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Sustained-release medical composition

A composition and polymer technology, applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problem of not being able to maintain the effective concentration of active ingredients for a long time, and achieve the effect of improving the sustained release ability

Inactive Publication Date: 2020-06-19
ISHIHARA SANGYO KAISHA LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above-mentioned preparations cannot maintain the effective concentration of the above-mentioned active ingredient in the living body for a long time, and in order to obtain the desired effect, it may be necessary to administer it several times.

Method used

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  • Sustained-release medical composition
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  • Sustained-release medical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0097] Hereinafter, although a test example and a reference example demonstrate this invention more concretely, the technical scope of this invention is not limited to these examples. It should be noted that, unless otherwise specified, all percentages or ratios used in the present invention are by mass. In addition, unless otherwise specified, the units and measurement methods described in this specification are based on JIS standards.

[0098] The substances used in Test Examples and Reference Examples are as follows.

[0099] Compound 1: N-(2-Ethylsulfonylamino-5-trifluoromethyl-3-pyridyl)cyclohexylcarboxamide · monosodium salt · monohydrate

[0100] Eudragit (registered trademark) RSPO: manufactured by Evonik (hereinafter referred to as Eudragit RS)

[0101] Eudragit (registered trademark) RLPO: Made by Evonik (called Eudragit RL)

[0102] Span 80: Made by Croda international PLC

[0103] NIKKOL Hexaglyn PR-15: Made by Japan SURFACTANT Industry Co., Ltd.

[0104] COCO...

reference example 1

[0136] Reference Example 1: Study on a composition (microparticle a) containing compound 1

reference example 1－1

[0137] Reference Example 1-1: Preparation of a composition (microparticle a) containing Compound 1

[0138] Compound 1 (8 mg) was mixed with purified water (0.8 mL) by a vortex mixer to obtain liquid a. PLGA (40 mg), Span 80 (40 mg) and acetone (1.2 mL) were mixed by vortex mixer to obtain liquid b. Mix liquid a and liquid b by a vortex mixer to obtain liquid c. NIKKOL Hexaglyn PR-15 (240 mg), COCONARD MT (12 mL) and hexane (8 mL) were mixed by vortex mixer to obtain liquid d. Polyvinyl alcohol (100 mg) and purified water (10 mL) were stirred by a magnetic stirrer to obtain liquid e. Liquid c was dropped into liquid d, and stirred at 15,000 rpm for 5 minutes using a homogenizer to obtain a suspension. The resulting suspension was centrifuged at 4° C. and 20,000 rpm for 10 minutes with a cooling centrifuge, and the supernatant was discarded to obtain a precipitate. Hexane (10 mL) was added to the obtained precipitate, stirred with a vortex mixer for 5 minutes to prepare a...

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Abstract

The present invention provides a composition for improving the sustained-release ability of N-(2-ethylsulfonylamino-5-trifluoromethyl-3-pyridyl)cyclohexanecarboxamide or a salt thereof. More specifically, the present invention provides a topical administration composition that contains a polycation polymer and N-(2-ethylsulfonylamino-5-trifluoromethyl-3-pyridyl)cyclohexanecarboxamide or a salt thereof.

Description

[0001] This patent application claims priority based on Japanese Patent Application No. 2017-213144 filed on November 2, 2017, and the entire disclosure content of the above-mentioned prior patent application is incorporated as a part of this specification by reference. technical field [0002] The present invention relates to a composition for topical administration comprising N-(2-ethylsulfonylamino-5-trifluoromethyl-3-pyridyl)cyclohexylcarboxamide or a salt thereof, and more particularly to a composition comprising N - A composition for topical administration of (2-ethylsulfonylamino-5-trifluoromethyl-3-pyridyl)cyclohexanecarboxamide or a salt thereof and a polycation polymer. Background technique [0003] N-(2-Ethylsulfonylamino-5-trifluoromethyl-3-pyridyl)cyclohexylcarboxamide or its salts are known to have phospholipase A2 inhibitory effect, as an active ingredient of anti-inflammatory drugs or anti-pancreatitis drugs is useful (Patent Document 1). [0004] Also known...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/44A61K9/06A61K9/10A61K9/14A61K47/32A61K47/34A61K47/36A61K47/42
CPCA61K9/06A61K31/44A61K47/34A61P17/00A61P29/00A61K9/0017A61K9/1641A61K9/1635A61K47/10A61K9/146A61K9/10A61K47/32A61K47/36A61K47/44A61K9/0019A61K9/0014A61K9/19A61K47/42
Inventor 尾上诚良佐藤秀行
Owner ISHIHARA SANGYO KAISHA LTD