CN107375310A - Cryptogenin is preparing the purposes in treating heart failure drugs - Google Patents
Cryptogenin is preparing the purposes in treating heart failure drugs Download PDFInfo
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- CN107375310A CN107375310A CN201710127199.8A CN201710127199A CN107375310A CN 107375310 A CN107375310 A CN 107375310A CN 201710127199 A CN201710127199 A CN 201710127199A CN 107375310 A CN107375310 A CN 107375310A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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Abstract
It is used for the purposes for preventing or treating heart failure the invention provides cryptogenin, cryptogenin of the invention can be obviously improved cardiac diastolic function, therefore can be used for the treatment of chronic heart failure.
Description
Technical field
The invention belongs to field of medicaments, and in particular to cryptogenin is preparing the purposes in treating heart failure drugs.
Background technology
Heart failure is due to cardiac pumping function obstacle, cardiac output deficiency occurs, and the hemoperfusion of tissue is reduced, no
It is enough the metabolism needs for maintaining body cell, and occurs the Comprehensive Clinical table of pulmonary circulatory stasis and (or) congestion of systemic circulation simultaneously
It is existing, have a strong impact on the Health and Living quality of patient.
Heart failure is clinically common disease and frequently-occurring disease in the elderly's heart disease, and it is more clinically to induce the sick factor.
Such as aging population, the change of rhythm of life, eating habit and life stress, and the protopathy related to heart failure
Such as raising of hypertension, coronary heart disease, hyperlipemia, diabetes, the myocardial infarction incidence of disease, it can all greatly increase heart failure
The incidence of disease.Heart failure lapses to as the final of heart disease latter stage at end, forms the major causes of death of cardiovascular system.
Heart failure incidence height has become main public health problem, and due to heart failure patient often due to various lure
Because aggravating symptom, make patient's repeated hospitalization, course of disease length, medical expense is expensive, has had a strong impact on the quality of life of family, significantly
Add social economical burden.
Problem of the heart failure as medical field, its method treated are explored and innovated continuous.With chronic mental and physical efforts
The transformation of failure patients' Therapeutic mode, based on conventional increase myocardial contractive power, till now different to improve neuroendocrine
Often, Ventricular Remodeling is reduced, blocks the Therapeutic mode based on vicious circle.The treatment of increase beta-blocker is arrived again, and these are all
It is the impressive progress of heart failure therapy, moreover, the progress of its opportunity used in medicine and drug combination, all anti-
Only, delay to remold with reverse myocardial, reduce in HF mortality rate and illness rate and show huge effect.But while
Such medicine can play more significant therapeutic effect to heart failure, but it often has strict limitation, and may
Serious adverse reaction can be caused, or even patient's water-electrolyte metabolism can be had a strong impact on, so that patient produces other complication
Probability greatly increases.If beta-blocker is for acute heart failure, heart failure not well control (vein with cardiotonic drug oedema not
Disappear), bronchospastic disease, bradycardia, two degree and more than two degree blocks etc. are all to avoid.These taboos
Curative effect is limited to a certain extent with side effect, and clinically heart failure is mostly Secondary cases, is existed along with complication,
The medicine of some heart failures treatment may be taboo for complication.Therefore a kind of evident in efficacy and low-cost control is found
Treatment mode or medicine have important social effect and economic implications.
Chinese medicine trilliaceae is traditional rare Chinese medicine, also known as RADIX ET RHIZOMA TRILLII, containing a variety of steroid saponins, flavones and terpene
Composition.With tranquilizing and allaying excitement, expelling wind and activating blood flow, promote longevity the effect of.Cure mainly have a dizzy spell, have a sleepless night, traumatic injury, wound go out
Diseases such as blood, neurasthenia, hypertension, postconcussion syndrome etc..The researchs such as Huang Liya show RADIX ET RHIZOMA TRILLII anti-aging effects
With enhancing brain tissue SOD, GSH-Px activity, it is relevant to reduce MDA accumulations.Also document finds that RADIX ET RHIZOMA TRILLII can significantly improve
Left heart function after ischemia reperfusion injury, SOD and GSH-Px activity in blood can be improved, reduce MDA content.
Cryptogenin is a kind of steroid saponin, has the effect such as reducing blood lipid, anti-freezing, anti-oxidizing activities, from lily
Section plant Trillium tschonoskii Maxim rhizome, also has document from dioscorea nipponica (Dioscorea
Nipponica Mak.) etc. isolated cryptogenin in plant.
But the record of heart failure can not be treated in existing literature for cryptogenin.
The content of the invention
In the first aspect, the present invention provides a kind of medicine for treating heart failure, is pharmaceutical activity comprising cryptogenin
Composition.Medicine provided by the present invention be used for heart failure treatment or prevention when it is curative for effect, poisonous side effect of medicine is small, tool
There is extensive medical application prospect.
It is a further object to provide cryptogenin to prepare for preventing or treating in the medicine of heart failure
Application.
Inventor has found that cryptogenin can be obviously improved cardiac diastolic function, have positivity flesh by investigative test
Power acts on, and can be used for the treatment of heart failure particularly chronic heart failure.
The medicine of the present invention is suitably formulated into preparation, and these preparations are suitable to oral administration (such as tablet), for intestines
Inject outside stomach (as sterile solution or suspension), for body cavity or bone cavity local administration (such as aseptic injectable solution
Or suspension) form.
Generally, above-mentioned preparation can be prepared in a usual manner using pharmaceutical carriers or diluent.Include people's in treatment
In mammal, the daily dosage of compound of the invention is about 0.01 to 250mg/kg body weight, in stomach in oral administration
It is about 0.001 during external administration to 250mg/kg body weight.The usual daily dose of active component can in interior change in a big way, and
It will depend on various factors, such as disease severity, method of administration, the age of patient, body weight and sex, and can be by
Doctor rule of thumb determines.
The active component of the present invention can be used alone, but will generally be administered in the form of a pharmaceutical preparation, wherein described
Compound combines with pharmaceutically acceptable diluent or carrier.According to administering mode, the pharmaceutical preparation can include 0.05 to
99 %w/w, such as 0.10 to 50%w/w active component.
The pharmaceutical composition or pharmaceutical preparation can also contain selective additive, such as pharmaceutical acceptable carrier or dilute
Release agent, flavouring, sweetener, preservative, dyestuff, adhesive, dispersant, colouring agent, disintegrant, excipient, film forming agent, profit
Lubrication prescription, binder, edible oil or above two or a variety of any combinations.
Appropriate pharmaceutical acceptable carrier or diluent includes but is not limited to, ethanol, water, glycerine, propane diols, magnesium carbonate,
Potassium phosphate, vegetable oil, animal oil etc..
Appropriate adhesive includes but is not limited to, starch, gelatin, sugar, such as glucose, sucrose and lactose, natural and conjunction
It is tragacanth and natural plant gum, mosanom, carboxymethyl cellulose, hydroxypropyl methyl cellulose, poly- into gummy such as Arabic gum
Ethylene glycol, polyvinylpyrrolidone, wax etc..
Appropriate disintegrant includes but is not limited to, starch, methylcellulose, agar, bentonite, xanthans, starch glycolate
Sodium, PVPP etc..
Appropriate lubricant includes but is not limited to, enuatrol, odium stearate, stearyl fumarate, magnesium stearate, benzene first
Sour sodium, sodium acetate, sodium chloride etc..
Appropriate dispersant includes but is not limited to, synthesis and natural gum, such as natural plant gum, bassora gum, Arabic gum；Algae
Hydrochlorate, glucan, sodium carboxymethylcellulose, methylcellulose, polyvinylpyrrolidone and gelatin.
Appropriate film forming agent includes but is not limited to, hydroxypropyl methyl cellulose, ethyl cellulose and polymethacrylates.
Appropriate binder includes but is not limited to, the polyethylene glycol and propane diols of different molecular weight.
Appropriate colouring agent includes but is not limited to, iron oxides, titanium dioxide etc..
Appropriate edible oil includes but is not limited to, cottonseed oil, sesame oil, coconut oil and peanut oil.
The example of other additives includes but is not limited to, D-sorbite, talcum powder, stearic acid, calcium phosphate and polydextrose.
Tablet can comprise additionally in disintegrant and/or can be coated (for example, with enteric coating, or with coating agent such as hydroxyl
Propyl methocel is coated).
The present invention further provides the method for the pharmaceutical preparation for preparing the present invention, it is as defined above that it includes mixing
Compound and pharmaceutically acceptable diluent or inert carrier.
Pharmaceutical preparation for treating or preventing heart failure can be the above-mentioned medicine system for including cryptogenin of the present invention
Agent, such as its tablet, capsule or supensoid agent, the cryptogenin tablet is preferably its sustained-release tablet, the cryptogenin glue
Wafer is preferably its Duracaps.
The present invention compared with prior art, has advantage following prominent：
1) after cryptogenin use, there is positive inotropic action to heart, strengthen myocardial contractive power, increase coronary flow
Amount, cardiac muscle cell is protected, improve cardiac function.Can be obviously improved the hemodynamics disturbance of patients with heart failure, improve heart function and
Left ventricular remodeling.The present invention can effectively treat heart failure, correct hemodynamics disturbance, improve the heart function of heart failure person, improve
Short term effect；Exhaustion cardiac muscle remodeling ventricle can be reversed, so as to the prognosis at a specified future date for the person that improves heart failure；Also prompting can prolonged application
And non-evident effect.
2) cryptogenin is the active component extracted in natural plants, and it is used for secondary work during the treatment or prevention of heart failure
With low, the compliance height of patient, so as to strengthen the therapeutic effect of medicine.
Embodiment
The present invention is further illustrated below by way of specific embodiment, but those skilled in the art should know the tool of the present invention
Body embodiment is not limit the invention in any way, and any equivalent substitution made on the basis of the present invention is each fallen within
Protection scope of the present invention.
Therapeutic action of the cryptogenin of embodiment 1 to congestive heart failure model in rats
This experiment mainly influence of the observation cryptogenin to heart failure rat model.
The foundation of Heart Failure Wistar Rats model：
Experimental animal is male SD rat, in 10~12 weeks, body weight 250-300g mouse age, is tested by The 2nd Army Medical College dynamic
Thing center provides.Chronic heart failure model is established with aortic coaractation method.Rat is with 1% yellow Jackets (0.5ml/100g) abdominal cavity
Injecting anesthetic, dorsal position are fixed, go belly wool, sterilization, cut skin and muscle layer along abdomen median line, abdominal aorta is isolated, in kidney
After abdominal aorta is ligatured together with blunt nosed No. 9 probes (external diameter 0.7mm) above artery, syringe needle is carefully extracted out.It is postoperative intraperitoneal
Instillation penicillin, muscle layer and skin are sutured respectively.Ligature indwelling continues constriction abdominal aorta, increases afterload, progressively enters
Open up to heart failure.
Animal model and packet administration
According to above-mentioned modeling method modeling, the successful rat of modeling is randomly divided into following 5 groups, and normal control is set
Group, every group 10, raise under standard environment.Each group administering mode is as described below：
Normal group：Gavage gives the physiological saline of same volume；
Model group：Gavage gives the physiological saline of same volume；
High group of cryptogenin：Gavage gives 50mg；
Low group of cryptogenin：Gavage gives 25mg；
Captopril group：Gavage gives 30mg；
Each group gastric infusion, is administered once a day, successive administration 4 weeks, and administration determines heart as follows after terminating
Hemodynamic parameter.The assay method of cardiac hemodynamic：With 1% Nembutal sodium solution according to 30mg/kg dosage abdomens
Chamber injecting anesthetic, diagonal otch is done in right common carotid artery, insertion is full of the PE-50 polyethylene catheters of heparin-saline,
Ventricular chamber is slowly inserted into, stable waveform is recorded and obtains LVSP, LVEDP, +/- dp/ using BL-420 softwares calculating waveform
The achievement datas such as dtmax.
3rd, experimental result
Therapeutic effect of the 1 each administration group of table to rat chronic heart failure model
Compared with normal group,##P ＜ 0.01；Compared with model group,*P ＜ 0.05,**P ＜ 0.01；
As can be seen from Table 1：Compared with normal group, the index such as its LVSP, LVEDP, ± dp/dtmax is respectively provided with model group
The difference of conspicuousness, Chronic heart failure model modeling success.Compared with model group, Captopril group and cryptogenin group have
Play the role of to reduce LVEDP and rise ± dp/dtmax, in the influence for LVSP, cryptogenin group shows to raise
Effect, shows that cryptogenin can be used for the therapeutic action of chronic heart failure.In addition, to reduce model group big for cryptogenin
The LVEDP and rise ± dp/dtmax of mouse, hence it is evident that improve cardiac diastolic function.Cryptogenin can significantly improve these indexs,
Show that it has positive inotropic action.
Embodiment 2
The present invention is studied heart function, the blood plasma BNP of the drug therapy heart failure patient of the present invention.By 60 hearts
Force failure patient is randomly divided into two groups, and control group (30) gives doctor trained in Western medicine routine heart failure resistance to treat, and treatment group (30) takes
Cryptogenin, two groups of courses for the treatment of are 8 weeks；With B ultrasound detection Left Ventricular Ejection Fraction (LVEF), the often amount of fighting (SV), cardiac output
(CO), E/A values, measure serum heart failure quantitative marker (BNP) is horizontal, and evaluates clinical efficacy.As a result treatment group, right is found
Heart function curative effect total effective rate according to group is respectively 86.67%, 46.67%, statistically significant (the P ＜ of Different therapeutical effect between group
0.01).After two groups of treatments, BNP levels decline (P ＜ 0.05, P ＜ 0.01) before relatively treating, and BNP water after treatment group's treatment
It is flat to be less than control group (P ＜ 0.01).Two groups of LVEF, SV, CO improve (P ＜ 0.05) after treatment, and after treatment group's treatment
LVEF, SV, CO, E/A value improve and are better than control group (P ＜ 0.05, P ＜ 0.01).
The pretherapy and post-treatment blood plasma BNP of 2 two groups of table compares
The pretherapy and post-treatment echocardiography results contrast of 14 two groups of table
Above-mentioned treatment results show that cryptogenin has the function that good treatment heart failure.
Claims (7)
1. a kind of medicine for treating heart failure, it is active constituents of medicine comprising cryptogenin.
2. medicine as claimed in claim 1, it is characterised in that cryptogenin oral administration amount is 0.01 to 250mg/kg bodies
Weight.
3. medicine as claimed in claim 2, it is characterised in that the cryptogenin be in parenteral about 0.001 to
250mg/kg body weight.
4. medicine as claimed in claim 1, it is characterised in that the cryptogenin is oral formulations.
5. medicine as claimed in claim 4, it is characterised in that the oral formulations of the cryptogenin are its tablet, capsule
Or supensoid agent.
6. cryptogenin is preparing the application in being used to prevent or treat the medicine of heart failure.
7. application as claimed in claim 7, it is characterised in that described heart failure is chronic heart failure.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710127199.8A CN107375310A (en) | 2017-03-06 | 2017-03-06 | Cryptogenin is preparing the purposes in treating heart failure drugs |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710127199.8A CN107375310A (en) | 2017-03-06 | 2017-03-06 | Cryptogenin is preparing the purposes in treating heart failure drugs |
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| Publication Number | Publication Date |
|---|---|
| CN107375310A true CN107375310A (en) | 2017-11-24 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710127199.8A Pending CN107375310A (en) | 2017-03-06 | 2017-03-06 | Cryptogenin is preparing the purposes in treating heart failure drugs |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101791365A (en) * | 2010-03-10 | 2010-08-04 | 深圳市药品检验所 | Discorea nipponica makino extractive and application thereof in preparing medicaments for resisting free radicals and reducing blood fat |
| CN104288168A (en) * | 2013-07-17 | 2015-01-21 | 吉林敖东洮南药业股份有限公司 | Application of trillin in preparation of drug used for treating and/or preventing diseases mediated by microglial cells |
-
2017
- 2017-03-06 CN CN201710127199.8A patent/CN107375310A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101791365A (en) * | 2010-03-10 | 2010-08-04 | 深圳市药品检验所 | Discorea nipponica makino extractive and application thereof in preparing medicaments for resisting free radicals and reducing blood fat |
| CN104288168A (en) * | 2013-07-17 | 2015-01-21 | 吉林敖东洮南药业股份有限公司 | Application of trillin in preparation of drug used for treating and/or preventing diseases mediated by microglial cells |
Non-Patent Citations (1)
| Title |
|---|
| 陈显兵等: "延龄草正丁醇萃取物对大鼠非酒精性脂肪性肝病的改善作用及对抗氧化酶活性和肝内质网应激的影响", 《中国药理学与毒理学杂志》 * |
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Application publication date: 20171124 |
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