CN105310994A - Compound nicotinic acid slow-release tablet and preparation method thereof - Google Patents
Compound nicotinic acid slow-release tablet and preparation method thereof Download PDFInfo
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- CN105310994A CN105310994A CN201410307889.8A CN201410307889A CN105310994A CN 105310994 A CN105310994 A CN 105310994A CN 201410307889 A CN201410307889 A CN 201410307889A CN 105310994 A CN105310994 A CN 105310994A
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- nicotinic acid
- lovastatin
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Abstract
The invention discloses a compound nicotinic acid slow-release tablet which includes a nicotinic acid layer, a lovastatin layer and a thin film coat. The nicotinic acid layer includes 500 parts of nicotinic acid, 320-400 parts of stearic acid, 90-120 parts of hydroxypropylmethyl cellulose, 2-10 parts of silicon dioxide and 2-10 parts of magnesium stearate; the lovastatin layer includes 20 parts of lovastatin, 20-80 parts of microcrystalline cellulose, 5-10 parts of crosslinked carboxymethyl cellulose sodium, 5-15 parts of 10% povidone k30 and 50% ethanol, and 0.5-1 part of magnesium stearate; the thin film coat includes 5-10 parts of hydroxypropylmethyl cellulose, 0.1-1 part of polyethylene glycol 6000, 1-5 parts of propylene glycol, 2-8 parts of titanium dioxide and 70-90 parts of 80% ethanol ester. The invention also discloses a preparation method of the compound nicotinic acid slow-release tablet. The compound nicotinic acid slow-release tablet conforms to the specification in the second section in the "Chinese Pharmacopoeia" (2010 edition), is stable in composition, is good in slow-release effects and is low in production cost.
Description
Technical field
The present invention relates to medical art, particularly, relate to a kind of compound niacin sustained release tablet and preparation method thereof.
Background technology
In recent years, cardiovascular disease is as a class disease of serious harm human health, M & M is all the situation that obviously rises, add up according to World Health Organization (WHO), and the cardiovascular disease of more than 80% is caused by hyperlipemia, past the world of medicine's prevention and cure of cardiovascular disease stresses in the use of depressor, has successively invented many effective depressor, but along with the development of medical science, people recognize that hyperlipidemia is that coronary heart disease and hypertensive Major Risk Factors occur.Hyperlipemia initial stage majority does not have clinical symptoms, the infringement of this disease to health be concealment, gradually, Progressive symmetric erythrokeratodermia and general.Systemic atherosclerosis is accelerated in its direct infringement, because the vitals of whole body all will rely on tremulous pulse blood supply, oxygen supply, once tremulous pulse is blocked by atheromatous plaque, will cause serious consequence.The renal failure etc. that arteriosclerosis causes, all closely related with hyperlipemia.A large amount of research data shows, hyperlipemia is apoplexy, coronary heart disease, myocardial infarction, cardiac sudden death independently important risk factor.In addition, hyperlipemia is also the important risk factor promoting hypertension, impaired glucose tolerance, diabetes.Hyperlipemia also can cause fatty liver, liver cirrhosis, cholelithiasis, pancreatitis, retinal hemorrhage, blind, peripheral vascular disease, limping, hyperuricemia.Also can there is xanthoma, arcus juvenilis etc. around tendon shape, nodositas, palm plane and eye socket in some constitutional and familial hyperlipidemia patient; Therefore, as the research and development of the medicine for the treatment of hyperlipemia, the emphasis in drug research field is become.
Nicotinic acid is a kind of water soluble vitamins, and after being converted into nicotiamide in vivo, play pharmacological action, the latter is nadide and coenzyme II ingredient, participates in HypercholesterolemicRats, and the oxidizing process of Tissue respiration and sugar are without the process of decomposing.Nicotinic acid also can reduce the utilization of coenzyme A; Affect the synthesis of cholesterol by suppressing the synthesis of density protein, heavy dose of concentration that still can reduce serum cholesterol and triglyceride, and have peripheral vasodilation effect; Lovastatin (Lovastatin) has been listed in China's national essential drugs, it is a kind of HMG-CoA reductase inhibitor, its action character: (1) stops the synthesis of endogenous cholesterol, reduces low-density, extra-low density and intermediate density lipoprotein (IDL) (LDL, VLDL, TDL) in blood; (2) can slight high density lipoprotein increasing (HDL), few side effects and light; Be mainly used in heterozygous familial hypercholesterolemia, severe primary hypercholesterolemia, light-duty primary hypercholesterolemia etc. clinically.By the compound preparation that lovastatin and nicotinic acid form, from result of the test, its lipid-lowering effect is very good, be better than any one of two kinds of composition medicines, and side effect does not increase, therefore, preparation research of the two combination is we a medical scientific research worker difficult problem anxious to be resolved.
Chinese patent 200510112698.7 " compound niacin sustained release preparation ", disclose preparation method nicotinic acid and lovastatin being prepared into slow releasing capsule, this patent system standby compound nicotinic acid slow releasing capsule niacin sustained release part release too fast, within 12 hours, reach the release of more than 90%, although meet the requirement of slow releasing preparation to a certain extent, but in Clinical practice, not fine to the compliance of patient medication, need to take twice in one day, to a lot of patient particularly gerontal patient, easily forget and take, if can in slow-releasing medicated adjuvant, further excavation, the number of times of taking made reduces, will to compound niacin preparation at Clinical practice, bring huge change.
Summary of the invention
In order to overcome the deficiencies in the prior art, the object of the present invention is to provide one to meet in " Chinese Pharmacopoeia " 2010 editions two and specify, component is stablized, had good sustained release effect, the compound niacin sustained release tablet that production cost is low; Another object of the present invention is to the preparation method that a kind of compound niacin sustained release tablet is provided, production technology is more stable, controlled, be easy to industrialization.
For solving the problem, the technical solution adopted in the present invention is as follows:
A kind of compound niacin sustained release tablet, comprise nicotinic acid layer, lovastatin layer and film-coat, described nicotinic acid layer comprises following parts by weight of component:
Described lovastatin layer comprises following parts by weight of component:
Described film-coat comprises following parts by weight of component:
Preferably, described compound niacin sustained release tablet comprises nicotinic acid layer, lovastatin layer and film-coat, and described nicotinic acid layer comprises following parts by weight of component:
Described lovastatin layer comprises following parts by weight of component:
Described film-coat comprises following parts by weight of component:
A preparation method for compound niacin sustained release tablet, comprises step:
(1) preparation of nicotinic acid granule
(1.1) stearic process, take stearic acid put in 80 DEG C of water-baths be heated to melt.
(1.2) mix, take nicotinic acid, hypromellose, silicon dioxide mix homogeneously, add in the stearic acid melted, be uniformly mixed.
(1.3) granulate.Granulate with 20 mesh sieves.
(1.4) dry.Wet granular is put in drying baker, bake out temperature 50 DEG C, air blast.
(1.5) granulate, mixing.20 mesh sieve granulate, add magnesium stearate, mix homogeneously.
(2) preparation of lovastatin granule
(2.1) preparation of supplementary material and pretreatment.Lovastatin crosses 120 mesh sieves.Microcrystalline cellulose excipients, cross-linked carboxymethyl cellulose sodium cross 100 mesh sieves respectively.
(2.2) preparation of bonding agent.Taking 10% polyvidone puts in volumetric flask, adds 50% alcoholic solution, stirring and dissolving, standardize solution.
(2.3) weighing of supplementary material.Pretreated lovastatin, microcrystalline Cellulose, cross-linked carboxymethyl cellulose sodium is taken by component ratio.
(2.4) mixing of adjuvant.Lovastatin and microcrystalline Cellulose, cross-linked carboxymethyl cellulose sodium progressively increase with equivalent and mix homogeneously, and cross 40 mesh sieve 6 times, obtain mixed powder.
(2.5) soft material processed.In mixed powder, add bonding agent, mix homogeneously, make soft material.
(2.6) granulate.20 mesh sieves are granulated.
(2.7) dry.Wet granular is put in drying baker, bake out temperature 60 DEG C, air blast.
(2.8) granulate, mixing.20 mesh sieve granulate.Add magnesium stearate, mix homogeneously.
(3) tabletting.With special-shaped punching press double-layer tablet (capsule-type).
(4) coating.Coating pan rotating speed 45 revs/min, blast temperature 50-55 DEG C, coating weight gain 4%.
Compared to existing technology, beneficial effect of the present invention is:
1. in the present invention, compound niacin sustained release tablet component is stablized, had good sustained release effect, can continue compound niacin blood drug level in holder and, effectively treating on concentration, ensure drug effect;
2. in the present invention, compound niacin sustained release tablet preparation cost is low, efficacy stability, significantly can reduce patient to former dependence of grinding medicine;
3. in the present invention the production technology of compound niacin sustained release tablet more stable, controlled, be easy to industrialization.
Detailed description of the invention
Below in conjunction with detailed description of the invention, the present invention is described in further detail.
Supplementary material involved in the present invention is existing product, and meets regulation in " Chinese Pharmacopoeia " 2010 editions two.
Embodiment 1-5
Compound niacin sustained release tablet is prepared according to following table 1 Raw proportioning:
Table 1, compound niacin sustained release tablet proportioning raw materials
For the compound niacin sustained release tablet of above-mentioned five embodiments, adopt following preparation method:
(1) preparation of nicotinic acid granule
(1.1) stearic process.Take stearic acid put in 80 DEG C of water-baths be heated to melt.
(1.2) mix.Take nicotinic acid, hypromellose, silicon dioxide mix homogeneously, add in the stearic acid melted, be uniformly mixed.
(1.3) granulate.Granulate with 20 mesh sieves.
(1.4) dry.Wet granular is put in drying baker, bake out temperature 50 DEG C, air blast.
(1.5) granulate, mixing.20 mesh sieve granulate.Add magnesium stearate, mix homogeneously.
(2) preparation of lovastatin granule
(2.1) preparation of supplementary material and pretreatment.Lovastatin crosses 120 mesh sieves.Microcrystalline cellulose excipients, cross-linked carboxymethyl cellulose sodium cross 100 mesh sieves respectively.
(2.2) preparation of bonding agent.Taking 10% polyvidone puts in volumetric flask, adds 50% alcoholic solution, stirring and dissolving, standardize solution.
(2.3) weighing of supplementary material.Pretreated lovastatin, microcrystalline Cellulose, cross-linked carboxymethyl cellulose sodium is taken by component ratio.
(2.4) mixing of adjuvant.Lovastatin and microcrystalline Cellulose, cross-linked carboxymethyl cellulose sodium progressively increase with equivalent and mix homogeneously, and cross 40 mesh sieve 6 times, obtain mixed powder.
(2.5) soft material processed.In mixed powder, add bonding agent, mix homogeneously, make soft material.
(2.6) granulate.20 mesh sieves are granulated.
(2.7) dry.Wet granular is put in drying baker, bake out temperature 60 DEG C, air blast.
(2.8) granulate, mixing.20 mesh sieve granulate.Add magnesium stearate, mix homogeneously.
(3) tabletting.
By special-shaped punching press double-layer tablet.
(4) coating
Coating pan rotating speed 45 revs/min, blast temperature 50-55 DEG C, coating weight gain 4%.
Release degree of niacin test is carried out to the compound niacin sustained release tablet of appeal embodiment
To compound niacin sustained release tablet in embodiment 1-5, the release of the spectrophotometry compound niacin specified according to Chinese Pharmacopoeia version in 2000 two annex IVA, testing result is as shown in table 2 below:
Table 2, embodiment 1-4 compound niacin sustained release tablet release detect data
To compound niacin sustained release tablet in embodiment 1-5, the survey Syrups by HPLC lovastatin dissolution specified according to Chinese Pharmacopoeia version in 2000 two annex XC first methods, detects data as following table 3:
Table 3, embodiment 1-5 lovastatin Dissolution experiments detect data
Table 4, embodiment 1-5 Acceleration study detect data
Table 2,3,4 shows, and in the present invention prepared by the present invention, compound niacin sustained release tablet component is stablized, had good sustained release effect, can continue compound niacin blood drug level in holder and, effectively treating on concentration, ensure drug effect lastingly.
To one skilled in the art, according to technical scheme described above and design, other various corresponding change and deformation can be made, and all these change and deformation all should belong within the protection domain of the claims in the present invention.
Claims (3)
1. a compound niacin sustained release tablet, is characterized in that: comprise nicotinic acid layer, lovastatin layer and film-coat, and described nicotinic acid layer comprises following parts by weight of component:
Described lovastatin layer comprises following parts by weight of component:
Described film-coat comprises following parts by weight of component:
2. compound niacin sustained release tablet as claimed in claim 1, it is characterized in that, comprise nicotinic acid layer, lovastatin layer and film-coat, described nicotinic acid layer comprises following parts by weight of component:
Described lovastatin layer comprises following parts by weight of component:
Described film-coat comprises following parts by weight of component:
3. the preparation method of compound niacin sustained release tablet according to claim 1, comprises step:
(1) preparation of nicotinic acid granule
(1.1) stearic process, take stearic acid put in 80 DEG C of water-baths be heated to melt;
(1.2) mix, take nicotinic acid, hypromellose, silicon dioxide mix homogeneously, add in the stearic acid melted, be uniformly mixed;
(1.3) granulate, granulate with 20 mesh sieves;
(1.4) dry, wet granular is put in drying baker, bake out temperature 50 DEG C, air blast;
(1.5) granulate, mixing, 20 mesh sieve granulate.Add magnesium stearate, mix homogeneously;
(2) preparation of lovastatin granule
(2.1) preparation of supplementary material and pretreatment, lovastatin crosses 120 mesh sieves.Microcrystalline cellulose excipients, cross-linked carboxymethyl cellulose sodium cross 100 mesh sieves respectively;
(2.2) preparation of bonding agent, takes 10% polyvidone and puts in volumetric flask, add 50% alcoholic solution, stirring and dissolving, standardize solution;
(2.3) weighing of supplementary material, takes pretreated lovastatin, microcrystalline Cellulose, cross-linked carboxymethyl cellulose sodium by component ratio;
(2.4) mixing of adjuvant, lovastatin and microcrystalline Cellulose, cross-linked carboxymethyl cellulose sodium progressively increase with equivalent and mix homogeneously, and cross 40 mesh sieve 6 times, obtain mixed powder;
(2.5) soft material processed, adds bonding agent in mixed powder, and mix homogeneously makes soft material;
(2.6) granulate, 20 mesh sieves are granulated;
(2.7) dry, wet granular is put in drying baker, bake out temperature 60 DEG C, air blast;
(2.8) granulate, mixing, 20 mesh sieve granulate.Add magnesium stearate, mix homogeneously;
(3) tabletting
By special-shaped punching press double-layer tablet;
(4) coating
Coating pan rotating speed 45 revs/min, blast temperature 50-55 DEG C, coating weight gain 4%.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410307889.8A CN105310994A (en) | 2014-06-30 | 2014-06-30 | Compound nicotinic acid slow-release tablet and preparation method thereof |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101756923A (en) * | 2008-11-21 | 2010-06-30 | 扬子江药业集团北京海燕药业有限公司 | Lovastatin and nicotinic acid double-layer sustained release tablets and preparation process |
| US20100178341A1 (en) * | 2008-06-11 | 2010-07-15 | Ranbaxy Laboratories Limited | BILAYERED TABLET COMPRISING NIACIN AND HMG-CoA REDUCTASE INHIBITOR |
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2014
- 2014-06-30 CN CN201410307889.8A patent/CN105310994A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20100178341A1 (en) * | 2008-06-11 | 2010-07-15 | Ranbaxy Laboratories Limited | BILAYERED TABLET COMPRISING NIACIN AND HMG-CoA REDUCTASE INHIBITOR |
| CN101756923A (en) * | 2008-11-21 | 2010-06-30 | 扬子江药业集团北京海燕药业有限公司 | Lovastatin and nicotinic acid double-layer sustained release tablets and preparation process |
Non-Patent Citations (1)
| Title |
|---|
| 罗明生，等: "《中国药用辅料》", 30 April 2006, 化学工业出版社 * |
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Application publication date: 20160210 |