CN102008712A - Trandolapril-containing compound preparation for curing hypertension - Google Patents
Trandolapril-containing compound preparation for curing hypertension Download PDFInfo
- Publication number
- CN102008712A CN102008712A CN 201010231091 CN201010231091A CN102008712A CN 102008712 A CN102008712 A CN 102008712A CN 201010231091 CN201010231091 CN 201010231091 CN 201010231091 A CN201010231091 A CN 201010231091A CN 102008712 A CN102008712 A CN 102008712A
- Authority
- CN
- China
- Prior art keywords
- trandolapril
- levamlodipine
- compound preparation
- blood pressure
- hypertension
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 206010020772 Hypertension Diseases 0.000 title claims abstract description 24
- VXFJYXUZANRPDJ-WTNASJBWSA-N Trandopril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](C[C@H]2CCCC[C@@H]21)C(O)=O)CC1=CC=CC=C1 VXFJYXUZANRPDJ-WTNASJBWSA-N 0.000 title claims abstract description 23
- 229960002051 trandolapril Drugs 0.000 title claims abstract description 23
- 150000001875 compounds Chemical class 0.000 title claims abstract description 20
- HTIQEAQVCYTUBX-KRWDZBQOSA-N (S)-amlodipine Chemical compound CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)[C@@H]1C1=CC=CC=C1Cl HTIQEAQVCYTUBX-KRWDZBQOSA-N 0.000 claims abstract description 21
- 229950008554 levamlodipine Drugs 0.000 claims abstract description 21
- JZUFKLXOESDKRF-UHFFFAOYSA-N Chlorothiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NCNS2(=O)=O JZUFKLXOESDKRF-UHFFFAOYSA-N 0.000 claims abstract description 12
- 229960002003 hydrochlorothiazide Drugs 0.000 claims abstract description 12
- 150000003839 salts Chemical class 0.000 claims abstract description 11
- 239000000203 mixture Substances 0.000 claims description 7
- 238000011282 treatment Methods 0.000 claims description 7
- 239000003826 tablet Substances 0.000 claims description 5
- 239000002552 dosage form Substances 0.000 claims description 4
- 239000002775 capsule Substances 0.000 claims description 3
- 239000003795 chemical substances by application Substances 0.000 claims description 3
- 239000008187 granular material Substances 0.000 claims description 3
- 239000007924 injection Substances 0.000 claims description 3
- 238000002347 injection Methods 0.000 claims description 3
- 239000002075 main ingredient Substances 0.000 claims description 3
- 239000000843 powder Substances 0.000 claims description 3
- 239000007901 soft capsule Substances 0.000 claims description 3
- 238000013270 controlled release Methods 0.000 claims description 2
- 239000003814 drug Substances 0.000 abstract description 23
- 230000036772 blood pressure Effects 0.000 abstract description 16
- 230000000694 effects Effects 0.000 abstract description 16
- 229940079593 drug Drugs 0.000 abstract description 10
- 230000008901 benefit Effects 0.000 abstract description 3
- 230000000295 complement effect Effects 0.000 abstract description 2
- 206010067484 Adverse reaction Diseases 0.000 abstract 1
- 230000006838 adverse reaction Effects 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 239000000463 material Substances 0.000 abstract 1
- 238000009472 formulation Methods 0.000 description 5
- 239000002671 adjuvant Substances 0.000 description 4
- 230000001631 hypertensive effect Effects 0.000 description 4
- 239000002220 antihypertensive agent Substances 0.000 description 3
- 229940127088 antihypertensive drug Drugs 0.000 description 3
- 239000000890 drug combination Substances 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- 230000003276 anti-hypertensive effect Effects 0.000 description 2
- 238000007796 conventional method Methods 0.000 description 2
- 210000000088 lip Anatomy 0.000 description 2
- 230000010534 mechanism of action Effects 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 239000005541 ACE inhibitor Substances 0.000 description 1
- 102000015427 Angiotensins Human genes 0.000 description 1
- 108010064733 Angiotensins Proteins 0.000 description 1
- 229940127291 Calcium channel antagonist Drugs 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 206010013710 Drug interaction Diseases 0.000 description 1
- 206010059866 Drug resistance Diseases 0.000 description 1
- 230000001133 acceleration Effects 0.000 description 1
- 230000032683 aging Effects 0.000 description 1
- 239000002333 angiotensin II receptor antagonist Substances 0.000 description 1
- 229940125364 angiotensin receptor blocker Drugs 0.000 description 1
- 230000004872 arterial blood pressure Effects 0.000 description 1
- 239000000480 calcium channel blocker Substances 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 238000011981 development test Methods 0.000 description 1
- 230000035487 diastolic blood pressure Effects 0.000 description 1
- 238000001647 drug administration Methods 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000005555 hypertensive agent Substances 0.000 description 1
- 206010025482 malaise Diseases 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000035488 systolic blood pressure Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 238000011269 treatment regimen Methods 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention provides a trandolapril-containing compound preparation for curing hypertension. The compound preparation comprises the following components: Levamlodipine or Levamlodipine pharmaceutical salt, hydrochlorothiazide and trandolapril or trandolapril pharmaceutical salt which serve as main components, as well as a pharmaceutical carrier serving as an auxiliary material, wherein in each preparation unit, the weight of the Levamlodipine or Levamlodipine pharmaceutical salt is 2.5-10.0mg. According to the mechanism of using drugs jointly to give full play to complementary actions of the drugs, the compound preparation has the advantages that the curative effect is enhanced, the standard can be reached rapidly, the blood pressure compliance rate is up to 82%, adverse reactions related to a certain increased dosage can be reduced, and the duration of time is longer; and the compound preparation has the characteristics of quick response, high blood pressure compliance rate, less side effect and low cost.
Description
Technical field:
The present invention relates to a kind of compound preparation that hypertension contains trandolapril 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 (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 trandolapril, it includes following composition: Levamlodipine (Levamlodipine) or Levamlodipine officinal salt, hydrochlorothiazide (hydrochlorothiazide), trandolapril (trandolapril) or its officinal salt are Main Ingredients and Appearance, being equipped with pharmaceutically suitable carrier forms, in wherein every preparation unit, described Levamlodipine (Levamlodipine) or Levamlodipine officinal salt, count 2.5-10.0mg with Levamlodipine, described trandolapril (trandolapril) or its officinal salt, count 0.5-4.0mg with trandolapril, described hydrochlorothiazide (hydrochlorothiazide) is 6.25-25.0mg.
It is a kind of that to treat the compound preparation that hypertension contains trandolapril 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 82%, 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 1-4 is listed as follows:
Use the conventional method in the pharmaceuticals industry among the embodiment, the according to the form below formulation becomes tablet, makes the used pharmaceutically suitable carrier of tablet--and adjuvant is the conventional adjuvant of this area.Wherein the proportioning of its Main Ingredients and Appearance is as follows:
| Embodiment | Count (mg/ sheet) with Levamlodipine | In trandolapril (mg/ sheet) | Hydrochlorothiazide (mg/ sheet) |
| 1 | Levamlodipine 2.5 | Trandolapril 0.5 | Hydrochlorothiazide 6.25 |
| 2 | Levamlodipine 2.5 | Trandolapril 4.0 | Hydrochlorothiazide 25.0 |
| 3 | Levamlodipine 5.0 | Trandolapril 2.0 | Hydrochlorothiazide 12.5 |
| 4 | Levamlodipine 10.0 | Trandolapril 4.0 | Hydrochlorothiazide 12.5 |
Use the conventional method in the pharmaceuticals industry simultaneously among the embodiment, can also be prepared into capsule, soft capsule, granule, powder, controlled release agent or injection dosage form,, pharmaceutically suitable carrier--used adjuvant is the conventional adjuvant of this area of this dosage form.
Embodiment 5: 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 400 routine hypertension philtrums, age 40--50 year, 150 examples; Age 51--60 year, 150 examples, age 61--70 year, 100 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 4 groups, every group of this compound formulation medicine that adopts embodiment of the invention 1-4 gained respectively with 400 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, 4 groups of the embodiment of the invention are totally 400 routine hypertension philtrums, and it is up to standard to amount to 330 routine patient's blood pressures, promptly returns to " normally " or " ideal " level, mean blood pressure compliance rate 82% 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 |
| 400 | 330 | 70 | 82％ |
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 (2)
1. treat the compound preparation that hypertension contains trandolapril for one kind, it is characterized in that, it includes following composition: Levamlodipine or Levamlodipine officinal salt, hydrochlorothiazide, trandolapril or its officinal salt be Main Ingredients and Appearance, be equipped with pharmaceutically suitable carrier forms, in wherein every preparation unit, described Levamlodipine or Levamlodipine officinal salt, count 2.5-10.0mg with Levamlodipine, described trandolapril or its officinal salt, count 0.5-4.0mg with trandolapril, described hydrochlorothiazide is 6.25-25.0mg.
2. according to the described a kind of compound preparation that hypertension contains trandolapril 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.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201010231091 CN102008712B (en) | 2009-07-14 | 2010-07-08 | Trandolapril-containing compound preparation for curing hypertension |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200910139997.8 | 2009-07-14 | ||
| CN200910139997 | 2009-07-14 | ||
| CN 201010231091 CN102008712B (en) | 2009-07-14 | 2010-07-08 | Trandolapril-containing compound preparation for curing hypertension |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102008712A true CN102008712A (en) | 2011-04-13 |
| CN102008712B CN102008712B (en) | 2012-12-26 |
Family
ID=43709405
Family Applications (9)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 201010231039 Active CN102008707B (en) | 2009-07-14 | 2010-07-08 | Quinapril-contained compound preparation for treating hypertension |
| CN 201010231077 Active CN102008710B (en) | 2009-07-14 | 2010-07-08 | Lisinopril-containing compound preparation for treating hypertension |
| CN 201010231091 Active CN102008712B (en) | 2009-07-14 | 2010-07-08 | Trandolapril-containing compound preparation for curing hypertension |
| CN 201010231054 Pending CN102008491A (en) | 2009-07-14 | 2010-07-08 | Fosinopril-containing compound preparation for treating hypertension |
| CN 201010231082 Active CN102008711B (en) | 2009-07-14 | 2010-07-08 | Compound preparation containing enalapril for treating hypertension |
| CN 201010231068 Active CN102008709B (en) | 2009-07-14 | 2010-07-08 | Moexipril-contained compound preparation for treating hypertension |
| CN 201010230017 Pending CN101985035A (en) | 2009-07-14 | 2010-07-08 | Perindopril-containing compound preparation for treating hypertension |
| CN 201010230019 Pending CN101984972A (en) | 2009-07-14 | 2010-07-08 | Benazepril-containing compound preparation for treating high blood pressure |
| CN 201010231061 Active CN102008708B (en) | 2009-07-14 | 2010-07-08 | Ramipril-contained compound preparation for treating hypertension |
Family Applications Before (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 201010231039 Active CN102008707B (en) | 2009-07-14 | 2010-07-08 | Quinapril-contained compound preparation for treating hypertension |
| CN 201010231077 Active CN102008710B (en) | 2009-07-14 | 2010-07-08 | Lisinopril-containing compound preparation for treating hypertension |
Family Applications After (6)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 201010231054 Pending CN102008491A (en) | 2009-07-14 | 2010-07-08 | Fosinopril-containing compound preparation for treating hypertension |
| CN 201010231082 Active CN102008711B (en) | 2009-07-14 | 2010-07-08 | Compound preparation containing enalapril for treating hypertension |
| CN 201010231068 Active CN102008709B (en) | 2009-07-14 | 2010-07-08 | Moexipril-contained compound preparation for treating hypertension |
| CN 201010230017 Pending CN101985035A (en) | 2009-07-14 | 2010-07-08 | Perindopril-containing compound preparation for treating hypertension |
| CN 201010230019 Pending CN101984972A (en) | 2009-07-14 | 2010-07-08 | Benazepril-containing compound preparation for treating high blood pressure |
| CN 201010231061 Active CN102008708B (en) | 2009-07-14 | 2010-07-08 | Ramipril-contained compound preparation for treating hypertension |
Country Status (1)
| Country | Link |
|---|---|
| CN (9) | CN102008707B (en) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102342948B (en) * | 2011-07-14 | 2012-12-05 | 海南锦瑞制药股份有限公司 | New oral solid medicinal composition and preparation method thereof |
| CN102319252B (en) * | 2011-07-22 | 2012-10-10 | 海南锦瑞制药股份有限公司 | Amlodipine and fosinopril sodium medical composition and preparation method thereof |
| CN102423482B (en) * | 2011-11-17 | 2013-09-25 | 南京瑞尔医药有限公司 | preparation method of compound amlodipine-lisinopril tablets |
| CN102423483A (en) * | 2011-11-24 | 2012-04-25 | 西北农林科技大学 | Compound ramipril nano-emulsion for antihypertension |
| CN107029208A (en) * | 2017-06-13 | 2017-08-11 | 江苏黄河药业股份有限公司 | It is a kind of to treat lisinopril compound preparation of angiocardiopathy and preparation method thereof |
| CN110755390A (en) * | 2018-07-26 | 2020-02-07 | 北京市石景山区高血压联盟研究所 | Compound antihypertensive drug tablet and application thereof |
| GR1010675B (en) * | 2023-02-17 | 2024-04-23 | Ιουλια Κλεωνος Τσετη | Orally administrated anti-hypertension drug composed of a triple combination of an ace inhibitor, a calcium antagonist and a diuretic composition |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101137367A (en) * | 2003-10-20 | 2008-03-05 | 诺瓦提斯公司 | Benazapril and amlodipine besylate for reducing cardiovascular morbidity |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1237966C (en) * | 2003-09-12 | 2006-01-25 | 启东盖天力药业有限公司 | Compound preparation for lowering the blood pressure |
-
2010
- 2010-07-08 CN CN 201010231039 patent/CN102008707B/en active Active
- 2010-07-08 CN CN 201010231077 patent/CN102008710B/en active Active
- 2010-07-08 CN CN 201010231091 patent/CN102008712B/en active Active
- 2010-07-08 CN CN 201010231054 patent/CN102008491A/en active Pending
- 2010-07-08 CN CN 201010231082 patent/CN102008711B/en active Active
- 2010-07-08 CN CN 201010231068 patent/CN102008709B/en active Active
- 2010-07-08 CN CN 201010230017 patent/CN101985035A/en active Pending
- 2010-07-08 CN CN 201010230019 patent/CN101984972A/en active Pending
- 2010-07-08 CN CN 201010231061 patent/CN102008708B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101137367A (en) * | 2003-10-20 | 2008-03-05 | 诺瓦提斯公司 | Benazapril and amlodipine besylate for reducing cardiovascular morbidity |
Also Published As
| Publication number | Publication date |
|---|---|
| CN101984972A (en) | 2011-03-16 |
| CN102008712B (en) | 2012-12-26 |
| CN102008711A (en) | 2011-04-13 |
| CN101985035A (en) | 2011-03-16 |
| CN102008710B (en) | 2013-02-20 |
| CN102008709A (en) | 2011-04-13 |
| CN102008710A (en) | 2011-04-13 |
| CN102008711B (en) | 2012-12-26 |
| CN102008491A (en) | 2011-04-13 |
| CN102008707A (en) | 2011-04-13 |
| CN102008708A (en) | 2011-04-13 |
| CN102008707B (en) | 2012-12-26 |
| CN102008709B (en) | 2012-12-26 |
| CN102008708B (en) | 2013-02-20 |
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Free format text: FORMER OWNER: WU LINYUN Effective date: 20140827 Owner name: INNER MONGOLIA YUANHE PHARMACEUTICAL CO., LTD. Free format text: FORMER OWNER: WU LINXIANG Effective date: 20140827 |
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Effective date of registration: 20140827 Address after: The 010080 the Inner Mongolia Autonomous Region economic and Technological Development Zone of Hohhot district two gold Patentee after: Inner Mongolia Yuanhe Pharmaceutical Co., Ltd. Address before: Two gold and 010080 the Inner Mongolia Autonomous Region Hohhot City pharmaceutical road Jinchuan Economic Development Zone Patentee before: Wu Linxiang Patentee before: Wu Linyun |
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Address after: The 010080 the Inner Mongolia Autonomous Region economic and Technological Development Zone of Hohhot district two gold Patentee after: YUANHE PHARMACEUTICAL CO., LTD. Address before: Jinchuan District of Hohhot economic and Technological Development Zone gold two Patentee before: Inner Mongolia Yuanhe Pharmaceutical Co., Ltd. |