CN101756976A - Novel antihypertensive drug - Google Patents
Novel antihypertensive drug Download PDFInfo
- Publication number
- CN101756976A CN101756976A CN200810155782A CN200810155782A CN101756976A CN 101756976 A CN101756976 A CN 101756976A CN 200810155782 A CN200810155782 A CN 200810155782A CN 200810155782 A CN200810155782 A CN 200810155782A CN 101756976 A CN101756976 A CN 101756976A
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- Prior art keywords
- felodipine
- metoprolol
- compound preparation
- dosage
- drug
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention discloses a compound preparation for curing hypertension, which includes 2-10mg of felodipine and 5-50mg of metoprolol. The invention provides a novel compound preparation which solves the problem that when only one of felodipine and metoprolol is used clinically, in order to ensure the curative effect, the dosage of the drug is increased, which leads to obvious increase of the side effects. Felodipine and metoprolol are used together, so synergic and complementary curative effect can be produced. The novel antihypertensive drug enhances the tolerance of the patient, improves the compliance and reduces the dosage and the adverse reaction, and is convenient to take and cheap in price.
Description
Technical field
The present invention relates to medical technical field, disclose the hypertensive medicine of a kind of treatment.
Background technology
Hypertension is modal cardiovascular disease, is the great public health problem in the global range.China has carried out sample census in 1991 to 940,000 crowds more than 15 years old, and statistics shows: China's hypertension prevalence has reached 11.26%, and than increasing 25% in the period of the 1979-1980 10, the existing hyperpietic of China surpasses 1.3 hundred million.And the impetus of this rising is still continuing.Statistics shows also that simultaneously hypertension therapeutic rate city is 17.4%, and the rural area is 5.4%; Control rate (through treatment systolic pressure<140mmHg, diastolic pressure<90mmHg) only 2.9%.From above-mentioned statistics as can be seen China's hypertension prevalence constantly increase, but treatment rate, control rate are low, form huge contrast.According to the WTO prediction, will account for 79% of China's cause of death to the year two thousand twenty noninfectious, wherein the cardiovascular diseases will account for the first place.
The bad hypertension of long-term control can produce grievous injury to target organs such as the heart, brain, kidneys, actively the blood pressure lowering treatment can significantly reduce main cardiovascular diseases's M ﹠ M, and most hypertensive patients need could be with controlling of blood pressure in target blood pressure level ideally with depressor.
Treatment hypertension drug commonly used has calcium antagonist felodipine and beta-blocker metoprolol.
Felodipine (Felodipine), chemistry 4-(2,3 Dichlorobenzene base)-1 by name, 4-dihydro-2,6-dimethyl-3 dipicolinic acid ethyl ester methyl ester, molecular formula is C
18H
19Cl
2NO
4, molecular weight: 384.25, shown in the structural formula:
The felodipine structural formula
Felodipine is used for gently, the treatment of moderate essential hypertension.Felodipine is the selectivity calcium ion antagonist, mainly suppresses the interior stream of the outer calcium of small artery smooth muscle cell, and selectivity expansion small artery does not have this effect to vein, does not cause postural hypotension; Cardiac muscle also there is not obvious inhibitory action.Reducing renovascular resistance simultaneously, do not influence glomerular filtration rate and creatinine clearance rate, renal blood flow no change even increase is arranged slightly has short natruresis and diuresis.Can increase output and cardiac index, significantly reduce afterload, and cardiac systolic function, preload and heart rate are not had obvious influence.
Behind 10 healthy adult human oral this product 10mg, peak time is (2.01 ± 0.63) hour, and peak concentration is (4.78 ± 0.89) ng/ml, eliminates the phase half-life and is (16.09 ± 6.07) hour.According to the data bibliographical information, this product is mainly discharged from urine with metabolite form by liver metabolism, elimination, about 70% felodipine, and 10% left and right sides medicine is discharged by feces.The old people was about 36 hours the half-life.
Metoprolol (Hydrochlorothiazide), chemistry 1-isopropylamino-3-[by name is right-(2-methoxyethyl) phenoxy group]-2-propanol L (+)-tartrate, molecular formula is (C
15H
25NO
3)
2C
4H
6O
6, molecular weight: 684.82, shown in the structural formula:
The metoprolol structural formula
Metoprolol is a kind of with β
1The adrenoreceptor retardation is the medicine of main (heart selectivity), therefore is well suited for treatment hypertension and angina pectoris, reduces the incidence rate of myocardial infarction, the mortality rate after the reduction myocardial infarction.This product is owing to the excitement of retardance ectopia cordis pacemaker adrenoreceptor can be used for treating the tachy-arrhythmia that supraventricular tachy-arrhythmia, ventricular arrhythmia, Folium Digitalis Purpureae class and catecholamine cause.This product energy antagonism catecholamine effect can be treated the arrhythmia that hyperthyroidism causes.When therapeutic dose, this product is not obvious to the effect of shrinking bronchus and peripheral vessels, and airway resistance can be increased after indivedual case medications, uses β but add
1Receptor stimulating agent can be corrected.Be mainly used in and keep treatment, arrhythmia, hyperthyroidism after treatment hypertension, angina pectoris, the myocardial infarction.
Single treat hypertension than the strong dose thing and bring some untoward reaction sometimes with a kind of; blood pressure reduces the compensation response that triggers during as single therapy; take medicine after weak, dizzy, drowsiness, tinnitus, nauseating, vomiting, epigastric discomfort, constipation appear in regular meeting; sometimes also phenomenons such as postural hypotension, muscular spasm, insomnia can appear; though these phenomenons mostly dying away in the drug administration process continuously, also can be brought inconvenience to the patient.
Goal of the invention
Product of the present invention has overcome when using felodipine and metoprolol clinically now, is to guarantee that curative effect increases drug dose during singly with a medicine, causes side effect obviously to increase; During drug combination,, and use clinical medicine dose inaccurate, influence the defective of curative effect of medication because of nothing meets the pharmaceutical preparation of drug combination dosage.Felodipine and metoprolol two medicines share, collaborative, complementary action that curative effect has; Reduce consumption, alleviate untoward reaction, taking convenience, cheap.
Summary of the invention
The objective of the invention is to defective, a kind of compound preparation is provided at the prior art existence.
The present invention is achieved by the following technical solutions:
The hypertensive compound preparation of a kind of treatment, contain the component of following dosage:
Felodipine 2-10mg
Metoprolol 20-100mg
A kind of preferred as technique scheme, a kind ofly treat the component that hypertensive compound preparation contains following dosage:
Felodipine 4-6mg
Metoprolol 40-60mg
As the hypertensive compound preparation of a kind of more excellent treatment, it contains the component of following dosage:
Felodipine 5mg
Metoprolol 50mg
Beneficial effect of the present invention is: the present invention is that two kinds of antihypertensive drugs of low dose of use in conjunction are treated hypertensive, better and untoward reaction is less than single with heavy dose of wherein a kind of medicine antihypertensive effect, the treatment of associating lattice can improve efficacy of antihypertensive treatment, in and the untoward reaction that causes of different pharmaceutical, be applicable to that hyperpietic in various degree takes for a long time.
This preparation also contains a certain amount of adjuvant except that containing above two kinds of active drug; In pharmacy procedure, the addition of adjuvant can be determined according to actual needs.
The adjuvant that this preparation is commonly used has: microcrystalline Cellulose, pregelatinized Starch, low-substituted hydroxypropyl cellulose, silicon dioxide, Pulvis Talci, lactose, dextrin, magnesium stearate, carboxymethylstach sodium, calcium sulfate etc.
Compound preparation of the present invention can have multiple mode, as compound recipe felodipine-metoprolol sheet (ordinary tablet, slow releasing tablet and other special tablets), compound recipe felodipine-metoprolol capsule dosage forms such as (conventional capsule, slow releasing capsule and other special capsule preparations).
Embodiment 1
A kind of compound preparation, contain following component:
Felodipine 5mg
Metoprolol 50mg
Starch 40mg
Calcium sulfate 20mg
Pulvis Talci 2mg
Silica 1 .5mg
Carboxymethylstach sodium 2mg
Magnesium stearate 0.5mg
Present embodiment can be made into compound recipe felodipine-metoprolol sheet, and preparation method can adopt the preparation method of common pharmaceutical preparation.
Claims (3)
1. treat hypertensive compound preparation for one kind, contain the component of following dosage:
Felodipine 2-10mg
Metoprolol 20-100mg.
2. the hypertensive compound preparation of treatment according to claim 1 is characterized in that compound preparation contains the component of following dosage:
Felodipine 4-6mg
Metoprolol 40-60mg.
3. the hypertensive compound preparation of treatment according to claim 2 is characterized in that compound preparation contains the component of following dosage:
Felodipine 5mg
Metoprolol 50mg.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN200810155782A CN101756976A (en) | 2008-10-15 | 2008-10-15 | Novel antihypertensive drug |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN200810155782A CN101756976A (en) | 2008-10-15 | 2008-10-15 | Novel antihypertensive drug |
Publications (1)
Publication Number | Publication Date |
---|---|
CN101756976A true CN101756976A (en) | 2010-06-30 |
Family
ID=42488458
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN200810155782A Pending CN101756976A (en) | 2008-10-15 | 2008-10-15 | Novel antihypertensive drug |
Country Status (1)
Country | Link |
---|---|
CN (1) | CN101756976A (en) |
-
2008
- 2008-10-15 CN CN200810155782A patent/CN101756976A/en active Pending
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PB01 | Publication | ||
C10 | Entry into substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
WD01 | Invention patent application deemed withdrawn after publication |
Open date: 20100630 |