CN112263558A - Rosuvastatin tablet - Google Patents
Rosuvastatin tablet Download PDFInfo
- Publication number
- CN112263558A CN112263558A CN202011327148.8A CN202011327148A CN112263558A CN 112263558 A CN112263558 A CN 112263558A CN 202011327148 A CN202011327148 A CN 202011327148A CN 112263558 A CN112263558 A CN 112263558A
- Authority
- CN
- China
- Prior art keywords
- parts
- rosuvastatin
- alkalizer
- anhydrous calcium
- medicament
- 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
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Inorganic Chemistry (AREA)
- Obesity (AREA)
- Biophysics (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention relates to a rosuvastatin tablet, which comprises 3.47 parts of rosuvastatin calcium, 20 parts of microcrystalline cellulose, 4 parts of crospovidone, 2 magnesium stearate, 61.53-63.53 parts of lactose and 7-9 parts of alkalizer, wherein the alkalizer is anhydrous calcium hydrophosphate, the particle size of the anhydrous calcium hydrophosphate is D10 smaller than 50 mu m, D50 is 50-90 mu m, and D90 is 90-140 mu m. Compared with the prior art, the invention determines the dosage and the particle size range by selecting the alkalizer anhydrous calcium hydrophosphate, effectively improves the pH value of the micro-environment of the medicament in vivo, avoids the medicament from being degraded in an acid environment, and thus improves the stability of the medicament in vivo.
Description
Technical Field
The invention relates to a rosuvastatin tablet.
Background
Rosuvastatin calcium tablet is developed by IPR PAHRMACEUTICAL INCORPORATED, is a selective HMG-CoA reductase inhibitor, and can be used for treating hyperlipidemia. The rosuvastatin calcium tablet is suitable for adjuvant therapy of patients with primary hypercholesterolemia or mixed dyslipidemia when diet or exercise therapy is not ideal, can be suitable for patients with homozygous familial hypercholesterolemia, can be used alone or in combination with diet or other lipid-lowering means, and is a first-line medicament for clinically treating hyperlipidemia at present.
The rosuvastatin calcium raw material is unstable under the conditions of acid, high humidity, high temperature, strong oxidation and illumination, so the requirements of selection, dosage and the like of an alkalizer are considered when auxiliary materials are screened in a prescription, and the damage and degradation effects of gastric acid on the medicine after the medicine enters the body are improved, so that the stability of the medicine in the body is improved.
Disclosure of Invention
The object of the present hairstyle is to overcome the disadvantages of the prior art and to provide a rosuvastatin tablet.
In order to realize the purpose of the invention, the invention adopts the technical scheme that: rosuvastatin tablet comprises 3.47 parts of rosuvastatin calcium, 20 parts of microcrystalline cellulose, 4 parts of crospovidone, 2 parts of magnesium stearate, 61.53-63.53 parts of lactose and 7-9 parts of alkalizer, wherein the alkalizer is anhydrous calcium hydrogen phosphate.
Furthermore, the particle size of the anhydrous calcium hydrophosphate is D10 less than 50 μm, D50 is between 50 and 90 μm, and D90 is between 90 and 140 μm
Compared with the prior art, the invention determines the dosage and the particle size range by selecting the alkalizer anhydrous calcium hydrophosphate, effectively improves the pH value of the micro-environment of the medicament in vivo, avoids the medicament from being degraded in an acid environment, and thus improves the stability of the medicament in vivo.
Detailed Description
The present invention will be described in further detail with reference to specific embodiments.
Example 1
Rosuvastatin tablet comprises 3.47 parts of rosuvastatin calcium, 20 parts of microcrystalline cellulose, 4 parts of crospovidone, 2 parts of magnesium stearate, 63.53 parts of lactose and 7 parts of anhydrous calcium hydrophosphate, wherein the particle size of the anhydrous calcium hydrophosphate is D10: 43 μm, D50:78 μm, D90: 132 μm.
Example 2
Rosuvastatin tablet comprises 3.47 parts of rosuvastatin calcium, 20 parts of microcrystalline cellulose, 4 parts of crospovidone, 2 parts of magnesium stearate, 62.53 parts of lactose and 8 parts of anhydrous calcium hydrophosphate, wherein the particle size of the anhydrous calcium hydrophosphate is D10: 30 μm, D50: 68 μm, D90: 125 μm.
Example 3
Rosuvastatin tablet comprises 3.47 parts of rosuvastatin calcium, 20 parts of microcrystalline cellulose, 4 parts of crospovidone, 2 parts of magnesium stearate, 61.53 parts of lactose and 9 parts of anhydrous calcium hydrogen phosphate, wherein the particle size of the anhydrous calcium hydrogen phosphate is D10: 16 μm, D50: 56 μm, D90: 112 μm.
The dissolution rates of the tablets prepared in each example at pH1.2 and pH6.6 were as follows:
as can be seen from the above table, there was no significant difference in dissolution rates of the tablets at pH1.2 and pH6.6.
The stability of the tablets at 50 ℃/90% RH for 2 and 4 weeks was examined and the results are as follows:
it can be seen that the tablets of the examples have both the lactones and impurities meeting the standard requirements and the data are much lower than the standard line.
The tablet details for each example are as follows:
the identification, disintegration time and content uniformity of the detection items of each embodiment all meet the standard requirements, the content, dissolution rate and related substances are within the standard requirement range, and the difference among the embodiments is small.
Claims (2)
1. The rosuvastatin tablet is characterized by comprising 3.47 parts of rosuvastatin calcium, 20 parts of microcrystalline cellulose, 4 parts of crospovidone, 2 parts of magnesium stearate, 61.53-63.53 parts of lactose and 7-9 parts of an alkalizer, wherein the alkalizer is anhydrous calcium hydrogen phosphate.
2. Rosuvastatin tablet according to claim 1, wherein the anhydrous dibasic calcium phosphate has a particle size D10 of less than 50 μm, D50 of 50-90 μm and D90 of 90-140 μm.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202011327148.8A CN112263558A (en) | 2020-11-23 | 2020-11-23 | Rosuvastatin tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202011327148.8A CN112263558A (en) | 2020-11-23 | 2020-11-23 | Rosuvastatin tablet |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN112263558A true CN112263558A (en) | 2021-01-26 |
Family
ID=74339603
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202011327148.8A Pending CN112263558A (en) | 2020-11-23 | 2020-11-23 | Rosuvastatin tablet |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN112263558A (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104398484A (en) * | 2014-12-04 | 2015-03-11 | 石家庄四药有限公司 | Rosuvastatin calcium tablet and preparation method thereof |
| CN104473899A (en) * | 2014-12-19 | 2015-04-01 | 河南润弘制药股份有限公司 | Rosuvastatin calcium tablet and preparation method thereof |
-
2020
- 2020-11-23 CN CN202011327148.8A patent/CN112263558A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104398484A (en) * | 2014-12-04 | 2015-03-11 | 石家庄四药有限公司 | Rosuvastatin calcium tablet and preparation method thereof |
| CN104473899A (en) * | 2014-12-19 | 2015-04-01 | 河南润弘制药股份有限公司 | Rosuvastatin calcium tablet and preparation method thereof |
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|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20210126 |
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| RJ01 | Rejection of invention patent application after publication |