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Tofacitinib citrate composition and preparation method thereof

A technology of tofacitinib and citric acid, which is applied in the field of medicine and can solve problems such as inability to administer drugs

Active Publication Date: 2019-06-18
南京安美医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, tofacitinib citrate tablets or sustained-release tablets that have been marketed at home and abroad are oral solid preparations, which need to be swallowed with water and are usually only suitable for adults without dysphagia. For children or elderly patients who have difficulty swallowing no medicine

Method used

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  • Tofacitinib citrate composition and preparation method thereof
  • Tofacitinib citrate composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] prescription:

[0054] Tofacitinib citrate (according to Tofacitinib) 50mg

[0055] Sucralose 30mg

[0056] Proper amount of citric acid (final solution pH value to 3.8)

[0057] Orange flavor 20mg

[0058] Benzyl alcohol 50mg

[0059] Water, add appropriate amount to 100ml

[0060] Preparation method: Add the prescribed amount of tofacitinib citrate, sucralose, orange essence, and benzyl alcohol into 85% purified water, stir well to dissolve it, and then adjust the pH value of the solution with 1mol / L citric acid solution 3.46, add water to the full amount, and check the pH value again to be 3.83, that is to say. This oral solution is marked as Ex2.

Embodiment 2

[0062] prescription:

[0063] Tofacitinib citrate (according to Tofacitinib) 50mg

[0064] Sucralose 30mg

[0065] Appropriate amount of citric acid (final solution pH value to 3.9)

[0066] Orange flavor 20mg

[0067] Propionic acid 50mg

[0068] Water, add appropriate amount to 100ml

[0069] Preparation method: Add the prescribed amount of tofacitinib citrate, sucralose, orange essence, and propionic acid into 85% purified water, stir well to dissolve it, and then adjust the pH value of the solution with 1mol / L citric acid solution 3.38, make up the water to the full amount, and check the pH value again to be 3.89, that is to say. This oral solution is marked as Ex2.

Embodiment 3

[0071] prescription:

[0072] Tofacitinib citrate (according to Tofacitinib) 10mg

[0073] Sucrose 10g

[0074] Appropriate amount of hydrochloric acid (final solution pH value to 3.3)

[0075] Strawberry flavor 5mg

[0076] Sodium Benzoate 25mg

[0077] Water, add appropriate amount to 100ml

[0078] Preparation method: Add the prescribed amount of tofacitinib citrate, strawberry essence, and sodium benzoate into 85% purified water, stir well to dissolve, then adjust the pH value of the solution to 3.04 with 1mol / L hydrochloric acid solution, and make up the water to the full amount , and the pH value was detected again to be 3.32, that is to say. The oral solution is labeled Ex3.

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Abstract

The invention relates to a tofacitinib citrate oral solution, in particular to a tofacitinib citrate oral solution with more stable pharmaceutical properties and a preparation method of the tofacitinib citrate oral solution. The tofacitinib citrate oral solution is prepared from tofacitinib citrate, a pH regulator, a preservative, a flavoring agent and water. The tofacitinib citrate oral solutionhas better stability and is suitable for children and old people with dysphagia.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to 3-{(3R, 4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]- The composition of pyridin-1-yl)}-3-oxo-propionitrile-citrate, especially relates to the preparation method of tofacitinib citrate oral solution. Background technique [0002] Tofacitinib citrate, the chemical name is 3-{(3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)- Amino]-piperidin-1-yl)}-3-oxo-propionitrile monocitrate, the structural formula is as follows: [0003] [0004] Tofacitinib is a novel JAK (Janus kinase) pathway inhibitor. Unlike most other current RA (rheumatoid arthritis) drugs that mainly act on extracellular targets, tofacitinib targets intracellular signal transduction pathways and acts on the core part of cytokines. Tofacitinib, as a new class of DMARDs drug approved by the FDA for the first time in ten years, is a new type of JAK inhibitor. It relieves symptoms and s...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/519A61K47/12A61K47/04A61P19/02A61P29/00
Inventor 谢吉元冯金华李孝成
Owner 南京安美医药科技有限公司
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