CN105640903A - Stable tedizolid phosphate medicine composition - Google Patents
Stable tedizolid phosphate medicine composition Download PDFInfo
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- CN105640903A CN105640903A CN201410628830.9A CN201410628830A CN105640903A CN 105640903 A CN105640903 A CN 105640903A CN 201410628830 A CN201410628830 A CN 201410628830A CN 105640903 A CN105640903 A CN 105640903A
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- China
- Prior art keywords
- safe ground
- amine
- azoles amine
- microcrystalline cellulose
- croscarmellose sodium
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Abstract
The invention discloses a stable tedizolid phosphate medicine composition, which is characterized in that a recipe for preparing 1000 tablets comprises the following ingredients including 200 to 400g of tedizolid phosphate, 70 to 140g of microcrystalline cellulose, 0.5 to 1g of superfine silica gel powder, 50 to 100g of croscarmellose sodium and a proper amount of a 10-percent amylum pregelatinisatum solution. The invention also relates to a preparation method of a tedizolid phosphate tablet. The tedizolid phosphate prepared by the recipe and the preparation method provided by the invention has the advantages of high dissolution rate, high bioavailability and good curative effect.
Description
Technical field
The present invention relates to a kind of stable safe ground azoles drug amine composition and its preparation method.
Background technology
Phosphoric acid safe ground azoles amine (tedizolidphosphate, SIVEXTRO) it is develop by Cubist drugmaker, obtain FDA approval on June 20th, 2014, it is that a kind of oxazolidinones antibacterium medicine is useful in and grows up for treatment is by specifying acute bacterial skin and skin structure infection (ABSSSI) caused by susceptible bacteria. For lowering the generation of drug-resistant bacteria and maintain the validity of SIVEXTRO and other antibacterium medicines, SIVEXTRO is only applied to treatment or prevention is proved to be or strong doubt is infected caused by bacterium.
Its structural formula:
By the research to prior art, safe ground azoles amine bioavailability in human body is low is still puzzlement people's urgent problem. In addition, kind and the consumption of suitable preparation method and processing condition, weighting agent are most important to result of extraction, the mobility of tablet. Conventional weighting agent lactose, Microcrystalline Cellulose, starch etc., conventional disintegrating agent has Microcrystalline Cellulose, sodium starch glycolate etc. But, how obtaining more excellent solubility rate by the dissolution rate adjustment formula of described safe ground azoles amine and technique adjustment, prior art does not provide further prompting, and in view of this, spy proposes this invention.
Summary of the invention
The present invention is intended to overcome the problems such as the mobility of existing safe ground azoles drug amine composition is not good, dissolution rate is low, change the dissolution rate of safe ground azoles amine and the low shortcoming of bioavailability, it is to increase curative effect. According to existing auxiliary material and working condition, in guarantee, there is lower production cost and simple preparation technology, under being suitable for the prerequisite of large-scale industrial production, it is necessary to study out a kind of suitable prescription composition and preparation technology, safe ground azoles amine is made to have good bioavailability.
Therefore, it is an object of the invention to provide a kind of safe ground azoles amine sheet, it is characterised in that, the formula making 1000 is composed as follows:
Safe ground azoles amine 200-400g
Croscarmellose sodium 50-100g
Microcrystalline Cellulose 70-140g
Micropowder silica gel 0.5-1g
10% pregelatinized Starch solution is appropriate.
Preferably, to make the formula of 1000 composed as follows for the safe ground azoles amine of the present invention:
Safe ground azoles amine 200g
Croscarmellose sodium 50g
Microcrystalline Cellulose 70g
Micropowder silica gel 0.5g
10% pregelatinized Starch solution is appropriate.
In the present invention, Microcrystalline Cellulose does weighting agent, and pregelatinized Starch plays dual parts bonding and disintegration, promotes disintegration of tablet.
The present invention determines the assembly application of Microcrystalline Cellulose and pregelatinized Starch by prescription screening, and prepared safe ground azoles amine tablet dissolution rate is better, and determines the optimizing prescriptions of the present invention through auxiliary material shaker test. Prescription screening is tested and be the results are shown in down:
From above test-results: prescription 1 stripping trend is better than other prescription.
Another object of the present invention is to provide the preparation method of safe ground of the present invention azoles drug amine composition, it is characterised in that the method comprises the steps:
1) respectively by dry to Thailand's ground azoles amine, croscarmellose sodium, Microcrystalline Cellulose, pulverize, sieve, obtain safe ground azoles amine powder, croscarmellose sodium powder and Microcrystalline Cellulose powder respectively;
2) get the safe ground azoles amine of recipe quantity, croscarmellose sodium and Microcrystalline Cellulose, mix, then add 10% pregelatinized Starch solution and make softwood in right amount, cross 40 eye mesh screens and granulate, obtain safe ground azoles amine wet granular;
3) above-mentioned safe ground azoles amine wet granular is dried to moisture under 60 DEG C of conditions and it is less than 5%, obtain the safe ground dry particle of azoles amine;
4) the above-mentioned safe ground dry particle of azoles amine being crossed the 40 whole grains of eye mesh screen, then add lubricant, mix, after quality inspection is qualified, compressing tablet, obtains safe ground azoles amine tablet.
In above-mentioned preparation method, sieving of step 1) was 100 order sieves.
Preferably, the object of screening is the material in order to obtain relatively uniform particle size. This has important meaning smoothly to what drug quality and preparation were produced. The unit operations such as mixing, granulation, compressing tablet sieve the mobility on mixedness, particle, etc. have obvious impact. Remix after former, auxiliary material being pulverized, sieved in the present invention, former, auxiliary material can be made to be evenly distributed, what mix is more even, and the present invention adopts Microcrystalline Cellulose and major ingredient pulverize rear remix respectively, mixedness can be made, the mobility of particle is significantly improved thus makes medicine better play drug effect.
In addition, heating can cause the degraded of safe ground azoles amine, therefore, it is determined that the drying temperature being applicable to is very important. Thailand's ground azoles amine particle is dried to moisture by the present invention under 60 DEG C of conditions and is less than 5%, obtain the safe ground dry particle of azoles amine, not only avoid the degraded heated safe ground azoles amine, and drying effect is good.
Embodiment
Below in conjunction with embodiment, the present invention is described in further detail, it should be appreciated that the non-scope being only limitted to these embodiments of the scope of the present invention.
Embodiment 1
It is composed as follows that safe ground azoles amine makes the formula of 1000:
Safe ground azoles amine 200g
Croscarmellose sodium 50g
Microcrystalline Cellulose 70g
Micropowder silica gel 0.5g
10% pregelatinized Starch solution is appropriate
Preparation method
1) respectively by dry to Thailand's ground azoles amine, croscarmellose sodium and Microcrystalline Cellulose, pulverize, cross 100 orders sieves, obtain safe ground azoles amine powder, croscarmellose sodium and Microcrystalline Cellulose powder respectively;
2) get the safe ground azoles amine of recipe quantity, croscarmellose sodium and Microcrystalline Cellulose, mix, then add 10% pregelatinized Starch solution and make softwood in right amount, cross 40 eye mesh screens and granulate, obtain safe ground azoles amine wet granular;
3) above-mentioned safe ground azoles amine wet granular is dried to moisture under 60 DEG C of conditions and it is less than 5%, obtain the safe ground dry particle of azoles amine
4) the above-mentioned safe ground dry particle of azoles amine being crossed the 40 whole grains of eye mesh screen, then add lubricant, mix, after quality inspection is qualified, compressing tablet, obtains safe ground azoles amine tablet.
Embodiment 2
It is composed as follows that safe ground azoles amine makes the formula of 1000:
Safe ground azoles amine 400g
Croscarmellose sodium 100g
Microcrystalline Cellulose 140g
Micropowder silica gel 1g
10% pregelatinized Starch solution is appropriate
Preparation method
1) respectively by dry to Thailand's ground azoles amine, croscarmellose sodium and Microcrystalline Cellulose, pulverize, cross 100 orders sieves, obtain safe ground azoles amine powder and Microcrystalline Cellulose powder respectively;
2) get the safe ground azoles amine of recipe quantity, croscarmellose sodium and Microcrystalline Cellulose, mix, then add 10% pregelatinized Starch solution and make softwood in right amount, cross 40 eye mesh screens and granulate, obtain safe ground azoles amine wet granular;
3) above-mentioned safe ground azoles amine wet granular is dried to moisture under 60 DEG C of conditions and it is less than 5%, obtain the safe ground dry particle of azoles amine;
4) the above-mentioned safe ground dry particle of azoles amine being crossed the 40 whole grains of eye mesh screen, then add lubricant, mix, after quality inspection is qualified, compressing tablet, obtains safe ground azoles amine tablet.
The useful effect of the safe ground azoles amine tablet of the present invention is described below by way of test example, comparative example.
The study on the stability of [test example 1] product of the present invention
Adopt the safe ground azoles amine tablet that prescription of the present invention and preparation method obtain, through the test of study of pharmacy influence factor, investigate and the results are shown in down:
Conclusion: factors influencing under high temperature, high wet, illumination condition, product appearance of the present invention observe unchanged, disintegration time and content all stable.
The comparative result of [comparative example 1] product of the present invention safe ground azoles amine tablet and its commercially available product dissolution rate
Comparing test with the product of the embodiment of the present invention 1 and commercially available product capsule, result is as follows:
As can be seen from the above table, the stripping trend of the safe ground azoles amine tablet of the present invention is better than existing preparation, and stripping trend is fast.
Claims (5)
1. a stable safe ground azoles drug amine composition, it is characterised in that the formula making 1000 is composed as follows:
Safe ground azoles amine 200-400g
Croscarmellose sodium 50-100g
Microcrystalline Cellulose 70-140g
Micropowder silica gel 0.5-1g
10% pregelatinized Starch solution is appropriate.
2. safe ground according to claim 1 azoles drug amine composition, it is characterised in that the formula making 1000 is composed as follows:
Safe ground azoles amine 200g
Croscarmellose sodium 50g
Microcrystalline Cellulose 70g
Micropowder silica gel 0.5g
10% pregelatinized Starch solution is appropriate.
3. safe ground according to claim 1 azoles drug amine composition, it is characterised in that the formula making 1000 is composed as follows:
Safe ground azoles amine 400g
Croscarmellose sodium 100g
Microcrystalline Cellulose 140g
Micropowder silica gel 1g
10% pregelatinized Starch solution is appropriate.
4. the preparation method of safe ground azoles amine described in claim 1 or 2 or 3, it is characterised in that described preparation method comprises the steps:
1) respectively by dry to Thailand's ground azoles amine, croscarmellose sodium, Microcrystalline Cellulose, pulverize, sieve, obtain safe ground azoles amine powder, croscarmellose sodium powder and Microcrystalline Cellulose powder respectively;
2) get the safe ground azoles amine of recipe quantity, croscarmellose sodium and Microcrystalline Cellulose, mix, then add 10% pregelatinized Starch solution and make softwood in right amount, cross 40 eye mesh screens and granulate, obtain safe ground azoles amine wet granular;
3) above-mentioned safe ground azoles amine wet granular is dried to moisture under 60 DEG C of conditions and it is less than 5%, obtain the safe ground dry particle of azoles amine;
4) the above-mentioned safe ground dry particle of azoles amine being crossed the 40 whole grains of eye mesh screen, then add lubricant, mix, after quality inspection is qualified, compressing tablet, obtains safe ground azoles amine sheet.
5. preparation method according to claim 4, it is characterised in that sieving in step 1) referred to 100 order sieves.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410628830.9A CN105640903A (en) | 2014-11-11 | 2014-11-11 | Stable tedizolid phosphate medicine composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410628830.9A CN105640903A (en) | 2014-11-11 | 2014-11-11 | Stable tedizolid phosphate medicine composition |
Publications (1)
| Publication Number | Publication Date |
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| CN105640903A true CN105640903A (en) | 2016-06-08 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410628830.9A Pending CN105640903A (en) | 2014-11-11 | 2014-11-11 | Stable tedizolid phosphate medicine composition |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106236718A (en) * | 2016-08-29 | 2016-12-21 | 海南通用康力制药有限公司 | A kind of pharmaceutical composition of Tedizolid Phosphate and preparation method thereof |
| CN107519143A (en) * | 2017-09-20 | 2017-12-29 | 甘宜玲 | A kind of antibacterial combination and preparation method thereof |
| CN107625737A (en) * | 2017-09-20 | 2018-01-26 | 山东裕欣药业有限公司 | A kind of preparation method of Tedizolid Phosphate composition tablet |
-
2014
- 2014-11-11 CN CN201410628830.9A patent/CN105640903A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106236718A (en) * | 2016-08-29 | 2016-12-21 | 海南通用康力制药有限公司 | A kind of pharmaceutical composition of Tedizolid Phosphate and preparation method thereof |
| CN107519143A (en) * | 2017-09-20 | 2017-12-29 | 甘宜玲 | A kind of antibacterial combination and preparation method thereof |
| CN107625737A (en) * | 2017-09-20 | 2018-01-26 | 山东裕欣药业有限公司 | A kind of preparation method of Tedizolid Phosphate composition tablet |
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Application publication date: 20160608 |