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External preparation containing pantethine phosphate ester

A technology of pantethine phosphate and external preparations, applied to medical preparations containing active ingredients, skin care preparations, organic active ingredients, etc., can solve problems such as odor, strong, and inability to add external preparations, and achieve Improves the effect of whitening activity

Inactive Publication Date: 2012-07-18
DAIICHI FINE CHEM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the other hand, pantetheine, which exhibits whitening activity, has poor stability and strong odor due to its SH group, so it cannot be added to external preparations (Patent Document 11)

Method used

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  • External preparation containing pantethine phosphate ester
  • External preparation containing pantethine phosphate ester
  • External preparation containing pantethine phosphate ester

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Example 1 (pantethine-4', 4"-barium diphosphate, pantethine and pantetheine -S-calcium sulfonate pH stability comparison)

[0083] Each buffer (pH3-9.5) containing 0.1% (w / v) pantethine-4', 4"-barium diphosphate was prepared at 50 mM. Sodium citrate buffer was used as pH3, 4, 5 and 6. Buffer. Sodium phosphate buffer was used as the buffer of pH 6.5 and 7. Tris-HCl buffer was used as the buffer of pH 8 and 9.5. 0.4 mL of pantethine- Each solution of 4', 4"-barium diphosphate was sealed in a 1 mL glass ampoule and heated at 40°C for 6 months. The samples before and after heating were analyzed by HPLC to determine the content of pantethine-4', 4"-diphosphate. The same operation was also carried out for the same concentration of pantethine and pantetheine-S-calcium sulfonate , compare the result ( figure 1 ).

[0084] As a result, there was no difference in the stability of pantethine-4',4"-diphosphate, pantethine, and pantethein-S-calcium sulfonate at pH 5 to 6. Th...

Embodiment 2

[0085] Example 2 (pantethine-4', 4"-diphosphate, pantethine-4'-phosphate and pantethine pH Stability Comparison of Amines)

[0086] Prepare 50 mM of each buffer (pH3-9.5) containing 0.1% (w / v) pantethine-4', 4"-sodium diphosphate. Sodium citrate buffer was used as the buffer of pH3, 4, 5 and 6 solution. Use sodium phosphate buffer as the buffer solution with pH 7. Use Tris-HCl buffer solution as the buffer solution with pH 8 and 9.5. Seal 0.4 mL of each solution into a 1 mL glass ampoule and heat at 40°C for 3 months .The samples before and after heating were analyzed by HPLC to determine the content of pantethine-4',4"-diphosphoric acid. The same operation is also carried out for pantethine and pantethine-4'-phosphoric acid of the same concentration, and the results are compared ( figure 2 ).

[0087] As a result, there was no difference in the stability of pantethine, pantethine-4'-phosphate, and pantethine-4',4"-diphosphate at pH 5 to 6. However, at pH In the pH reg...

Embodiment 3

[0088] Example 3 (pantethine-4', 4 "-two-α-glucoside, pantethine-4'-α-glucose glycosides and pantethine stability comparison)

[0089] Prepare 50mM sodium citrate buffer solution (pH3~9.5) containing 0.1% (w / v) pantethine-4', 4"-di-α-glucoside. Use sodium citrate buffer solution as pH3, 4, 5 and 6 buffers. Use sodium phosphate buffer as the buffer at pH 7. Use Tris-HCl buffer as the buffer at pH 8 and 9.5. Seal 0.4 mL of each solution into a 1 mL glass ampoule and store at 40°C Heated for 6 months. The samples before and after heating were analyzed by HPLC to measure the content of pantethine-4', 4 "-di-α-glucoside. The same operation is also carried out for pantethine-4'-α-glucoside and pantethine of the same concentration, and the results are compared ( image 3 ).

[0090] There was no difference in the stability of pantethine-4',4"-di-α-glucoside, pantethine-4'-α-glucoside, and pantethine at pH 5 to 6 However, in the pH region where the pH is below 4 or the pH is ab...

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Abstract

A pantethine phosphate ester represented by formula (1) or formula (2) has an excellent inhibitory effect on tyrosinase activity and an excellent inhibitory effect on melanin production.

Description

technical field [0001] The present invention relates to an external preparation containing pantethine phosphate. Background technique [0002] Pantethine (pantethine) is used in (1) the prevention and treatment of pantothenic acid deficiency, (2) wasting disease, hyperthyroidism, pregnant women, lactating women, etc. have increased demand for pantothenic acid and insufficient dietary intake (3) prevention and treatment of hyperlipidemia, flaccid constipation, side effects caused by streptomycin and kanamycin; improvement of acute eczema, chronic eczema, blood platelet count and bleeding tendency , it is presumed to be a useful drug used in cases related to pantothenic acid deficiency or metabolic disorders (Non-Patent Document 1). It is also known to have a preventive effect on diarrhea (Patent Document 1) and an effect on proliferation of intestinal bifidobacteria (Patent Document 2). [0003] In addition, when pantethine is used as an external preparation, the following ...

Claims

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Application Information

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IPC IPC(8): A61K8/67A61K31/661A61P17/00A61Q5/02A61Q19/02
CPCA61Q5/02A61K8/55A61Q1/02A61Q19/02A61K31/661A61P17/00A61P19/02A61P43/00A61K8/67
Inventor 和田浩一鹫见浩一下村志帆子
Owner DAIICHI FINE CHEM CO LTD
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