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Skin irritation suppressant and transdermal preparation

A skin irritation and inhibitor technology, applied in the field of skin irritation inhibitors, can solve the problem that cholesterol does not have anti-inflammatory activity, and achieve the effect of reducing skin irritation

Inactive Publication Date: 2013-01-02
HISAMITSU PHARM CO INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] It is known that steroids having a steroidal skeleton generally have an anti-inflammatory effect, but as described in Patent Document 3, for example, cholesterol does not have anti-inflammatory activity

Method used

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  • Skin irritation suppressant and transdermal preparation
  • Skin irritation suppressant and transdermal preparation
  • Skin irritation suppressant and transdermal preparation

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1）

[0072] To study the changes in the amount of skin stimulating media produced by the test substance when the skin stimulating substance is applied to a human three-dimensional cultured epidermis model.

[0073] A human three-dimensional cultured epidermal model (LabCyteEPI-MODEL, manufactured by Japan Tissue Engineering Co., Ltd.) was used in which human normal epidermal cells were cultured in layers. LabCyte is cultured skin cultured in Transwell culture plates. When performing experiments, use both LabCyte and Transwell plates.

[0074] The test substance is a candidate for a skin irritation inhibitor, and cholesterol (manufactured by Wako Pure Chemical Industries, Ltd.), β-sitosterol (manufactured by Tama Biochemical Co., Ltd.), α-spinasterol (manufactured by ChromaDex), and ergosterol (manufactured by ChromaDex Corporation) were used. Wako Pure Chemical Industries, Ltd.), campesterol (Tama Biochemical Co., Ltd.), glycyrrhizic acid (Wako Pure Chemical Industries, Ltd.), gly...

experiment example 2）

[0089]

[0090] Cholesterol was used as the test substance. Drugs shown in Table 2 were used as skin irritating substances.

[0091] Experiments were performed using the following composition configurations.

[0092] • Drug addition group alone: ​​a group in which only the drug was dispersed in the medium as a test solution. Drug concentrations are shown in Table 2.

[0093] · Drug+cholesterol addition group: a group in which a drug and 1% by mass of cholesterol were dispersed in a medium as a test solution. Drug concentrations are shown in Table 2.

[0094] The other conditions were the same as in Experimental Example 1, and the experiment was performed. The results are shown in Table 2. According to Table 2, cholesterol has the effect of inhibiting the production of skin-irritating mediators in a wide range of drugs.

[0095] Table 2

[0096]

experiment example 3）

[0098]

[0099]Using croton oil (Wako Pure Chemical Industries, Ltd.) as an edema-inducing substance, the suppression of ear edema in mice was studied. Experiments were performed using 7-week-old ddY female (SPF) mice. Cholesterol, glycyrrhizic acid, glycyrrhetinic acid, squalene, ergosterol, squalane, and lanosterol were used as test substances. Acetone (Wako Pure Chemical Industries, Ltd.) was used as the medium.

[0100] Experiments were performed using the following composition configurations.

[0101] · Positive control group: a group in which only the vehicle was administered as a test solution once, and a 2% croton oil solution was administered as a test solution twice after 1 hour.

[0102] · Test substance group: a group in which only the vehicle was administered as a test solution once, and a 2% croton oil solution containing 1% by mass of the test substance was administered as a test solution twice as a test solution one hour later.

[0103] The auricle edema i...

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Abstract

Provided is a skin irritation suppressant for transdermal preparations, said skin irritation suppressant having an acknowledged effect of adequately reducing skin irritation caused by drugs. Also provided is a transdermal preparation containing said skin irritation suppressant. One embodiment of the invention is a skin irritation suppressant for reducing skin irritation caused by pharmaceutical adjuvants used in drugs and transdermal preparations other than drugs, said skin irritation suppressant comprising sterol compounds selected from a group comprising cholesterol, cholesterol derivatives and cholesterol analogs. Said drug is one or more basic drugs selected from a group comprising tolterodine, asenapine, bisoprolol, risperidone, nicotine, and mitalopram, and pharmacologically acceptable salts thereof.

Description

technical field [0001] The present invention relates to a skin irritation inhibitor and a transdermal preparation containing the skin irritation inhibitor. Background technique [0002] Compared with injections and oral preparations, percutaneous absorption preparations administered from the skin have the advantages of avoiding a sharp rise in the blood concentration of the drug, making it easier to continue the drug absorption, avoiding the first-pass effect of the liver, and stopping the administration when side effects appear. medicine etc. On the other hand, when a drug is administered by using a percutaneous absorption preparation, skin irritation such as itching, flushing, rash, pain, eczema, and dermatitis may occur on the applied skin. [0003] Patent Document 1 discloses that the skin irritation of serotonin reuptake inhibitors can be selectively reduced by adding hydroquinone glycoside, pantethine, tranexamic acid, or lecithin. In addition, Patent Document 2 desc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/10A61K9/70A61K31/137A61K31/138A61K31/343A61K31/407A61K31/465A61K31/517
CPCA61K31/138A61K9/7061A61K9/703A61K31/407A61K31/343A61K9/7053A61K31/137A61K31/517A61K31/465A61K47/28A61P17/00A61P25/28
Inventor 隈秀和新健治铃木一弘间和之助
Owner HISAMITSU PHARM CO INC
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