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Phytospingosine derivative and composition containing same

A technology of phytosphingosine and derivatives, which is applied in the direction of drug combination, sugar derivatives, sugar derivatives, etc., can solve the problems of prone to sedimentation, achieve the effect of improving stability and improving antibacterial effect

Active Publication Date: 2018-01-09
AMOREPACIFIC CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Republic of Korea Registered Patent Publication No. 0690103 proposes a method for preparing an aqueous solution using liposomes (Liposome) with a size below 100nm containing high-concentration phytosphingosine, but there are still deposits that easily occur during long-term storage or due to Problems in use caused by high viscosity of the formula

Method used

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  • Phytospingosine derivative and composition containing same
  • Phytospingosine derivative and composition containing same
  • Phytospingosine derivative and composition containing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1: the synthesis of phytosphingosine derivative

[0048] Put 3.17 g of phytosphingosine, 3.78 g of maltose monohydrate and 30 μL of acetic acid into 40 mL of methanol for circulation, and the reaction time is 12 hours. After the reaction, the solution was cooled at room temperature, and the product was precipitated after adding acetone. The precipitated phytosphingosine derivative was filtered and then dried.

[0049] 1 H NMR (300MHz,D 2 O)δ:0.89(3H),1.10-1.50(26H),2.90-3.20(4H),3.25-4.20(14H),4.66&5.20-5.45(1H)

Embodiment 2

[0050] Embodiment 2: the synthesis of phytosphingosine derivative

[0051] Except that lactose monohydrate (Lactose monohydrate) was used instead of maltose monohydrate, others were prepared by the same method as in Example 1 to prepare phytosphingosine.

[0052] 1 H NMR (300MHz,D 2 O)δ:0.89(3H),1.10-1.50(26H),2.90-3.20(4H),3.25-4.20(14H),4.66&5.20-5.45(1H)

experiment example 1

[0053] Experimental Example 1: Solubility Test of Phytosphingosine Derivatives

[0054] Dissolve the phytosphingosine derivatives obtained in Example 1 and Example 2 in distilled water at 50-60°C so that the weight of the overall aqueous solution is 0.1% by weight and 1.0% by weight for comparison, and then put it at room temperature, observe the following The precipitation results at different times. As a comparative example, using the same phytosphingosine to carry out the same experiment, the results are as follows figure 1 shown.

[0055] Table 1

[0056]

[0057] ○: Not yet precipitated

[0058] △: Although precipitation is not visible to the naked eye, fine particles are generated.

[0059] x: Precipitation was seen with the naked eye.

[0060] As shown in Table 1 above, compared with the phytosphingosine of the comparative example, the solubility in water of the phytosphingosine derivative of the present invention is increased, and it will not be precipitated ...

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Abstract

The present invention relates to a phytospingosine derivative generated by a condensation reaction of phytospingosine and maltose or lactose, which is an aldose-based disaccharide, and to a composition containing the same. The phytospingosine derivative of the present invention has high solubility in water compared with phytospingosine, is easy to formulate since the stabilization problem in a solution is solved, and maintains or further enhances the antibacterial effect of phytospingosine.

Description

technical field [0001] This application claims the benefit of priority based on Korean Patent Application No. 10-2015-0044835 filed on March 31, 2015, and all the contents disclosed in the Korean Patent Application Document are included in this specification as a part of this specification. [0002] The invention relates to a phytosphingosine derivative and a composition containing it, in particular to a phytosphingosine and an aldose disaccharide maltose (Maltose) or lactose (Lactose) to undergo a condensation reaction to produce a plant Sphingosine derivatives and compositions containing this active ingredient. Background technique [0003] Sphingoid, which is a component of living cell membranes, is based on a long chain called sphingoid long chain (Sphingoid Long Chain Base) of sphingosine, phytosphingosine, and dihydrosphinganine. framed. It is found that the phytosphingosine in the skin is generated after the decomposition of ceramide (Ceramaid) by ceramidase (Cerami...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/12C07H1/00A61K31/7032A61K8/68A61Q19/00A61Q17/00A61P31/04A61P31/10A61P17/00A61P17/06A61P17/04
CPCC07H15/12A61P17/10A61P31/04A61K31/133C07H15/04A61K8/60A61K8/68A61Q19/00C07C215/10
Inventor 俞载元朴泰训金容震李存桓
Owner AMOREPACIFIC CORP
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