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Tofacitinib citrate

A technology of cloth citrate and cloth citric acid, which is applied in the field of medicine, can solve the problems of poor viscosity and fluidity, and is not suitable for direct compression, and achieves the effects of good dissolution and dissolution performance, good dissolution rate, and good fluidity.

Active Publication Date: 2016-08-17
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Generally, active substances with small particle sizes are viscous or have poor flowability, therefore, those skilled in the art noticed that active substances with small particle sizes are not suitable for direct compression

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0135] Embodiments of the present invention first disclose tofacitinib citrate having a median particle size of less than 40 μm. Although various embodiments have been disclosed in the present invention, various adjustments and modifications can be made by those skilled in the art within the scope of the present invention based on common knowledge in the art. The modification includes equivalent replacement of any aspect of the invention with a solution that is basically the same or included in the present invention that is obvious to those skilled in the art in order to achieve substantially the same effect. Numerical ranges are inclusive of the numerical values ​​defining the range. Furthermore, numerical ranges are provided such that in addition to reciting individually specific numerical values ​​within the range, also numerical ranges outside the range are also recited.

[0136] N-((3R4R)-1-benzyl-4-methylpiperidin-3-yl)-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine as dis...

Embodiment A

[0137] The preparation of embodiment A Tofacitinib citrate

[0138] Into a round bottom flask equipped with hydrogen was added 10% palladium hydroxide on carbon (0.56 g), methanol (20 ml), acetic acid (0.5 g) and N-methyl-N-{(3R,4R)-1-benzyl Base-4-methylpiperidin-3-yl}-7H-pyrrole[2,3-d]pyrimidin-4-amine (2.8g), was first replaced by nitrogen, and then hydrogen (1atm). The resulting mixture was reacted at 50°C for about 6 hours. After the reaction was complete, the solid was removed by filtration, the filtrate was concentrated, and ethanol (20ml) was added to the obtained concentrate. Monocarb-7-ene (3.8g), ethyl cyanoacetate (3.7g), and the mixture was stirred at room temperature for about 6 hours. Add citric acid (3.5g) and water (18ml) directly without treatment, stir at room temperature, and a solid precipitates, which is filtered to obtain tofacitinib citrate. The particle size distribution measurement results are as follows: D50 is 56.973 μm, D10 is 17.348 μm, D90 is 2...

Embodiment 1

[0139] Example 1: Preparation of Tofacitinib Citrate Form A

[0140] Tofacitinib citrate (10g, prepared according to the method of Example A), ethanol (100ml), water (60ml), was added to a round bottom flask to form a mixed solution, stirred at a speed of 300rpm and heated to reflux to form a solution, The solution was stirred at reflux temperature for 1 hour and then cooled to 40°C. After being kept at 40°C for 1 hour, the mixture was cooled to 10°C and maintained at this temperature for 2 hours, filtered, and vacuum-dried at 45°C for 10 hours to obtain tofacitinib citrate Crystal 9.52g. The X-ray powder diffraction pattern of gained tofacitinib citrate crystal is shown in figure 1 .

[0141] The particle size distribution results of the obtained tofacitinib citrate crystals are: D50 is 5.816 μm, D10 is 1.837 μm, D90 is 16.782 μm, detection instrument: Malvern Mastersizer 2000 particle size analyzer, dispersion pressure is 3.0Bar, sample injection The rate is 50%.

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Abstract

Crystalline particle of tofacitinib citrate, process for the preparation of a crystalline particle of tofacitinib citrate, pharmaceutical composition, substantially pure amorphous form of tofacitinib citrate, process for preparing the substantially pure amorphous form of tofacitinib citrate, and use of the crystalline particle of tofacitinib citrate, and the pharmaceutical composition are provided.

Description

[0001] Cross-Referenced Related Applications [0002] This application claims the priority of the patent application No. 201310464169.8 submitted to the State Intellectual Property Office of China on October 8, 2013, the entire content of which is cited as a reference. technical field [0003] The invention relates to the field of medicine, in particular to tofacitinib citrate, more specifically to tofacitinib citrate crystal particles, a preparation method for tofacitinib citrate crystal particles, a pharmaceutical composition and the use. Background technique [0004] Tofacitinib citrate, also known as 3-[(3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)- Amino]-piperidin-1-yl]-3-oxo-propionitrile citrate, the structure is as shown in formula (I): [0005] [0006] PCT application WO2003048162 discloses a new crystal form of tofacitinib citrate and its preparation method, but the crystal particle size prepared according to the method of WO2003048162 is rela...

Claims

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Application Information

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IPC IPC(8): C07D487/04C07C51/43C07C59/265A61K31/519A61P37/06A61P37/02A61P19/02A61P29/00A61P17/06A61P3/10A61P35/00A61P17/00A61P11/06A61P1/04A61P25/28A61P35/02
CPCA61P1/04A61P3/10A61P11/06A61P17/00A61P17/06A61P19/02A61P25/28A61P29/00A61P35/00A61P35/02A61P37/02A61P37/06C07C51/43C07C59/265C07D487/04
Inventor 雷鑫彭锦安郭朕
Owner SUNSHINE LAKE PHARM CO LTD
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