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Synthetic capsaicin analogues as bioenhancers

A technology of bioenhancement and action, applied in animal feed, drug delivery, food science, etc., can solve the problems of inefficiency and low yield

Pending Publication Date: 2020-07-31
アクシシェムアクティエボラーグ
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This can be an inefficient process resulting in low yields and / or the presence of undesired species

Method used

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  • Synthetic capsaicin analogues as bioenhancers
  • Synthetic capsaicin analogues as bioenhancers
  • Synthetic capsaicin analogues as bioenhancers

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0086] Example 1. Dosage determination of phenylcapsaicin in drug delivery

[0087] A compound of formula 1, such as phenylcapsaicin, is mixed with a pharmaceutically active ingredient. There may be several mixtures in which the concentration of the compound and / or pharmaceutically active ingredient is varied. The objective is to assess at what concentration a formulation comprising the compound and the ingredient has similar or improved bioavailability compared to a standard dose of the ingredient. Standard doses may have low bioavailability. The experiment may be performed in a suitable in vitro assay and / or a suitable in vivo experiment. It assesses whether the bioavailability of the dose of the component combined with the compound is similar, decreased or increased compared to the standard dose. It can also be assessed whether the bioavailability of a reduced amount of the dose of the component combined with the compound is similar to the bioavailability of the standard...

Embodiment 2

[0088] Example 2. Determination of the dosage of phenyl capsaicin in fish feed

[0089]A compound of formula 1, such as phenylcapsaicin, is mixed into salmon feed. Astaxanthin (the coloring agent that turns salmon flesh pink) is also mixed into the feed. Wild salmon consume astaxanthin through their diet and develop their pink flesh, while farmed salmon must have astaxanthin in their feed to develop their characteristic pink flesh. It is also possible to mix phenylcapsaicin and astaxanthin together before incorporating them into the feed. It is also possible to add phenylcapsaicin to the feed after adding astaxanthin (F+P+A). Three additional salmon diets were prepared: a diet containing phenylcapsaicin but no astaxanthin (F+P-A); a regular diet with astaxanthin (F-P+A); and a diet without phenylcapsaicin and astaxanthin (F-P-A) feed. The salmon were divided into 4 feed groups, where each group was fed with one of the four feeds for the period of time required to obtain pi...

Embodiment 3

[0091] Example 3. Dosage determination of ethyl capsaicin in supplements

[0092] Compounds of formula 1, such as ethyl capsaicin, are mixed into supplements, such as vitamin supplements. Group vitamin deficient individuals. Each group received a supplement containing ethyl capsaicin and vitamins (S+E+Vit); a supplement containing ethyl capsaicin but no vitamins (S+E-Vit); Supplement (S-E-Vit); or regular supplement with vitamins (S-E+Vit). The individual takes the supplement at predetermined intervals for a predetermined duration known to restore vitamin deficiency with conventional supplementation. There may be several S+E+Vit groups, where each group receives supplements containing different concentrations of ethyl capsaicin and / or vitamins. The vitamin concentration was reduced compared to that of S-E+Vit. At the end of the predetermined period, an assessment is made which individuals have a vitamin deficiency and which individuals have overcome their vitamin deficienc...

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Abstract

The present invention relates to synthetic capsaicin analogues, tautomers or salts thereof and their use as bioenhancers. The invention provides substituted capsaicyns for use as a bioenhancer, use asa bioenhancer on active substances, in compositions preferably for oral administration, such as in feed, food, pharmaceutical compositions or supplements.

Description

[0001] field of invention [0002] The present invention relates to the synthesis of capsaicin (capsaicin) analogues, tautomers or salts thereof and their use as biological enhancers. Furthermore, the invention relates to compositions comprising the compounds used. Such compositions or compounds may preferably be used for oral administration, feed, food or supplement. [0003] Background of the invention [0004] Absorption of a substance and metabolism of the substance affect the amount of the substance absorbed in the body. Dosing of the poorly absorbable substance in larger doses or other adjustments to the dosing regimen is required to allow the poorly absorbable substance to function in the body. A poorly absorbed substance has low bioavailability. [0005] Substances with poor bioavailability have several drawbacks. Higher amounts of substance are required to achieve the desired effect. This may cause undesired side effects. Unreasonable amounts of the substance may...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/165A23L33/10A23K20/111C07C233/20
CPCA61K31/165A23K20/111A23L33/10A23K50/80Y02A40/818A61K9/0053A61K9/0056A61K45/06
Inventor T·赫尔辛
Owner アクシシェムアクティエボラーグ