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Tofacitinib tablet and preparation method thereof

A technology of tofacitinib and cloth tablets, which is applied in anti-inflammatory agents, pill delivery, pharmaceutical formulations, etc. It can solve the problems of large weight difference, poor powder fluidity, and lobes, and achieve qualified quality, stable properties, and avoid degradation. Effect

Inactive Publication Date: 2015-05-20
CHONGQING HUAPONT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the direct compression method faces many challenges: 1) The type and dosage of active ingredients and excipients are very picky; 2) The fluidity of the powder is poor; 3) The weight difference is large; 4) It is easy to cause splits
Based on the above problems, at present, there is no process report on the direct compression method of tofacitinib

Method used

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  • Tofacitinib tablet and preparation method thereof
  • Tofacitinib tablet and preparation method thereof
  • Tofacitinib tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] a recipe

[0040] Tofacitinib 5.0g

[0041] Directly compressed lactose 40g

[0042] Microcrystalline Cellulose 50g

[0043] Croscarmellose Sodium 2g

[0044] Magnesium Stearate 2g

[0045] Coating powder Opadry 33G28523 weight gain 3%

[0046] Specification: 5mg

[0047] Two system method

[0048] (1) Ingredients: Weigh the prescribed amount of tofacitinib, direct-pressed lactose, microcrystalline cellulose, croscarmellose sodium, and magnesium stearate, pass the tofacitinib raw material through a 100-mesh sieve, and set aside .

[0049] (2) Mixing: Mix tofacitinib with direct-pressed lactose, microcrystalline cellulose and croscarmellose sodium for 10-20 minutes to make them uniform, and pass through a 100-mesh sieve.

[0050] (3) Add the prescribed amount of magnesium stearate to the medicated powder mixed uniformly in step (2), and mix for 5 minutes to make it uniform.

[0051] (4) Directly compress the uniformly mixed medicinal powder in step (3), and cont...

Embodiment 2

[0054] The formula is as follows:

[0055] Tofacitinib 10.0g

[0056] Directly compressed lactose 80g

[0057] Microcrystalline Cellulose 25g

[0058] Croscarmellose Sodium 6g

[0059] Magnesium stearate 0.8g

[0060] Coating powder Opadry 33G28523 weight gain 3%

[0061] Specification: 5mg

[0062] For the preparation method, refer to Example 1, and the hardness is controlled within the range of 75-100N.

Embodiment 3

[0064] The formula is as follows:

[0065] Tofacitinib 10.0g

[0066] Directly compressed lactose 120g

[0067] Microcrystalline Cellulose 20g

[0068] Croscarmellose Sodium 6g

[0069] Magnesium stearate 0.8g

[0070] Specification: 5mg

[0071] For the preparation method, refer to Example 1. The fluidity and compressibility of the prepared granules do not meet the requirements of the tableting process.

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PUM

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Abstract

The invention belongs to the field of medicine preparations, and particularly relates to a tofacitinib tablet and a preparation method thereof. Direct-pressed lactose and microcrystalline cellulose with good mobility and compression formability are selected by the tablet as a diluent and a drying adhesive. The tablet is prepared by direct powder compression method. The tablet is simple in technology, time-saving and energy-saving; the prepared tofacitinib composition is controllable in quality; and the stability of the product is ensured.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a tofacitinib tablet composition and a preparation method thereof. Background technique [0002] Tofacitinib, chemical name: 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino Piperidin-1-yl)-3-oxopropionitrile, the molecular formula is C 16 h 20 N 6 O, the molecular weight is 504.5, the chemical structure formula is: [0003] [0004] Tofacitinib is a JAK kinase inhibitor. It is used for adult patients with moderate to severe rheumatoid arthritis who have not responded well to methotrexate or are allergic to methotrexate. This product can be used alone or in combination with methotrexate or other non-biological disease-modifying antirheumatic drugs (DMARDs). [0005] Chinese patent application number 201310581713.7 discloses a tofacitinib composition and a preparation method thereof. The excipients disclosed in the composition inc...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/36A61K31/519A61K47/38A61K47/26A61P29/00A61P19/02
Inventor 徐宏杨兰昌云程刚胡渝慧张莉
Owner CHONGQING HUAPONT PHARMA
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