Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Tofacitinib-citrate tablet and method for preparing tofacitinib-citrate tablet

A technology of citric acid and cloth tablets, which is applied in anti-inflammatory agents, pill delivery, and pharmaceutical formulations. The effect of punching and process reproducibility is good

Inactive Publication Date: 2017-02-22
山东淄博新达制药有限公司
View PDF5 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] (1) The raw materials are easily hydrolyzed when exposed to water, so this product is not suitable for wet granulation;
[0005] (2) The raw materials are astringent, and the powder is easy to stick to the direct pressure;
[0006] (3) The reproducibility and operability of the dry granulation process are poor, the requirements for equipment are high, and the process is cumbersome

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 tablet and method for preparing tofacitinib-citrate tablet
  • Tofacitinib-citrate tablet and method for preparing tofacitinib-citrate tablet
  • Tofacitinib-citrate tablet and method for preparing tofacitinib-citrate tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] (1) Formula composition:

[0041] Table 1-1 Recipe 1

[0042]

[0043]

[0044] (2) Preparation:

[0045] ①Pretreatment: Pass magnesium stearate through a 40-mesh sieve, and other raw and auxiliary materials through a 80-mesh sieve, and set aside.

[0046] ②Initial mixing: weigh tofacitinib citrate, microcrystalline cellulose, lactose, and croscarmellose sodium and mix for 20 minutes. Take 3 samples from different positions, detect the content of each point and calculate the RSD, if RSD≤2.0%, it is judged that the mixture is uniform.

[0047] ③Total blending: Weigh the formula amount of magnesium stearate and add it to the above powder, mix for 10 minutes, take samples at the 5th and 10th minutes respectively, take 3 samples at three different positions each time, measure the content of each point and calculate the RSD , RSD≤2.0% judges that the mixture is uniform.

[0048] ④Detect the angle of repose of the powder.

[0049] ⑤ Tablets.

[0050] (3) Testing: ...

Embodiment 2

[0056] (1) Formula composition:

[0057] Table 2-1 Recipe 2

[0058]

[0059] (2) Preparation:

[0060] The preparation process is the same as that in Example 1.

[0061] (3) Detection: See Table 2-2 for the results.

[0062] Table 2-2 Determination results of formula 2

[0063]

[0064] (4) Dissolution test; the results are shown in Table 2-3.

[0065] Table 2-3 Dissolution comparison between formulation 2 tablet and reference drug (medium: 0.1mol / L hydrochloric acid)

[0066] sampling time commercially available Recipe 3 5min 87.9％ 64.8％ 10min 96.8％ 88.5％ 15min 99.8％ 100.4％ 30min 102.3％ 102.0％ 45min 102.5％ 101.8％

[0067] (5 Conclusion:

[0068]The disintegration time limit of the formulation 2 tablet was basically the same as that of the control drug, but the initial dissolution rate was significantly slower than that of the control drug. Lactose in the formula is a soluble excipient that has a solubilizing ef...

Embodiment 3

[0070] (1) Formula composition:

[0071] Table 3-1 Recipe 3

[0072]

[0073] (2) Preparation:

[0074] The preparation process is the same as that in Example 1.

[0075] (3) Testing, the results are shown in Table 3-2.

[0076] Table 3-2 Determination results of formula 3

[0077]

[0078] (4) Dissolution determination:

[0079] Table 3-3 Dissolution comparison between formula 3 tablet and reference drug (medium: 0.1mol / L hydrochloric acid)

[0080] sampling time commercially available Recipe 4 5min 87.9％ 71.8％ 10min 96.8％ 89.3％ 15min 99.8％ 99.4％ 30min 102.3％ 100.0％ 45min 102.5％ 102.1％

[0081] (5 Conclusion:

[0082] The initial dissolution rate of the formula 3 tablet was faster than that of the formula 2 tablet, but still slower than that of the reference drug. Therefore, continue to increase the amount of lactose in the formula, accelerate the initial dissolution rate, and design formula 4.

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
Hardnessaaaaaaaaaa
Login to View More

Abstract

The invention relates to a tofacitinib-citrate tablet and a method for preparing the tofacitinib-citrate tablet, and belongs to the technical field of medical preparations. The tofacitinib-citrate tablet provided by the invention is prepared from an active ingredient, an auxiliary material and coating powder, wherein the active ingredient is tofacitinib citrate; the auxiliary material is prepared from the following raw materials in percentage by weight: 57 to 62 percent of microcrystalline cellulose, 30 to 35 percent of lactose, 2.0 to 3.0 percent of croscarmellose sodium, 3.0 to 4.0 percent of compound lubricant and 0.5 to 1.5 percent of glidant; metering is carried out according to that the total mass of the active ingredient and the auxiliary material is 100 percent. According to the tofacitinib-citrate tablet provided by the invention, the raw material formula is changed; the sticking problem is solved. The invention provides a method for preparing the tofacitinib-citrate tablet, which is simple to operate and good in reproducibility, at the same time.

Description

technical field [0001] The invention relates to a tofacitinib citrate tablet and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Tofacitinib, also known as tofacitinib, is a novel oral JAK pathway inhibitor developed by Pfizer. Unlike most other current RA therapeutic drugs that mainly act on extracellular targets, tofacitinib targets intracellular signal transduction pathways and acts on the core part of the cytokine network. The inhibitory effect of tofacitinib on JAK3 is 5-100 times that of JAK1 and JAK2. Tofacitinib is the first drug developed for the treatment of rheumatoid arthritis. The FDA approved JAK inhibitors on November 6, 2012 for the treatment of adults with moderate to severe disease that is active and does not respond well to methotrexate. patients with rheumatoid arthritis. Tofacitinib can be used alone or in combination with methotrexate and other selected standard therapy drug...

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
IPC IPC(8): A61K9/30A61K47/38A61K47/26A61K47/12A61K47/02A61K31/519A61P29/00A61P19/02
CPCA61K9/2866A61K9/2009A61K9/2013A61K9/2018A61K9/2054A61K31/519
Inventor 吴照刚贾法强赵玉周梅
Owner 山东淄博新达制药有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com