CN101889975A - Rosuvastatin calcium sustained-release preparation and preparation method thereof - Google Patents
Rosuvastatin calcium sustained-release preparation and preparation method thereof Download PDFInfo
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- CN101889975A CN101889975A CN2010102376815A CN201010237681A CN101889975A CN 101889975 A CN101889975 A CN 101889975A CN 2010102376815 A CN2010102376815 A CN 2010102376815A CN 201010237681 A CN201010237681 A CN 201010237681A CN 101889975 A CN101889975 A CN 101889975A
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Abstract
The invention relates to a rosuvastatin calcium sustained-release preparation and a preparation method thereof. The rosuvastatin calcium sustained-release preparation basically contains 5 to 10mg of rosuvastatin calcium, and the balance of sustained-release framework material and other pharmaceutical excipients. The preparation method is simple; and all the materials are proportioned and the preparation is prepared by the preparation method for common tablets, granules or capsules. The rosuvastatin calcium sustained-release preparation prepared by the method avoids adverse reactions such as rhabdomyolysis, proteinuria, nephrosis, kidney failure, hepatotoxicity and the like caused by overdosage of medicaments; meanwhile, due blood concentration and time for treating diseases after the medicaments are taken can be maintained, and the peak valley phenomenon of the blood concentration is effectively avoided.
Description
Technical field
The present invention relates to a kind of medicament slow release preparation, specifically a kind of rosuvastatin calcium sustained-release and preparation method thereof.
Background technology
In recent years, cardiovascular system diseases has occupied the front three of the cause of death in China, and atherosclerosis is the main pathological basis of cardiovascular and cerebrovascular disease, and preventing and treating atherosclerosis then is the important measures of control cardiovascular and cerebrovascular disease.Some blood fat or lipoprotein exceed then becomes hyperlipemia normal range.It is generally acknowledged that hyperlipemia can promote the formation and development of atherosclerotic lesion.The blood plasma level of Epidemiological study T-CHOL (TC) and low density lipoprotein, LDL (LDL) and the sickness rate and the mortality rate of coronary heart disease and cerebrovascular are closely related, and drug application reduces plasma TC and LDL, can corresponding minimizing evidence of coronary heart diseases and mortality rate.The blood lipid regulation medicine is the key component of antiatherosclerotic, existing multinomial large-scale experiment proof blood lipid regulation medicine is as one-level or the secondary prevention and the treatment of cardiovascular and cerebrovascular disease, all can significantly reduce its M ﹠ M, improve the prognosis of interventional therapy.Statins promptly is the blood lipid regulation medicine that mainly reduces TC and LDL.
Rosuvastain calcium is a kind of selectivity, emulative HMG-CoA reductase inhibitor, and it can be used to treat, and atherosclerosis, blood fat are too high, familial hypercholesterolemia and similar disease.A lot of clinical datas show, Rosuvastatin can reduce the LDL-cholesterol to a greater degree than other statinses that gone on the market, HDL-cholesterol simultaneously raises, it is the best statins of present curative effect, and can when starting dose, can reach the purpose of blood fat reducing, help improving patient's compliance, be described as " super he spit of fland ".But untoward reaction such as rhabdomyolysis, albuminuria, nephropathy, renal failure, liver toxicity, pharyngitis, headache and influenza-like symptom (may take place 10～40mg) time heavy dose of in it.Institute thinks the reduction adverse reaction rate, and Rosuvastatin should begin to take from low dose.There is " peak valley " fluctuation in ordinary preparation blood drug level, can keep curative effect in the valid density scope for guaranteeing medicine, is necessary the slow release method of Rosuvastatin is studied.
Summary of the invention
The object of the present invention is to provide a kind of rosuvastatin calcium sustained-release, can overcome the defective that there is " peak valley " fluctuation in rosuvastain calcium ordinary preparation blood drug level, in the valid density scope, keep curative effect, can avoid surpassing the toxic and side effects of treatment blood drug level scope again, drug safety, effectiveness and compliance are increased.
Another object of the present invention is to provide the preparation method of rosuvastain calcium slow releasing preparation.
The object of the present invention is achieved like this: a kind of rosuvastatin calcium sustained-release, it is characterized in that: it contains rosuvastain calcium, sustained-release matrix material and other pharmaceutic adjuvants substantially, wherein the dosage of rosuvastain calcium in unit formulation is 5～10mg, the sustained-release matrix material accounts for 5～80%, and other pharmaceutic adjuvants account for 1～20%.
Above-mentioned sustained-release matrix material is one or more combination of hydrophilic gel matrix material, erodible framework material, water-insoluble framework material.
Above-mentioned hydrophilic gel matrix material is one or more a combination in any of methylcellulose, sodium carboxymethyl cellulose, hypromellose, polyvidone, carbopol, alginic acid sodium salt, chitosan;
Above-mentioned erodible framework material is one or more a combination in any of fat, wax class, stearic acid, hexadecanol, octadecanol, Polyethylene Glycol;
Above-mentioned water-insoluble framework material is one or more combination of ethyl cellulose, polyethylene, polypropylene, polysiloxanes, polysiloxanes, ethylene-vinyl acetate copolymer, polymethyl methacrylate.
The preparation of above-mentioned rosuvastatin calcium sustained-release can be adopted direct compression, with making granule, capsule, tablet behind wet method or the dry granulation.
The specific embodiment
The following example is intended to further describe the present invention and unrestricted the present invention.
Embodiment 1: rosuvastain calcium hydrogel matrix slow releasing tablet
Prescription is formed:
Rosuvastain calcium 5.2mg
Hypromellose K4M 72mg
Lactose 82mg
10% polyvinylpyrrolidone is an amount of
60% ethanol is an amount of
Magnesium stearate 1.6mg
The heavy 160mg of sheet
Preparation technology: rosuvastain calcium is pulverized 80 mesh sieves, with behind hypromellose K4M and the lactose mix homogeneously with granulating after 10% polyvinylpyrrolidone and the 60% ethanol moistening, in 50 ℃ of dry back granulate, add the magnesium stearate mix homogeneously, tabletting, promptly.
Release test: for investigating the extracorporeal releasing characteristic of Rosuvastatin sustained release tablet of calcium, according to Chinese Pharmacopoeia two appendix XC in 2010, first method (basket method), with water 900ml is dissolution medium, rotating speed is that per minute 100 changes, and operation in accordance with the law was respectively at sampling in 2,6,12,16,20,24 hours, filter with organic filter membrane, get subsequent filtrate as need testing solution.With high performance liquid chromatography (2010 editions two appendix VD of Chinese Pharmacopoeia), detect record chromatogram, the release of calculation sample in the 242nm place.
Experimental result sees Table 1
Table 1
Embodiment 2: rosuvastain calcium hydrogel matrix slow releasing tablet
Prescription is formed:
Rosuvastain calcium 5.2mg
Hypromellose K15M 64mg
Microcrystalline Cellulose 90mg
10% polyvinylpyrrolidone is an amount of
60% ethanol is an amount of
Magnesium stearate 1.6mg
The heavy 160mg of sheet
Preparation technology: rosuvastain calcium is pulverized 80 mesh sieves, with behind hypromellose K15M and the microcrystalline Cellulose mix homogeneously with granulating after 10% polyvinylpyrrolidone and the 60% ethanol moistening, in 50 ℃ of dry back granulate, add the magnesium stearate mix homogeneously, tabletting, promptly.
The release test: test method is with embodiment 1
Experimental result sees Table 2
Table 2
Embodiment 3: rosuvastain calcium hydrogel matrix slow releasing tablet
Prescription is formed:
Rosuvastain calcium 5.2mg
Sodium alginate 58mg
Microcrystalline Cellulose 96mg
10% polyvinylpyrrolidone is an amount of
60% ethanol is an amount of
Magnesium stearate 1.6mg
The heavy 160mg of sheet
Preparation technology: rosuvastain calcium is pulverized 80 mesh sieves, with behind sodium alginate and the microcrystalline Cellulose mix homogeneously with granulating after 10% polyvinylpyrrolidone and the 60% ethanol moistening, in 50 ℃ of dry back granulate, add the magnesium stearate mix homogeneously, tabletting, promptly.
The release test: test method is with embodiment 1
Experimental result sees Table 3
Table 3
Embodiment 4: rosuvastain calcium waxiness matrix sustained release tablet
Prescription is formed:
Rosuvastain calcium 9mg
COMPRITOL
R888ATO 45mg
Microcrystalline Cellulose 96mg
Water is an amount of
The heavy 150mg of sheet
Preparation technology: rosuvastain calcium is pulverized 80 mesh sieves, with COMPRITOL
RBehind 888ATO and the microcrystalline Cellulose mix homogeneously with granulating after the water-wet, in 50 ℃ of dry back granulate, tabletting, promptly.
The release test: test method is with embodiment 1
Experimental result sees Table 4
Table 4
Embodiment 5: the insoluble matrix sustained release tablet of rosuvastain calcium
Prescription is formed:
Rosuvastain calcium 7mg
Ethyl cellulose 80mg
5%EC is an amount of
85% ethanol is an amount of
Pulvis Talci 4mg
Magnesium stearate 9mg
The heavy 100mg of sheet
Preparation technology: rosuvastain calcium is pulverized 80 mesh sieves, with behind the ethyl cellulose mix homogeneously with granulating after 5%EC, the 85% ethanol moistening, in 50 ℃ of dry back granulate, add Pulvis Talci and magnesium stearate mix homogeneously, tabletting, promptly.
The release test: test method is with embodiment 1
Experimental result sees Table 5
Table 5
Claims (6)
1. rosuvastatin calcium sustained-release is characterized in that: be made up of rosuvastain calcium and slow release framework material and other pharmaceutic adjuvants.Each weight percentages of components is:
Rosuvastain calcium 5～10mg
Sustained-release matrix material 5～80%
Other pharmaceutic adjuvants 1～20%
2. rosuvastatin calcium sustained-release according to claim 1 is characterized in that: the dosage of rosuvastain calcium in unit formulation is 5～10mg, preferred 5～7mg.
3. according to claim 1 rosuvastain calcium slow releasing preparation, it is characterized in that: slow-release material is selected one or more combination of methylcellulose, sodium carboxymethyl cellulose, hypromellose, polyvidone, carbopol, alginic acid sodium salt, chitosan, fat, wax class, stearic acid, hexadecanol, octadecanol, Polyethylene Glycol, ethyl cellulose, polyethylene, polypropylene, polysiloxanes, polysiloxanes, ethylene-vinyl acetate copolymer, polymethyl methacrylate for use.
4. according to claim 1 or 3 described rosuvastain calcium slow releasing preparation, it is characterized in that: other pharmaceutic adjuvants are selected filler, binding agent, disintegrating agent and lubricant for use.
5. rosuvastain calcium slow releasing preparation according to claim 4 is characterized in that: filler is selected one or more in lactose, dextrin, calcium sulfate, sucrose, starch, cellulose, calcium hydrogen phosphate, glucose, the pregelatinized Starch for use; Binding agent is selected a kind of among water, ethanol, starch slurry, the hypromellose aqueous solution for use; Disintegrating agent is selected a kind of among carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, the polyvinylpolypyrrolidone for use.
6. the preparation method of rosuvastain calcium slow releasing preparation according to claim 1 can adopt direct compression, with making granule, capsule, tablet behind wet method or the dry granulation.
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102475705A (en) * | 2010-11-27 | 2012-05-30 | 鲁南制药集团股份有限公司 | Medicine composition used for treating hypertension |
| CN102860994A (en) * | 2011-07-04 | 2013-01-09 | 石药集团中奇制药技术（石家庄）有限公司 | Rosuvastatin calcium tablet and preparation method |
| CN102908335A (en) * | 2012-11-19 | 2013-02-06 | 山东罗欣药业股份有限公司 | Rosuvastatain calcium composition and preparation method thereof |
| CN103494788A (en) * | 2013-10-10 | 2014-01-08 | 齐晓彤 | Pharmaceutical composition of rosuvastatin calcium tablets and preparation method of pharmaceutical composition |
| CN109381446A (en) * | 2018-11-26 | 2019-02-26 | 正大制药（青岛）有限公司 | A kind of cyclobenzaprine hydrochloride spansule |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1827169A (en) * | 2005-02-28 | 2006-09-06 | 鲁南制药集团股份有限公司 | Composite preparation containing nitrate esters medicine and HMG-CoA reductase inhibitor |
| CN101756990A (en) * | 2008-11-10 | 2010-06-30 | 鲁南制药集团股份有限公司 | Medical composition for losing weight or treating hyperlipidemia |
-
2010
- 2010-07-27 CN CN2010102376815A patent/CN101889975A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1827169A (en) * | 2005-02-28 | 2006-09-06 | 鲁南制药集团股份有限公司 | Composite preparation containing nitrate esters medicine and HMG-CoA reductase inhibitor |
| CN101756990A (en) * | 2008-11-10 | 2010-06-30 | 鲁南制药集团股份有限公司 | Medical composition for losing weight or treating hyperlipidemia |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102475705A (en) * | 2010-11-27 | 2012-05-30 | 鲁南制药集团股份有限公司 | Medicine composition used for treating hypertension |
| CN102475705B (en) * | 2010-11-27 | 2015-06-24 | 鲁南制药集团股份有限公司 | Medicine composition used for treating hypertension |
| CN102860994A (en) * | 2011-07-04 | 2013-01-09 | 石药集团中奇制药技术（石家庄）有限公司 | Rosuvastatin calcium tablet and preparation method |
| CN102908335A (en) * | 2012-11-19 | 2013-02-06 | 山东罗欣药业股份有限公司 | Rosuvastatain calcium composition and preparation method thereof |
| CN102908335B (en) * | 2012-11-19 | 2015-04-08 | 山东罗欣药业集团股份有限公司 | Rosuvastatain calcium composition and preparation method thereof |
| CN103494788A (en) * | 2013-10-10 | 2014-01-08 | 齐晓彤 | Pharmaceutical composition of rosuvastatin calcium tablets and preparation method of pharmaceutical composition |
| CN103494788B (en) * | 2013-10-10 | 2015-08-05 | 齐晓彤 | Pharmaceutical composition of rosuvastatin calcium tablets and preparation method thereof |
| CN109381446A (en) * | 2018-11-26 | 2019-02-26 | 正大制药（青岛）有限公司 | A kind of cyclobenzaprine hydrochloride spansule |
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Application publication date: 20101124 |