CN101897708A - Sustained-release composition for treating blood lipid dysbolism - Google Patents
Sustained-release composition for treating blood lipid dysbolism Download PDFInfo
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- CN101897708A CN101897708A CN2009100855649A CN200910085564A CN101897708A CN 101897708 A CN101897708 A CN 101897708A CN 2009100855649 A CN2009100855649 A CN 2009100855649A CN 200910085564 A CN200910085564 A CN 200910085564A CN 101897708 A CN101897708 A CN 101897708A
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- nicotinic acid
- aspirin
- compositions
- slow releasing
- release
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Abstract
The invention provides a sustained-release composition for treating dyslipidemia. The slow-release composition comprises a double-layer tablet consisting of a nicotinic slow-release part and an aspirin quick-release part. The sustained-release composition more effectively reduces side effects and provides conveniences for a patient to take while bringing the therapeutic effect of nicotinic acid into play.
Description
Technical field
The present invention relates to a kind of compositions that contains slow release and aspirin, said composition is a double-layer tablet.
Background technology
Dyslipidemia and atherosclerosis (AS) especially with the relation of coronary heart disease (CHD) after deliberation century nearly, in recent years, the research of this respect is very active, more and more studies show that, hyperlipidemia is one of risk factor of CHD morbidity unusually.Therefore, must take necessary means, to reduce the sickness rate of relevant disease to the important risk factor lipid metabolic disorder that causes the heart, cerebrovascular disease, hypertension, diabetes.
Nicotinic acid is Nicotinicum Acidum again, belongs to vitamin B group, the molecular formula of nicotinic acid: C
6H
5NO
2, molecular weight: 123.11, structural formula:
It is unusual that nicotinic acid is used for the treatment of lipoprotein metabolism, and nicotinic acid is that unique known at present can make all lipids substantially towards the chemical compound of correct direction development.Its maximum effect is to increase high density lipoprotein (HDL), main triglyceride reducing (TMG), and (TC) also has the reduction effect to cholesterol.Studies show that nicotinic acid can reduce the mortality rate of the incidence rate and the coronary heart disease of myocardial infarction.But the untoward reaction of nicotinic acid is many, has limited its clinical practice.Heavy dose of nicotinic acid on probation, flushing and liver toxic and side effects often appear, for this reason, developed niacin sustained-release preparation,, the appearance of flushing side effect has been arranged when finding still to be in the use though this scheme decreases the incidence rate of flushing, general clinical recommendation is, before taking the nicotinic acid medicine, take nonsteroidal anti-inflammatory agent such as aspirin, alleviate or prevent to take the side effect of face's flushing that nicotinic acid brings.
Report is arranged, and nicotinic acid and aspirin drug combination have synergism, also can reduce the incidence rate and the occurrence degree of face's flushing to the blood vessel dilating effect of antiniacin.Two medicines share the activity of the blood plasma LPL that can significantly raise, and the effect that reduces TG is better than single effect with nicotinic acid.Aspirin can suppress epoxidase, is TXA2 and that minimizing of planning, share with nicotinic acid, has both brought into play their blood fat reducing and antiplatelet effect separately, can overcome the side effect of the blood vessel dilating of nicotinic acid again.
We study niacin sustained release part and aspirin is made double-layer tablet, have removed the inconvenience that patient's gradation is taken medicine, and the while has been reduced incidence rate and the occurrence degree of taking face's flushing that niacin preparation brings again.
Summary of the invention
A kind of preparation technology is simple, curative effect is reliable in order to provide.The compositions of the treatment dyslipidemia that side effect is little, pharmaceutical composition of the present invention is made up of two-layer, and one deck is the slow release nicotinic acid of clinical effective dose, and another layer is for containing the aspirin release layer.
Gel skeleton material that adds in the niacin sustained release layer or water-insoluble controlled release fertilizer adjuvant.Used adjuvant is the adjuvant of accepting on the preparation.
Absorb the effect of playing prevention in order before the release of nicotinic acid, just there to be aspirin to discharge, in double-layer tablet, skin is the aspirin release layer, and internal layer is the niacin sustained release layer, the preparation process is that repress was made for double-layer tablet after nicotinic acid and aspirin were granulated respectively, and concrete technical scheme is as described below:
1. get nicotinic acid and aspirin and cross 100 mesh sieves respectively, remaining adjuvant is crossed 80 mesh sieves respectively, and is standby.
2. nicotinic acid and slow-release auxiliary material and or conventional mixing diluents cross 60 mesh sieve mix homogeneously, add binding agent or the mixed soft material of wetting agent, cross 16 mesh sieves and granulate.
3. granule is 60 ℃ of dryings 2 hours, takes out to add lubricant or fluidizer mixes, and crosses 18 mesh sieve granulate, the niacin sustained release granule.
4. get aspirin and mixing diluents in addition, add binding agent or the mixed soft material of wetting agent, cross 16 mesh sieves and granulate, granule is 60 ℃ of dryings 2 hours, takes out to add lubricant or fluidizer mixes, and crosses 18 mesh sieve granulate, aspirin granule.
5. measure the particulate content of two parts respectively, determine every layer of weight, the compacting double-layer tablet.
The specific embodiment
The following examples are used to describe in detail the present invention, without any the limitation of the present invention effect on the meaning.
Embodiment 1
Prescription
Technical process: get nicotinic acid, aspirin and cross 100 mesh sieves respectively, all the other adjuvants are crossed 80 mesh sieves respectively, and are standby.Get nicotinic acid, HPMC, polyvidone, the mixing of recipe quantity, add 70% ethanol system soft material, cross 16 mesh sieves and granulate; Granule 60 ℃ dry 2 hours down, take out the back and add stearic acid and mix, cross 18 mesh sieve granulate, the nicotinic acid granule; Aspirin, starch, lactose that other gets recipe quantity mix, and add 70% ethanol system soft material, cross 16 mesh sieves and granulate, and granule is dry under 60 ℃, take out to add the stearic acid mixing, cross 18 mesh sieve granulate, get aspirin granule; Detect two kinds of particulate medicament contgs respectively, determine every layer weight, the compacting double-layer tablet.
Embodiment 2
Prescription:
Technical process is with embodiment 1.
Embodiment 3
Prescription:
Technical process is with embodiment 1.
Embodiment 4
Prescription:
Technical process is with embodiment 1.
Embodiment 5
Prescription:
Technical process is with embodiment 1.
Embodiment 6
Nicotinic acid is put method (Chinese Pharmacopoeia version appendix in 2005) according to drug release determination, adopt the device of dissolution method second method, (dissolving 1.38g sodium dihydrogen phosphate is to the water of 900ml with phosphate buffer, regulating pH to 7.0 with the sodium hydroxide of 1M, be diluted with water to 1000ml, shake up promptly) 900ml is solvent, rotating speed is that per minute 50 changes, operation in accordance with the law, the release of the sample of mensuration embodiment 1-5, the result is as follows:
The cumulative release degree (%) of embodiment sample
Claims (6)
1. slow releasing composition for the treatment of dyslipidemia is made up of nicotinic acid and aspirin and pharmaceutically acceptable other adjuvants.
2. the described compositions of claim 1, the content range that it is characterized in that nicotinic acid is 500mg to 1000mg, the content range of aspirin is 300mg to 500mg.
3. the described compositions of claim 1 is characterized in that compositions gives with the dosage form of double-layer tablet.
4. the compositions that requires of claim 3 is characterized in that in the double-layer tablet that one deck contains nicotinic acid and acceptable slow releasing preparation adjuvant pharmaceutically, and another layer contains aspirin and pharmaceutically acceptable rapid release or slow releasing preparation adjuvant.
5. claim 1 or 4 compositionss that require is characterized in that said rapid release or slow releasing preparation adjuvant comprise hydrophilic gel matrix material or water-insoluble framework material.
6. the compositions of claim 5 requirement is characterized in that hydrophilic gel matrix material includes carbomer, hydroxypropyl methylcellulose and polyacrylamide base polymer; Insoluble framework material comprises: ethyl cellulose, higher fatty acids, alcohol, glyceryl monostearate etc.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009100855649A CN101897708A (en) | 2009-05-25 | 2009-05-25 | Sustained-release composition for treating blood lipid dysbolism |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009100855649A CN101897708A (en) | 2009-05-25 | 2009-05-25 | Sustained-release composition for treating blood lipid dysbolism |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101897708A true CN101897708A (en) | 2010-12-01 |
Family
ID=43223851
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2009100855649A Pending CN101897708A (en) | 2009-05-25 | 2009-05-25 | Sustained-release composition for treating blood lipid dysbolism |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101897708A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014179845A1 (en) * | 2013-05-09 | 2014-11-13 | Zeenar Enterprises Pty Ltd | Niacin formulation |
-
2009
- 2009-05-25 CN CN2009100855649A patent/CN101897708A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014179845A1 (en) * | 2013-05-09 | 2014-11-13 | Zeenar Enterprises Pty Ltd | Niacin formulation |
| US10105358B2 (en) | 2013-05-09 | 2018-10-23 | Zeenar Enterprises Pty Ltd | Niacin formulation |
| US10335403B2 (en) | 2013-05-09 | 2019-07-02 | Zeenar Enterprise Pty Ltd | Niacin formulation |
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| PB01 | Publication | ||
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Open date: 20101201 |