CN101756974A - Method for preparing antihypertensive preparation - Google Patents
Method for preparing antihypertensive preparation Download PDFInfo
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- CN101756974A CN101756974A CN200810155777A CN200810155777A CN101756974A CN 101756974 A CN101756974 A CN 101756974A CN 200810155777 A CN200810155777 A CN 200810155777A CN 200810155777 A CN200810155777 A CN 200810155777A CN 101756974 A CN101756974 A CN 101756974A
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- felodipine
- candesartan
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Abstract
The invention discloses a complex preparation for curing hypertension. The preparation comprises 2.5 to 50mg of felodipine and 2 to 40mg of candesartan. The preparation overcomes the defect that obviously increased side effects caused by increasing the medicament dosage to ensure the curative effect in single medicament when the felodipine and the candesartan are used clinically, and provides the novel complex preparation. Combination of the felodipine and the candesartan has synergic and complementary curative effect. The complex preparation increases tolerance of patients, improves compliance, reduces dosage, lightens adverse reactions, is convenient for taking, and has low price.
Description
Technical field
The present invention relates to medical technical field, disclose a kind of preparation method of antihypertensive preparation.
Background technology
Hypertension is modal cardiovascular disease, is the great public health problem in the global range.China has 100,000,000 hypertensive patients at present approximately.The Epidemiological study result showed in 1991, and China city and rural area hypertension awareness are 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 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.
Treatment hypertension drug commonly used has calcium antagonist felodipine and angiotensin receptor antagonist Candesartan.
Felodipine (Felodipine), chemistry 4-(2, the 3-Dichlorobenzene base)-1 by name, 4-dihydro-2,6-dimethyl-3,5-pyridine dicarboxyl ethyl-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 cerebrocrast, 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.This product does not influence glomerular filtration rate and creatinine clearance rate when reducing renal vascular resistance, renal blood flow no change even increase is arranged slightly has short natruresis and diuresis.This product can increase output and cardiac index, significantly reduces 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 (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 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.
Candesartan (Candesartan), chemistry 2-ethyoxyl-3-[[4-[2-(1H-tetrazolium-5-yl) phenyl by name] phenyl] methyl]-3H-benzimidazole-4-carboxylic acid, molecular formula is C
24H
20N
6O
3, molecular weight: 440.45, shown in the structural formula:
The Candesartan structural formula
Candesartan is the 5th non-peptide class Angiotensin II (AII) antagonist of listing after Irb, and in this class antihypertensive of listing so far, it and Irb may be two members the most effective.A II is the strongest vasoconstrictor substance of known effect, and it causes various biological effects by combining with specific receptor (A II receptor) on the various target organ cell membrane.Can divide AT1 and two types of AT2 by the pharmacological characteristics aii receptor, they all are to contain 360 the amino acid whose polypeptide of having an appointment.The AT1 receptor mainly is present in some vitals such as brain, the heart, blood vessel and kidney, and the AT2 receptor mainly is present in positions such as brain, adrenal medulla, uterus and ovary.The aminoacid sequence that these two types of receptors are identical only accounts for 30%, so basic difference is arranged.Whole effects of present not clear AT1 receptor, but known its mediation AII all known physiologic function comprise that pressor effect, vasoconstriction, stimulation kidney sodium heavily absorb, the growth and the propagation of aldosterone release, cardiac muscle and cells of vascular wall.The effect of AT2 receptor is still a mystery so far.Yet, found that at present the AT2 receptor has the positivity cardiovascular effect.The AII of AII and replacement such as peptide, saralasin Saralasin and AT1 and AT2 receptor can both in conjunction with.All A II antagonisies and AT1 receptor listing at present and that be in development late stage have high affinity, and their actual AT1 receptor antagonists that is are not with the AT2 receptors bind.Otherwise PD123177 and CGP42112AT2 receptor antagonist and AT2 receptor have high affinity, do not combine with the AT1 receptor.(ACEI) is different with angiotensin-convertion enzyme inhibitor, and the AT1 antagonist does not suppress the degraded of Kallidin I fully, side effect such as less cough.In addition, compare with ACEI, another advantage of AT1 antagonist is that blocking-up A II is more complete with combining of AT1 receptor, because this effect is direct, and the mechanism of action of ACEI is that to transform A I by blocking-up ACE be due to the AII, but AII can also be by non-ACE dependency bypass generation.Moreover according to new discovery prompting, the advantage of AT1 antagonist also moreover, it is by the ill-effect of the receptor-mediated A II of selective exclusion AT1, also just increased simultaneously the combination of A II and AT2 receptor, strengthened the useful effect of A II, so the dual function of expelling pathogenetic factors and reinforcing antipathogenetic qi is arranged.This can make them have advantage above ACEI in theory, but is still waiting affirming of clinical practice.But the AT1 receptor antagonist is the best antihypertensive of toleration so far, few side effects, and very big advantage that Here it is can improve compliance, directly increases effect.This product has intensive and the specificity antagonism to vascular smooth muscle and glomerule aii receptor.
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 Candesartan 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 Candesartan 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 2.5-50mg
Candesartan 2-40mg
A kind of preferred as technique scheme, a kind ofly treat the component that hypertensive compound preparation contains following dosage:
Felodipine 5-20mg
Candesartan 4-16mg
As the hypertensive compound preparation of a kind of more excellent treatment, it contains the component of following dosage:
Felodipine is with 10mg
Candesartan 8mg
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-Candesartan sheet (ordinary tablet, slow releasing tablet and other special tablets), compound recipe felodipine-Candesartan 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 10mg
Candesartan 8mg
Starch 30mg
Calcium sulfate 1mg
Pulvis Talci 1mg
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 hypertensive compound preparation for one kind, contain the component of following dosage:
Felodipine 2.5-50mg
Candesartan 2-40mg.
2. the hypertensive compound preparation of treatment 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 of treatment 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 |
|---|---|---|---|
| CN200810155777A CN101756974A (en) | 2008-10-15 | 2008-10-15 | Method for preparing antihypertensive preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200810155777A CN101756974A (en) | 2008-10-15 | 2008-10-15 | Method for preparing antihypertensive preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101756974A true CN101756974A (en) | 2010-06-30 |
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ID=42488456
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200810155777A Pending CN101756974A (en) | 2008-10-15 | 2008-10-15 | Method for preparing antihypertensive preparation |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101756974A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104758284A (en) * | 2014-01-02 | 2015-07-08 | 江苏吉贝尔药业有限公司 | Method for preparing antihypertensive preparation |
-
2008
- 2008-10-15 CN CN200810155777A patent/CN101756974A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104758284A (en) * | 2014-01-02 | 2015-07-08 | 江苏吉贝尔药业有限公司 | Method for preparing antihypertensive preparation |
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|---|---|---|---|
| C06 | Publication | ||
| 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 |