CN103006663A - Rosuvastatin calcium pharmaceutical composition - Google Patents
Rosuvastatin calcium pharmaceutical composition Download PDFInfo
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- CN103006663A CN103006663A CN 201110285404 CN201110285404A CN103006663A CN 103006663 A CN103006663 A CN 103006663A CN 201110285404 CN201110285404 CN 201110285404 CN 201110285404 A CN201110285404 A CN 201110285404A CN 103006663 A CN103006663 A CN 103006663A
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- pharmaceutical composition
- rosuvastatin calcium
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Abstract
The invention provides a rosuvastatin calcium pharmaceutical composition. The rosuvastatin calcium pharmaceutical composition comprises 1.0 to 10.0% of rosuvastatin calcium, 75 to 97.5% of a low-moisture filler, 0 to 5.0% of a dry binder, 1.0 to 5.0% of a disintegrating agent and 0.5 to 5.0% of a lubricant. Through utilization of the low-moisture filler as an auxiliary material in production, rosuvastatin calcium and other auxiliary materials can be mixed uniformly and the mixture is directly compressed into tablets or is subjected to dry granulation tabletting so that introduction of water in wet granulation is avoided; production energy consumption is reduced; product stability is guaranteed; and a cost is reduced.
Description
Technical field
The invention belongs to drug world, relate to a kind of pharmaceutical composition of rosuvastain calcium, rosuvastain calcium Pharmaceutical composition of particularly a kind of low moisture adjuvant that contains, and employing dry granulation tabletting or the preparation of direct compression technique and preparation method thereof.
Background technology
Rosuvastatin is a kind of selectivity HMG-CoA reductase inhibitor.The HMG-CoA reductase inhibitor be change the precursor that 3-hydroxy-3-methylglutaryl-coenzyme A is first valerate-cholesterol-rate-limiting enzyme.The Main Function position of Rosuvastatin is the target organs of liver-cholesterol reducing.Rosuvastatin has increased liver LDL cell surface receptor number, promotes absorption and the catabolism of LDL, and the liver that has suppressed VLDL is synthetic, reduces thus the sum of VLDL and LDL microgranule.
The rosuvastatin calcium tablets of small dimension is that 5mg(is in Rosuvastatin), principal agent proportion in formulation products is low, generally≤10%, thereby in preparation solid preparation process, rosuvastain calcium and pharmaceutic adjuvant are difficult to mix homogeneously, very easily cause the solid preparation product content uneven, and wet granulation can solve this problem.The packaged form of rosuvastatin calcium tablets listing product is two aluminum packings, product is described to moist lability, should be noted that protection against the tide during storage but at present.In addition, known to those skilled in the art, wet granulation is compared with other preparation methoies, belong to energy consumption higher, affect a more technique of parameter, higher to the quality control requirement in the production process.The catabolite of rosuvastain calcium mainly contains two, and one is oxidation impurities, and one is lactone impurity.The existence meeting accelerated degradation reaction of moisture, the impact very large on the mass formation of product.
The technical problem that this patent need solve provides a kind of Pharmaceutical composition that contains the Rosuvastatin of low moisture adjuvant, and can make in process of production principal agent and adjuvant be easy to adopt direct compression or dry granulation tabletting behind the mix homogeneously, both avoided the introducing of water, save again energy consumption, guaranteed the stability of product.
Summary of the invention
The object of the present invention is to provide a kind of low moisture adjuvant that comprises, adopt dry granulation or directly mix rosuvastain calcium Pharmaceutical composition that makes and preparation method thereof.During large-scale production, the rosuvastain calcium solid preparation that adopts the method to make can reach good stability.
The present invention is mixed together by Rosuvastatin calcium raw material drug and low-moisture adjuvant, if the method mix homogeneously that the dosage I adopts equivalent to progressively increase.Then add other an amount of adjuvants, make the solid preparation form.Overcome the hydrolabil characteristic of rosuvastain calcium, guaranteed product quality.
Rosuvastain calcium Pharmaceutical composition of the present invention comprises the rosuvastain calcium of 1.0%-10.0%, the low moisture filler of 75%-97.5%, the dry adhesives of 0%-5.0%, the disintegrating agent of 1.0%-5.0%, the lubricant of 0.5%-5.0%, above content are all by weight percentage.
Moisture or loss on drying≤1.5% of described all low moisture filler.
Described low moisture filler is selected from low moisture microcrystalline Cellulose, Lactis Anhydrous, calcium phosphate dibasic anhydrous, low moisture mannitol.
Described disintegrating agent is selected from polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose.
Can add the adhesion of dry adhesives increase storeroom in the prescription, promote grain forming.The dry adhesives that is fit to has copolyvidone, hydroxypropyl cellulose and hydroxypropyl methylcellulose, if the used filler of writing out a prescription itself has good compressibility, also can not add dry adhesives.
Described lubricant is selected from magnesium stearate, stearic acid, sodium stearyl fumarate, castor oil hydrogenated.
Rosuvastain calcium Pharmaceutical composition of the present invention can be made into the suitable oral Preparations such as tablet, capsule.
The preparation method of rosuvastain calcium Pharmaceutical composition of the present invention can have two kinds.
Preparation method one (dry granulation tabletting): (a) with the rosuvastain calcium raw material with in to add mixing of materials even, dry granulation.
(b) mixture that step (a) is made with add material, mix mixing.
(c) tabletting makes required product.
Wherein, if after the adding material mixture mobile better, easy mix homogeneously can be with (a) and (b) be merged into mixed once, again granulation.
Preparation method two (direct compression): (a) with rosuvastain calcium raw material and adjuvant mix homogeneously.
(b) direct compression makes required product.
Wherein, step (a) is bad according to flowability, the uniformity of mixture after the adding material, also can divide several steps to mix.
In addition, for above two methods, if when component ratio differs greatly, then be difficult for mix homogeneously, this adopts the equivalent mixing method of progressively increasing often.
The invention has the advantages that and adopted low-moisture adjuvant; adopt dry granulation or direct compression production after being beneficial to even mixing; guaranteed the stability of product; avoid the water (particularly aqueous water) of wet granulation use and the adding of organic solvent; thereby reduced damp and hot process; energy consumption is reduced, and be beneficial to quality control and the cost savings in the production process and strengthen workman's compliance.In whole preparation process, do not need special handling, as prevent that moisture from contacting with granule, therefore do not need the damp condition that controls environment especially yet, reduced cost.
The specific embodiment
The main equipment that uses is as follows among the embodiment.
| Equipment | Model | Producer |
| Mixer | HDB-10 | Canaan science and technology |
| Dry granulating machine | WP 120Pharma | The Alexandria |
| Tablet agent | 8Mx EU-B/D | IMA |
The following example purpose is to illustrate the present invention, but to scope of the present invention or spirit and unrestricted.
Embodiment 1
Prescription 1
Preparation technology
1, adds mixing of materials evenly (can adopt if necessary equivalent progressively increase method) in will be except magnesium stearate, add again the magnesium stearate mix homogeneously.
2, add dry granulation in the granulator.
3, the granule adding adds microcrystalline Cellulose, polyvinylpolypyrrolidone, mix homogeneously; Add again the magnesium stearate mix homogeneously.
4, tabletting makes required product.
Embodiment 2
Prescription 2
Preparation technology
1, mixing of materials evenly (can adopt if necessary equivalent progressively increase method) will be added in used.
2, add dry granulation in the granulator.
3, add mixing of materials outside granule adds even.
4, tabletting makes required product.
Embodiment 3
Prescription 3
Preparation technology
1, adds mixing of materials evenly (can adopt if necessary equivalent progressively increase method) in will be except magnesium stearate, add again the sodium stearyl fumarate mix homogeneously.
2, add dry granulation in the granulator.
3, granule adds that to add mixing of materials even.
4, tabletting makes required product.
Embodiment 4
Prescription 4
| Material | Ratio | The mg/ sheet |
| Rosuvastain calcium | 1.00% | 5.2 |
| Lactis Anhydrous | 60.00% | 312 |
| The low moisture microcrystalline Cellulose | 37.50% | 195 |
| Cross-linking sodium carboxymethyl cellulose | 1.00% | 5.2 |
| Magnesium stearate | 0.50% | 2.6 |
| Amount to | 100.00% | 520 |
Preparation technology
1, with the mixing of materials except magnesium stearate evenly (can adopt if necessary equivalent progressively increase method).
2, add magnesium stearate, mix homogeneously.
3, tabletting makes required product.
Embodiment 5
Prescription 5
| Material | Ratio | The mg/ sheet |
| Rosuvastain calcium | 5.20% | 5.2 |
| Low-substituted hydroxypropyl cellulose | 5.00% | 5 |
| The low moisture microcrystalline Cellulose | 87.80% | 87.8 |
| Castor oil hydrogenated | 2.00% | 2 |
| Amount to | 100.00% | 100 |
Preparation technology
1, with used mixing of materials evenly (can adopt if necessary equivalent progressively increase method).
2, tabletting makes required product.
Embodiment 6
Prescription 6
| Material | Ratio | The mg/ sheet |
| Rosuvastain calcium | 5.20% | 5.2 |
| Cross-linking sodium carboxymethyl cellulose | 3.00% | 3 |
| Lactis Anhydrous | 89.30% | 89.3 |
| Hydroxypropyl cellulose | 2.00% | 2 |
| Magnesium stearate | 0.50% | 0.5 |
| Amount to | 100.00% | 100 |
Preparation technology
1, with the mixing of materials except magnesium stearate evenly (can adopt if necessary equivalent progressively increase method).
2, add magnesium stearate, mix homogeneously.
3, tabletting makes required product.
Claims (3)
1. the pharmaceutical composition of a rosuvastain calcium, the rosuvastain calcium that wherein contains 1.0%-10.0%, the low moisture filler of 75%-97.5%, the dry adhesives of 0%-5.0%, the disintegrating agent of 1.0%-5.0%, the lubricant of 0.5%-5.0%, the moisture of wherein said low moisture filler or loss on drying≤1.5%.
2. pharmaceutical composition according to claim 1 is characterized in that the low moisture filler is selected from low moisture microcrystalline Cellulose, Lactis Anhydrous, calcium phosphate dibasic anhydrous, low moisture mannitol.
3. pharmaceutical composition according to claim 1 is characterized in that dry granulation or direct compression process are adopted in the preparation of compositions.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201110285404 CN103006663A (en) | 2011-09-23 | 2011-09-23 | Rosuvastatin calcium pharmaceutical composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201110285404 CN103006663A (en) | 2011-09-23 | 2011-09-23 | Rosuvastatin calcium pharmaceutical composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103006663A true CN103006663A (en) | 2013-04-03 |
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ID=47956129
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 201110285404 Pending CN103006663A (en) | 2011-09-23 | 2011-09-23 | Rosuvastatin calcium pharmaceutical composition |
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| Country | Link |
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| CN (1) | CN103006663A (en) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017194432A1 (en) * | 2016-05-09 | 2017-11-16 | Adamed Sp. Z O.O. | Pharmaceutical composition |
| CN108174596A (en) * | 2015-10-09 | 2018-06-15 | 赫克萨尔股份公司 | Include 8- [(3R) -3- amino -1- piperidyls] -7- (2- butine -1- bases) -3, the pharmaceutical composition of 7- dihydro -3- methyl-1s-[4- methyl -2- quinazolyls) methyl] -1H- purine -2,6- diketone or its pharmaceutically acceptable salt |
| CN108245516A (en) * | 2017-11-09 | 2018-07-06 | 浙江京新药业股份有限公司 | A kind of pharmaceutical composition containing rosuvastain calcium and preparation method thereof |
| CN110974793A (en) * | 2019-12-26 | 2020-04-10 | 鲁南制药集团股份有限公司 | Rosuvastatin calcium tablet and preparation method thereof |
| CN111012749A (en) * | 2019-12-26 | 2020-04-17 | 常州千红生化制药股份有限公司 | A preparation capable of improving heat stability of tablet and kallidinogenase, and heat stable kallidinogenase tablet and its preparation method |
| CN113230223A (en) * | 2021-05-13 | 2021-08-10 | 宜昌人福药业有限责任公司 | Preparation method of atorvastatin calcium film coated tablet |
-
2011
- 2011-09-23 CN CN 201110285404 patent/CN103006663A/en active Pending
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108174596A (en) * | 2015-10-09 | 2018-06-15 | 赫克萨尔股份公司 | Include 8- [(3R) -3- amino -1- piperidyls] -7- (2- butine -1- bases) -3, the pharmaceutical composition of 7- dihydro -3- methyl-1s-[4- methyl -2- quinazolyls) methyl] -1H- purine -2,6- diketone or its pharmaceutically acceptable salt |
| WO2017194432A1 (en) * | 2016-05-09 | 2017-11-16 | Adamed Sp. Z O.O. | Pharmaceutical composition |
| CN108245516A (en) * | 2017-11-09 | 2018-07-06 | 浙江京新药业股份有限公司 | A kind of pharmaceutical composition containing rosuvastain calcium and preparation method thereof |
| CN108245516B (en) * | 2017-11-09 | 2019-04-12 | 浙江京新药业股份有限公司 | A kind of pharmaceutical composition and preparation method thereof containing rosuvastain calcium |
| CN110974793A (en) * | 2019-12-26 | 2020-04-10 | 鲁南制药集团股份有限公司 | Rosuvastatin calcium tablet and preparation method thereof |
| CN111012749A (en) * | 2019-12-26 | 2020-04-17 | 常州千红生化制药股份有限公司 | A preparation capable of improving heat stability of tablet and kallidinogenase, and heat stable kallidinogenase tablet and its preparation method |
| CN111012749B (en) * | 2019-12-26 | 2022-08-05 | 常州千红生化制药股份有限公司 | A preparation capable of improving heat stability of tablet and kallidinogenase, and heat stable kallidinogenase tablet and its preparation method |
| CN113230223A (en) * | 2021-05-13 | 2021-08-10 | 宜昌人福药业有限责任公司 | Preparation method of atorvastatin calcium film coated tablet |
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Application publication date: 20130403 |