CN105769793A - Simvastatin tablet and preparation method thereof - Google Patents
Simvastatin tablet and preparation method thereof Download PDFInfo
- Publication number
- CN105769793A CN105769793A CN201610202982.1A CN201610202982A CN105769793A CN 105769793 A CN105769793 A CN 105769793A CN 201610202982 A CN201610202982 A CN 201610202982A CN 105769793 A CN105769793 A CN 105769793A
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- China
- Prior art keywords
- simvastatin
- parts
- tablet
- kaolin
- preparation
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- 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.)
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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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
-
- 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
-
- 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
-
- 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
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
Abstract
The invention discloses a simvastatin tablet and a preparation method thereof. The tablet is prepared from the following components: 20 parts of simvastatin, 5 parts of L- tyrosine, 10 parts of kaolin, 15 parts of sodium starch glycolate, 2 parts of gum arabic and 1 part of a lubricating agent. The simvastatin tablet has good medicinal stability and quick dissolution, and the preparation process is relatively simple and is suitable for industrial production.
Description
Technical field
The invention belongs to medicine solid orally ingestible technical field, in particular to a kind of simvastatin tablet and system thereof
Preparation Method.
Background technology
Simvastatin (Simvastatin) is with lovastatin for the semisynthetic HMG-CoA reductase inhibitor of raw material,
Clinic is mainly used in treating hypercholesterolemia and hypertriglyceridemia.Simvastatin is liposoluble substance, can be fast after being administered orally
Speed absorbs, and reaches peak plasma concentrations in 1-2 hour, and the half-life is 2-4 hour, and activity is pravastatin in vivo
4 times, can development that effectively prevention of arterial is atherosis and heart disease recurrence, reduce non-lethal myocardial infarction and cardiac muscle blood
Pipe forms the danger of operation again.In recent years, Simvastatin Treatment hypercholesterolemia, coronary heart disease, obtain wide clinically
General application, the kind of the most domestic focus development.Simvastatin the most easily becomes under high temperature, illumination and Oxygen Condition
Change.
Summary of the invention
The invention provides a kind of simvastatin tablet and preparation method thereof.
The present invention realizes particular by following technical scheme:
A kind of simvastatin tablet, by the simvastatin 20 parts of following weight portion, TYR 5 parts, Kaolin 10
Part, Sodium Carboxymethyl Starch 15 parts, Radix Acaciae senegalis 2 parts, lubricant 1 part composition.
Described simvastatin tablet, described lubricant is magnesium stearate, micropowder silica gel, stearic acid, Pulvis Talci and mountain
One or more in Yu acid glyceride；Preferably magnesium stearate.
Described simvastatin tablet, preparation method comprises the steps: first by simvastatin and TYR, kaolinite
Soil, Sodium Carboxymethyl Starch carry out pretreatment；Pretreated simvastatin and Radix Acaciae senegalis are pelletized；Add profit
Lubrication prescription carries out tabletting process, and desiccant dehumidification is packed after processing, and prepares Simvastatin Tablets.
Compared with prior art, the simvastatin tablet that the present invention relates to and preparation technology thereof have the advantage that with significantly
Progressive: enhance the stability of medicine, improves the dissolution of medicine；Preparation technology is relatively simple, is suitable for industrialization
Big production.
Specific embodiment
Following example further describe beneficial effects of the present invention, and embodiment is only used for the purpose of illustration, is not intended to this
Bright protection domain, those of ordinary skill in the art is obviously changed according to what the present invention made and modifies also simultaneously
Comprise within the scope of the present invention.
Embodiment 1: simvastatin 20 parts, TYR 5 parts, Kaolin 10 parts, Sodium Carboxymethyl Starch 15 parts, I
Uncle natural gum 2 parts, magnesium stearate 1 part, first carry out pre-place by simvastatin and TYR, Kaolin, Sodium Carboxymethyl Starch
Reason；Pretreated simvastatin and Radix Acaciae senegalis are pelletized；Add lubricant and carry out tabletting process, be dried and remove
Pack after wet process, prepare Simvastatin Tablets.
Embodiment 2: simvastatin 20 parts, TYR 5 parts, Kaolin 10 parts, Sodium Carboxymethyl Starch 15 parts, Arab
Natural gum 2 parts, micropowder silica gel 1 part, first carry out pretreatment by simvastatin and TYR, Kaolin, Sodium Carboxymethyl Starch；
Pretreated simvastatin and Radix Acaciae senegalis are pelletized；Add lubricant and carry out tabletting process, at desiccant dehumidification
Pack after reason, prepare Simvastatin Tablets.
Embodiment 3: simvastatin 20 parts, TYR 5 parts, Kaolin 10 parts, Sodium Carboxymethyl Starch 15 parts, Arab
Natural gum 2 parts, Pulvis Talci 1 part, first carry out pretreatment by simvastatin and TYR, Kaolin, Sodium Carboxymethyl Starch；
Pretreated simvastatin and Radix Acaciae senegalis are pelletized；Add lubricant and carry out tabletting process, at desiccant dehumidification
Pack after reason, prepare Simvastatin Tablets.
Comparative example: the method recording embodiment 1 according to CN103330692B prepares Simvastatin Tablets.
Embodiment 4: each embodiment Simvastatin Tablets have related substance and dissolution determination
1, about substance-measuring: take sample fine powder prepared by each embodiment appropriate, be the most quantitatively configured to every 1mL with flowing
In contrast solution containing simvastatin 6 μ g in need testing solution containing about simvastatin 0.30mg and every 1mL.Take comparison
Solution 20 μ l, injects chromatograph of liquid, regulates detection sensitivity, makes the peak height of main constituent chromatographic peak be about full scale
10%～20%；The most accurately measuring each 20 μ l of above two solution, be injected separately into chromatograph of liquid, record chromatogram is extremely
2 times asked during main peak reservation.In need testing solution chromatograph, the peak area of single impurity peaks cannot be greater than in contrast solution main
The 1/4 (0.5%) of the peak area of one-tenth swarming, the peak area sum of each impurity peaks cannot be greater than main constituent peak in contrast solution
Peak area 1/2 (1.0%).
2, dissolution determination: with phosphate buffer (pH4.5)-normal propyl alcohol (2:1) 900mL as solvent, rotating speed is
5Or/min, operates in accordance with the law, when 15min, takes solution 10mL, filters, and takes subsequent filtrate as need testing solution, separately takes
Simvastatin reference substance is appropriate, accurately weighed, adds above-mentioned solution and dissolves and make in every 1mL the solution conduct containing about 12 μ g
Reference substance solution.Take need testing solution respectively and reference substance solution each 2O μ L notes people's chromatograph of liquid, according to high-efficient liquid phase color
Spectrometry (two annex VD of " Chinese Pharmacopoeia " version in 2010) measures, and calculates the stripping quantity of every.
The relevant substance-measuring result of table 1 each embodiment Simvastatin Tablets
| Sample | 0 day result | 40 DEG C, 75%RH accelerates 6 months |
| Embodiment 1 | Single miscellaneous 0.14%, the most miscellaneous 0.36% | Single miscellaneous 0.27%, the most miscellaneous 0.51% |
| Embodiment 2 | Single miscellaneous 0.15%, the most miscellaneous 0.32% | Single miscellaneous 0.24%, the most miscellaneous 0.53% |
| Embodiment 3 | Single miscellaneous 0.17%, the most miscellaneous 0.38% | Single miscellaneous 0.25%, the most miscellaneous 0.43% |
| Comparative example 1 | Single miscellaneous 0.18%, the most miscellaneous 0.35% | Single miscellaneous 0.52%, the most miscellaneous 1.32% |
From the relevant substance-measuring result of table 1 it can be seen that embodiment 1-3 uses the technology of the present invention, sample accelerates 6 months,
Related substance is had to be increased slightly；Comparative example 1 uses ordinary adjuvants, therefore has related substance to increase substantially, beyond standard-required.
The 15min dissolution determination result of table 2 each embodiment Simvastatin Tablets
| Sample | 0 day result (%) | 40 DEG C, 75%RH accelerates 6 months (%) |
| Embodiment 1 | 97.9 | 98.3 |
| Embodiment 2 | 98.7 | 101.4 |
| Embodiment 3 | 102.4 | 99.8 |
| Comparative example 1 | 65.9 | 58.9 |
From the dissolution result of table 2 it can be seen that embodiment 1-3 uses the technology of the present invention, sample dissolution is rapid, 15min base
This dissolution is complete；Comparative example 1 uses ordinary adjuvants, and solubilising power is limited, and dissolution is incomplete.
Tables 1 and 2 result further demonstrates that, the present invention just simvastatin and TYR, Kaolin, glycolic starch
Simvastatin Tablets good stability prepared by sodium compatibility, dissolution is rapid, and preparation technology is relatively simple simultaneously, is suitable for industrialization big
Produce.
Claims (3)
1. a simvastatin tablet, it is characterised in that: by the simvastatin 20 parts of following weight portion, TYR 5
Part, Kaolin 10 parts, Sodium Carboxymethyl Starch 15 parts, Radix Acaciae senegalis 2 parts, lubricant 1 part composition.
Simvastatin tablet the most according to claim 1, it is characterised in that: described lubricant be magnesium stearate,
One or more in micropowder silica gel, stearic acid, Pulvis Talci and Glyceryl Behenate；Preferably magnesium stearate.
Simvastatin tablet the most according to claim 1, it is characterised in that: preparation method comprises the steps:
First simvastatin and TYR, Kaolin, Sodium Carboxymethyl Starch are carried out pretreatment；By pretreated simvastatin
Pelletize with Radix Acaciae senegalis；Adding lubricant and carry out tabletting process, desiccant dehumidification is packed after processing, and prepares pungent
Cut down statin sheet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610202982.1A CN105769793A (en) | 2016-04-04 | 2016-04-04 | Simvastatin tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610202982.1A CN105769793A (en) | 2016-04-04 | 2016-04-04 | Simvastatin tablet and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105769793A true CN105769793A (en) | 2016-07-20 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610202982.1A Pending CN105769793A (en) | 2016-04-04 | 2016-04-04 | Simvastatin tablet and preparation method thereof |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102657628A (en) * | 2012-06-05 | 2012-09-12 | 康普药业股份有限公司 | Medicinal composition containing simvastatin and preparation method thereof |
| CN103002883A (en) * | 2010-05-14 | 2013-03-27 | 韩美科学株式会社 | Pharmaceutical formulation in the form of bilayered tablets comprising HMG-CoA reductase inhibitor and irbesartan |
| CN103191072A (en) * | 2013-04-07 | 2013-07-10 | 广东彼迪药业有限公司 | Simvastatin tablets and preparation method thereof |
| CN103585146A (en) * | 2013-11-09 | 2014-02-19 | 李友香 | Medicine composition of simvastatin |
-
2016
- 2016-04-04 CN CN201610202982.1A patent/CN105769793A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103002883A (en) * | 2010-05-14 | 2013-03-27 | 韩美科学株式会社 | Pharmaceutical formulation in the form of bilayered tablets comprising HMG-CoA reductase inhibitor and irbesartan |
| CN102657628A (en) * | 2012-06-05 | 2012-09-12 | 康普药业股份有限公司 | Medicinal composition containing simvastatin and preparation method thereof |
| CN103191072A (en) * | 2013-04-07 | 2013-07-10 | 广东彼迪药业有限公司 | Simvastatin tablets and preparation method thereof |
| CN103585146A (en) * | 2013-11-09 | 2014-02-19 | 李友香 | Medicine composition of simvastatin |
Non-Patent Citations (1)
| Title |
|---|
| 《中国药业》 * |
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Application publication date: 20160720 |