CN101756978A - Preparation method of novel compound antihypertensive preparation - Google Patents
Preparation method of novel compound antihypertensive preparation Download PDFInfo
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- CN101756978A CN101756978A CN200810155781A CN200810155781A CN101756978A CN 101756978 A CN101756978 A CN 101756978A CN 200810155781 A CN200810155781 A CN 200810155781A CN 200810155781 A CN200810155781 A CN 200810155781A CN 101756978 A CN101756978 A CN 101756978A
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- benidipine
- hydrochlorothiazide
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Abstract
The invention discloses a compound preparation for curing hypertension, which includes 1-10mg of benidipine and 5-50mg of hydrochlorothiazide. Aiming at solving the problem that when only one of benidipine and hydrochlorothiazide 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, the invention discloses a novel compound preparation. Benidipine and hydrochlorothiazide are used together, so synergic and complementary curative effect can be produced. The novel compound antihypertensive preparation 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 a kind of preparation method of new compound 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 angiotensin receptor antagonist irbesartan and angiotensin converting enzyme inhibitor fosinopril.
Benidipine (Benidipine), chemical being called (R, R)-(+/-)-2,6-dimethyl-4-(3-Nitrobenzol)-1,4-dihydro-3,5-dipicolinic acid-methyl-(R)-and 1-benzyl-3-piperidyl ester, molecular formula is C
28H
31N
3O
6, molecular weight: 505.53, shown in the structural formula:
The benidipine structural formula
Candesartan is used for hypertension and anginal treatment, and this product is the dihydropyridine type calcium antagonists antihypertensive.Can suppress to stride stream in the film calcium, reduce endocellular liberation calcium concentration and utilization rate, thereby optionally lax blood vessel reduces its resistance and produces hypotensive effect.Also can obviously increase the blood flow of arteria coronaria and vertebra tremulous pulse simultaneously.Oral absorption is rapid, and 2mg/ time, 4mg/ time, 8mg/ time, the 12mg/ time about 1h that take medicine reaches medicine blood concentration peak value, and T1/2 is 1-2.6h, and the serum albumin combination rate can reach more than 98%, and excretion rate is about 59% from feces, and excretion rate about 36% in the urine.
Hydrochlorothiazide (Hydrochlorothiazide), chemistry 6-chloro-3 by name, 4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide-1, the 1-dioxide, molecular formula is C
7H
8ClN
3O
4S
2, molecular weight: 297.74, shown in the structural formula:
The hydrochlorothiazide structural formula
The main marrow that suppresses is mixed the again absorption of ascending branch cortex portion to Na+ and Cl-, thereby promotes kidney that the drainage of sodium chloride is produced diuresis.Be to imitate diuretic in one.This product also has the effect of faint inhibition carbonic anhydrase, and therefore HCO3-loses lighter in the urine.Appearance effect in oral back 1 hour reached the peak in about 2 hours, kept 12-18 hour.
This product also has hypotensive effect, and can strengthen the hypotensive effect of other depressor.Pressure reduction effect is weak but certain, uses as basic depressor and other depressor compatibilities clinically.Also have antidiuretic activity, reduce diabetes insipidus patient's urine amount, but the too late pituitrin of curative effect, mechanism of action is not quite clear.
Be used for various edema (with better), each phase hypertension and diabetes insipidus clinically to the cardiac edema curative effect.
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 benidipine and hydrochlorothiazide 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.Benidipine and hydrochlorothiazide 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:
Benidipine 1-10mg
Hydrochlorothiazide 5-50mg
A kind of preferred as technique scheme, a kind ofly treat the component that hypertensive compound preparation contains following dosage:
Benidipine 2-5mg
Hydrochlorothiazide 10-20mg
As the hypertensive compound preparation of a kind of more excellent treatment, it contains the component of following dosage:
Benidipine 4mg
Hydrochlorothiazide 12.5mg
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 benidipine-hydrochlorothiazide tablet (ordinary tablet, slow releasing tablet and other special tablets), compound recipe benidipine-hydrochlorothiazide 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:
Benidipine 4mg
Hydrochlorothiazide 12.5mg
Starch 30mg
Calcium sulfate 3mg
Pulvis Talci 0.5mg
Present embodiment can be made into compound recipe benidipine-hydrochlorothiazide tablet, 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:
Benidipine 1-10mg
Hydrochlorothiazide 5-50mg.
2. the hypertensive compound preparation of treatment according to claim 1 is characterized in that compound preparation contains the component of following dosage:
Benidipine 2-5mg
Hydrochlorothiazide 10-20mg.
3. the hypertensive compound preparation of treatment according to claim 2 is characterized in that compound preparation contains the component of following dosage:
Benidipine 4mg
Hydrochlorothiazide 12.5mg.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200810155781A CN101756978A (en) | 2008-10-15 | 2008-10-15 | Preparation method of novel compound antihypertensive preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200810155781A CN101756978A (en) | 2008-10-15 | 2008-10-15 | Preparation method of novel compound antihypertensive preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101756978A true CN101756978A (en) | 2010-06-30 |
Family
ID=42488460
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200810155781A Pending CN101756978A (en) | 2008-10-15 | 2008-10-15 | Preparation method of novel compound antihypertensive preparation |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101756978A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104758293A (en) * | 2014-01-02 | 2015-07-08 | 江苏吉贝尔药业有限公司 | Method for preparing novel compound anti-hypertension preparation |
-
2008
- 2008-10-15 CN CN200810155781A patent/CN101756978A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104758293A (en) * | 2014-01-02 | 2015-07-08 | 江苏吉贝尔药业有限公司 | Method for preparing novel compound anti-hypertension 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 |