Baricitinib cream and preparation method and application thereof

A technology of baricitinib and Ni cream, which is applied in the direction of ointment delivery, pharmaceutical formula, emulsion delivery, etc. It can solve the problems such as difficult to obtain cream with particle size distribution, and achieve the goal of being suitable for industrial production and having good coating performance , the effect of not easy to separate oil and water

Pending Publication Date: 2021-01-05
南京康川济医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The following problems generally exist in the preparation process of cream: when mixing the two phases of oil and water, high-speed stirring is required to obtain a fine and stable emulsion, and the ob

Method used

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  • Baricitinib cream and preparation method and application thereof
  • Baricitinib cream and preparation method and application thereof
  • Baricitinib cream and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Recipe for Cream 1

[0061] The composition of the preparation prescription is the content of components in every 100 grams of cream:

[0062] Baricitinib 250 mg;

[0063] Polyethylene glycol-7 stearate (tefose 63) 22 grams;

[0064] Purified water was added to make up to 100 g.

[0065] making process:

[0066] (a) Polyethylene glycol-7 stearate is melted at 60°C;

[0067] (b) heating the purified water to 60°C;

[0068] (c) under continuous stirring at 800 rpm, transfer the hot purified water into the polyethylene glycol-7 stearate liquid, and stir for 30 minutes;

[0069] (d) Turn the mixture to 30°C, stir continuously at 800 rpm for 15 minutes, add baricitinib and stir evenly;

[0070] (e) filling to obtain baricitinib emulsifiable cream.

[0071] The morphology of the obtained cream was observed under an optical microscope, and the cream was placed at 40 degrees Celsius and 60 degrees Celsius for 10 days, and cooled to room temperature after taking it out to...

Embodiment 2

[0073] Recipe for Cream 2

[0074] The composition of the preparation prescription is the content of components in every 100 grams of cream:

[0075] Baricitinib 250 mg;

[0076] Polyethylene glycol-7 stearate (tefose 63) 18 grams;

[0077] 5.5 grams of liquid paraffin;

[0078] Phenoxyethanol 0.45 g;

[0079] Appropriate amount of sodium hydroxide;

[0080] Purified water was added to make up to 100 g.

[0081] making process:

[0082] (a) Polyethylene glycol-7 stearate and liquid paraffin are melted at 60°C;

[0083] (b) heating purified water to 60°C, adding ethyl p-hydroxybenzoate to dissolve;

[0084] (c) under continuous stirring at 1200 rpm, transfer (b) into (a) and stir for 20 minutes;

[0085] (d) Turn the mixture to 35°C, stir continuously at 1200 rpm for 15 minutes, add baricitinib and stir evenly, then add sodium hydroxide solution to adjust the pH value to 6.0-7.0;

[0086] (e) filling to obtain baricitinib emulsifiable cream.

[0087] The morphology of...

Embodiment 3

[0089] Recipe for Cream 3

[0090] The composition of the preparation prescription is the content of components in every 100 grams of cream:

[0091] Baricitinib 250 mg;

[0092] Polyethylene glycol-7 stearate (Tefose 63) 14.5 grams;

[0093] 6 grams of liquid paraffin;

[0094] Carbopol (Carbopol 980) 0.02 grams;

[0095] Phenoxyethanol 0.45 g;

[0096] 0.005 grams of disodium edetate;

[0097] Appropriate amount of sodium hydroxide;

[0098] Purified water was added to make up to 100 g.

[0099] making process:

[0100] (a) Polyethylene glycol-7 stearate and liquid paraffin are melted at 60°C;

[0101] (b) Swell the carbomer with water for 6 hours, heat to 60°C, add phenoxyethanol and disodium edetate to dissolve;

[0102] (c) under continuous stirring at 1200 rpm, transfer (b) into (a) and stir for 20 minutes;

[0103] (d) Turn the mixture to 35°C, stir continuously at 1200 rpm for 15 minutes, add baricitinib and stir evenly, add sodium hydroxide solution to adjus...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a Baricitinib cream and a preparation method and application thereof. The Baricitinib cream comprises Baricitinib or pharmaceutically acceptable salt thereof and polyethylene glycol-7 stearate. In the preparation process of the Baricitinib cream, the Baricitinib cream which is fine and smooth, has the particle size meeting the quality requirement of Chinese pharmacopoeia for the cream and is good in coating performance can be prepared through low-speed stirring; and the cream has better high-temperature-resistant stability, and oil-water separation is not prone to occurring. Therefore, the Baricitinib cream is more suitable for industrial production and better in stability.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a baricitinib cream and its preparation method and application. Background technique [0002] The chemical name of baricitinib is 1-(ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-D]pyrimidin-4-yl)-1H-pyrazol-1-yl] -3-Azaheterocycle, a signal transduction pathway kinase inhibitor, selectively inhibits JAK2 and JAK1, thereby targeting multiple RA-related cytokine pathways, thereby reducing the activation and activation of key immune cells in inflammatory cells proliferation. The current dosage form of baricitinib is only oral tablets, and the specifications of the tablets are 1mg and 2mg. [0003] However, for psoriasis, atopic dermatitis, systemic lupus erythematosus, rheumatoid arthritis (RA) and other diseases, topical creams have significant advantages, such as fast onset of action, good analgesic effect, and convenient medication. The following problems generall...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K47/14A61K31/519A61P29/00A61P37/02A61P19/02A61P19/08A61P17/06A61P17/00A61P1/04A61P1/00A61P17/14
CPCA61K9/06A61K9/0014A61K47/14A61K31/519A61P29/00A61P37/02A61P19/02A61P19/08A61P17/06A61P17/00A61P1/04A61P1/00A61P17/14
Inventor 尹来生陈金脱朱春莉李国源冯婧劼
Owner 南京康川济医药科技有限公司
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