CN101954082A - Angiotensin-converting enzyme inhibitor-containing compound preparation for treating hypertension - Google Patents

Angiotensin-converting enzyme inhibitor-containing compound preparation for treating hypertension Download PDF

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Publication number
CN101954082A
CN101954082A CN2009101399910A CN200910139991A CN101954082A CN 101954082 A CN101954082 A CN 101954082A CN 2009101399910 A CN2009101399910 A CN 2009101399910A CN 200910139991 A CN200910139991 A CN 200910139991A CN 101954082 A CN101954082 A CN 101954082A
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enzyme inhibitor
angiotensin
compound preparation
amlodipine
pharmaceutically
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邬林祥
邬林云
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Abstract

The invention relates to an angiotensin-converting enzyme inhibitor-containing compound preparation for treating hypertension. The preparation consists of the following components: amlodipine or pharmaceutically-acceptable salt thereof, hydrochlorothiazide and giotensin-converting enzyme inhibitor or pharmaceutically-acceptable salt thereof which serve as main ingredients and a pharmaceutically-acceptable carrier, wherein each preparation unit comprises the following components: 2.5 to 15 milligrams of amlodipine or pharmaceutically-acceptable salt thereof, 0.5 to 100 milligrams of angiotensin-converting enzyme inhibitor or pharmaceutically-acceptable salt thereof, and 6.25 to 37.5 milligrams of hydrochlorothiazide. The compound preparation gives full play to the complementary action mechanism of medicaments according to combined medication to enhance curative effect, reach the standard quickly, ensure that the standard reaching rate of blood pressure reaches 81 percent, reduce the adverse reaction related with increasing of a certain dose and maintain the long effect time. The compound preparation has the characteristics of quick response, high standard reaching rate of the blood pressure, small side effect and low cost.

Description

A kind ofly treat the compound preparation that hypertension contains angiotensin-convertion enzyme inhibitor
Technical field:
The present invention relates to a kind of compound preparation that hypertension contains angiotensin-convertion enzyme inhibitor for the treatment of, belong to drug world.
Background technology:
Along with China's rapid growth of economy, the drastic change of people life style, the acceleration of urbanization, aging, the cardiovascular diseases has become first or second cause of the death of rural and urban population.Especially patients with hypertension, its sickness rate accounts for total population about 15%.Morbidity colony is so big, seeks medicine evident in efficacy, that side effect is little and seems more important.
The hypertensive medicine of treatment has multiple at present, such as calcium antagonist (CCBs), converting enzyme inhibitor (ACEI), angiotensin ii receptor antagonist (ARBs) etc., but single medicine treatment hypertension is difficult up to standard in a short time, and Most patients need be taken two or more antihypertensive drug can reach the blood pressure lowering target.Especially blood pressure exceeds desired value 20/10mmHg, and beginning need be taken two kinds of medicines often.Single medicine is prone to drug resistance, and because the bigger probability that toxicity occurs of dosage is also bigger.Majority is to give two or more drug administration treatments simultaneously.But several drugs is taken simultaneously, and patient's compliance is poor, and the collocation of the dosage of several drugs is not because the problem of formulation dosage and doctor's the degree of awareness often are optimized proportionings.In recent years, though the depressor of much new good effect few side effects is arranged, the controlling blood pressure compliance rate is relatively low.But drug combination can be used two or more depressor, and the dosage of every kind of medicine is little, and the therapeutical effect of medicine should have collaborative or the effect of addition at least, and its ill effect can be cancelled out each other or not overlapping at least or addition.Medicine kind number used during drug combination is too much unsuitable, and crossing to have complicated drug interaction at most.Therefore, select to merge very difficulty of medication amount and kind, need a large amount of development tests.
Therefore, a kind of new treatment pattern is applied to clinical gradually, and the compound hypertension medicine preparation is internationally recognized a kind of orientation treatment.Because the compound antihypertensive drug prescription is followed the principle that different mechanism of action medicines carry out proportioning usually, therefore show as the advantage that increases curative effect or reduce side effect, obtained better controlling of blood pressure effect.
Summary of the invention:
The object of the present invention is to provide a kind of side effect little, taking convenience can effectively be treated the compound preparation of three kinds of antihypertensive drugs of hypertensive combination, and this compound preparation is controlling blood pressure effectively.
Purpose of the present invention is implemented by following technical scheme: a kind ofly treat the compound preparation that hypertension contains angiotensin-convertion enzyme inhibitor, it includes following composition: amlodipine or amlodipine officinal salt, hydrochlorothiazide, angiotensin-convertion enzyme inhibitor (ACE-I) or its officinal salt are Main Ingredients and Appearance, being equipped with pharmaceutically suitable carrier forms, in wherein every preparation unit, described amlodipine or amlodipine officinal salt are 2.5-15.0mg, described angiotensin-convertion enzyme inhibitor (ACE-I) or its officinal salt are 0.5-100mg, and described hydrochlorothiazide is 6.25-37.5mg.
A kind ofly treat the compound preparation preferred version that hypertension contains angiotensin-convertion enzyme inhibitor and be: in every preparation unit, described amlodipine or amlodipine officinal salt are 2.5-10.0mg, described angiotensin-convertion enzyme inhibitor (ACE-I) or its officinal salt are 1.0-80.0mg, and described hydrochlorothiazide is 6.25-25.0mg.
A kind of hypertension for the treatment of contains that angiotensin-convertion enzyme inhibitor (ACE-I) is selected from perindopril (perindopril) described in the compound preparation of angiotensin-convertion enzyme inhibitor, trandolapril (trandola pril), ramipril (ramipril), fosinopril (fosinopril), enalapril (enalapril), benazepril (benazepril), U.S. western Puli (moexipril), lisinopril (lisinopril), any of any or its officinal salt of quinapril (quinapri).
It is a kind of that to treat the compound preparation that hypertension contains angiotensin-convertion enzyme inhibitor be capsule, soft capsule, granule, tablet, powder, slow releasing agent or injection dosage form.
Advantage of the present invention: be to give full play to the complementary mechanism of action of medicine according to drug combination to increase curative effect, up to standard fast, make the blood pressure compliance rate reach 81%, reduce with a certain dosage and increase relevant untoward reaction.Compound formulation of the present invention has instant effect, blood pressure compliance rate height, and side effect is little, the characteristics that cost is low.
The specific embodiment:
Further set forth medicine of the present invention by the following examples, these embodiment are only presented for purposes of illustration, do not limit the scope of the invention.
Embodiment 1-39 is listed as follows:
Use the conventional method in the pharmaceuticals industry among the embodiment, the according to the form below formulation becomes tablet,
Figure B2009101399910D0000031
Figure B2009101399910D0000041
Figure B2009101399910D0000051
Embodiment 40: the present invention treats hypertensive compound preparation clinical trial:
To illustrate that pharmaceutical composition of the present invention is to hypertensive therapeutical effect by the human body pharmacodynamic experiment below.
1, physical data:
Clinical 390 routine hypertension philtrums, age 40--50 year, 140 examples; Age 51--60 year, 120 examples, age 61--70 year, 130 examples.
2, diagnostic criteria: according to " Chinese hypertension prevention and control guide ", hypertension is defined as: do not obey under the antihypertensive situation systolic pressure 〉=140mmHg and/or diastolic pressure 〉=90mmHg.
3, Therapeutic Method:, adopt randomized to be divided into 39 groups, every group of this compound formulation medicine that adopts embodiment of the invention 1-39 gained respectively with 390 routine hypertensive patients, make tablet, every day is once oral, according to the dose difference of tablet, each a slice or two took 6 days.
4, efficacy assessment standard:
Draft according to " Chinese hypertension prevention and control guide ".The target of antihypertensive therapy is blood pressure to be returned to " normally " or " ideal " level.40-60 year patient be depressurized to ideal or normal arterial pressure (≤130/85mmHg), 60-70 year patient be depressurized at least normal high value (≤140/90mmHg).
5, therapeutic outcome: administration begins to carry out respectively in the 1st day, 2 days, 3 days, 4 days, 5 days, 6 days blood pressure determination.The result shows that medication is after 6 days, 39 groups of the embodiment of the invention are totally 390 routine hypertension philtrums, and it is up to standard to amount to 316 routine patient's blood pressures, promptly returns to " normally " or " ideal " level, mean blood pressure compliance rate 81% illustrates that the present embodiment compound medicine has good curing hypertension effect.
Curative effect sees the following form:
Case load Blood pressure case sum up to standard The below standard case sum of blood pressure The mean blood pressure compliance rate
390 316 74 81%
Discuss
This product is the compound formulation that brings high blood pressure down, and is applicable to treatment hypertension, and its blood pressure compliance rate is higher.

Claims (4)

1. treat the compound preparation that hypertension contains angiotensin-convertion enzyme inhibitor for one kind, it is characterized in that, it includes following composition: amlodipine or amlodipine officinal salt, hydrochlorothiazide, angiotensin-convertion enzyme inhibitor or its officinal salt be Main Ingredients and Appearance, be equipped with pharmaceutically suitable carrier forms, in wherein every preparation unit, described amlodipine or amlodipine officinal salt are 2.5-15.0mg, described angiotensin-convertion enzyme inhibitor or its officinal salt are 0.5-100mg, and described hydrochlorothiazide is 6.25-37.5mg.
2. according to the described a kind of compound preparation that hypertension contains angiotensin-convertion enzyme inhibitor for the treatment of of claim 1, it is characterized in that, in every preparation unit, described amlodipine or amlodipine officinal salt are 2.5-10.0mg, described angiotensin-convertion enzyme inhibitor or its officinal salt are 1.0-80.0mg, and described hydrochlorothiazide is 6.25-25.0mg.
3. a kind of compound preparation that hypertension contains angiotensin-convertion enzyme inhibitor for the treatment of according to claim 1 and 2, it is characterized in that, described angiotensin-convertion enzyme inhibitor is selected from any of perindopril, trandolapril, ramipril, fosinopril, enalapril, benazepril, U.S. western Puli, lisinopril, quinapril, or any of its officinal salt.
4. according to the described a kind of compound preparation that hypertension contains angiotensin-convertion enzyme inhibitor for the treatment of of claim 1, it is characterized in that described compound preparation is capsule, soft capsule, granule, tablet, powder, controlled release agent or injection dosage form.
CN2009101399910A 2009-07-14 2009-07-14 Angiotensin-converting enzyme inhibitor-containing compound preparation for treating hypertension Pending CN101954082A (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108245661A (en) * 2018-02-11 2018-07-06 浙江大学 Compound chitosan skin repair preparation containing angiotensin converting enzyme inhibitor

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108245661A (en) * 2018-02-11 2018-07-06 浙江大学 Compound chitosan skin repair preparation containing angiotensin converting enzyme inhibitor

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Application publication date: 20110126