Application of Taurine Chelated Calcium in Preparation of Transdermal Absorption Preparation

A technology of taurine and chelated calcium, which is applied in skin care preparations, drug combinations, skin diseases, etc., can solve problems such as interference with calcium ion absorption, insufficient physiological activity, and difficulty in maintaining stable calcium ion balance in the epidermis. Effect of repairing skin barrier function, solving percutaneous absorption problem, and excellent percutaneous absorption effect

Active Publication Date: 2020-12-15
北京乳凝创新生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] When the human body is in a state of calcium deficiency, the calcium supplemented by oral supplementation is preferentially used to supplement the combined calcium required by bones and teeth. At this time, the supplemented calcium has lost its physiological activity and cannot be supplemented or can only be supplemented in a very small amount. Ionized calcium, but this is insufficient for regulating the physiological activity of the body, so it is very difficult to maintain the balance and stability of the epidermal calcium ion by transporting calcium ions to the epidermis through blood circulation in the case of calcium deficiency in the human body
[0007] Oral calcium preparations are difficult to absorb, have a low absorption rate, and are affected by many and complicated factors, which are mainly caused by the complex environment of the gastrointestinal tract
Oral supplemented calcium is digested and absorbed through the gastrointestinal tract. The environment of the stomach is a strongly acidic environment with a pH value varying between 0.8 and 3.6. The environment of the small intestine is weakly alkaline and the pH value varies between 7.2 and 8.0. This change in the acid-base environment is unfavorable for the absorption of calcium ions. For example, calcium ions tend to form gelatinous calcium hydroxide precipitates in the alkaline intestinal environment, making it difficult for calcium ions to be absorbed by the body. At the same time, this gelatinous Thick matter can adhere to the intestinal wall, further affecting the absorption of other nutrients
In particular, oral calcium is easily polluted by anions in the gastrointestinal tract to form insoluble calcium, resulting in a significant reduction in the absorption rate of calcium ions, such as phytic acid, oxalic acid, alkaline phosphate, fat, and dietary fiber contained in the ingested food. Uronic acid residues, nucleotides, uric acid, etc. can react with calcium ions to form insoluble or insoluble calcium oxalate, calcium phytate, basic calcium phosphate, calcium urate, etc., which not only interfere with the absorption of calcium ions, but also Causing calcium to precipitate in tissues to become calcification foci, and to form stones in organs, affecting health
[0008] 2. There is no blood circulation system in the human epidermal system, and it is difficult to transport calcium ions with physiological activity.
[0010] 3. There is currently a lack of targeted calcium supplements for external use on the market
[0011] All kinds of calcium supplements currently on the market are oral preparations, including various calcium tablets and oral liquids, which are mainly developed for the special digestive system of the gastrointestinal tract. The pH value of the gastrointestinal tract is between 0.8 and 3.6. It belongs to a strong acid environment, and there are also various fungi, organic acids, and anions that pollute calcium ions and become insoluble substances that cannot be absorbed by the human body. The normal pH value of the human epidermis is between 5.2 and 6.5, which belongs to a weakly acidic environment. , so oral calcium preparations generally used for digestion and absorption through the gastrointestinal tract are difficult to absorb through the skin
At the same time, the general oral calcium preparations mostly use inorganic calcium and ionic organic acid calcium such as calcium chloride, calcium carbonate, calcium lactate, calcium propionate, calcium citrate, calcium gluconate, etc. These calcium preparations are all in ionic state, and at the same time Some calcium salts also have the problem of poor solubility. In the field of percutaneous absorption, insoluble compounds and ionic compounds are very difficult to absorb
[0012] At the same time, no scholars have studied the problem of percutaneous absorption of calcium, so it is very necessary to study calcium supplements that are conducive to percutaneous absorption, and it is also a very innovative research topic. The body supplements with physiologically active ionic calcium, especially the targeted calcium supplementation to the epidermis system that does not exist in the blood circulation system, and has high absorption efficiency, and is not affected by the special and complex environment of the gastrointestinal tract. The ions are easily polluted by anions, which leads to the problem of low absorption and utilization

Method used

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  • Application of Taurine Chelated Calcium in Preparation of Transdermal Absorption Preparation
  • Application of Taurine Chelated Calcium in Preparation of Transdermal Absorption Preparation
  • Application of Taurine Chelated Calcium in Preparation of Transdermal Absorption Preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] 1. Preparation of chelated calcium taurine: In the experiment, taurine was used as a ligand, and calcium chloride, calcium carbonate, calcium phosphate, calcium hydrogen phosphate, calcium silicate, calcium lactate, calcium propionate, lemon One of calcium gluconate and calcium gluconate is used as a calcium source to provide central ion calcium to prepare amino acid chelated calcium for further experimental research, as follows:

[0064] 1) Weigh 45 g of taurine, dissolve it in a three-necked flask with 150 ml of deionized water, and heat it in a water bath to a constant temperature of 80°C until glutamic acid is completely dissolved;

[0065] 2) Weigh 20g of calcium lactate, completely dissolve in enough water, and adjust the pH to 7.8;

[0066] 3) Slowly add the calcium lactate solution prepared in 2) to the taurine solution in 1) drop by drop, stir gently while adding the calcium lactate solution, and keep a constant temperature during the stirring process;

[0067...

Embodiment 2

[0078] In this experiment, taurine was used as a ligand, and any one of calcium chloride, calcium carbonate, calcium phosphate, calcium hydrogen phosphate, calcium silicate, calcium lactate, calcium propionate, calcium citrate, and calcium gluconate was selected as the ligand. The calcium source of the central ion calcium is provided, and taurine chelated calcium with different chelation ratios is prepared.

[0079] Preparation of taurine-chelated calcium with a chelation ratio of taurine:calcium = 2:1

[0080] 1) Weigh 45 g of taurine, dissolve it in a three-necked flask with 150 ml of deionized water, and heat it in a water bath to a constant temperature of 80°C until the taurine is completely dissolved;

[0081] 2) Weigh 20g of calcium lactate, completely dissolve in enough water, and adjust the pH to 7.8;

[0082] 3) Slowly add the calcium lactate solution prepared in 2) to the taurine solution in 1) drop by drop, stir gently while adding the calcium lactate solution, and...

Embodiment 3

[0092] Stability investigation of calcium taurine chelate aqueous solution: this experiment is raw material with the taurine chelate calcium prepared in embodiment 1, and selects glutamic acid chelate calcium as comparison object, compares taurine chelate calcium and For the stability of the aqueous solution of other amino acid chelated calcium, preservatives should be added in the prepared aqueous solution, and the experimental results are as follows:

[0093] Table, stability of aqueous solutions of calcium taurine chelate-calcium glutamate chelate under different conditions

[0094]

[0095] As can be seen from the above test results: the stability of the aqueous solution of taurine chelated calcium is better than that of glutamic acid chelated calcium. For external liquid preparations, this stability is very necessary, indicating that it is more suitable for Preparation of aqueous preparations for external use, such as sprays, gels, lotions, liniments, etc.

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Abstract

The invention relates to the application of taurine chelated calcium in the preparation of percutaneous absorption preparations. The method of percutaneous absorption and calcium supplementation can give priority to supplementing the physiologically active ionic calcium required by the body to the greatest extent, especially this kind of ionic calcium that can be absorbed through the skin. The method of calcium supplementation can directly and quickly realize the supplementation of calcium to the epidermal system without blood circulation system, and solve the problem that the oral calcium supplement is first used for bone formation and becomes non-physiologically active. The problem of calcium deficiency, at the same time, taurine has the function of regulating the concentration of calcium ions inside and outside the cells of the body, that is, it inhibits the concentration of calcium ions at high concentrations, and promotes it at low concentrations, which can adjust the problems of calcium deficiency and excess calcium in skin cells. An important adjustment method of internal and external calcium ion balance, the role of taurine chelated calcium that can be absorbed through the skin in the present invention can be used in the preparation of external pharmaceutical preparations, medical and sanitary materials, external health care preparations, and cosmetics.

Description

technical field [0001] The invention relates to a kind of taurine chelated calcium for percutaneous absorption and treatment of skin diseases or systemic calcium supplementation, which has excellent transdermal absorption effect and can quickly transdermally supplement calcium ions and taurine required by the skin. It has the function of regulating the concentration of calcium ions inside and outside the epidermal cells of the body and repairing the skin barrier function. At the same time, because its stability in aqueous solution is far superior to the characteristics of other protein amino acids, it is more suitable for the preparation of aqueous external preparations, such as smears, creams, liniments, sprays, gels, etc. . It is especially suitable for preparing pharmaceutical external preparations, medical and health preparations, health care external preparations, and cosmetics, and can be used for treating various skin diseases caused by skin calcium deficiency, repairi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/185A61P17/00A61P17/18A61P17/02A61P17/10A61P31/02A61P37/08A61P3/02A61K8/58A61Q19/08A61Q19/02A61Q19/00A61Q17/00
CPCA61Q17/005A61Q19/00A61Q19/008A61Q19/02A61Q19/08A61K8/58A61K9/0014A61K9/08A61K31/185
Inventor 侯玉庆刘彦宏陶几中马丹徐健梅侯天歌
Owner 北京乳凝创新生物科技有限公司
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