CN103585126A - Tofacitinib composition and preparation method thereof - Google Patents

Tofacitinib composition and preparation method thereof Download PDF

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Publication number
CN103585126A
CN103585126A CN201310581713.7A CN201310581713A CN103585126A CN 103585126 A CN103585126 A CN 103585126A CN 201310581713 A CN201310581713 A CN 201310581713A CN 103585126 A CN103585126 A CN 103585126A
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China
Prior art keywords
buddhist nun
strengthening vital
expelling pathogens
pharmaceutical composition
pathogens
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Pending
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CN201310581713.7A
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Chinese (zh)
Inventor
王雪根
何凌云
张用杰
龚丽霞
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NANJING NMG-ADDS Co Ltd
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NANJING NMG-ADDS Co Ltd
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Priority to CN201310581713.7A priority Critical patent/CN103585126A/en
Publication of CN103585126A publication Critical patent/CN103585126A/en
Pending legal-status Critical Current

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Abstract

The invention provides a tofacitinib composition and a preparation method thereof, and belongs to the technical field of medicines. Tofacitinib is an active component, is matched with pharmaceutically acceptable auxiliary materials, and is prepared into the tofacitinib composition by adopting the existing preparation technique. The preparation technique accords with the production requirements, and can guarantee the stability and safety of the preparation. The tofacitinib composition is convenient to transport and preserve, and provides a novel medicine selection for the active phase of adults and the moderate or severe patients suffered from rheumatoid arthritis and not responding well to methotrexate.

Description

A kind of expelling pathogens by strengthening vital QI is for nylon 6 combination and preparation method
Technical field: this relates to a kind of expelling pathogens by strengthening vital QI for Buddhist nun's pharmaceutical composition and preparation method, belongs to medical technical field.
Background technology:
Expelling pathogens by strengthening vital QI for Buddhist nun be a kind of Janus inhibitors of kinases, for methotrexate for treatment is replied insufficient or do not tolerate to severe active rheumatoid arthritis (RA) adult patient.Different in extracellular target spot from other RA medicine Main Functions of current majority, expelling pathogens by strengthening vital QI be take intracellular signal transduction path as target spot for Buddhist nun, acts on the core of cytokine network.Expelling pathogens by strengthening vital QI is to 5~100 of JAK1 and JAK2 times for Buddhist nun (tofacitinib) to the inhibition strength of JAK3.Expelling pathogens by strengthening vital QI is that exploitation is for the pioneering medicine (first-in-class drug) of rheumatoid arthritis treatment for Buddhist nun.
Summary of the invention:
The object of the present invention is to provide a kind of expelling pathogens by strengthening vital QI for Buddhist nun's pharmaceutical composition and preparation method thereof, for provide clinically a kind of economy, safely, facilitate antirheumatic.
The present invention aims to provide a kind of expelling pathogens by strengthening vital QI for Buddhist nun's pharmaceutical composition, it is characterized in that containing active component expelling pathogens by strengthening vital QI for Buddhist nun or its esters and pharmaceutically acceptable excipient substance.
Described expelling pathogens by strengthening vital QI, for Buddhist nun's pharmaceutical composition, is characterized in that described excipient substance is one or more in microcrystalline Cellulose, Lactis Anhydrous, lactose monohydrate, starch, hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose, polyvinylpyrrolidone, crospolyvinylpyrrolidone, magnesium stearate, silicon dioxide.
Described expelling pathogens by strengthening vital QI, for Buddhist nun's pharmaceutical composition, is characterized in that active component is that expelling pathogens by strengthening vital QI replaces Buddhist nun or citric acid expelling pathogens by strengthening vital QI for Buddhist nun.
Described expelling pathogens by strengthening vital QI replaces Buddhist nun's pharmaceutical composition, it is characterized in that, active component and excipient substance quality ratio range are: 1:10-1:90, preferably 1:12-1:50, more preferably 1:15-1:30, most preferably 1:20-1:25.
Described expelling pathogens by strengthening vital QI replaces Buddhist nun's pharmaceutical composition, it is characterized in that, final products are made tablet, capsule or granule, preferred tablet.
Described expelling pathogens by strengthening vital QI, for the preparation method of Buddhist nun's pharmaceutical composition, is characterized in that wet granulation dry granulation alive, preferably wet granulation.
Described expelling pathogens by strengthening vital QI for the preparation method of Buddhist nun's pharmaceutical composition, is characterized in that, comprises following steps;
A): expelling pathogens by strengthening vital QI is replaced to Buddhist nun and excipient substance mix homogeneously;
B): adopt appropriate water to make soft material; And make 18-30 order granule;
C): after dry, obtain dry granule, add hard magnesium, silicon dioxide, by every, containing expelling pathogens by strengthening vital QI, replace Buddhist nun 5mg tabletting, both.
Described expelling pathogens by strengthening vital QI, for Buddhist nun's pharmaceutical composition, is characterized in that preparing the purposes of rheumatism or rheumatoid arthritis.
The specific embodiment:
Below in conjunction with specific embodiment, the invention will be further described, to help understanding content of the present invention.
Example one
Figure BDA0000416843400000021
Method for making: A): expelling pathogens by strengthening vital QI is replaced to Buddhist nun and excipient substance mix homogeneously;
B): adopt appropriate water to make soft material; And make 18-30 order granule;
C): after dry, obtain dry granule, add hard magnesium, silicon dioxide, by every, containing expelling pathogens by strengthening vital QI, replace Buddhist nun 5mg tabletting, both.
Example two
Figure BDA0000416843400000022
Method for making: A): expelling pathogens by strengthening vital QI is replaced to Buddhist nun and excipient substance mix homogeneously;
B): adopt appropriate water to make soft material; And make 18-30 order granule;
C): after dry, obtain dry granule, add hard magnesium, silicon dioxide, by every, containing expelling pathogens by strengthening vital QI, replace Buddhist nun 5mg tabletting, both.

Claims (8)

1. expelling pathogens by strengthening vital QI, for Buddhist nun's pharmaceutical composition, contains active component expelling pathogens by strengthening vital QI for Buddhist nun or its esters and pharmaceutically acceptable excipient substance.
2. described in claims 1, expelling pathogens by strengthening vital QI, for Buddhist nun's pharmaceutical composition, is characterized in that described excipient substance is one or more in microcrystalline Cellulose, Lactis Anhydrous, lactose monohydrate, starch, hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose, polyvinylpyrrolidone, crospolyvinylpyrrolidone, magnesium stearate, silicon dioxide.
3. expelling pathogens by strengthening vital QI, for Buddhist nun's pharmaceutical composition, is characterized in that active component is that expelling pathogens by strengthening vital QI replaces Buddhist nun or citric acid expelling pathogens by strengthening vital QI for Buddhist nun as claimed in claim 1.
4. expelling pathogens by strengthening vital QI, for Buddhist nun's pharmaceutical composition, is characterized in that as claimed in claim 3, and active component and excipient substance quality ratio range are: 1:10-1:90, preferably 1:12-1:50, more preferably 1:15-1:30, most preferably 1:20-1:25.
5. expelling pathogens by strengthening vital QI, for Buddhist nun's pharmaceutical composition, is characterized in that as claimed in claim 4, and final products are made tablet, capsule or granule, preferred tablet.
6. as described in as arbitrary in claim 1-5, expelling pathogens by strengthening vital QI is for the preparation method of Buddhist nun's pharmaceutical composition, it is characterized in that wet granulation live dry granulation, preferably wet granulation.
7. described in claim 6, expelling pathogens by strengthening vital QI, for the preparation method of Buddhist nun's pharmaceutical composition, is characterized in that, comprises following steps;
A): expelling pathogens by strengthening vital QI is replaced to Buddhist nun and excipient substance mix homogeneously;
B): adopt appropriate water to make soft material; And make 18-30 order granule;
C): after dry, obtain dry granule, add hard magnesium, silicon dioxide, by every, containing expelling pathogens by strengthening vital QI, replace Buddhist nun 5mg tabletting, both.
8. described in claim 1-7, expelling pathogens by strengthening vital QI, for Buddhist nun's pharmaceutical composition, is characterized in that preparing the purposes of rheumatism or rheumatoid arthritis.
CN201310581713.7A 2013-11-18 2013-11-18 Tofacitinib composition and preparation method thereof Pending CN103585126A (en)

Priority Applications (1)

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Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103845302A (en) * 2014-03-24 2014-06-11 江苏圣宝罗药业有限公司 Tofacitinib tablet with excellent property
CN104622827A (en) * 2015-03-05 2015-05-20 重庆华邦制药有限公司 Tofacitinib tablet and preparation method thereof
CN105878202A (en) * 2016-05-27 2016-08-24 湖北丽益医药科技有限公司 Tofacitinib citrate tablet and preparation method thereof
CN106176640A (en) * 2014-11-28 2016-12-07 四川海思科制药有限公司 Pharmaceutical composition containing tofacitinib citrate and preparation method thereof
CN106370757A (en) * 2016-11-16 2017-02-01 杭州朱养心药业有限公司 Tofacitinib citrate tablet pharmaceutical composition and quality control method
CN106389371A (en) * 2016-11-16 2017-02-15 杭州朱养心药业有限公司 Tofacitinib citrate pharmaceutical composition
CN106420648A (en) * 2016-11-22 2017-02-22 山东淄博新达制药有限公司 Tofacitinib citrate tablet and preparation method thereof
CN108640921A (en) * 2018-04-03 2018-10-12 山东科兴生物制品有限公司 Preparation method of tofacitinib citrate
CN110946834A (en) * 2018-09-27 2020-04-03 四川科伦药物研究院有限公司 Tofacitinib citrate tablet and preparation process thereof
WO2020135401A1 (en) * 2018-12-24 2020-07-02 正大天晴药业集团股份有限公司 Treatment use of pyrrolopyrimidine compound, and solid pharmaceutical composition of pyrrolopyrimidine compound
WO2021129735A1 (en) * 2019-12-25 2021-07-01 上海宣泰医药科技股份有限公司 Solid preparation, and preparation method therefor and use thereof
RU2810112C2 (en) * 2018-12-24 2023-12-21 Чиа Тай Тянцин Фармасьютикал Груп Ко., Лтд. Medical use of pyrrolopyrimidine compound and solid pharmaceutical composition of pyrrolopyrimidine compound

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CN1325498A (en) * 1998-11-07 2001-12-05 泰科电子雷伊化学有限公司 A panel for supporting a plurality of fibre optic connectors
CN1325498C (en) * 2001-12-06 2007-07-11 辉瑞产品公司 Novel crystalline compound
WO2012100949A1 (en) * 2011-01-27 2012-08-02 Ratiopharm Gmbh Oral dosage forms for modified release comprising tasocitinib

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Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103845302B (en) * 2014-03-24 2016-03-30 江苏知原药业有限公司 A kind of expelling pathogens by strengthening vital QI of excellent performance replaces the tablet of Buddhist nun
CN103845302A (en) * 2014-03-24 2014-06-11 江苏圣宝罗药业有限公司 Tofacitinib tablet with excellent property
CN106176640A (en) * 2014-11-28 2016-12-07 四川海思科制药有限公司 Pharmaceutical composition containing tofacitinib citrate and preparation method thereof
CN104622827A (en) * 2015-03-05 2015-05-20 重庆华邦制药有限公司 Tofacitinib tablet and preparation method thereof
CN105878202A (en) * 2016-05-27 2016-08-24 湖北丽益医药科技有限公司 Tofacitinib citrate tablet and preparation method thereof
CN106389371B (en) * 2016-11-16 2019-03-15 杭州朱养心药业有限公司 tofacitinib citrate pharmaceutical composition
CN106370757A (en) * 2016-11-16 2017-02-01 杭州朱养心药业有限公司 Tofacitinib citrate tablet pharmaceutical composition and quality control method
CN106389371A (en) * 2016-11-16 2017-02-15 杭州朱养心药业有限公司 Tofacitinib citrate pharmaceutical composition
CN106420648A (en) * 2016-11-22 2017-02-22 山东淄博新达制药有限公司 Tofacitinib citrate tablet and preparation method thereof
CN108640921A (en) * 2018-04-03 2018-10-12 山东科兴生物制品有限公司 Preparation method of tofacitinib citrate
CN110946834A (en) * 2018-09-27 2020-04-03 四川科伦药物研究院有限公司 Tofacitinib citrate tablet and preparation process thereof
WO2020135401A1 (en) * 2018-12-24 2020-07-02 正大天晴药业集团股份有限公司 Treatment use of pyrrolopyrimidine compound, and solid pharmaceutical composition of pyrrolopyrimidine compound
CN113242859A (en) * 2018-12-24 2021-08-10 正大天晴药业集团股份有限公司 Therapeutic use of pyrrolopyrimidine compounds and solid pharmaceutical compositions thereof
RU2810112C2 (en) * 2018-12-24 2023-12-21 Чиа Тай Тянцин Фармасьютикал Груп Ко., Лтд. Medical use of pyrrolopyrimidine compound and solid pharmaceutical composition of pyrrolopyrimidine compound
WO2021129735A1 (en) * 2019-12-25 2021-07-01 上海宣泰医药科技股份有限公司 Solid preparation, and preparation method therefor and use thereof
EP4082534A4 (en) * 2019-12-25 2023-12-13 Sinotherapeutics Inc. Solid preparation, and preparation method therefor and use thereof

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Application publication date: 20140219