CN101766609A - Amlodipine besylate compound preparation and preparation method thereof - Google Patents
Amlodipine besylate compound preparation and preparation method thereof Download PDFInfo
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- CN101766609A CN101766609A CN200810246675A CN200810246675A CN101766609A CN 101766609 A CN101766609 A CN 101766609A CN 200810246675 A CN200810246675 A CN 200810246675A CN 200810246675 A CN200810246675 A CN 200810246675A CN 101766609 A CN101766609 A CN 101766609A
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- amlodipine besylate
- olmesartan medoxomil
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Abstract
The invention relates to the field of medicinal preparation, in particular to an amlodipine besylate compound preparation and a preparation method thereof. The preparation is characterized in that each unit preparation consists of 2 to 50mg of amlodipine besylate, 5 to 50mg of olmesartan medoxomil and auxiliary materials, and particularly, each unit preparation contains 10mg of amlodipine besylate and 10mg of olmesartan medoxomil. The invention also discloses a preparation method for the compound preparation. The preparation is used for curing primary hypertension, has good synergistic effect, and offsets adverse effect caused by respective medicament while increasing the effect of reducing hypertension.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, be specifically related to a kind of amlodipine besylate compound preparation and preparation method thereof.
Background technology
Hypertension is one of the most common at present clinical, most important cardiovascular disease.Report demonstration according to International Society of Hypertension, at present global nearly 9.72 hundred million people suffer from hypertension or blood pressure is higher, are equivalent to adult population's 26.4% a few days ago.Along with improving constantly of people's living standard, the hypertensive prevalence of China is also increasing year by year.According to hypertension statistics, China's hypertensive prevalence of being grown up rises to present 11.68% by 5.1% of nineteen fifty-nine.Hypertension can be the caused a kind of clinical manifestation of different reasons and disease on the one hand, and it can be used as the infringement that reason causes important organs such as the heart, brain, kidney again on the other hand.Target organ damages such as the Secondary cases heart that is caused by hypertension, brain, kidney have a strong impact on the disease that life-span of patient and quality of life have become serious threat human health and life.
Amlodipine Besylate Tablet, chemical name is: (-) 3-ethyl-5-methyl-2-(2-ammonia ethoxymethyl)-4-(2-chlorphenyl)-1,4-dihydro-6-methyl-3,5-pyridine dicarboxylate benzene sulfonate, molecular formula: C20H25N2O5ClC6H6O3S, molecular weight: 567.1.
Amlodipine Besylate Tablet is dihydropyridine type calcium antagonists (calcium ion antagonist or a slow channel blocking agent), and alternative inhibition calcium ion is striden film and entered smooth muscle cell and myocardial cell.Amlodipine Besylate Tablet is the peripheral arterial expander, directly acts on vascular smooth muscle, reduces peripheral vascular resistance, thereby brings high blood pressure down.Amlodipine Besylate Tablet does not influence plasma calcium concentration.Light moderate hypertension patient is respond well, can reduce clinostatism and orthostatic blood pressure in 24 hours, and life-time service does not cause that heart rate or blood plasma catechlolamine significantly change.The Amlodipine Besylate Tablet antihypertensive effect is steady, and the peak-to-valley value difference is little.It is similar that Amlodipine Besylate Tablet reduces acting in old people and the youngster of diastolic pressure, and the effect that reduces systolic pressure is stronger to the old people.
The oral post-absorption of Amlodipine Besylate Tablet fully but slowly reached peak concentration in 6-12 hour.Absolute bioavailability is 64%-90%, not influenced by diet.Amlodipine Besylate Tablet has good tolerability in the dosage range of 10mg/ day.
Olmesartan medoxomil is angiotensin receptor antagonist (ARB).The effect of the Angiotensin II-AT1 receptor of olmesartan medoxomil by optionally blocking vascular smooth muscle suppresses the blood vessel function that contracts of Angiotensin II, and it is to strong 12500 times than AT2 receptor of the affinity of AT1 receptor.Studies show that: olmesartan medoxomil is noncompetitive receptor antagonist.The level of the plain nervous plain II of rising blood vessel is to the not influence of its therapeutical effect, thereby the half-life of these angiotensin ii receptor antagonist (ARBS) is longer, and 1 administration every day just can be at 24 hours inner control blood pressures.And the drug action of competitive receptor antagonist (as eprosartan and losartan and active metabolite thereof) can be lowered by the level of rising Angiotensin II, thereby acting duration is shorter, then wants twice administration every day just at 24 hours inner control blood pressures with irbesartan and losartan treatment.
Olmesartan medoxomil is as prodrug, and can take off ester rapidly fully by gastrointestinal absorption becomes the active metabolite Olmesartan,
The bioavailability of Olmesartan is about 26%, and is similar to losartan and valsartan.Behind the oral administration, Olmesartan just reached peak serum concentration (Cmax) in 1～2 hour, and the final half-life of eliminating is 13 hours, can reach stable state at 3～5d, and 1 administration every day can not produce blood plasma and accumulates; Its plasma protein reaches 99% for the rate of closing.
Drug combination is a kind of method commonly used in the hypertension therapeutic.Reasonably drug combination can strengthen the curative effect of blood pressure lowering, and the untoward reaction that alleviates medicine improves patient's compliance, makes the acceptant secular therapeutic scheme of patient.
The principle of olmesartan medoxomil and Amlodipine Besylate Tablet drug combination is that calcium antagonist (CCB) share with angiotensin receptor antagonist (ARB).
Summary of the invention
The invention provides a kind of amlodipine besylate compound preparation and preparation method thereof.A kind of amlodipine besylate compound preparation per unit preparation is by Amlodipine Besylate Tablet 2-50mg, and olmesartan medoxomil 5-50mg and adjuvant are formed.Adjuvant is one or more in starch, microcrystalline Cellulose, lactose and carboxymethyl starch sodium, hydroxypropyl cellulose, hydroxypropyl methylcellulose, crospolyvinylpyrrolidone and cross-linked carboxymethyl cellulose sodium, the magnesium stearate.Preferred specification is to contain Amlodipine Besylate Tablet 10mg, olmesartan medoxomil 10mg in the per unit preparation.Preparation method is: with Amlodipine Besylate Tablet, olmesartan medoxomil and adjuvant mix homogeneously, and tabletting, or encapsulated.
The present invention is used for the treatment of essential hypertension, Amlodipine Besylate Tablet, olmesartan medoxomil have good synergism, when increasing antihypertensive effect or offset because drug-induced untoward reaction separately, drug side effect is little, is particularly suitable for the gerontal patient and takes for a long time.
The specific embodiment
Following examples illustrate the present invention but do not limit the present invention
Embodiment 1: 1000 of specifications
Prescription: Amlodipine Besylate Tablet 10g
Olmesartan medoxomil 15g
Lactose 25g
Microcrystalline Cellulose 40g
Mannitol 25g
Polyvinylpolypyrrolidone 10g
Aspartame 0.1g
Fruit latt essence 0.1g
Micropowder silica gel 0.75g
Magnesium stearate 0.75g
30% alcoholic solution of 8% polyvidone is an amount of
Method for making: Amlodipine Besylate Tablet, olmesartan medoxomil, microcrystalline Cellulose, lactose, mannitol, the polyvinylpolypyrrolidone of getting recipe quantity sieve, mix homogeneously, make soft material in the 30% alcoholic solution adding said mixture with an amount of 8% polyvidone, cross 20 mesh sieves and granulate, 60 ℃ of dryings 6 hours, 20 mesh sieve granulate, add fruit latt essence, magnesium stearate, aspartame, micropowder silica gel, with 30 purpose screen cloth granulate, mixing, tabletting or promptly encapsulated.
Embodiment 2: 1000 of specifications
Amlodipine Besylate Tablet 10g
Olmesartan medoxomil 10g
Microcrystalline Cellulose 50g
Carboxymethyl starch sodium 2.5g
Lactose 20g
Mannitol 20g
Polyvinylpolypyrrolidone 9g
Aspartame 0.1g
Fruit latt essence 0.1g
Micropowder silica gel 0.75g
Magnesium stearate 0.75g
30% alcoholic solution of 8% polyvidone is an amount of
Method for making: Amlodipine Besylate Tablet, olmesartan medoxomil, microcrystalline Cellulose, carboxymethyl starch sodium, lactose, mannitol, the polyvinylpolypyrrolidone of getting recipe quantity sieve, mix homogeneously, make soft material in the 30% alcoholic solution adding said mixture with an amount of 8% polyvidone, cross 20 mesh sieves and granulate, 60 ℃ of dryings 6 hours, 20 mesh sieve granulate, add fruit latt essence, magnesium stearate, aspartame, micropowder silica gel, with 30 purpose screen cloth granulate, mixing, tabletting or promptly encapsulated.
Embodiment 3: 1000 of specifications
Prescription: Amlodipine Besylate Tablet 10g
Olmesartan medoxomil 10g
Lactose 25g
Microcrystalline Cellulose 40g
Mannitol 25g
Polyvinylpolypyrrolidone 10g
Aspartame 0.1g
Fruit latt essence 0.1g
Micropowder silica gel 0.75g
Magnesium stearate 0.75g
30% alcoholic solution of 8% polyvidone is an amount of
Method for making: Amlodipine Besylate Tablet, olmesartan medoxomil, microcrystalline Cellulose, lactose, mannitol, the polyvinylpolypyrrolidone of getting recipe quantity sieve, mix homogeneously, make soft material in the 30% alcoholic solution adding said mixture with an amount of 8% polyvidone, cross 20 mesh sieves and granulate, 60 ℃ of dryings 6 hours, 20 mesh sieve granulate, add fruit latt essence, magnesium stearate, aspartame, micropowder silica gel, with 30 purpose screen cloth granulate, mixing, tabletting or promptly encapsulated.
Embodiment 4: 1000 of specifications
Amlodipine Besylate Tablet 10g
Olmesartan medoxomil 10g
Microcrystalline Cellulose 50g
Carboxymethyl starch sodium 2.5g
Lactose 20g
Mannitol 20g
Polyvinylpolypyrrolidone 9g
Aspartame 0.1g
Fruit latt essence 0.1g
Micropowder silica gel 0.75g
Magnesium stearate 0.75g
30% alcoholic solution of 8% polyvidone is an amount of
Method for making: Amlodipine Besylate Tablet, olmesartan medoxomil, microcrystalline Cellulose, carboxymethyl starch sodium, lactose, mannitol, the polyvinylpolypyrrolidone of getting recipe quantity sieve, mix homogeneously, make soft material in the 30% alcoholic solution adding said mixture with an amount of 8% polyvidone, cross 20 mesh sieves and granulate, 60 ℃ of dryings 6 hours, 20 mesh sieve granulate, add fruit latt essence, magnesium stearate, aspartame, micropowder silica gel, with 30 purpose screen cloth granulate, mixing, tabletting or promptly encapsulated.
Among the above embodiment, preferred embodiment 2 and 3.
Claims (4)
1. amlodipine besylate compound preparation is characterized in that: the per unit preparation is by Amlodipine Besylate Tablet 2-50mg, and olmesartan medoxomil 5-50mg and adjuvant are formed.
2. the described preparation of claim 1 is capsule or tablet, it is characterized in that: described adjuvant is by in starch, microcrystalline Cellulose, lactose and carboxymethyl starch sodium, hydroxypropyl cellulose, hydroxypropyl methylcellulose, crospolyvinylpyrrolidone and cross-linked carboxymethyl cellulose sodium, the magnesium stearate one or more.
3. contain Amlodipine Besylate Tablet 10mg in the described preparation of claim 1, olmesartan medoxomil 10mg.
4. the preparation method of claim 1 or 2 described preparations is characterized in that: Amlodipine Besylate Tablet, olmesartan medoxomil mixed with adjuvant, and tabletting, or encapsulated.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN200810246675A CN101766609A (en) | 2008-12-29 | 2008-12-29 | Amlodipine besylate compound preparation and preparation method thereof |
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| CN200810246675A CN101766609A (en) | 2008-12-29 | 2008-12-29 | Amlodipine besylate compound preparation and preparation method thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2407159A1 (en) * | 2010-07-16 | 2012-01-18 | Sanovel Ilac Sanayi ve Ticaret A.S. | Pharmaceutical compositions of olmesartan |
| CN103565807A (en) * | 2012-07-25 | 2014-02-12 | 天津市汉康医药生物技术有限公司 | Olmesartan medoxomil/amlodipine pharmaceutical composition |
| CN109875972A (en) * | 2015-07-08 | 2019-06-14 | 南京正大天晴制药有限公司 | A kind of olmesartan medoxomil/amlodipinepharmaceutical pharmaceutical composition |
-
2008
- 2008-12-29 CN CN200810246675A patent/CN101766609A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2407159A1 (en) * | 2010-07-16 | 2012-01-18 | Sanovel Ilac Sanayi ve Ticaret A.S. | Pharmaceutical compositions of olmesartan |
| TR201005867A1 (en) * | 2010-07-16 | 2012-02-21 | Sanovel İlaç Sanayi̇ Ve Ti̇caret Anoni̇m Şi̇rketi̇ | Olmesartan pharmaceutical compositions. |
| CN103565807A (en) * | 2012-07-25 | 2014-02-12 | 天津市汉康医药生物技术有限公司 | Olmesartan medoxomil/amlodipine pharmaceutical composition |
| CN103565807B (en) * | 2012-07-25 | 2015-11-04 | 天津市汉康医药生物技术有限公司 | A kind of olmesartan medoxomil/amlodipinepharmaceutical pharmaceutical composition |
| CN109875972A (en) * | 2015-07-08 | 2019-06-14 | 南京正大天晴制药有限公司 | A kind of olmesartan medoxomil/amlodipinepharmaceutical pharmaceutical composition |
| CN109875972B (en) * | 2015-07-08 | 2021-08-03 | 南京正大天晴制药有限公司 | Olmesartan medoxomil and amlodipine pharmaceutical composition |
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Application publication date: 20100707 |