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Pharmaceutical composition containing pharmaceutically acceptable salt of tofacitinib, preparation and application

A technology of tinib pharmacy and tofacitinib, applied in the field of pharmaceutical compositions of salts, can solve problems such as poor stability of free state tofacitinib, and achieve the effects of good drug efficacy, optimal drug exposure, and simplified processing difficulty

Pending Publication Date: 2022-01-28
HANGZHOU HERTZ PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patent document CN103459394B proposes to make ointment with free tofacitinib. In Example 15, the stability of free tofacitinib is poor, and the purity is only 97.3% when stored at 40°C for 4 weeks

Method used

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  • Pharmaceutical composition containing pharmaceutically acceptable salt of tofacitinib, preparation and application
  • Pharmaceutical composition containing pharmaceutically acceptable salt of tofacitinib, preparation and application
  • Pharmaceutical composition containing pharmaceutically acceptable salt of tofacitinib, preparation and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0097] Example 1: Synthesis of Torker

[0098] Synthesis of tartaric tartaribini (1)

[0099] A 25 ml flask was added 500 mg (1.6 mmol) free trustteibi and 288 mg (1.9 mmol) tarttic acid, 7.5 ml of acetone, stirred and heated to 40 ° C for 2 h, cooled to room temperature, filtered and collected, and normal temperature was dried. The product was 717 mg, yield 96.9%.

[0100] Lagory synthesis of tartaric acid Trust Dibini (2)

[0101] Weighing free trust replacement 45.0g in a single-mouth reaction bottle, 25 ° C ± 5 ° C, add 21.6 g of L-tartaric acid and 225 ml of methanol, heating to reflux, after the solid is dissolved, heat filtration, recover the mother liquor, concentrate to the dry Then, then 450 ml of n-hexane was stirred at 25 ° C ± 5 ° C, stirring, and filtered to obtain a solid, 70 ± 5 ° C for 48 h in a blower oven to obtain a tartaric acid trunk, yield of 95.0%.

[0102] Synthesis of sulfuric acid tunibi

[0103] A 25 ml flask was added 500 mg (1.6 mmol) free state trunk...

Embodiment 2

[0106] Example 2: Preparation of different external formulations

[0107] Table 1-1 Tarten Tourist Digent Cream Formula

[0108]

[0109]

[0110] Note: In Table 1-1, the percentage of each component in the aqueous phase and the oil phase and the outer phase is calculated based on the total amount of the oil phase and the aqueous phase.

[0111] Table 1-2 Tourness Tourist Dibini's cream formula

[0112]

[0113] Note: The percentage of each component in the aqueous phase and the oil phase and the outer phase in the B6 to B11 is calculated based on the total amount of the oil phase and the aqueous phase.

[0114] Table 1-3 Tourness Trust Trust Dibini's cream formula

[0115]

[0116] Note: The percentage of each component in Table 1-3 is calculated based on the total amount of the oil phase, the aqueous phase, and the outer phase.

[0117] Table 1-4 Tarten Tourist Dieni's cream formula

[0118]

[0119] Note: The percentage of each component in Table 1-4 is calculated bas...

Embodiment 3

[0140] Example 3: Dissolution of Different Salt Types Dissolved Properties Test

[0141] In order to improve the transdermal ability of the partial preparation and the stability of the drug, the solubility of the drug is very critical in the excipient, so the solubility of the raw material is an important indicator of the drug. Therefore, in the development of prescriptions, a balanced solubility study is carried out: taking excess raw materials (citrate Trust Dibini, tartaric acid Trust Dibin, sulfate Thaifini, phosphate Tutibi) placed in 2 ml PE In the addition, different solvents were added, dissolved at room temperature, and the solubility was calculated using high performance liquid chromatography after 24 h.

[0142] Table 4: Solubility of different salt types in different solvents

[0143]

[0144]

[0145] In the table: ">" means "greater than", "<" means "less than".

[0146] This trial, we accidentally found that in a monoethyl ether of the permeable dietary dihydrat...

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Abstract

The invention discloses a pharmaceutical composition. The pharmaceutical composition comprises tofacitinib, a pharmaceutically acceptable salt of tofacitinib and a penetration enhancer. The invention further discloses a pharmaceutical preparation prepared from the composition and application thereof. According to the invention, the selected pharmaceutically acceptable salt of tofacitinib has better solubility, the preparation processing difficulty is simplified, and the permeability of the preparation in the skin is increased; compared with free tofacitinib, the tofacitinib is more stable, and the safety and good efficacy of the medicine are ensured. According to the invention, diethylene glycol monoethyl ether is selected as a solvent and an absorption enhancer, so that no irritation is caused; the preparation disclosed by the invention has an anti-inflammatory effect in a dinitrofluorobenzene-induced delayed hypersensitivity reaction model, can also reduce the area of white spots of leucoderma patients and treat atopic dermatitis, and can be used for treating and preventing autoimmune diseases such as leucoderma, alopecia areata, scleroderma, psoriasis, atopic dermatitis and the like.

Description

Technical field [0001] The present invention belongs to the technical findings of the pharmaceutical composition R & D technology, and in particular, to a pharmaceutical composition, formulation and application of atrikilic acid-based salt. Background technique [0002] TofacitiniB, chemically called 3 - {(3R, 4R) -4-methyl-3- [methyl (7H-pyrrole [2,3-D] pyrimidine-4-yl) amino] Piperidine-1-yl} -3-oxpropionitrile: [0003] Totibib is a Jak inhibitor, which can be used for organ transplantation, xenograft, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, psoriasis, 1 diabetes, and other types of diabetes, cancer, Asthma, specialty dermatitis (Atopic Dermatitis, also known as specific dermatitis), autoimmune thyroid disease, ulcerative colitis, Crohn disease, Alzheimer's disease, leukemia, and other indications in immunosuppression Therapy immunosuppressive agent. [0004] Citizen Tourist is currently approved in the United States. Sales in the form of tablets, containi...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61K9/00A61K47/10A61P37/02A61P29/00A61P17/00A61P17/14A61P17/06
CPCA61K31/519A61K9/0014A61K47/10A61P37/02A61P29/00A61P17/00A61P17/14A61P17/06A61K9/00A61K47/06A61K45/06A61K31/69
Inventor 周星露钟诗春朱建荣胡苗罗文华
Owner HANGZHOU HERTZ PHARMA
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