CN101411697A - Medicinal composition for treating angiocardiopathy - Google Patents
Medicinal composition for treating angiocardiopathy Download PDFInfo
- Publication number
- CN101411697A CN101411697A CNA200810223045XA CN200810223045A CN101411697A CN 101411697 A CN101411697 A CN 101411697A CN A200810223045X A CNA200810223045X A CN A200810223045XA CN 200810223045 A CN200810223045 A CN 200810223045A CN 101411697 A CN101411697 A CN 101411697A
- Authority
- CN
- China
- Prior art keywords
- probucol
- fenofibrate
- described compositions
- compositions
- pharmaceutical composition
- 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.)
- Pending
Links
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention relates to a medicament composition for treating cardiovascular diseases. The composition contains Fenofibrate, Probucol and pharmaceutically acceptable carrier or excipient with effective dose for treating.
Description
Technical field
The present invention relates to the Drug therapy field, more specifically to the pharmaceutical composition of treatment cardiovascular disease.
Background technology
In China, cardiovascular and cerebrovascular disease is causing death's first cause of disease.Along with growth in the living standard, people's dietary structure changes, and activity reduces, and the intake of cholesterol and Body Mass Index are all increasing, and these all are the risk factors that causes cardiovascular and cerebrovascular disease.China recent years cardiovascular and cerebrovascular disease sickness rate rises year by year.
Hypertension in the cardiovascular disease, myocardial infarction and angina pectoris are one of modal causes of the death of masculinity and femininity.Except the arteria coronaria disease, cerebrovascular and apoplexy also are modal cause of the death diseases.In addition, the cardiovascular diseases causes that being derived from apoplexy, congestive heart failure, peripheral vascular disease, venous insufficiency and multi-infarct dementia significantly disables.Most of cardiovascular diseasess are atherosclerotic direct results.
Multiple medicine can be used for the treatment of cardiovascular disease.Can not obtain at single medicine under the situation of ideal treatment, compound recipe and medication combined application often are used to the clinical treatment cardiovascular disease.The present invention relates to treat the fenofibrate of cardiovascular disease and the pharmaceutical composition of probucol.
Fenofibrate, English Fenofibrate by name, its chemistry 2-methyl-2-(4-(4-chlorobenzene formacyl) phenoxy group) isopropyl propionate by name.Chemical structural formula is as follows:
Fenofibrate is a chlorine shellfish butanoic acid derivative class blood lipid regulation medicine, also its catabolism is increased by the generation that suppresses very low density lipoprotein (VLDL) and triglyceride, reduces blood low density lipoprotein, LDL, cholesterol and triglyceride; ApoA 1 and A11 are generated to be increased, thus high density lipoprotein increasing.Fenofibrate still has the blood uric acid effect that reduces normal person and hyperuricemia patient.The clinical unfavorable hyperlipemia of adult's diet control therapy effect that is used for the treatment of of fenofibrate, its triglyceride reducing and combined hyperlipidemia familial effect are obvious than the cholesterol effect.
After fenofibrate was oral, gastrointestinal absorption was good, with clothes the absorption of fenofibrate was increased with food.About 4-7 hours blood drug level peakings in oral back.Half-life α and half-life β were respectively 4.9 hours and 26.6 hours behind the single oral dose, and apparent volume of distribution is 0.9L/kg; Half-life β is 21.7 hours behind the continued treatment.Plasma protein binding rate is approximately 99%, does not find behind the multiple dose administration to accumulate.It is many to absorb back distribution in liver, kidney, intestinal, is lung, the heart and adrenal gland secondly, has a small amount of in testis, spleen, skin.In liver and the nephridial tissue intracellular metabolite, through carboxyl reduction and glucuronic acidization, metabolite is in the great majority with the glucuronic acid product, through the radiation labelling, about 60% metabolite is arranged through renal excretion, and 25% metabolite is through the stool discharge.The elimination half-life of this product is 20 hours, therefore administration once a day.Studies show that the Insufficient patient of severe renal significantly descends to the clearance rate of this product, long-term prescription can cause to be accumulated.
Probucol, English name: Probucol; Chemistry is by name: 4,4 '-[(1-methyl ethylidene) two (sulfur)]-two [2, two (1, the 1-dimethyl ethyl) phenol of 6-].Its chemical structural formula is as follows:
Probucol is the blood lipid regulation medicine and has study of anti-atherogenic effect.Its effect for reducing fat is with promoting cholesterol decomposition cholesterolemia and low density lipoprotein, LDL to be reduced by cholesterol reducing is synthetic, also changes the character and the function of high density lipoprotein hypotype, and the blood HDL-C is lowered.Probucol is little to the influence of blood triglyceride.Probucol has significant antioxidant role, can suppress the formation of foam cell, delays the formation of atheromatous plaque, and established atheromatous plaque disappears.The clinical hypercholesterolemia that is used for the treatment of of probucol.
Probucol is limited and irregular through gastrointestinal absorption, as making its absorption reach maximum with food with clothes.Reached the blood drug level peak value in 18 hours after once oral this product, T1/2 is 52-60 hour.Obey this product every day, blood drug level increases gradually, and 3-4 reached steady-state level in individual month.This product produces metabolite in vivo.84% of oral dose is discharged from feces, and 1%-2% discharges from urine, in the feces based on original shape, in the urine based on metabolite.
Therefore probucol is almost insoluble in water, probucol can't be made injection, adopts solid preparation such as tablet to be applied to clinical usually.Probucol is difficult to be absorbed into blood, nearly all drains with original shape.On the other hand, the absorption rate of probucol and absorbtivity are obvious at the individual patients differences.Research worker is improved the method that probucol absorbs and reduce absorption difference between individuality in research always.
Summary of the invention
The present invention relates to a kind of pharmaceutical composition for the treatment of cardiovascular disease.Compositions of the present invention contains fenofibrate, probucol and acceptable accessories.Combination treatment cardiovascular disease of the present invention not only can improve the separately effect of treatment of fenofibrate and probucol, and has synergism, preparation of pharmaceutical compositions of the present invention is become the compliance that can improve patient after the pharmaceutical preparation.
Pharmaceutical composition of the present invention contains the fenofibrate as active component.The pharmaceutical composition of the present invention of per unit preparation contains the fenofibrate of 20mg-500mg.Preferred 50mg-200mg, more preferably 100mg.
Pharmaceutical composition of the present invention contains the probucol as active component.The pharmaceutical composition of the present invention of per unit preparation contains the probucol of 0.1g-1g.Preferred 0.2g-0.5g, more preferably 0.5g.
Acceptable accessories in the pharmaceutical composition of the present invention can be anyly can be prepared into pharmaceutical preparation with fenofibrate and probucol, and be used for the adjuvant of clinical treatment.Adjuvant of the present invention includes but not limited to: filler, wetting agent and adhesive, disintegrating agent, lubricant etc.Filler comprises lactose, microcrystalline Cellulose, starch, Icing Sugar, dextrin, mannitol, calcium sulfate etc.The preferred lactose of filler, microcrystalline Cellulose.Wetting agent and adhesive comprise sodium carboxymethyl cellulose, hydroxypropyl cellulose, hydroxypropyl emthylcellulose, gelatin, sucrose, polyvinylpyrrolidone etc.The preferred hydroxypropyl cellulose of wetting agent and adhesive, hydroxypropyl emthylcellulose.Disintegrating agent comprises carboxymethyl starch sodium (CMS-Na), crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose etc.The preferred carboxymethyl starch sodium of disintegrating agent (CMS-Na).Lubricant comprises magnesium stearate, micropowder silica gel, Pulvis Talci, hydrogenated vegetable oil, Polyethylene Glycol, magnesium laurylsulfate etc.The preferred magnesium stearate of lubricant, Pulvis Talci.
Pharmaceutical composition of the present invention preferably contains one or more acceptable accessories in lactose, microcrystalline Cellulose, corn starch, pregelatinized Starch, hydroxypropyl cellulose, hydroxypropyl emthylcellulose, titanium dioxide, magnesium stearate, Pulvis Talci, ferrum oxide, the sodium carboxymethylstarch except that containing fenofibrate and probucol.
Pharmaceutical composition of the present invention is by preparing fenofibrate, probucol and mixing acceptable accessories.The preferred oral administration drug treatment of pharmaceutical composition of the present invention cardiovascular disease.The pharmaceutical composition of the present invention of oral administration administration can adopt dosage forms such as being prepared into conventional tablet, granule, capsule, powder, slow releasing tablet.Be preferably conventional tablet or capsule.Pharmaceutical composition of the present invention can adopt technology commonly used in the pharmaceutical preparation to be prepared into tablet and capsule.
" unit formulation " of description of the present invention refers to the minimum individual of every kind of dosage form, as " sheet " of tablet, capsular " grain ".
The specific embodiment
Embodiment 1
Prescription (per 1000):
Fenofibrate 100g
Probucol 500g
Carboxymethyl starch sodium 50g
Corn starch 3000g
Magnesium stearate 300g
Fenofibrate, probucol are crossed 40 mesh sieves.According to recipe quantity with fenofibrate, probucol and corn starch, the abundant mixing of carboxymethylstach sodium, and with the magnesium stearate mixing after tabletting, promptly.
Embodiment 2
Prescription (per 1000):
Fenofibrate 100g
Probucol 500g
Carboxymethyl starch sodium 50g
Lactose 1000g
Magnesium stearate 200g
Fenofibrate, probucol are crossed 40 mesh sieves.According to recipe quantity with fenofibrate, probucol and lactose, the abundant mixing of carboxymethylstach sodium, and with the magnesium stearate mixing after tabletting, promptly.
Embodiment 3
Prescription (per 1000):
Fenofibrate 100g
Probucol 500g
Sodium Hydroxymethyl Stalcs 40g
Gonak (1%) 50g
Microcrystalline Cellulose 800g
Magnesium stearate 200g
Fenofibrate, probucol are crossed 80 mesh sieves.According to recipe quantity with fenofibrate, probucol and microcrystalline Cellulose, the abundant mixing of carboxymethylstach sodium after, Gonak with recipe quantity prepares soft material, granulate, oven dry, 18 mesh sieve granulate, with encapsulated behind the abundant mixing of magnesium stearate of recipe quantity, promptly.
Claims (7)
1. a pharmaceutical composition for the treatment of cardiovascular disease contains fenofibrate, probucol and acceptable accessories.
2. the described compositions of claim 1, wherein per unit preparation medicine compositions contains fenofibrate 20mg-500mg, probucol 0.1g-1g.
3. the described compositions of claim 1, wherein per unit preparation medicine compositions contains fenofibrate 50mg-200mg, probucol 0.2g-0.5g.
4. the described compositions of claim 1, wherein per unit preparation medicine compositions fenofibrate 100mg, probucol 0.5g.
5. any described compositions of claim 1-4, wherein acceptable accessories comprises one or more in filler, wetting agent and adhesive, disintegrating agent, the lubricant.
6. the described compositions of claim 5, wherein filler is lactose or microcrystalline Cellulose, and wetting agent and adhesive are hydroxypropyl cellulose or hydroxypropyl emthylcellulose, and disintegrating agent is that carboxymethyl starch sodium, lubricant are magnesium stearate or Pulvis Talci.
7. any described compositions of claim 1-4, wherein acceptable accessories comprises one or more in lactose, microcrystalline Cellulose, corn starch, pregelatinized Starch, hydroxypropyl cellulose, hydroxypropyl emthylcellulose, titanium dioxide, magnesium stearate, Pulvis Talci, ferrum oxide, the sodium carboxymethylstarch.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200810223045XA CN101411697A (en) | 2008-09-26 | 2008-09-26 | Medicinal composition for treating angiocardiopathy |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200810223045XA CN101411697A (en) | 2008-09-26 | 2008-09-26 | Medicinal composition for treating angiocardiopathy |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101411697A true CN101411697A (en) | 2009-04-22 |
Family
ID=40592577
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA200810223045XA Pending CN101411697A (en) | 2008-09-26 | 2008-09-26 | Medicinal composition for treating angiocardiopathy |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101411697A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103301095A (en) * | 2012-03-13 | 2013-09-18 | 中国科学院上海药物研究所 | Porous composite medicine-loaded composition for improving oral absorption for probucol, and preparation method of porous composite medicine-loaded composition |
| CN105251010A (en) * | 2015-10-30 | 2016-01-20 | 钟霞 | Medicinal composition for treating atherosclerosis and preparation method of medicinal composition |
-
2008
- 2008-09-26 CN CNA200810223045XA patent/CN101411697A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103301095A (en) * | 2012-03-13 | 2013-09-18 | 中国科学院上海药物研究所 | Porous composite medicine-loaded composition for improving oral absorption for probucol, and preparation method of porous composite medicine-loaded composition |
| CN103301095B (en) * | 2012-03-13 | 2016-04-13 | 中国科学院上海药物研究所 | The composite drug-loaded composition and method of making the same of a kind of porous for improving probucol oral absorption |
| CN105251010A (en) * | 2015-10-30 | 2016-01-20 | 钟霞 | Medicinal composition for treating atherosclerosis and preparation method of medicinal composition |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN103181552A (en) | Health care food for regulating blood lipid and preparation method thereof | |
| CN102008477B (en) | Method for preparing tablet drug composition containing Rosuvastatin calcium | |
| CN102357096A (en) | Statins zinc salt-containing blood fat-reducing composite | |
| KR20200135739A (en) | Herbal complex medication used in manufacture of pharmaceutical composition for improving metabolism of cholesterol and triglyceride | |
| CN101658519B (en) | Medicinal composition for treating hyperuricemia | |
| CN101411697A (en) | Medicinal composition for treating angiocardiopathy | |
| CN108272814A (en) | A kind of composition and its application containing cordycepin | |
| US6890941B1 (en) | Compositions containing HMG Co-A reductase inhibitors and policosanol | |
| CN101757019B (en) | Medical composition for losing weight or treating metabolic syndromes | |
| CA2534660A1 (en) | Single unit pharmaceutical composition comprising a mixture of a fibrate and an homocysteine reducing agent | |
| CN101756993B (en) | Medical composition for losing weight or treating metabolic syndromes | |
| CN101297825B (en) | Compound formulation of ginkgo leaf extract | |
| CN101411703A (en) | Medicinal composition for treating angiocardiopathy | |
| CN100531729C (en) | Composition containing fibrate drug and taurine | |
| CN100364553C (en) | Natural medicinal composition for preparing diabete drug | |
| CN102349906B (en) | Atorvastatin calcium and nicotinic acid composition and preparation method thereof | |
| CN101455842A (en) | Medicine composition of HMG-CoA reductase inhibitor and probucol | |
| CN1969855B (en) | Pharmaceutical composition having target organ protection function and usage thereof | |
| CN104840480B (en) | Metformin/folic acid/vitamin B12New application of pharmaceutical composition | |
| CN101559057A (en) | Drug compound for curing hyperlipoidemia and preparation method thereof | |
| CN102516166A (en) | Nicotinic acid derivative of fenofibrate and preparation method of nicotinic acid derivative | |
| CN101502516B (en) | Glipizide enteric-coated formulation composition and method for preparing the same | |
| CN101543628A (en) | Medicament and preparation thereof for treating hyperlipemia and atherosclerosis | |
| CN1814197A (en) | Application of alpha-amylase inhibitor in preparation of medicine for preventing and treating hyperlipidemia and atherosclerosis | |
| CN100358526C (en) | Composite for treating hyperlipidemia |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Open date: 20090422 |