Tofacitinib citrate tablets and preparation method thereof

A technology of tofacitinib and citric acid, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve problems such as poor stability, uneven product content, and slow dissolution rate, etc. problems, to achieve the effect of fast dissolution rate, high content uniformity and stable chemical properties

Inactive Publication Date: 2016-08-24
HUBEI LIYI PHARM TECH CO LTD +1
View PDF3 Cites 17 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although wet granulation is beneficial to improve the fluidity and compressibility of granules, we found in actual production that tofacitinib citrate is a highly soluble compound, which is prone to migration during the granulation and drying process, resulting in low product content. Uniform, but there are also problems such as slow dissolution rate and poor stability

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Tofacitinib citrate tablets and preparation method thereof
  • Tofacitinib citrate tablets and preparation method thereof
  • Tofacitinib citrate tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] The prescription of table 1 embodiment 1

[0026] type

name

%(w / w)

API

Tofacitinib citrate

13.0

filler

Celactose 80

78.1

disintegrant

Croscarmellose Sodium

4.9

Glidant

silica

1.0

Coating agent

Gastric film coating premix

3.0

[0027] The preparation method is as follows:

[0028] 1) Weigh the raw material and auxiliary materials in proportion, and crush tofacitinib citrate to a particle size of 10-30 μm;

[0029] 2) Mix the tofacitinib citrate powder with the microcrystalline cellulose lactose premix whose model is Celactose80 first, then add croscarmellose sodium and mix evenly; finally add silicon dioxide and mix evenly;

[0030] 3) Tablet pressing: when pressing, the ambient temperature is controlled to be 15°C, the humidity is 60%, and the pressure of the tablet press is 25KN;

[0031] 4) Dissolving the stomach-soluble film coating premix with 60% ethanol, and then applyi...

Embodiment 2

[0033] The prescription of table 2 embodiment 2

[0034] type

name

%(w / w)

API

Tofacitinib citrate

8.5

filler

Celactose 80

81.3

disintegrant

Low-substituted hydroxypropyl cellulose

4.3

Glidant

Magnesium stearate

1.9

Coating agent

Gastric film coating premix

4

[0035] The preparation method is as follows:

[0036] 1) Weigh the raw material and auxiliary materials in proportion, and crush tofacitinib citrate to a particle size of 40-60 μm;

[0037] 2) Mix the tofacitinib citrate powder with the microcrystalline cellulose lactose premix whose model is Celactose80, then add low-substituted hydroxypropyl cellulose and mix evenly; finally add magnesium stearate and mix evenly;

[0038] 3) Tablet compression: when the tablet is pressed, the ambient temperature is controlled to be 20°C, the humidity is 40%, and the pressure of the tablet press is 30KN;

[0039] 4) Dissolving the stomach-sol...

Embodiment 3

[0041] The prescription of table 3 embodiment 3

[0042] type

name

%(w / w)

API

Tofacitinib citrate

4.4

filler

Celactose 80

87.2

disintegrant

Cross-linked polyvinylpyrrolidone

2.8

Glidant

talcum powder

1.1

Coating agent

Gastric film coating premix

4.5

[0043] The preparation method is as follows:

[0044] 1) Weigh the raw materials and auxiliary materials in proportion, and crush tofacitinib citrate to a particle size of 70-90 μm;

[0045] 2) Mix tofacitinib citrate powder with the microcrystalline cellulose lactose premix whose model is Celactose80 first, then add cross-linked polyvinylpyrrolidone and mix evenly; finally add talc powder and mix evenly;

[0046] 3) Tablet compression: control the ambient temperature to be 10° C., the humidity to be 50% during tablet compression, and the pressure of the tablet press to be 28KN;

[0047] 4) Dissolving the stomach-soluble film-coating p...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
Login to view more

Abstract

The invention discloses Tofacitinib citrate tablets composed of Tofacitinib citrate and pharmaceutically acceptable auxiliary materials. The auxiliary materials comprise filler, disintegrating agent, flow aid and coating materials. The filler is microcrystalline cellulose lactose premix with the model of Celactose80, and the weight ratio of the Tofacitinib citrate to the microcrystalline cellulose lactose premix with the model of Celactose80 is 1:5-25. The invention further discloses a preparation method. The Tofacitinib citrate tablets has high content uniformity and have the advantages of being high in dissolving-out speed, stable in chemical property and the like.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a tofacitinib citrate tablet and a preparation method thereof. Background technique [0002] Tofacitinib citrate is a new oral JAK pathway inhibitor developed by Pfizer, which was approved by the FDA in 2012 for the treatment of adults with moderate to severe rheumatoid arthritis who are active and do not respond well to methotrexate . This product can be used alone or in combination with other methotrexate or antirheumatic drugs. [0003] Most of the tofacitinib citrate tablets reported in the literature at present adopt the process of mixing the raw material drug and auxiliary materials first, then wet granulation, and then compressing the tablet. The auxiliary materials used mainly include lactose, microcrystalline cellulose, and starch. Wait. Although wet granulation is beneficial to improve the fluidity and compressibility of granules, we f...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K31/519A61K47/38A61K47/26A61P19/02A61P29/00
CPCA61K9/28A61K9/2018A61K9/2054A61K9/2059A61K31/519
Inventor 洪华云陈贵娣罗松贺娟刘俊
Owner HUBEI LIYI PHARM TECH CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap