CN110420196A - A kind of preparation method of metoprolol tartrate sustained release preparation - Google Patents
A kind of preparation method of metoprolol tartrate sustained release preparation Download PDFInfo
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- CN110420196A CN110420196A CN201910833450.1A CN201910833450A CN110420196A CN 110420196 A CN110420196 A CN 110420196A CN 201910833450 A CN201910833450 A CN 201910833450A CN 110420196 A CN110420196 A CN 110420196A
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- sustained release
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- metoprolol
- metoprolol tartrate
- oil
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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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
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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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/282—Organic compounds, e.g. fats
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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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- Hospice & Palliative Care (AREA)
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Abstract
The present invention relates to a kind of preparation methods of metoprolol tartrate sustained release preparation, are mixed, pelletized, dried, tabletting after metoprolol tartrate raw material powder is added adhesive, and when mixing granulation can not use framework material；After tabletting, tablet is coated using sustained release coating pre-mixing agent, while according to rate of release needs, adjusting sustained release coating pre-mixing agent dosage, reaching expected rate of release.The present invention stablizes release metoprolol, keeps blood concentration steady, thus stability contorting blood pressure by coating production controlled release tablet.
Description
Technical field
The present invention relates to medicine manufacture technology field, in particular to a kind of preparation side of metoprolol tartrate sustained release preparation
Method and preparation method thereof.
Background technique
Metoprolol can be used for treating hypertension, angina pectoris, stable slow of symptom with Assessment of Left Ventricular Systolic Function exception
The diseases such as heart failure.Its therapy mechanism is to play antihypertensive effect by the excessive activation of antagonism stomodaeal nervous system, main
The Hypotensive Mechanism wanted is related to reducing cardiac output, improves the blood pressure adjustment section function of pressoreceptor, and inhibits feritin blood vessel
Angiotensin Converting Enzyme aldosterone system.
Metoprolol has two kinds of acylate products of metoprolol tartrate and metroprolol succinate, tartaric acid Mei Tuoluo
Your metoprolol content is high, is the common raw material of metoprolol drug.Metoprolol tartrate is soluble easily in water, and disintegration absorbs not
Vulnerable to interference, quality is stablized, but it is soluble easily in water also result in it and be not easy to be made into matrix sustained release tablet, producting process difficulty is larger, control
It is bad last rate of release to be influenced.
It can be seen that by the preparation method of metoprolol sustained-release piece in the prior art, it can not be compared with low production cost
And under conditions of process control, the fast finished product of pharmacological property rate of release is produced.
Summary of the invention
For the defect and problem in the presence of above-mentioned background technique, it is an object of the present invention to provide a kind of tartaric acid Mei Tuoluo
The preparation method of your sustained release preparation.This method production cost is low, the metoprolol slow-release tablet drug effect controllability being prepared is strong,
Rate of release is fast.
In order to achieve the above object, the invention provides the following technical scheme:
The present invention provides a kind of preparation methods of metoprolol tartrate sustained release preparation, comprising the following steps:
Step 1 is mixed after metoprolol tartrate raw material powder is added adhesive, is pelletized, is dried, tabletting；
Step 2 after tabletting, is coated tablet using sustained release coating pre-mixing agent, while according to rate of release needs,
Adjust sustained release coating pre-mixing agent dosage.
Further, the weight ratio of the sustained release coating pre-mixing agent and Metoprolol Tablets is 4-10: 90-96.
Further, the weight ratio of the sustained release coating pre-mixing agent and Metoprolol Tablets is 4-8: 92-96.
Further, the sustained release coating pre-mixing agent is made of the raw material of following weight percent:
The ethyl cellulose of 20-80%, the anti-wear additive of 20-80%, the flexibilizer additive of 10-20%.
Further, the flexibilizer additive is rapeseed oil, soybean oil, olive oil, walnut oil, peanut oil, cocoa butter, sunflower
One of seed oil, condensed milk, sesame oil, palm oil, corn oil are a variety of.
Further, the anti-wear additive be silica, it is titanium dioxide, talcum powder, plant carbon black, Black Rouge, red
One of iron oxide, yellow ferric oxide are a variety of.
Further, described adhesive is starch slurry, sodium carboxymethylcellulose, hydroxypropyl cellulose, hydroxypropyl methyl fiber
One of element, gelatin solution, sucrose solution are a variety of.
Compared with the prior art, the present invention has the following advantages:
1, production controllability is good, and the mixed effect of existing framework material and raw material can not detect, and it is even more impossible to field monitorings to sentence
Not, it once rate of release is not inconsistent standardization, can not do over again again, although the present invention can not directly control practical coating thickness when being coated
(practical coating is lossy, and loss can be fluctuated in a certain range), but can be by controlling coating powder weight when preparation coating solution, in turn
Maximum coating weight gain is arranged causes practical weight gain small, rate of release is faster than standard model if loss ratio normal condition is big when coating
It encloses, the benefit that can do over again coating, to meet the range of rate of release standard；
2, production cost is low, since framework material unit price is significantly larger than metoprolol tartrate cost of material, skeleton system
Sustained release tablets be effective extended release time, framework material accounting can be bigger, generally accounts for 30% or so of finished product, even more
More, the present invention is generally 4% to 8%, does not exceed 10%, therefore cost is greatly reduced by coated slow release, slow-release material；
3, controlled-release effect is good, due to skeleton slow-releasing system pharmacological property release from outside to inside, internal metoprolol discharge when by
Increasingly thicker framework material interference, rate of release can be slower and slower, the definition according to pharmacopeia to slow controlled release, can only be known as slow
It releases, is coated slow controlled release, be by the channel release in thin layer clothing film, rate of release is at the uniform velocity to discharge, and it is right in pharmacopeia to meet
The definition of controlled release, controlled release are more preferable than slow release effect；
4, production equipment is at low cost, metoprolol sustained-release pellet disclosed in the prior art, although controllability is better than skeleton
Sustained release, but coating of pellets needs the seed-coating machine that boils, and equipment is expensive, and energy consumption is high, and most manufacturing enterprises do not have, therefore the system
Preparation Method versatility is not strong, and the equipment used in the present invention is conventional tablet production equipment, without adding special installation.
Specific embodiment
Below in conjunction with the embodiment of the present invention, technical solution of the present invention is clearly and completely described, it is clear that
Described embodiments are only a part of the embodiments of the present invention, instead of all the embodiments.Based on the implementation in the present invention
Example, every other embodiment obtained by those of ordinary skill in the art without making creative efforts belong to
The scope of protection of the invention.
Embodiment 1
A kind of preparation method of metoprolol tartrate sustained release preparation of the embodiment of the present invention 1, comprising the following steps:
Step 1 is mixed after metoprolol tartrate raw material powder is added adhesive, is pelletized, is dried, tabletting；
Step 2 after tabletting, is coated tablet using sustained release coating pre-mixing agent, while according to rate of release needs,
Adjust sustained release coating pre-mixing agent dosage.
Each raw material accounting in manufactured metoprolol slow-release tablet are as follows: Metoprolol Tablets 90%, sustained release coating pre-mixing agent
10%, wherein accounting of each component in finished product in sustained release coating pre-mixing agent are as follows: ethyl cellulose 7%, talcum powder 2%, olive
Oil 1%.
Embodiment 2
A kind of preparation method of metoprolol tartrate sustained release preparation of the embodiment of the present invention 2, comprising the following steps:
Step 1 is mixed after metoprolol tartrate raw material powder is added adhesive, is pelletized, is dried, tabletting；
Step 2 after tabletting, is coated tablet using sustained release coating pre-mixing agent, while according to rate of release needs,
Adjust sustained release coating pre-mixing agent dosage.
Each raw material accounting in manufactured metoprolol slow-release tablet are as follows: Metoprolol Tablets 92%, sustained release coating pre-mixing agent
8%, wherein accounting of each component in finished product in sustained release coating pre-mixing agent are as follows: ethyl cellulose 5%, silica 2%, palm fibre
Palmitic acid oil 1%.
Embodiment 3
A kind of preparation method of metoprolol tartrate sustained release preparation of the embodiment of the present invention 3, comprising the following steps:
Step 1 is mixed after metoprolol tartrate raw material powder is added adhesive, is pelletized, is dried, tabletting；
Step 2 after tabletting, is coated tablet using sustained release coating pre-mixing agent, while according to rate of release needs,
Adjust sustained release coating pre-mixing agent dosage.
Each raw material accounting in manufactured metoprolol slow-release tablet are as follows: Metoprolol Tablets 94%, sustained release coating pre-mixing agent
6%, wherein accounting of each component in finished product in sustained release coating pre-mixing agent are as follows: ethyl cellulose 4%, plant carbon black 1%, core
Peach oil 1%.
The above description is merely a specific embodiment, but scope of protection of the present invention is not limited thereto, any
Those familiar with the art in the technical scope disclosed by the present invention, can easily think of the change or the replacement, and should all contain
Lid is within protection scope of the present invention.Therefore, the protection scope of the present invention shall be subject to the protection scope of the claims.
Claims (7)
1. a kind of preparation method of metoprolol tartrate sustained release preparation, which comprises the following steps:
Step 1 is mixed after metoprolol tartrate raw material powder is added adhesive, is pelletized, is dried, tabletting；
Step 2 after tabletting, is coated tablet using sustained release coating pre-mixing agent, while according to rate of release needs, adjusting
Sustained release coating pre-mixing agent dosage.
2. a kind of preparation method of metoprolol tartrate sustained release preparation according to claim 1, which is characterized in that described
The weight ratio of sustained release coating pre-mixing agent and Metoprolol Tablets is 4-10: 90-96.
3. a kind of preparation method of metoprolol tartrate sustained release preparation according to claim 2, which is characterized in that described
The weight ratio of sustained release coating pre-mixing agent and Metoprolol Tablets is 4-8: 92-96.
4. a kind of preparation method of metoprolol tartrate sustained release preparation according to claim 3, which is characterized in that described
Sustained release coating pre-mixing agent is made of the raw material of following weight percent:
The ethyl cellulose of 20-80%, the anti-wear additive of 20-80%, the flexibilizer additive of 10-20%.
5. a kind of preparation method of metoprolol tartrate sustained release preparation according to claim 4, which is characterized in that described
Flexibilizer additive is rapeseed oil, soybean oil, olive oil, walnut oil, peanut oil, cocoa butter, sunflower oil, condensed milk, sesame oil, palm fibre
One of palmitic acid oil, corn oil, triacetyl glycerine, triethyl citrate, diethyl phthalate are a variety of.
6. a kind of preparation method of metoprolol tartrate sustained release preparation according to claim 5, which is characterized in that described
Anti-wear additive is silica, titanium dioxide, talcum powder, plant carbon black, Black Rouge, red ferric oxide, yellow ferric oxide, shallow lake
One of powder, dextrin are a variety of.
7. a kind of preparation method of metoprolol tartrate sustained release preparation according to claim 1, which is characterized in that described
Adhesive is that starch slurry, sodium carboxymethylcellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, gelatin solution, sucrose are molten
One of liquid, polyvinylpyrrolidone are a variety of.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910833450.1A CN110420196A (en) | 2019-09-04 | 2019-09-04 | A kind of preparation method of metoprolol tartrate sustained release preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910833450.1A CN110420196A (en) | 2019-09-04 | 2019-09-04 | A kind of preparation method of metoprolol tartrate sustained release preparation |
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| CN110420196A true CN110420196A (en) | 2019-11-08 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201910833450.1A Pending CN110420196A (en) | 2019-09-04 | 2019-09-04 | A kind of preparation method of metoprolol tartrate sustained release preparation |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200301139A (en) * | 2001-12-20 | 2003-07-01 | Pharmacia Corp | Zero-order sustained release dosage forms and method of making same |
| CN102626396A (en) * | 2012-04-28 | 2012-08-08 | 海南华益泰康药业有限公司 | Metoprolol slow-release tablet and preparation method thereof |
| CN103385862A (en) * | 2012-05-08 | 2013-11-13 | 重庆国中医药有限公司 | Metoprolol tartrate sustained-release tablet and preparation method thereof |
| CN104758937A (en) * | 2014-01-02 | 2015-07-08 | 石药集团中奇制药技术（石家庄）有限公司 | Metoprolol sustained-release pellet preparation |
-
2019
- 2019-09-04 CN CN201910833450.1A patent/CN110420196A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200301139A (en) * | 2001-12-20 | 2003-07-01 | Pharmacia Corp | Zero-order sustained release dosage forms and method of making same |
| CN102626396A (en) * | 2012-04-28 | 2012-08-08 | 海南华益泰康药业有限公司 | Metoprolol slow-release tablet and preparation method thereof |
| CN103385862A (en) * | 2012-05-08 | 2013-11-13 | 重庆国中医药有限公司 | Metoprolol tartrate sustained-release tablet and preparation method thereof |
| CN104758937A (en) * | 2014-01-02 | 2015-07-08 | 石药集团中奇制药技术（石家庄）有限公司 | Metoprolol sustained-release pellet preparation |
Non-Patent Citations (4)
| Title |
|---|
| 上海卡乐康包衣技术有限公司: ""乙基纤维素干粉包衣的美托洛尔缓释多颗粒的稳定性评估"", 《中国医药工业杂志》 * |
| 余祥彬等: "《药剂学与药物动力学实验指导》", 31 January 2014, 厦门大学出版社 * |
| 方亮主编: "《药剂学》", 31 March 2016, 中国医药科技出版社 * |
| 黄健等: ""酒石酸美托洛尔缓释微丸的制备及处方因素考察"", 《中国新药杂志》 * |
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Application publication date: 20191108 |