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Pharmaceutical composition containing (r)-n-[1-(3,5-difluoro-4-methansulfonylamino-phenyl)-ethyl]-3-(2-propyl-6-trifluoromethyl-pyridin-3-yl)-acrylamide

A composition and drug technology, applied in the direction of drug combination, drug delivery, active ingredients of heterocyclic compounds, etc., can solve problems such as unavailability

Pending Publication Date: 2020-04-10
AMOREPACIFIC CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, such methods cannot provide specific data to suppress crystallization to such an extent that the shelf-life of the drug product as a complete product for a pharmaceutical composition for external use can be ensured (J.DRUG DEL.SCI.TECH., 21(6)509- 516 2011, Int. J App Pharm)

Method used

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  • Pharmaceutical composition containing (r)-n-[1-(3,5-difluoro-4-methansulfonylamino-phenyl)-ethyl]-3-(2-propyl-6-trifluoromethyl-pyridin-3-yl)-acrylamide
  • Pharmaceutical composition containing (r)-n-[1-(3,5-difluoro-4-methansulfonylamino-phenyl)-ethyl]-3-(2-propyl-6-trifluoromethyl-pyridin-3-yl)-acrylamide
  • Pharmaceutical composition containing (r)-n-[1-(3,5-difluoro-4-methansulfonylamino-phenyl)-ethyl]-3-(2-propyl-6-trifluoromethyl-pyridin-3-yl)-acrylamide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0060] Item 1. A pharmaceutical composition comprising a compound (R)-N-[1-(3,5-difluoro-4-methanesulfonylamino-phenyl) represented by the following formula (1) -Ethyl]-3-(2-propyl-6-trifluoromethyl-pyridin-3-yl)-acrylamide and cellulose polymers:

[0061] Formula 1)

[0062]

[0063] Item 2. The pharmaceutical composition according to Item 1, wherein the cellulosic polymer inhibits crystal formation of the compound of formula (1).

[0064] Item 3. The pharmaceutical composition according to item 1 or 2, wherein when observed using an optical microscope at a magnification of 100 or greater, preferably at a magnification of 500 or greater, more preferably at a magnification of 1000 or greater, No crystals of the compound of formula (1) were observed in the pharmaceutical composition.

[0065] Clause 4. The pharmaceutical composition according to Clause 3, wherein said optical microscope is equipped with a polarizing filter.

[0066] Clause 5. The pharmaceutical compositio...

experiment example 1

[0082] Preliminary Experimental Example 1: Select a solvent suitable for the compound of formula (1)

[0083] In order to select a solvent capable of dissolving the compound of formula (1) which is poorly soluble in water and oil, solubility experiments of the compound of formula (1) were carried out in various solvents listed in Table 1 below. Since a small amount of solvent ensuring high solubility can dissolve the compound of formula (1) compared to a solvent ensuring low solubility, the solvent ensuring high solubility may contain a relatively high content of water, especially when formulated for topical use When the pharmaceutical composition is used, the feeling of use is further enhanced.

[0084] An excess of the compound of formula (1) was added to 1 mL of each solvent described in Table 1 below, and stirred at 25° C. with shaking at 200 rpm for 24 hours (shaking incubator, SI 600R, JEIO TECH, Korea). Thereafter, it was centrifuged at 10,000 rpm for 10 minutes, and...

preparation example 1

[0089] Preparation Example 1: Preparation of the composition of the reference example of the present invention

[0090] 1) Preparation of cellulose polymer

[0091] Prepare 8 kinds of cellulose polymers, namely methyl cellulose (MC, Metolose, Shinetsu), hydroxyethyl cellulose (HEC, Natrosol, Ashland), hydroxypropyl cellulose (HPC , Klucel, Ashland) LF and EF grades and 3, 4.5, 6 and 15 mPa types of hypromellose (Hypromellose, Shinetsu) 2910.

[0092] Table 2:

[0093] cellulosic polymer Vis(mPa s) Reference example 1 MC 12.0-18.0 Reference example 2 HEC 7.1-13.3 Reference example 3 HPC LF 6.0-10.0 Reference example 4 HPC EF 150-400 Reference example 5 Hypromellose 3 2.4-3.6 Reference example 6 Hypromellose 4.5 4.0-6.0 Reference example 7 Hypromellose 6 4.8-7.2 Reference example 8 Hypromellose 15 12.0-18.0

[0094] 2) Preparation of compositions 1 to 8 of the reference examples of the pharmace...

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Abstract

The present invention relates to a pharmaceutical composition which comprises (R)-N-[1-(3,5-difluoro-4-methansulfonylamino-phenyl)-ethyl]-3-(2-propyl-6-trifluoromethyl-pyridin-3-yl)-acrylamide as a first component and a cellulosic polymer as a second component, wherein the composition of the present invention has a formulation characteristic in which crystal formation is delayed for a long time.

Description

technical field [0001] This application claims the benefit of Korean Patent Application No. 10-2017-0102316 filed on Aug. 11, 2017, the entire contents of which are hereby incorporated by reference. [0002] The present invention relates to a compound containing (R)-N-[1-(3,5-difluoro-4-methanesulfonylamino-phenyl)-ethyl]-3-(2-propyl- Pharmaceutical compositions of 6-trifluoromethyl-pyridin-3-yl)-acrylamide. Background technique [0003] Compound (R)-N-[1-(3,5-difluoro-4-methanesulfonylamino-phenyl)-ethyl]-3-(2-propyl-6-trifluoromethyl-pyridine- 3-yl)-acrylamide by formula (1) express. This compound is disclosed in Example 23 of WO 2008 / 013414. [0004] Compounds of formula (1) have antagonistic activity on vanilloid receptors and are very useful compounds expected to be useful as effective therapeutic agents for pain, nervous system disorders and skin diseases (eg atopic dermatitis), inflammatory diseases and the like. In particular, in the case of muscular pain or sk...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/38A61K31/44
CPCA61K31/44A61K47/38A61K9/06A61P17/00A61K47/10A61K9/0014
Inventor 崔俊镐赵原庆申光炫禹柄英李玘和金砇秀卢钟和朴美英朴永镐朴恩实朴题弘
Owner AMOREPACIFIC CORP