CN105294804A - Medicine composition for treating heart failure - Google Patents
Medicine composition for treating heart failure Download PDFInfo
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- CN105294804A CN105294804A CN201510896073.8A CN201510896073A CN105294804A CN 105294804 A CN105294804 A CN 105294804A CN 201510896073 A CN201510896073 A CN 201510896073A CN 105294804 A CN105294804 A CN 105294804A
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Abstract
The invention relates to a medicine composition for treating heart failure. The medicine composition comprises an effective amount of a compound and a pharmaceutically acceptable carrier, wherein the compound has a structure as shown in the specification. The compound can be used for effectively improving indexes of heart functions of a rat with heart failure, and can be developed into a clinically effective medicine composition.
Description
Technical field
The present invention relates to field of medicaments, specifically, the present invention relates to a kind of pharmaceutical composition for the treatment of heart failure.
Background technology
Chronic heart failure (CHF) is a kind of clinical symptom group of complexity, and be the end stage eventually of various heart disease, its sickness rate is high, and mortality ratio is high.According to statistics, general population's morbidity is about 1.0% ~ 2.0%, and over-65s can reach 6% ~ 10%.China is to the result of 35 ~ 74 years old urban and rural residents totally 15518 people's random sampling: heart failure morbidity is 0.9%, and about have 4,000,000 patients with heart failure by calculating, wherein the male sex is 0.7%, and women is 1.0%, and women is higher than the male sex.Along with the aging of population, its morbidity is in rising trend.Over-65s patient, CHF is the main reason of being in hospital.For this reason, the treatment of the CHF most important thing that will be every cardiovascular doctor.
The pharmacological agent of CHF mainly contains following several in Western medicine: 1) angiotensin-convertion enzyme inhibitor (ACEI), be applicable to the patients with heart failure that all left ventricular ejection fractions reduce (being less than 0.40), to improve the life quality of patient, symptom and heart function, and reduce the hospital stays.ACEI treats the problems such as the CHF existing difference at dissimilar hypertensin inhibitor, target dose and common dose gap, ability to shoulder economically, untoward reaction, incidence are higher.2) hydragog(ue), the liquid storage that diuretic(s) alleviates Patients with Cardiac Failure by diuretic properties is stayed, is improved heart function, symptom and exercise tolerance, and single diuretic(s) is inadequate.Combined utilization ACEI, beta-blockers, digitaloid drugs can reduce the compensatory danger of clinical mistake.Low blood sodium, acid base imbalance, hyperuricemia can be there is in hydragog(ue), the untoward reactions such as hypomagnesemia, can be there is the untoward reaction such as hypokalemia, hypomagnesemia, low blood sodium, peracid hematuria, impaired glucose tolerance, acid base imbalance in thiazides, therefore patient needs often to detect serum creatinine and electrolyte level.3) beta receptor blocking agent, beta-blockers treatment CHF pathophysiological basis---reduce myocardial consumption of oxygen, improve heart function: but different clinical effects may be there is in the beta receptor blocking agent different for Patients with Cardiac Failure.Receptor antagonist is not suitable for acute heart failure, can only use at steady state.4) angiotensin II receptor blockers, to the symptomatic heart failure that can not tolerate ACEI, the alternative ACEI of angiotensin II receptor blockers uses, to reduce case fatality rate and complication.
Angiotensin II receptor blockers and ACEI reduce for the case fatality rate of chronic heart failure and sickness rate and seem to have similar effect.Angiotensin receptor blocking agent also can cause ypotension, hyperkalemia and renal function exacerbation, should note blood pressure, blood electrolyte and renal function during application.4) Aldosterone Inhibitors, aldosterone has the undesirable action independent of angiotensin II on cardiac structure and function, promotes myocardial fibrosis, easily causes ventricular arrhythmia and extremely broken.Current FDA ratifies eplerenone only for the treatment of patients with heart failure after acute myocardial infarction, should detect patient's blood potassium and serum creatinine level in Aldosterone Inhibitors application process.In sum, novel C HF medicine is researched and developed still necessary.
Summary of the invention
The object of the present invention is to provide a kind of pharmaceutical composition for the treatment of heart failure.
In order to realize object of the present invention, the invention provides a kind of compound for the treatment of heart failure, this compound has having structure:
The present invention also provides a kind of and treats pharmaceutical composition in heart failure, and described pharmaceutical composition includes the compound of effective amount and pharmaceutically acceptable carrier, and described compound has having structure:
Preferably, described pharmaceutically acceptable carrier is thinner, disintegrating agent, tackiness agent, lubricant, stablizer or corrigent.
Preferably, described thinner is sugar derivatives, starch derivative or derivatived cellulose.
Preferably, described thinner is lactose.
Preferably, described pharmaceutical composition is powder, microgranules, granule, capsule or tablet.
The present invention also provides the purposes of compound in the medicine of preparation treatment heart failure, and this compound has having structure:
Term used herein " pharmaceutically acceptable " refers to not eliminate the biologic activity of compound as herein described or the material of character, as carrier or thinner.This kind of material is applied to and individual does not cause undesirable biological action or not with harmful way and any component interaction comprised in its composition.
" pharmaceutically acceptable carrier " comprises any and all solvents as the term is employed herein, dispersion medium, coating material, tensio-active agent, antioxidant, sanitas (such as antiseptic-germicide, anti-mycotic agent), isotonic agent, absorption delay agent, salt, sanitas, drug stabilizing agent, tackiness agent, vehicle, disintegrating agent, lubricant, sweeting agent, correctives, dyestuff etc. and its combination, this is well-known to those skilled in the art (for example, see Remington ' sPharmaceuticalSciences, 18thEd.MackPrintingCompany, 1990, pp.1289-1329).Except with except the inconsistent carrier of activeconstituents, consider to use any conventional carrier in treatment or pharmaceutical composition.
Compound of the present invention effectively can improve the parameters of left ventricular function of induced heart failure rats, can be developed to pharmaceutical composition effectively new clinically.
Embodiment
Below by way of the description of embodiment, the invention will be further described, but this is not limitation of the present invention, those skilled in the art are according to basic thought of the present invention, various amendment or improvement can be made, but only otherwise depart from basic thought of the present invention, all within the scope of the present invention.
Experimental example
The structural formula of target compound is:
The foundation of chronic heart failure rat model
Select healthy Wistar male rat, body weight 200-250g, adopt the method establishment chronic heart failure rats model of abdominal injection Zorubicin.After rat adaptability is fed one week, with sterile saline, Zorubicin pulvis is dissolved into the injection liquid of 0.2mg/mL, by the low dose of intraperitoneal injection of 2mL/kg, 3 times/week, until there is lassitude in rat, weak, eyelid secretory product increases, mobility decline, movable and feed obvious minimizing compared with blank group, have depilation phenomenon, namely model is successfully prepared.
Grouping
Successful for modeling rat is divided into blank group (10), model group (10), positive drug digoxin group (10) and target compound group (10).
Administration
Each group starts administration or physiological saline after modeling success, and administering mode is gavage, totally 2 weeks.Blank group is normal rat, gives physiological saline according to the dosage of 1mL/100g body weight; Model group gives physiological saline according to the dosage of 1mL/100g body weight; Digoxin group, the dosage of 0.8g/100g body weight; Target compound group, the dosage of 0.5g/100g body weight.
Heart function detects
Experimental rat 10% Chloral Hydrate 35mg/100g intraperitoneal injection is anaesthetized, lies on the back also fixing on operator's console, do heart function and detect.The results are shown in following table 1.
Table 1 respectively group rat heart function detection case (
)
| Group | HR (secondary/min) | LVSP(mmHg) | LVEDP(mmHg) | LVEF(％) |
| Blank group | 362±15 | 145.6±6.3 | 6.2±2.8 | 85.35±5.81 |
| Model group | 312±11 | 81.5±5.2 | 12.6±4.3 | 63.18±5.33 |
| Digoxin group | 359±12 | 133.7±6.9 | 7.3±3.6 | 81.26±5.22 |
| Target compound group | 357±13 | 131.1±6.1 | 7.4±3.9 | 80.08±5.17 |
From table 1, the effect there was no significant difference (P > 0.05) of target compound group and digoxin group.
Claims (7)
1. treat a compound in heart failure, it is characterized in that, this compound has having structure:
2. treat a pharmaceutical composition in heart failure, it is characterized in that, described pharmaceutical composition includes the compound of effective amount and pharmaceutically acceptable carrier, and described compound has having structure:
3. the pharmaceutical composition that treatment according to claim 2 is in heart failure, it is characterized in that, described pharmaceutically acceptable carrier is thinner, disintegrating agent, tackiness agent, lubricant, stablizer or corrigent.
4. the pharmaceutical composition that treatment according to claim 3 is in heart failure, it is characterized in that, described thinner is sugar derivatives, starch derivative or derivatived cellulose.
5. the pharmaceutical composition that treatment according to claim 4 is in heart failure, it is characterized in that, described thinner is lactose.
6. the pharmaceutical composition that treatment according to claim 3 is in heart failure, it is characterized in that, described pharmaceutical composition is powder, microgranules, granule, capsule or tablet.
7. the purposes of compound in the medicine of preparation treatment heart failure, it is characterized in that, this compound has having structure:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510896073.8A CN105294804A (en) | 2015-12-07 | 2015-12-07 | Medicine composition for treating heart failure |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510896073.8A CN105294804A (en) | 2015-12-07 | 2015-12-07 | Medicine composition for treating heart failure |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105294804A true CN105294804A (en) | 2016-02-03 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| CN201510896073.8A Pending CN105294804A (en) | 2015-12-07 | 2015-12-07 | Medicine composition for treating heart failure |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106727583A (en) * | 2016-12-12 | 2017-05-31 | 范旭升 | A kind of pharmaceutical composition for treating diastolic heart failure |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1638777A (en) * | 2002-01-25 | 2005-07-13 | 法玛西雅公司 | Aldosterone blocker therapy to prevent or treat inflammation-related disorders |
| CN104873482A (en) * | 2015-05-05 | 2015-09-02 | 青岛市市立医院 | Pharmaceutical composition for resisting chronic cardiac failure |
| CN105330676A (en) * | 2015-12-08 | 2016-02-17 | 彭冬青 | Drug combination for treating chronic cardiac failure |
-
2015
- 2015-12-07 CN CN201510896073.8A patent/CN105294804A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1638777A (en) * | 2002-01-25 | 2005-07-13 | 法玛西雅公司 | Aldosterone blocker therapy to prevent or treat inflammation-related disorders |
| CN104873482A (en) * | 2015-05-05 | 2015-09-02 | 青岛市市立医院 | Pharmaceutical composition for resisting chronic cardiac failure |
| CN105330676A (en) * | 2015-12-08 | 2016-02-17 | 彭冬青 | Drug combination for treating chronic cardiac failure |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106727583A (en) * | 2016-12-12 | 2017-05-31 | 范旭升 | A kind of pharmaceutical composition for treating diastolic heart failure |
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Application publication date: 20160203 |