CN106606493A - Tofacitinib medicine composite and preparation method thereof - Google Patents
Tofacitinib medicine composite and preparation method thereof Download PDFInfo
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- CN106606493A CN106606493A CN201510685937.1A CN201510685937A CN106606493A CN 106606493 A CN106606493 A CN 106606493A CN 201510685937 A CN201510685937 A CN 201510685937A CN 106606493 A CN106606493 A CN 106606493A
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- tropsch imatinib
- pharmaceutical composition
- microcrystalline cellulose
- pregelatinized starch
- tofacitinib
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Abstract
The invention discloses a tofacitinib medicine composite. The tofacitinib medicine composite contains tofacitinib, a disintegrating agent, microcrystalline cellulose and pregelatinized starch. The tofacitinib medicine composite is characterized in that the weight ratio between the microcrystalline cellulose and the pregelatinized starch is 1:2. The tofacitinib medicine composite has good stability and has more remarkable advantages of improving the product yield, reducing cost, achieving industrialization and being better applied to clinical practice. The dissolution rate of the tofacitinib medicine composite can be effectively improved, and the bioavailability of the tofacitinib medicine composite is significantly improved.
Description
Technical field
The invention belongs to pharmaceutical technology field, and in particular to tropsch imatinib pharmaceutical composition and preparation method thereof.
Background technology
Tropsch imatinib (tofacitinib) is a kind of novel oral Janus kinases (JAK) inhibitor, the medicine is found and is developed by Pfizer scientist, (trade name, XELJANZ) is listed at present for the treatment of moderate to severe chronic psoriasis in plaques adult patient.
Tropsch imatinib has a kind of mechanism of action of novelty, it is intended to suppress JAK paths, these paths are considered as having played important function in psoriasises chronic inflammatory reaction.Cytokine signaling conduction, the gene expression of cytokine induction and the activation of cell can be reduced by suppressing these JAK paths, tofacitinib.
The present inventor is through the research to prior art, have been surprisingly found that, using tropsch imatinib pharmaceutical composition prepared by special adjuvant, special process, reliable in quality, dissolution rate is fast, not only successfully solve the problems, such as that tropsch imatinib is unstable, and be easy to industrialization, reduce production cost, it is easy to implement, remarkable in economical benefits.
The content of the invention
The first object of the present invention is to provide a kind of tropsch imatinib pharmaceutical composition, and the tropsch imatinib pharmaceutical composition to good stability, to improving product yield, realize industrialization, be preferably applied to clinic, with more obvious advantage by reduces cost.
The second object of the present invention is the preparation method for providing tropsch imatinib pharmaceutical composition of the present invention, simple, the prepared tropsch imatinib pharmaceutical composition of the method, steady quality reliability.
To realize the first object of the present invention, present inventors have surprisingly found that a kind of pharmaceutical composition of tropsch imatinib, said composition contains tropsch imatinib, disintegrating agent, Microcrystalline Cellulose and pregelatinized Starch, it is characterised in that Microcrystalline Cellulose is 1-2 with the weight ratio of pregelatinized Starch.
Specifically, the pharmaceutical composition containing tropsch imatinib of the invention, the component and percentage by weight that it contains be：
Tropsch imatinib 10%
Disintegrating agent 3-6%
Microcrystalline Cellulose 30-60%
Pregelatinized Starch 30-60%
Wherein, described disintegrating agent is selected from polyvinylpolypyrrolidone, one or more in Croscarmellose Sodium or CCMS-Na.Preferred disintegrating agent is selected from polyvinylpolypyrrolidone.
Microcrystalline Cellulose and pregelatinized Starch are the filleies of the present invention, can contain appropriate lubricant as needed, for example, can contain appropriate micropowder silica gel or one or two the mixture in magnesium stearate.
The preparation method of the pharmaceutical composition containing tropsch imatinib is above：The adjuvant for taking tropsch imatinib and formula ratio is crushed, and is sieved for subsequent use；Tropsch imatinib is mixed homogeneously with adjuvant mixture；Mixture content of dispersion is determined, piece weight is calculated, tabletting, coating are obtained final product.
The present invention preferred version be：
Tropsch imatinib
10%
Polyvinylpolypyrrolidone 6%
Microcrystalline Cellulose 40%
Pregelatinized Starch 40%
Magnesium stearate
2%
Micropowder silica gel
2%
The concrete preparation method of above-mentioned tropsch imatinib pharmaceutical composition comprises the steps：
1)
Prepare：Polyvinylpolypyrrolidone, pregelatinized Starch, Microcrystalline Cellulose, magnesium stearate and micropowder silica gel are dried 4 hours under the conditions of 80 DEG C, it is standby；
2)
The pregelatinized Starch of recipe quantity, Microcrystalline Cellulose and tropsch imatinib are put in container, after mix homogeneously, granularity is ground in 80 ± 10um, it is standby；
3)
By 2）Mix homogeneously with the polyvinylpolypyrrolidone of recipe quantity, magnesium stearate and micropowder silica gel；
4)
Tabletting：Suitable stiff and piece weight are adjusted, tabletting is carried out；
5)Coating：The film coating agent of recipe quantity is configured to into the solution that content is 10% with 70% ethanol, coating pan rotating speed, inlet temperature, pressure is adjusted, is coated；
6)
Packaging：Packed using aluminium-plastic bubble plate packing machine；
7)
Warehouse-in.
On the basis of existing pharmaceutical adjunct and preparation technology, the present inventor is had found through substantial amounts of experimental study, filler is selected, find the necessary proportion relation of two kinds of filleies, during so that tropsch imatinib pharmaceutical composition being above-mentioned formula and preparation technology, described drug regimen amount of substance is effectively ensured.
Compared with prior art, the invention has the advantages that：
1)
For improving the yield of the product, reducing production cost, be preferably applied to clinical treatment has very big help to tropsch imatinib pharmaceutical composition provided by the present invention.
2) new tropsch imatinib compositionss Jing industrialized great production provided by the present invention and study on the stability, it was demonstrated that product quality is stable.
3) preparation method of new tropsch imatinib compositionss provided by the present invention, simple, the prepared tropsch imatinib pharmaceutical composition reliable in quality of the method.
4) new tropsch imatinib compositionss provided by the present invention, dissolution are fast, and with higher bioavailability, being rapidly reached needs concentration.
Specific embodiment
Following examples are only used for explaining the present invention, rather than limit the present invention.Unless otherwise indicated, the experiment condition in the embodiment of the present invention is the conventional experiment condition in this area.
Embodiment
1
Per the tropsch imatinib pharmaceutical composition described in 1000, its formula is consisted of：
Tropsch imatinib
5g
Polyvinylpolypyrrolidone
3g
Microcrystalline Cellulose 20g
Pregelatinized Starch
20g
Magnesium stearate
1g
Micropowder silica gel
1g
Preparation technology：
1)
Prepare：Polyvinylpolypyrrolidone, pregelatinized Starch, Microcrystalline Cellulose, magnesium stearate and micropowder silica gel are dried 4 hours under the conditions of 80 DEG C, it is standby；
2)
The pregelatinized Starch of recipe quantity, Microcrystalline Cellulose and tropsch imatinib are put in container, after mix homogeneously, granularity is ground in 80 ± 10um, it is standby；
3)
By 2）Mix homogeneously with the polyvinylpolypyrrolidone of recipe quantity, magnesium stearate and micropowder silica gel；
4)
Tabletting：Suitable stiff and piece weight are adjusted, tabletting is carried out；
5)Coating：The film coating agent of recipe quantity is configured to into the solution that content is 10% with 70% ethanol, coating pan rotating speed, inlet temperature, pressure is adjusted, is coated；
6)
Packaging：Packed using aluminium-plastic bubble plate packing machine；
7)
Warehouse-in.
Embodiment
2
Per the tropsch imatinib pharmaceutical composition described in 1000, its formula is consisted of：
Tropsch imatinib
5g
Polyvinylpolypyrrolidone
3g
Microcrystalline Cellulose 26.7g
Pregelatinized Starch
13.3g
Magnesium stearate
1g
Micropowder silica gel
1g
Preparation technology：With embodiment 1.
Test example
1
The test example is to investigate the stability of tropsch imatinib compositionss provided by the present invention.
The accelerated test of tropsch imatinib pharmaceutical composition
Method according to embodiment of the present invention 1-2 prepares tropsch imatinib pharmaceutical composition, and at 40 DEG C ± 2 DEG C, the condition of RH75% ± 5% is placed 6 months, and period is sampled respectively at the 1st, 2,3,6 months, is detected according to stability inspection project, and is compared with 0 day data.
1st, investigate project
High spot reviews：Character, about material and content.
2nd, accelerated test result
Above conclusion (of pressure testing) can be seen that：Embodiments of the invention 1-2 places 6 months every Testing index no significant differences compared with 0 month under the conditions of accelerated test, and good stability, impurity content are few, while having preferable dissolution.
Test example 2
Using 2010 editions annex X C the second methods of dissolution method of Chinese Pharmacopoeia（Slurry processes）75rpm.Using the Ph4.5 acetate buffers 900mL containing 0.2%SDS as dissolution medium, the stripping curve of tablet prepared by Example 1 and Example 2 of the present invention is detected, it is as a result as follows：
Testing result is illustrated, using the sample of method of the present invention preparation, with quick dissolution rate.
Claims (6)
1. a kind of tropsch imatinib pharmaceutical composition, said composition contain tropsch imatinib, disintegrating agent, Microcrystalline Cellulose and pregelatinized Starch, it is characterised in that Microcrystalline Cellulose is 1-2 with the weight ratio of pregelatinized Starch.
2. tropsch imatinib pharmaceutical composition according to claim 1, it is characterised in that the percentage by weight of each component is：
Tropsch imatinib 10%
Disintegrating agent 3-6%
Microcrystalline Cellulose 30-60%
Pregelatinized Starch 30-60%.
3. tropsch imatinib pharmaceutical composition according to claim 1 and 2, it is characterised in that described disintegrating agent is selected from polyvinylpolypyrrolidone.
4. tropsch imatinib pharmaceutical composition according to claim 3, it is characterised in that also containing one or two in magnesium stearate or micropowder silica gel.
5. tropsch imatinib pharmaceutical composition according to claim 4, it is characterised in that described component and percentage by weight are：
Tropsch imatinib
10%
Polyvinylpolypyrrolidone 6%
Microcrystalline Cellulose 40%
Pregelatinized Starch 40%
Magnesium stearate
2%
Micropowder silica gel
2%。
6. a kind of preparation method of the tropsch imatinib pharmaceutical composition according to claim 4-5 any one, the method comprise the steps：
1) Prepare：Polyvinylpolypyrrolidone, pregelatinized Starch, Microcrystalline Cellulose, magnesium stearate and micropowder silica gel are dried 4 hours under the conditions of 80 DEG C, it is standby；
2) The pregelatinized Starch of recipe quantity, Microcrystalline Cellulose and tropsch imatinib are put in container, after mix homogeneously, granularity is ground in 80 ± 10um, it is standby；
3) By 2）Mix homogeneously with the polyvinylpolypyrrolidone of recipe quantity, magnesium stearate and micropowder silica gel；
4) Tabletting：Suitable stiff and piece weight are adjusted, tabletting is carried out；
5)Coating：The film coating agent of recipe quantity is configured to into the solution that content is 10% with 70% ethanol, coating pan rotating speed, inlet temperature, pressure is adjusted, is coated；
6) Packaging：Packed using aluminium-plastic bubble plate packing machine；
7) Warehouse-in.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510685937.1A CN106606493A (en) | 2015-10-22 | 2015-10-22 | Tofacitinib medicine composite and preparation method thereof |
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|---|---|---|---|
| CN201510685937.1A CN106606493A (en) | 2015-10-22 | 2015-10-22 | Tofacitinib medicine composite and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN106606493A true CN106606493A (en) | 2017-05-03 |
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|---|---|---|---|
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107441054A (en) * | 2017-08-24 | 2017-12-08 | 福建省微生物研究所 | A kind of tropsch imatinib tablet and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104622827A (en) * | 2015-03-05 | 2015-05-20 | 重庆华邦制药有限公司 | Tofacitinib tablet and preparation method thereof |
-
2015
- 2015-10-22 CN CN201510685937.1A patent/CN106606493A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104622827A (en) * | 2015-03-05 | 2015-05-20 | 重庆华邦制药有限公司 | Tofacitinib tablet and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 石彦勃等: "采用预胶化淀粉消除传统辅料对片剂的不良影响", 《辽宁药物与临床》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107441054A (en) * | 2017-08-24 | 2017-12-08 | 福建省微生物研究所 | A kind of tropsch imatinib tablet and preparation method thereof |
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| TA01 | Transfer of patent application right | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20181017 Address after: 272000 6 East Outer Ring Road, hi tech Zone, Jining, Shandong Applicant after: Shandong Lukang Pharmaceutical Co., Ltd. Address before: 300409 88 Huashi Road, Beichen science and Technology Park, Beichen District, Tianjin Applicant before: Tianjin Hankang Pharmaceutical Biotechnology Co., Ltd. |
|
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20170503 |