CN104758284A - Method for preparing antihypertensive preparation - Google Patents
Method for preparing antihypertensive preparation Download PDFInfo
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- CN104758284A CN104758284A CN201410003391.2A CN201410003391A CN104758284A CN 104758284 A CN104758284 A CN 104758284A CN 201410003391 A CN201410003391 A CN 201410003391A CN 104758284 A CN104758284 A CN 104758284A
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- felodipine
- candesartan
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Abstract
The invention discloses a compound preparation for treating hypertension. The compound preparation comprises 2.5-50 mg of felodipine and 2-40 mg of candesartan. The novel compound preparation provided by the invention solves the problem that when felodipine and candesartan are clinically used at present, side effects are obviously increased due to dose increase to guarantee the curative effect because only one of felodipine and candesartan is used. According to the novel compound preparation provided by the invention, felodipine and candesartan are used together to achieve synergetic and complementary curative effects, the tolerance of patients is increased, the compliance is improved, the dose is reduced to relieve adverse effect, and the compound preparation for treating hypertension is convenient to take and low in price.
Description
Technical field
The present invention relates to medical art, disclose a kind of preparation method of antihypertensive preparation.
Background technology
Hypertension is modal cardiovascular disease, is the great public health problem in global range.About there are 100,000,000 hypertensive patients in China at present.Epidemiological study result display in 1991, China's city and country hypertension awareness is respectively 36% and 13%, and treatment rate is respectively 17% and 5%, and the form of hypertension prevention and control is quite severe.According to WTO prediction, will account for 79% of China's cause of death to the year two thousand twenty noninfectious, its cardiovascular disease will account for first place.
Conventional treatment hypertension drug has calcium antagonist felodipine and angiotensin receptor antagonist Candesartan.
Felodipine (Felodipine), chemistry 4-(2,3-Dichlorobenzene base)-Isosorbide-5-Nitrae-dihydro-2,6-dimethyl-3,5-pyridine dicarboxyethyl methyl ester by name, molecular formula is C
18h
19cl
2nO
4, molecular weight: 384.25, shown in structural formula:
Felodipine is used for treatment that is light, Moderate Essential Hypertension.Felodipine is selectivity cerebrocrast, the main interior stream suppressing the outer calcium of small artery smooth muscle cell, and selectivity expansion small artery, acts on without this vein, do not cause postural hypotension; To cardiac muscle also without obvious inhibitory action.This product is while reduction renal vascular resistance, and do not affect glomerular filtration rate and creatinine clearance rate, renal blood flow is unchanged even to be had increased slightly, and has short natruresis and diuresis.This product can increase output and cardiac index, significantly reduces afterload, and has no significant effect cardiac systolic function, preload and heart rate.
After 10 oral this product 10mg of normal adults, peak time (tmax) is 2.01 ± 0.63 hours, and peak concentration (Cmax) is 4.78 ± 0.89ng/ml, and eliminating the phase half-life (t1/2 β) is 16.09 ± 6.07 hours.According to data bibliographical information, this product is discharged from urine with metabolite form primarily of liver metabolism, elimination, about 70% felodipine, and about 10% medicine is discharged by feces.Old people is about 36 hours the half-life.
Candesartan (Candesartan), chemistry 2-ethyoxyl-3-[[4-[2-(1H-TETRAZOLE-5-base) phenyl] phenyl] methyl]-3H-benzimidazole-4-carboxylic acid by name, molecular formula is C
24h
20n
6o
3, molecular weight: 440.45, shown in structural formula:
Candesartan is the 5th non-peptide class Angiotensin II (AII) antagonist gone on the market after Irb, and in this class antihypertensive gone on the market 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 effect by combining with the specific receptor (aii receptor) on various target organ cell membrane.Can divide AT1 and AT2 two types by pharmacological characteristics aii receptor, they are all containing 360 amino acid whose polypeptide of having an appointment.AT1 receptor is mainly present in some vitals such as brain, the heart, blood vessel and kidney, and AT2 receptor is mainly present in the positions such as brain, adrenal medulla, uterus and ovary.The aminoacid sequence that this two types receptor is identical only accounts for 30%, therefore has basic difference.Whole effects of current not clear AT1 receptor, but its mediation AII all known physiologic function known, comprise pressor effect, vasoconstriction, stimulation kidney sodium heavily absorb, aldosterone release, the growth of cardiac muscle and cells of vascular wall and propagation.The effect of AT2 receptor is still a mystery so far.But, find that AT2 receptor has positivity cardiovascular effect at present.The AII of AII and replacement is as peptide, and saralasin Saralasin and AT1 and AT2 receptor can be in conjunction with.Current listing and be in all AII antagonisies of development late stage and AT1 receptor has high affinity, they are actual is AT1 receptor antagonist, not with AT2 receptors bind.Otherwise PD123177 and CGP42112AT2 receptor antagonist and AT2 receptor have high affinity, are not combined with AT1 receptor.Different from angiotensin-convertion enzyme inhibitor (ACEI), AT1 antagonist does not suppress the degraded of standby Kallidin I, the side effect such as less cough.In addition, compared with ACEI, another advantage of AT1 antagonist is that the combination of blocking-up AII and AT1 receptor is more complete, because this effect is direct, and the mechanism of action of ACEI transforms AI caused by AII by blocking ACE, but AII can also be produced by non-ACE dependency bypass.Moreover according to new discovery prompting, the advantage of AT1 antagonist also moreover, it is by the ill-effect of the receptor-mediated AII of selective exclusion AT1, also just add the combination of AII and AT2 receptor simultaneously, strengthen the useful effect of AII, therefore have the dual function of expelling pathogenetic factors and reinforcing antipathogenetic qi.This can make them have advantage more than ACEI in theory, but need the affirmative of clinical practice.But AT1 receptor antagonist is the antihypertensive that toleration is best so far, few side effects, and very large advantage that Here it is, can improve compliance, directly increase effect.This product has strong and specific antagonistic action to vascular smooth muscle and glomerule aii receptor.
The medicine of alone a kind of larger dose is treated hypertension and is with sometimes and serves untoward reaction; as blood pressure during single therapy reduces the compensation response triggered; there will be weak, dizzy, drowsiness, tinnitus, Nausea and vomiting, epigastric discomfort, constipation through often after taking medicine; sometimes also there will be the phenomenons such as postural hypotension, muscular spasm, insomnia; although these phenomenons are mostly died away in continuous drug administration process, also inconvenience can be brought to patient.
Goal of the invention
When product of the present invention overcomes and uses now felodipine and Candesartan clinically, for ensureing that curative effect increases drug dose during an alone medicine, side effect is caused obviously to increase; During drug combination, because nothing meets the pharmaceutical preparation of drug combination dosage, and use clinical medicine dose inaccurate, affect the defect of curative effect of medication.Felodipine and Candesartan two medicine share, and curative effect has collaborative, complementary action; Reduce consumption, alleviate untoward reaction, taking convenience, cheap.
Summary of the invention
The object of the invention is to the defect existed for prior art, provide a kind of compound preparation.
The present invention is achieved by the following technical solutions:
One treats hypertensive compound preparation, the component containing following dosage:
Felodipine 2.5-50mg
Candesartan 2-40mg
One as technique scheme is preferred, a kind of component for the treatment of hypertensive compound preparation and containing following dosage:
Felodipine 5-20mg
Candesartan 4-16mg
Preferably treat hypertensive compound preparation as one, it contains the component of following dosage:
Felodipine 10mg
Candesartan 8mg
Beneficial effect of the present invention is: the present invention is that low dose of use in conjunction two kinds of antihypertensive drugs are hypertensive to treat, better than wherein a kind of medicine antihypertensive effect of alone larger dose and untoward reaction is less, the treatment of associating lattice can improve efficacy of antihypertensive treatment, in and the untoward reaction that causes of different pharmaceutical, be applicable to hyperpietic's long-term taking in various degree.
This preparation, except containing except above two kinds of active drug, also contains a certain amount of adjuvant; In pharmacy procedure, the addition of adjuvant can be determined according to actual needs.
The adjuvant that this preparation is conventional 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 various ways, as dosage forms such as compound recipe felodipine-Candesartan sheet (ordinary tablet, slow releasing tablet and other special tablets), compound recipe felodipine-Candesartan capsules (conventional capsule, slow releasing capsule and other special capsule preparations).
Embodiment 1
A kind of compound preparation, containing following component:
The present embodiment can be made into compound recipe felodipine-Candesartan sheet, and preparation method can adopt the preparation method of common pharmaceutical preparation.
Claims (3)
1. treat a hypertensive compound preparation, the component containing following dosage:
Felodipine 2.5-50mg
Candesartan 2-40mg.
2. the hypertensive compound preparation for the treatment of according to claim 1, is characterized in that compound preparation contains the component of following dosage:
Felodipine 5-20mg
Candesartan 4-16mg.
3. the hypertensive compound preparation for the treatment of according to claim 2, is characterized in that compound preparation contains the component of following dosage:
Felodipine 10mg
Candesartan 8mg.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410003391.2A CN104758284A (en) | 2014-01-02 | 2014-01-02 | Method for preparing antihypertensive preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410003391.2A CN104758284A (en) | 2014-01-02 | 2014-01-02 | Method for preparing antihypertensive preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN104758284A true CN104758284A (en) | 2015-07-08 |
Family
ID=53640618
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410003391.2A Pending CN104758284A (en) | 2014-01-02 | 2014-01-02 | Method for preparing antihypertensive preparation |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN104758284A (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101756974A (en) * | 2008-10-15 | 2010-06-30 | 江苏吉贝尔药业有限公司 | Method for preparing antihypertensive preparation |
| CN101890165A (en) * | 2009-05-22 | 2010-11-24 | 北京奥萨医药研究中心有限公司 | Composition for lowering blood pressure and application thereof |
-
2014
- 2014-01-02 CN CN201410003391.2A patent/CN104758284A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101756974A (en) * | 2008-10-15 | 2010-06-30 | 江苏吉贝尔药业有限公司 | Method for preparing antihypertensive preparation |
| CN101890165A (en) * | 2009-05-22 | 2010-11-24 | 北京奥萨医药研究中心有限公司 | Composition for lowering blood pressure and application thereof |
Non-Patent Citations (1)
| Title |
|---|
| 秦树琴: "非洛地平联合坎地沙坦治疗高血压40例疗效观察", 《中西医结合心脑血管病杂志》 * |
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| PB01 | Publication | ||
| EXSB | Decision made by sipo to initiate substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20150708 |
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| WD01 | Invention patent application deemed withdrawn after publication |