Tofacitinib citrate sustained release tablet and preparation method thereof

A technology of tofacitinib and citric acid is applied in the directions of pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. Exhaust gas and other issues

Inactive Publication Date: 2020-05-22
JIANGSU ALICORN PHARMATECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The production process of this osmotic tablet is complicated, which is not conducive to large-scale industrial production and will generate a lot of waste gas, and the safety is not high

Method used

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  • Tofacitinib citrate sustained release tablet and preparation method thereof
  • Tofacitinib citrate sustained release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: Preparation of Tofacitinib Citrate Sustained Release Tablets:

[0020] Prescription composition of Tofacitinib Citrate Sustained-release Tablets: Specification 11mg (calculated as Tofacitinib)

[0021] Raw materials Dosage g Tofacitinib citrate 8.1 Compritol@888ATO 4.05 HPMC 24.3 MCC / Lactose 63.05 Magnesium stearate 0.5

[0022] Preparation Process:

[0023] (a) Glyceryl behenate is weighed, heated to 65-70°C for melting, and kept warm;

[0024] (b) Continue to keep warm, add tofacitinib citrate at the same time, use an electric stirrer to stir for more than 30 minutes until it melts, and quickly put it into an ice-water mixture to solidify. After it is completely solidified, grind it and pass it through an 80-mesh sieve to obtain the drug-loaded particles;

[0025] (c) Mix the drug-loaded granules with the prescribed amount of HPMC, MCC / lactose (passed through a 100-mesh sieve), and magnesium stearate, and p...

Embodiment 2

[0026] Embodiment 2: Preparation of Tofacitinib Citrate Sustained Release Tablets:

[0027] Prescription composition of Tofacitinib Citrate Sustained-release Tablets: Specification 11mg (calculated as Tofacitinib)

[0028] Raw materials Dosage g Tofacitinib citrate 8.1 Compritol@888ATO 8.1 HPMC 8.1 MCC / Lactose 75.2 Magnesium stearate 0.5

[0029] Preparation process: with embodiment 1.

Embodiment 3

[0030] Embodiment 3: Preparation of Tofacitinib Citrate Sustained Release Tablets:

[0031] Prescription composition of Tofacitinib Citrate Sustained-release Tablets: Specification 11mg (calculated as Tofacitinib)

[0032] Raw materials Dosage g Tofacitinib citrate 8.1 Compritol@888ATO 24.3 HPMC 24.3 MCC / Lactose 42.3 Magnesium stearate 1

[0033] Preparation process: with embodiment 1.

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Abstract

The invention belongs to the field of pharmaceutical preparations, and specifically relates to a tofacitinib citrate sustained release tablet and a preparation method thereof. The sustained release tablet includes tofacitinib citrate, a skeleton material and a filling agent; and the skeleton material includes a corrosive skeleton material and a hydrophilic gel skeleton material. The sustained release tablet is simple in preparation technology, high in process reproducibility and suitable for large-scale industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a tofacitinib citrate sustained-release tablet and a preparation method thereof. Background technique [0002] Tofacitinib Sustained Release Tablets is an oral drug for rheumatoid arthritis, developed by Pfizer and launched in the United States in 2016. Its chemical name is: 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)aminopyridine- 1-yl)-3-oxopropionitrile, the chemical structural formula is: [0003] [0004] Molecular formula is C 16 h 20 N 6 O, the molecular weight is 504.5, its properties are white to off-white powder, easily soluble in water. Tofacitinib is a JAK kinase inhibitor indicated for the treatment of adults with moderate to severe rheumatoid arthritis who have had an inadequate response to or are allergic to methotrexate. [0005] A tofacitinib citrate sustained-release tablet disclosed in patent WO2014147526A1 is p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K47/14A61K47/38A61K47/26A61K31/519A61P29/00A61P19/02
CPCA61K9/2013A61K9/2018A61K9/2054A61K31/519A61P19/02A61P29/00
Inventor 李莉董海红高超
Owner JIANGSU ALICORN PHARMATECH CO LTD
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