CN102106853A - Chemical medicine composition for treating hypertension - Google Patents
Chemical medicine composition for treating hypertension Download PDFInfo
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- CN102106853A CN102106853A CN2009102488146A CN200910248814A CN102106853A CN 102106853 A CN102106853 A CN 102106853A CN 2009102488146 A CN2009102488146 A CN 2009102488146A CN 200910248814 A CN200910248814 A CN 200910248814A CN 102106853 A CN102106853 A CN 102106853A
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- candesartan cilexetil
- hypertension
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- amlodipine besilate
- blood pressure
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Abstract
The invention discloses a chemical medicine composition for treating hypertension, which comprises the following effective ingredients: amlodipine besilate and candesartan cilexetil with the weight ratio 5:4; the hypertension can be treated through the combination of the amlodipine besilate and the candesartan cilexetil, the dose of the combined amlodipine besilate and candesartan cilexetil is lower compared with that of the used amlodipine besilate or candesartan cilexetil; the adverse reaction occurrence is effectively reduced; the dosage for treating the hypertension is more reasonable; the unreasonable drug use caused by doctors is avoided; and the combination of the two ingredients is strong in synergistic effect and wide in drug use people, such as adult patients, old patients, and thin and small patients or patients with an incomplete hepatic and renal function, and patients suffering from the hypertension which can not be treated by means of single preparation of amlodipine besilate or candesartan cilexetil. The composition can be taken for a long time at a low dose according to the monitoring condition of blood pressure after the patients take the composition; the blood pressure is stable after being lowered; and the medication compliance can be improved.
Description
Technical field the present invention relates to a kind of pharmaceutical composition, is the hypertensive antihypertensive medical composite of a kind of treatment specifically.
The existing depressor of background technology mainly contains two kinds of folk prescription depressor and compound hypertension medicines.
Folk prescription depressor mainly contains clinically: calcium antagonists, converting enzyme inhibitor, beta-blocker, diuretic antihypertensive medicine etc.
Calcium antagonists is that a class can optionally reduce the Ca of slow channel
2+Interior stream, thereby disturbed the Ca of cell
2+Concentration and influence the medicine of cell function.It once was called stream blocade in calcium channel blocker or the calcium.Mainly be divided into selectivity Ca
2+Channel blocking medicine: phenylalkylamine class, dihydropyridines, bentazepam class.Non-selective Ca
2+Channel blocking medicine: piperazines, prenylamine class and other classes.
Converting enzyme inhibitor is as captopril and Losartan etc.
The diuretic antihypertensive medicine: as: hydrochlorothiazide etc.
Compound hypertension medicine mainly contains clinically: enalapril (converting enzyme inhibitor) and hydrochlorothiazide (diuretic) share or with reserpine and diuretic are the FUFANG JIANGYA PIAN etc. of principal agent.
Clinical practice is many with drug combination, because folk prescription medication effect is single, effective percentage is low, though escalated dose can improve curative effect, but untoward reaction also increases the weight of with dosage and increases, even cause blood pressure physiology compensatory balance adjustment and influence antihypertensive effect, so the clinical drug combination that mostly adopts.It is discretionary by the doctor that the medication of drug combination is selected, and its curative effect is directly relevant with doctor's level, but not all doctor can both accomplish rational use of drug, so the untoward reaction that drug interaction causes often has generation.Compound hypertension medicine can remedy this shortcoming, thereby is subjected to doctor and patient's welcome.
Compound hypertension medicine in the market mainly be last century the seventies examine release, the good and the bad is difficult divides.With the FUFANG JIANGYA PIAN that relatively is subjected to clinical welcome is example, its main component is a reserpine, and modal untoward reaction has nasal obstruction, drowsiness, diarrhoea etc., and increases dosage and can not increase this product curative effect, its side effect is increased, and heavy dose can cause Parkinsonism.Prolonged application then can cause dysthymia, and a lot of untoward reaction such as may cause bleeding after stomach and 12 fat enteropathy human this product.
Amlodipine Besylate Tablet is dihydropyridine calcium channel blocker of new generation (CCB); Be mainly used in hypertension and anginal treatment clinically, compare with other drug of the same type, this medicine has the advantage of three blood pressure lowerings treatment: 1, high-quality blood pressure lowering: potent, steady, lasting, effectively control peak blood pressure in morning, better control centre's arterial pressure, the ideal of associating blood pressure lowering is selected; 2, safe: untoward reaction is less relatively, and is lighter, has higher drug compliance and treatment persistence; 3 good target organ protection functions can effectively be protected the heart, brain, kidney and cardiovascular function.
Candesartan Cilexetil (Candesartan) is the 5th non-peptide class Angiotensin II (AII) antagonist (ARB) of listing after Irb, and in a class antihypertensive of listing so far, it and Irb may be two members the most effective.AII is the strongest vasoconstrictor substance of known effect, and it causes various biological effects by combining with specific receptor (aii receptor) on the various target organ cell membrane.Can divide AT by the pharmacological characteristics aii receptor
1And AT
2Two types, they all are to contain 360 the amino acid whose polypeptide of having an appointment.AT
1Receptor mainly is present in some vitals such as brain, cardiovascular and kidney, now known all known physiologic functions of its mediation AII, comprise that pressor effect, vasoconstriction, stimulation kidney sodium heavily absorb the growth of aldosterone release, cardiac muscle and cells of vascular wall and propagation.
Amlodipine Besylate Tablet and candesartan Cilexetil all have effects such as blood pressure lowering, expansion blood vessel, can be used for preventing and treating cardiovascular system diseases such as hypertension, coronary heart disease, heart failure.
Studies show that now CCB and ARB share can certain synergism, disclose the compound antihypertensive drug of a kind of amlodipine and irbesartan as patent documentation CNZL03150996.7; CN1765362A discloses a kind of compositions that comprises amlodipine and angiotensin ii receptor antagonist (ARB), and the weight proportion of wherein having mentioned amlodipine and candesartan Cilexetil is 1: 10～10: 1; WO20061034631 discloses the compositions of a kind of amlodipine and ARB; CN200610081591.5 discloses a kind of pharmaceutical composition that comprises the treatment hypertension and cardiovascular disease of Levamlodipine officinal salt and ARB.Yet the amlodipine of different proportion has different synergistic action effects with ARB as can be seen from these documents, and amlodipine and different AR B share the usage ratio that will reach preferable synergy very big difference is arranged also.
Summary of the invention the object of the present invention is to provide the hypertensive chemicals compositions of a kind of treatment, its ratio optimization, synergism is better, make raising evident in efficacy, untoward reaction is significantly reduced, improve patient's compliance, reduce hypertensive patient's myocardial infarction and the sickness rate in the brain rate, effectively prevent and treat cardiovascular system diseases such as hypertension, coronary heart disease, heart failure.
The present invention share calcium ion antagonist and Angiotensin II antagonist, becomes a kind of novel compound hypertension medicine.
The present invention solves the problems referred to above by following scheme:
The active component that medicine of the present invention contains is: Amlodipine Besylate Tablet and candesartan Cilexetil, the weight ratio of above-mentioned Amlodipine Besylate Tablet and candesartan Cilexetil are 5: 4.
Above-mentioned Amlodipine Besylate Tablet is left-handed Amlodipine Besylate Tablet.
Above-mentioned candesartan Cilexetil is a Candesartan hexamethylene oxygen carbonyl 2-ethoxyethyl acetate.
Usage and dosage according to the 15th edition " new pharmacology " 328 pages:
The Amlodipine Besylate Tablet common dose is: initial dose 2.5mg can increase dosage to be no more than 5mg at every turn, once-a-day according to the state of an illness once a day.
Candesartan Cilexetil, adult's predose 4mg, 1 time/d, general 8mg1 the 1d of maintenance dose, maximal dose 16mg, 1 1d is not recommended among the child and uses.
According to " Chinese Pharmacopoeia clinical application notice " (version in 2005):
Amlodipine Besylate Tablet usage and consumption are: (1) adult usual amounts: treatment angina pectoris and hypertension: 5～10mg is oral, 1 time on the one, old modest patient's consumption: hepatic insufficiency person can 2.5mg begin treatment hypertension, and the treatment angina pectoris is from 5mg.(2) child's consumption: do not determine as yet.Candesartan Cilexetil usage and consumption are: oral (1) adult usual amounts: 4～8mg, and 1 time on the 1st, begin by 4mg on the one, increase to 12mg on the 1st in case of necessity.(2) severe renal functional defect: should be from 2mg, 1 time on the one beginning.Treat in principle high blood pressure disease, should be from low dose.
According to rat toxicological test result, the Amlodipine Besylate Tablet unit dose is 0.5～2mg/kg, and when the candesartan Cilexetil unit dose was 1～6mg/kg, both synergism and antihypertensive effect were preferable; More preferably the Amlodipine Besylate Tablet unit dose is 0.5～1mg/kg, the Candesartan unit dose is 1～4mg/kg, according to the Dose Problem in the design of " pharmacological experimental methodology " third edition (People's Health Publisher) pharmacological evaluation, rat and people's conversion coefficient is 6.25, and the actual operating position Amlodipine Besylate Tablet consumption of said two devices most preferably be 2.5～5mg/ people/time, the candesartan Cilexetil consumption most preferably be 4～16mg/ people/time.
According to above data: choose most preferably scheme of Amlodipine Besylate Tablet and candesartan Cilexetil, weight ratio is 5: 4 o'clock both synergism and antihypertensive effect the bests.Prescribed regimen 2.5mg and 2mg/ sheet or 5mg and 4mg/ sheet.
The present invention is used for the treatment of hypertension, coronary heart disease.Taking dose is each 1,1 time on the one, can increase each 2 according to the state of an illness, 2 times on the one.
The present invention has following superiority as the chemicals compositions that is used for the treatment of hypertension:
(1) the two combined therapy hypertension is low than the folk prescription consumption, has effectively reduced incidence rate of adverse reaction.
(2) the two combination makes that hypertensive patient's consumption is more reasonable, has avoided the non-rational use of drug that causes because of doctor's reason.
(3) the two combination, synergism is strengthened.Amlodipine Besylate Tablet, selectivity suppresses cardiac muscle and vascular smooth muscle is striden the film flow of calcium ions, and bigger to the vascular smooth muscle effect; Candesartan Cilexetil is converted into the active metabolite Candesartan fully in absorption and conversion process, make peripheral vascular resistance reduce, and the aldosterone secretion reduces, reduce sodium retention, simultaneously expansion artery and vein during heart failure lower forward and backward load, improve cardiac output.After the two combination, to generation effect inside and outside the blood vessel, reach good antihypertensive effect simultaneously.
(4) the two combination, synergism is remarkable to be the adduction of the two, has data to show, " clinical application notice ", the 184th page) beta-blocker and the same usefulness of amlodipine, well-tolerated, but note to cause excessive hypotension, just can reach hypotensive effect preferably by the low dosage administration.
(5) the two low dose makes up for old modest patient or hepatic and kidney function obstacle person and takes effectively controlling blood pressure of single preparations of ephedrine, and taking combination drug of the present invention is ideal selection.
(6) the two effect can be played rapid onset, slowly continues the effect of blood pressure lowering, reduces the discomfort that hyperpietic's rapid depressurization brings.Amlodipine list agent peak concentration is 6～9 hours, 24 hours action periods, and the oral back of Candesartan reached the blood drug level peak value in 2～4 hours, the half-life is 9 hours in the body, the two combination has reduced because of blood drug level increases suddenly, and the instantaneous hypotension danger that rapid depressurization brings to patient can be worked simultaneously in 24 hours, keep the blood pressure of relative equilibrium, help improving patient's compliance.
In sum, to have a medication crowd as the chemicals compositions of hypertensive patient's medication wide for medicine of the present invention: adult and old modest patient or hepatic and kidney function obstacle person and take effectively this product used of controlling blood pressure of single preparations of ephedrine; Dosage is little: the monitoring situation of blood pressure after can taking medicine according to the patient, and long-term low dose is taken; Compliance is good: side effect is little, blood pressure stabilization after the blood pressure lowering, can improve compliance.
The specific embodiment
Embodiment 1: left-handed Amlodipine Besylate Tablet 5g, Candesartan hexamethylene oxygen carbonyl 2-ethoxyethyl acetate 4g, adjuvant: starch 40g, carboxymethyl starch sodium 15g, hydroxypropyl cellulose 15g, microcrystalline Cellulose 20g, magnesium stearate 2g.
Process recipes: supplementary material is pulverized, behind 100 mesh sieves, mixed excessively with the equivalent method of progressively increasing, alcohol granulation, tabletting is made 1000.
Embodiment 2: Amlodipine Besylate Tablet 5g, Candesartan hexamethylene oxygen carbonyl 2-ethoxyethyl acetate 4g, adjuvant: starch 60g, carboxymethyl starch sodium 10g, hydroxypropyl cellulose 10g, microcrystalline Cellulose 20g, magnesium stearate 2g.
Process recipes: supplementary material is pulverized, cross 100 mesh sieves after, be equipped with granule with the equivalent legal system of progressively increasing, encapsulated, make 1000.
More than two prescriptions be intended to explanation preparation tablet and capsule is practical equally.
Embodiment 3: left-handed Amlodipine Besylate Tablet 2.5g, Candesartan hexamethylene oxygen carbonyl 2-ethoxyethyl acetate 2g, adjuvant: starch 50g, carboxymethyl starch sodium 10g, hydroxypropyl cellulose 10g, microcrystalline Cellulose 30g, magnesium stearate 2g.
Make 1000 or 1000.
Process recipes: supplementary material is pulverized, behind 100 mesh sieves, mixed excessively with the equivalent method of progressively increasing, alcohol granulation, tabletting, encapsulated, promptly.
Embodiment 3 is that the low dosage medicine is used for initial patient's use, and effect is better, and side effect is littler.
Above formula combination can be used for preparing tablet (dispersible tablet, chewable tablet, slow release, controlled release etc.), capsule (soft capsule, hard capsule), also can be prepared into granule etc.
When using medicine of the present invention, note: severe hepatic injury and cholestasis patient, anemia of pregnant woman and women breast-feeding their children's forbidding.Severe renal infringement, renal artery stenosis, aorta or tricuspid stenosis and the careful usefulness of obstructive hypertrophic cardiomyopathy patient.
Claims (3)
1. treat hypertensive chemicals compositions for one kind, it is characterized in that: the active ingredient that it contains is: Amlodipine Besylate Tablet and candesartan Cilexetil, the weight ratio of above-mentioned Amlodipine Besylate Tablet and candesartan Cilexetil are 5: 4.
2. the hypertensive chemicals compositions of treatment according to claim 1 is characterized in that: its Amlodipine Besylate Tablet is left-handed Amlodipine Besylate Tablet.
3. the hypertensive chemicals compositions of treatment according to claim 1 is characterized in that: its candesartan Cilexetil is a Candesartan hexamethylene oxygen carbonyl 2-ethoxyethyl acetate.
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|---|---|---|---|
| CN2009102488146A CN102106853A (en) | 2009-12-23 | 2009-12-23 | Chemical medicine composition for treating hypertension |
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|---|---|---|---|
| CN2009102488146A CN102106853A (en) | 2009-12-23 | 2009-12-23 | Chemical medicine composition for treating hypertension |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102342937A (en) * | 2011-07-20 | 2012-02-08 | 海南锦瑞制药股份有限公司 | Amlodipine and candesartan pharmaceutical composition and preparation method thereof |
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2009
- 2009-12-23 CN CN2009102488146A patent/CN102106853A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102342937A (en) * | 2011-07-20 | 2012-02-08 | 海南锦瑞制药股份有限公司 | Amlodipine and candesartan pharmaceutical composition and preparation method thereof |
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Application publication date: 20110629 |