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Menthol-containing preparation

Inactive Publication Date: 2006-06-08
CHUGAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0046] The formulation for inhibiting smooth muscle contraction, the emulsion of the invention remains stable over a long time, exhibits a high light transmittance, and causes little foam during filling in a container or in use, namely in administration. Therefore the formulation is useful as a contraction inhibitor to be used particularly in endoscopic examination of the digestive tract.

Problems solved by technology

This inhibitor formulation, however, required a relatively high content of the surfactant for transparency so that foaming occurred during filling the formulation into a container or during spraying through a tube to the affected area for endoscopic examination, and the foam made observation of the affected area difficult.

Method used

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  • Menthol-containing preparation

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0051] To 200 mL of water were added 4.0 g of polysorbate 80 (Tween 80, Rheodol TW-O120V, KAO Corporation) and 0.02 g of a polydimethylsiloxane-silicone dioxide mixture (KS-69, Shin-Etsu Chemical Co., Ltd.), followed by emulsification with a homomixer (liquid temperature: 60° C.) to give a polydimethylsiloxane-silicone dioxide mixture fluid. To 1600 mL of water were added 20.0 g of a sucrose fatty acid ester (Surfhope J1616, Mitsubishi-Kagaku Foods Corporation), 36.0 g of polyoxyethylene hydrogenated caster oil 60, (NIKKOL HCO-60, Nikko Chemicals Co., Ltd.), and 30.0 g of MCT (Coconad RK, Kao Corporation) were added and dispersed with a homomixer. To this liquid were added 16.0 g of L-menthol that was in compliance with the Japanese Pharmacopoeia standard (L-Menthol, The SUZUKI Menthol CO., LTD.) and the polydimethylsiloxane-silicone dioxide mixture fluid, followed by emulsification with a homomixer at a liquid temperature of 80° C. Water was added to this liquid to make the entire ...

example 2

[0052] To 200 mL of water were added 4.0 g of Tween 80 (Rheodol TW-O120V, KAO Corporation) and 0.06 g of a polydimethylsiloxane-silicone dioxide mixture (KS-69, Shin-Etsu Chemical Co., Ltd.), followed by emulsification with a homomixer (liquid temperature: 60° C.) to give a polydimethylsiloxane-silicone dioxide mixture fluid. To 1600 mL of water were added 20.0 g of a sucrose fatty acid ester (Surfhope J1616, Mitsubishi-Kagaku Foods Corporation), 36.0 g of HCO-60 (NIKKOL HCO-60, Nikko Chemicals Co., Ltd.), and 30.0 g of MCT (Coconad RK, Kao Corporation) and dispersed with a homomixer. To this liquid were added 16.0 g of L-menthol that was in compliance with the Japanese Pharmacopoeia standard (L-Menthol, The SUZUKI Menthol CO., LTD.) and the polydimethylsiloxane-silicone dioxide mixture fluid, followed by emulsification with a homomixer at a liquid temperature of 80° C. Water was added to this liquid to make the entire volume 2000 mL to give a desired emulsion. The average particle ...

example 3

[0053] To 200 mL of water were added 4.0 g of Tween 80 (Rheodol TW-O120V, KAO Corporation) and 0.10 g of a polydimethylsiloxane-silicone dioxide mixture (KS-69, Shin-Etsu Chemical Co., Ltd.), followed by emulsification with a homomixer (liquid temperature: 60° C.) to give a polydimethylsiloxane-silicone dioxide mixture fluid. To 1600 mL of water were added 20.0 g of a sucrose fatty acid ester (Surfhope J1616, Mitsubishi-Kagaku Foods Corporation), 36.0 g of HCO-60 (NIKKOL HCO-60, Nikko Chemicals Co., Ltd.), and 30.0 g of MCT (Coconad RK, Kao Corporation) and dispersed with a homomixer. To this liquid were added 16.0 g of L-menthol that was in compliance with the Japanese Pharmacopoeia standard (L-Menthol, The SUZUKI Menthol CO., LTD.) and the polydimethylsiloxane-silicone dioxide mixture fluid, followed by emulsification with a homomixer at a liquid temperature of 80° C. Water was added to this liquid to make the entire volume 2000 mL to give a desired emulsion. The average particle ...

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Abstract

It is known that L-menthol controls smooth muscle contraction. In order to use L-menthol in practice as a digestive tract contraction inhibiting agent in digestive tract endoscopy, it is required to devise means of giving a formulation in which an L-menthol-containing formulation remains stable and transparent or little cloudy over a long time after the production and which shows little foaming at the administration. In the present invention, an antifoaming agent is further added to a formulation for inhibiting smooth muscle contraction or a peristaltic contraction in a digestive tract containing a L-menthol emulsion having an average particle size of less than 100 nm. Thus, it is possible to obtain a formulation that remains stable over a long time, has a high light transmittance, and produces little foam when filled into a container and sprayed at a target area to inhibit contraction to facilitate observation of the area in endoscopic examination of the digestive tract etc.

Description

TECHNICAL FIELD [0001] The present invention relates to an L-menthol-containing formulation for inhibiting smooth muscle contraction or peristalsis, particularly a formulation for inhibiting digestive tract contraction, which remains stable over a long time, exhibits high light transmittance, and produces little foam when sprayed at a target area to inhibit contraction to facilitate observation of the area in endoscopic examination of the digestive tract etc. BACKGROUND ART [0002] Excessive contraction of the digestive tract during endoscopic examination of the digestive tract such as stomach and large intestine prevents correct diagnosis and allows a minute lesion such as a small-sized carcinoma to be missed. [0003] As a contraction inhibitor for endoscopic examination of the digestive tract, an anti-cholinergic agent scopolamine butylbromide (Trade name: Buscopan Injection, Nippon Boehringer Ingelheim Co., Ltd.) or glucagon has conventionally been prescribed. However scopolamine b...

Claims

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Application Information

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IPC IPC(8): A61K31/045A61K9/00A61B1/273A61B1/31A61K9/107A61K49/00
CPCA61B1/2736A61B1/31A61K9/1075A61K31/045A61K47/14A61K47/24A61K47/26A61K47/44A61K49/00A61P1/00A61P43/00A61K9/107
Inventor HAMAWAKI, TOMONORIKATAOKA, YOSUKEISODA, TAKAKO
Owner CHUGAI PHARMA CO LTD
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