivolol 1-40mg, preferably 2-10mg; Atenolol 20-500mg, preferably 20-200mg; Arotinolol 1-50mg, preferably 1-20mg.
19. pharmaceutical compositions as claimed in claim 3, is characterized in that the unit consumption that calcium antagonism connects is amlodipine 1-50mg, preferably 1-20mg; Levamlodipine 1-40mg, preferably 1-20mg; Felodipine 2-60mg, preferably 10-20mg.
20. pharmaceutical composition as claimed in claim 3, is characterized in that the consumption of ACE inhibitor is: enalapril 1-60mg, preferably 5-20mg; Ramipril 0.5-10mg, preferably 1-2.5mg; Captopril 10-200mg, preferably 10-50mg.
21. pharmaceutical compositions as claimed in claim 3, the consumption that it is characterized in that diuretic is hydrochlorothiazide 20-200mg, preferably 20-100mg.
22. pharmaceutical compositions claimed in claim 1, is characterized in that making oral formulations and comprise tablet, capsule and granule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210281577.5A CN103566372A (en) | 2012-08-09 | 2012-08-09 | Pharmaceutical composition for lowering blood pressure |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210281577.5A CN103566372A (en) | 2012-08-09 | 2012-08-09 | Pharmaceutical composition for lowering blood pressure |
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| CN103566372A true CN103566372A (en) | 2014-02-12 |
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| CN201210281577.5A Pending CN103566372A (en) | 2012-08-09 | 2012-08-09 | Pharmaceutical composition for lowering blood pressure |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104436155A (en) * | 2014-12-23 | 2015-03-25 | 南京先宇科技有限公司 | Pharmaceutical composition containing levamlodipine and perindopril and preparation method |
| CN104644632A (en) * | 2015-01-27 | 2015-05-27 | 美吉斯制药（厦门）有限公司 | Orally taken tablet containing Azilsartan and benzenesulfonate amlodipine and preparation method thereof |
| CN105853418A (en) * | 2016-05-23 | 2016-08-17 | 上海麦步医药科技有限公司 | Composition containing levorotatory amlodipine and azilsartan |
| CN106668016A (en) * | 2015-11-11 | 2017-05-17 | 江苏先声药业有限公司 | Solid preparation of azilsartan and levamlodpine besylate composition and preparation method of solid preparation |
| CN107007812A (en) * | 2017-04-05 | 2017-08-04 | 江苏大学 | A kind of method for extending captopril hypotensive efficacy time |
| WO2024055984A1 (en) * | 2022-09-14 | 2024-03-21 | 上海云晟研新生物科技有限公司 | Nebivolol and amlodipine composition, preparation method therefor, and use thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102225203A (en) * | 2011-06-29 | 2011-10-26 | 北京阜康仁生物制药科技有限公司 | Pharmaceutical composition used for lowering blood pressure |
| CN102342944A (en) * | 2011-07-14 | 2012-02-08 | 丁尧 | Medicament composition for treating hypertension |
| CN102580097A (en) * | 2012-03-16 | 2012-07-18 | 江苏先声药物研究有限公司 | Medicinal composition containing azilsartan |
-
2012
- 2012-08-09 CN CN201210281577.5A patent/CN103566372A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102225203A (en) * | 2011-06-29 | 2011-10-26 | 北京阜康仁生物制药科技有限公司 | Pharmaceutical composition used for lowering blood pressure |
| CN102342944A (en) * | 2011-07-14 | 2012-02-08 | 丁尧 | Medicament composition for treating hypertension |
| CN102580097A (en) * | 2012-03-16 | 2012-07-18 | 江苏先声药物研究有限公司 | Medicinal composition containing azilsartan |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104436155A (en) * | 2014-12-23 | 2015-03-25 | 南京先宇科技有限公司 | Pharmaceutical composition containing levamlodipine and perindopril and preparation method |
| CN104644632A (en) * | 2015-01-27 | 2015-05-27 | 美吉斯制药（厦门）有限公司 | Orally taken tablet containing Azilsartan and benzenesulfonate amlodipine and preparation method thereof |
| CN106668016A (en) * | 2015-11-11 | 2017-05-17 | 江苏先声药业有限公司 | Solid preparation of azilsartan and levamlodpine besylate composition and preparation method of solid preparation |
| CN106668016B (en) * | 2015-11-11 | 2020-06-23 | 江苏先声药业有限公司 | Solid preparation of azilsartan and amlodipine besylate composition and preparation method thereof |
| CN105853418A (en) * | 2016-05-23 | 2016-08-17 | 上海麦步医药科技有限公司 | Composition containing levorotatory amlodipine and azilsartan |
| CN107007812A (en) * | 2017-04-05 | 2017-08-04 | 江苏大学 | A kind of method for extending captopril hypotensive efficacy time |
| WO2024055984A1 (en) * | 2022-09-14 | 2024-03-21 | 上海云晟研新生物科技有限公司 | Nebivolol and amlodipine composition, preparation method therefor, and use thereof |
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Application publication date: 20140212 |