Tofacitinib tablet with excellent property

A tofacitinib and tablet technology, applied in the field of tofacitinib tablets, can solve problems such as the inability to meet the needs of patients with rheumatoid arthritis

Active Publication Date: 2014-06-11
JIANGSU SEMPOLL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, the preparations on the market are tablets released in a conventional way, which cann

Method used

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  • Tofacitinib tablet with excellent property
  • Tofacitinib tablet with excellent property
  • Tofacitinib tablet with excellent property

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Tofacitinib (160g), hydroxypropyl cellulose (150.0g), low-substituted hydroxypropyl cellulose (400.0g), lactose (1090g) and crystalline cellulose (200.0g) passed The high intensity mixer was mixed for 3 minutes, then magnesium stearate (20.0 g) was added, and the mixture was mixed again using the high intensity mixer to obtain a mixed powder.

[0044] The obtained mixed powder was compressed by using a rotary compressor under a tablet pressure of 6.9 kN so that the tablet mass became about 100 mg and the thickness was not more than 2 mm. The obtained uncoated tablet was sprayed with a mixture of polyvinyl alcohol (OPADRYAMB31W48994 (manufactured by Colorcon (Japan) Limited)), pullulan and sorbitol (wherein, polyvinyl alcohol: pullulan: sorbitol Sugar alcohol=1:1:0.2) and the coating solution that water forms, carry out film-coating in the disc coater, obtain the tablet (coating film gain is 10 to 40% of tablet mass) that contains test compound.

Embodiment 2

[0046] Tofacitinib (160g), hydroxypropyl cellulose (150.0g), low-substituted hydroxypropyl cellulose (400.0g), lactose (1090g) and crystalline cellulose (200.0g) passed The high intensity mixer was mixed for 3 minutes, then magnesium stearate (20.0 g) was added, and the mixture was mixed again using the high intensity mixer to obtain a mixed powder.

[0047] The obtained mixed powder was compressed by using a rotary tablet press under a tablet pressure of 6.9 kN so that the tablet mass became about 100 mg and the thickness was not more than 1 mm. The obtained uncoated tablet was sprayed with a mixture of polyvinyl alcohol (OPADRYAMB31W48994 (manufactured by Colorcon (Japan) Limited)), pullulan, PEG1250 (wherein, polyvinyl alcohol: pullulan: PEG1250=1 : 5: 0.5) and water, were coated in a disc coater to obtain tablets containing the test compound (the coating gain was 30 to 1000% of the mass of the tablet).

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Abstract

The invention discloses a tofacitinib coating tablet with excellent property. The coating tablet comprises a coating basic reagent, tofacitinib and an officinal additive, wherein the coating basic reagent is in a coating layer of the coating tablet and selected from polyvinyl alcohol and Pullulan; and the proportion (wt/wt) of the contents of the polyvinyl alcohol to the Pullulan in the coating tablet is 1: 1-1: 5. The coating tablet is excellent in mechanical property, high in stability, convenient in pharmacy, rapid in effect and efficient.

Description

【Technical field】 [0001] The invention relates to a tablet of tofacitinib with excellent properties. Specifically, it relates to a film-coated tablet of tofacitinib, which is fast and convenient to use, and has rapid and efficient drug action. 【technical background】 [0002] Although many patients with rheumatoid arthritis are using drugs such as Humira (adalimumab), Enli (etanercept), and gram (infliximab), the condition of many patients is still There is no relief, and these drugs are biological products containing large proteins that can only be given intravenously. Tofacitinib, a JAK inhibitor, can improve the life of patients who are ineffective with other drugs. The results of clinical trials suggest that the efficacy is better than that of adalimumab, and it is administered orally and is more convenient to use. [0003] Tofacitinib is a novel oral Janus kinase (JAK) inhibitor discovered and developed by Pfizer scientists and currently on the market (trade name, XELJ...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K31/52A61K47/32A61K47/36A61P19/02A61P29/00A61P17/06
Inventor 付劼王晶夏玲
Owner JIANGSU SEMPOLL PHARMA
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