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Tofacitinib controlled release tablet, preparation method and application of Tofacitinib controlled release tablet

A technology of tofacitinib and controlled-release tablets, which is applied in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the problems of inconvenient operation, long production cycle, environmental pollution, etc.

Active Publication Date: 2020-05-15
SHANGHAI BOCIMED PHARM RES CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to provide a tofacitinib control agent in order to overcome defects such as complex preparation process, inconvenient operation, long production cycle, serious environmental pollution and unsuitability for industrialized production in the prior art. Release tablet, preparation method and application thereof

Method used

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  • Tofacitinib controlled release tablet, preparation method and application of Tofacitinib controlled release tablet
  • Tofacitinib controlled release tablet, preparation method and application of Tofacitinib controlled release tablet
  • Tofacitinib controlled release tablet, preparation method and application of Tofacitinib controlled release tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Tablet core prescription

[0068] name Mass percentage (%) Tofacitinib citrate 8.9 lactose monohydrate 66.1 Crospovidone 12 Hydroxypropyl Cellulose 6 Copovidone 6 Magnesium stearate 1

[0069] Coating prescription

[0070]

[0071] * is the solid content of polyvinyl acetate 30% aqueous dispersion.

[0072] Step (1) Premixing: Weigh the prescribed amount of tofacitinib citrate, lactose monohydrate, crospovidone, hydroxypropyl cellulose, and copovidone in a three-dimensional mixer, and set the frequency to 30Hz for mixing 10 minutes to obtain a mixture. The obtained mixture was passed through a 30-mesh sieve, placed in a three-dimensional mixer, and mixed for 5 minutes to obtain a premix.

[0073] Step (2) total blending: the premix obtained in step (1) is added with a prescribed amount of magnesium stearate, added to a three-dimensional mixer, set at a frequency of 30 Hz, and mixed for 5 minutes to obtain a total...

Embodiment 2

[0079] Tablet core prescription

[0080] name Mass percentage (%) Tofacitinib citrate 8.9 lactose monohydrate 68.1 Crospovidone 8 Hydroxypropyl Cellulose 8 Copovidone 6 Magnesium stearate 1

[0081] Coating prescription

[0082]

[0083]

[0084] * is the solid content of polyvinyl acetate 30% aqueous dispersion.

[0085] Step (1) Premixing: Weigh the prescribed amount of tofacitinib citrate, lactose monohydrate, crospovidone, hydroxypropyl cellulose, and copovidone in a three-dimensional mixer, and set the frequency to 30Hz for mixing 10 minutes to obtain a mixture. The obtained mixture was passed through a 30-mesh sieve, placed in a three-dimensional mixer, and mixed for 5 minutes to obtain a premix.

[0086] Step (2) total blending: add the prescribed amount of magnesium stearate to the premix obtained in step (1), add it into a three-dimensional mixer, set the frequency to 30 Hz, and mix for 5 minutes to obtain a...

Embodiment 3

[0092] Tablet core prescription

[0093] name Mass percentage (%) Tofacitinib citrate 8.9 lactose monohydrate 70.1 Crospovidone 6 Hydroxypropyl Cellulose 8 Copovidone 6 Magnesium stearate 1

[0094] Coating prescription

[0095]

[0096] * is the solid content of polyvinyl acetate 30% aqueous dispersion.

[0097] Step (1) Premixing: Weigh the prescribed amount of tofacitinib citrate, lactose monohydrate, crospovidone, hydroxypropyl cellulose, and copovidone in a three-dimensional mixer, and set the frequency to 30Hz for mixing 10 minutes to obtain a mixture. The obtained mixture was passed through a 30-mesh sieve, placed in a three-dimensional mixer, and mixed for 5 minutes to obtain a premix.

[0098] Step (2) total blending: add the prescribed amount of magnesium stearate to the premix obtained in step (1), add it to a three-dimensional mixer, set the frequency to 30 Hz, and mix for 5 minutes to obtain the total blend; ...

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Abstract

The invention discloses a tofacitinib controlled release tablet, a preparation method and application of the tofacitinib controlled release tablet. The tofacitinib controlled release tablet consists of a medicine-containing tablet core and a controlled release coating film, wherein the medicine-containing tablet core contains a tofacitinib raw material and an auxiliary material; and the controlledrelease coating film contains a film-forming material, a pore-forming agent and / or an excipient. The preparation process of the tofacitinib controlled release tablet requires no laser drilling or special precision equipment, and is simple, easy to implement, low in production cost and short in period, and no organic solvent is used in a coating liquid preparation process, so that adverse effectson the human body and the environment are avoided, and the preparation process is suitable for industrial production.

Description

technical field [0001] Tofacitinib controlled-release tablet, preparation method and application thereof. Background technique [0002] Tofacitinib is an oral JAK inhibitor developed by Pfizer. Indicated for adults with moderately to severely active rheumatoid arthritis (RA) who have had insufficient response or intolerance to methotrexate, in combination with methotrexate or other nonbiologic disease-modifying antirheumatic drugs (DMARDs) use. Its chemical name is 3-((3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidine-1 -yl)-3-oxo-propionitrile, the chemical formula is C 16 h 20 N 6 O, the structural formula is as follows: [0003] [0004] The currently marketed products are Pfizer's Xeljanz and Xeljanz XR. Patents WO01 / 42246, WO02 / 096909 and WO03 / 048162 describe tofacitinib immediate release tablet dosage form, trade name is Xeljanz, this immediate release tablet dosage form needs to be taken twice a day, lacks convenience and poor com...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K9/22A61K47/32A61K47/38A61K31/519A61P19/02A61P29/00A61P37/06A61P17/06A61P3/10A61P11/06A61P25/28A61P35/02A61P17/00
CPCA61K9/2866A61K9/284A61K9/2054A61K9/2027A61K31/519A61P19/02A61P29/00A61P37/06A61P17/06A61P3/10A61P11/06A61P25/28A61P35/02A61P17/00
Inventor 何新怡徐鹏飞雷伯开王婷婷应述欢
Owner SHANGHAI BOCIMED PHARM RES CO LTD
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