Topical slimming preparation and a cosmetic containing a carnitine derivative

A technology of derivatives and preparations, applied in the field of slimming skin external preparations and cosmetics containing the preparations, can solve the problems of subcutaneous fat and sebum shortage, loss of skin vitality, rough skin and the like

Inactive Publication Date: 2007-05-09
SHOWA DENKO KK
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] On the other hand, even if fat metabolism is promoted and obesity is treated, excessive metabolism will cause a shortage of subcutaneous fat and sebum, resulting in loss of skin vitality, dry skin, and rough skin

Method used

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  • Topical slimming preparation and a cosmetic containing a carnitine derivative
  • Topical slimming preparation and a cosmetic containing a carnitine derivative
  • Topical slimming preparation and a cosmetic containing a carnitine derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0261] (Synthesis of Hexadecanoyl-L-Carnitine Hydrochloride)

[0262] In a 500ml-four-neck flask equipped with a dropping funnel, a thermometer and a cooling tube, L-carnitine (1mol) and trifluoroacetic acid (350ml) were charged, followed by stirring and heating at 60°C to obtain a solution. To the resulting homogeneous reaction liquid, hexadecanoyl chloride (1.1 mol) was added dropwise from the dropping funnel over 30 minutes. After the dropwise addition was completed, the reaction liquid was stirred at 60° C. for 2 hours. After that, trifluoroacetic acid was evaporated with an evaporator. The residue was dissolved in n-hexane (500ml), then water (500ml) was added, and stirred for 30 minutes. The liquid mixture was mixed with ethanol (500 ml) and methyl tert-butyl ether (500 ml) for extraction. The aqueous phase was collected and mixed with n-butanol (500ml) followed by water (100ml) for extraction. The n-butanol phase is separated and the solvent is evaporated off, yield...

Embodiment 2

[0264] (Synthesis of Hexanoyl-L-Carnitine Hydrochloride, Myristyl-L-Carnitine Hydrochloride and Octadecanoyl-L-Carnitine Hydrochloride)

[0265] In the same manner as in Synthesis Example 1, but using equimolar amounts of hexanoyl chloride, tetradecanoyl chloride and octadecanoyl chloride instead of hexadecanoyl chloride, hexanoyl-L-carnoyl chloride each having a purity of 99% was obtained. base hydrochloride, myristyl-L-carnitine hydrochloride and octadecanoyl-L-carnitine hydrochloride.

Embodiment 3

[0267] (Synthesis of Hydroxycitrate-2-palmitate)

[0268] (1) Synthesis of Tribenzyl Hydroxycitrate

[0269] 2.96 g (10.1 mmol) of calcium hydroxycitrate, 5.86 g (30.8 mmol) of benzenesulfonic monoanhydride, 10 g (92.5 mmol) of benzyl alcohol and 20 ml of toluene were charged in a 200 ml evaporating flask. Stirring was carried out at reflux for 4 hours to remove the azeotropic water. After natural cooling, the mixture was mixed with 50 ml of ethyl acetate, and stirred well. A small amount of the resulting mixture was introduced into a 50 ml beaker containing 100 ml of a 5% by mass aqueous sodium bicarbonate solution under stirring. Insolubles were removed, the aqueous phase was separated, and the organic phase was washed with water and dried over anhydrous sodium sulfate. The solvent and benzyl alcohol were removed by evaporation in vacuo, and the residue was analyzed by silica gel chromatography. Elution with a 5:1 mixture of hexane and ethyl acetate afforded 1.96 g of th...

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Abstract

The invention provides a slimming skin external preparation and a cosmetic that contain a carnitine derivative having excellent skin affinity and percutaneous absorption properties and capable of enhancing the fat metabolism, and that can treat, reduce or prevent the obesity by functioning as a lipolytic agent to enhance the fat metabolism of general or local subcutaneous fat tissues. The slimming skin external preparation contains a particular carnitine derivative such as a cylcarnitines and alcohol carnitine esters and preferably other slimming and skin-care ingredients.

Description

[0001] Refer to related application [0002] This application is an application filed under 35 U.S.C Part 111(a), pursuant to 35 U.S.C Part 119(e), claiming the benefit of a provisional application filed on June 14, 2004 under 35 U.S.C Part 111(b)60 / 578,851 filing date rights. field of invention [0003] The invention relates to an external preparation for slimming skin and cosmetics containing the preparation. More particularly, the present invention relates to external preparations and cosmetics containing carnitine derivatives and having an effect of promoting subcutaneous lipolysis. [0004] The present invention also relates to slimming skin external preparations and cosmetics containing carnitine derivatives and slimming and skin care ingredients. Background of the invention [0005] A large amount of fat in the body can lead to the accumulation of neutral fat in white fat cells, which is caused by the absorption of excess metabolic energy. Obesity means that exces...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/44A61Q19/00A61K8/365A61K8/49A61K8/67A61Q19/06A61Q90/00
CPCA61K8/365A61K8/676A61K8/678A61Q19/06A61K8/44A61K31/195A61K8/40A61Q90/00A61K8/36
Inventor 涩谷彰加藤咏子蒲池元昭青木裕史
Owner SHOWA DENKO KK
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