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Application of Polypeptide Chelated Calcium in Preparation of Transdermal Absorption Preparation

A polypeptide chelated calcium and preparation technology, which is applied in skin care preparations, drug combinations, skin diseases, etc., can solve the problems of low absorption and utilization of calcium ions, affecting the absorption of other nutrients, and unfavorable calcium ions

Active Publication Date: 2019-05-10
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

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
[0006] 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
[0007] 2. There is no blood circulation system in the human epidermal system, and it is difficult to transport calcium ions with physiological activity.
[0009] 3. There is currently a lack of targeted calcium supplements for external use on the market
[0010] 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 stomach is between 0.8 and 3.6, which belongs to In a strong acid environment, 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 range of the human epidermis is between 5.2 and 6.5, which is a weakly acidic environment. Therefore, 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 have 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
[0011] 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 Polypeptide Chelated Calcium in Preparation of Transdermal Absorption Preparation
  • Application of Polypeptide Chelated Calcium in Preparation of Transdermal Absorption Preparation
  • Application of Polypeptide Chelated Calcium in Preparation of Transdermal Absorption Preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Preparation of polypeptide chelated calcium: In this experiment, glutathione was used as a ligand, and calcium chloride, calcium carbonate, calcium phosphate, calcium hydrogen phosphate, calcium silicate, calcium lactate, calcium propionate, calcium citrate, One of calcium gluconate is used as a calcium source to provide central ion calcium to prepare polypeptide chelated calcium for further experimental research, as follows:

[0051] 1. Preparation of glutathione chelated calcium

[0052] 1) Weigh 100 g of glutathione, dissolve it in a three-necked flask with 350 ml of deionized water, and heat it in a water bath to a constant temperature of 60°C until glutathione is completely dissolved;

[0053] 2) Weigh 100g of calcium lactate, completely dissolve in enough water, and adjust the pH to 8.0;

[0054] 3) Slowly add the calcium lactate solution prepared in 2) to the glutathione solution in 1) drop by drop, stir gently while adding the calcium lactate solution, and keep...

Embodiment 2

[0066] This experiment compared the transdermal absorption effect of polypeptide chelated calcium and amino acid chelated calcium, inorganic calcium and organic acid calcium. In the test, isolated mouse skin was used, and the receiving solution was 0.9% sodium chloride aqueous solution. The test time was 10h. The polypeptide chelated calcium selected in the test is the glutathione chelated calcium prepared in Example 1, the amino acid chelated calcium is glutamic acid chelated calcium, the inorganic calcium is calcium chloride, and the organic acid calcium is calcium gluconate , the specific test method is to prepare glutathione chelated calcium, glutamate chelated calcium, calcium chloride, and calcium gluconate into solutions with the same mass concentration, and take the effective test area of ​​mouse skin as diameter d=1.5cm Take the same volume of three solutions and apply them evenly on the surface of mouse skin, test and compare glutathione chelated calcium, glutamate c...

Embodiment 3

[0071] In this experiment, the glutathione chelated calcium prepared in Example 1 was used as the test sample, and the effects of different concentrations of glutathione chelated calcium solutions on the transdermal effect were compared. In the test, isolated mouse skin was used, the receiving solution used was 0.9% sodium chloride aqueous solution, and the test time was 6 hours. Glutathione chelated calcium was formulated into solutions of different mass concentrations, and the effective test area of ​​the mouse skin was a circular size with a diameter of d=1.5cm, and glutathione chelated calcium solutions of various concentrations with the same volume were taken Apply evenly on the surface of mouse skin, test and compare with franz diffusion cell transdermal tester, the specific results are shown in Table 2 below:

[0072] Table 2. Transdermal effects of different concentrations of glutathione chelated calcium

[0073]

[0074] As can be seen from the above table, the tr...

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Abstract

The invention relates to application of polypeptide chelated calcium in preparing a transdermic absorbent. The purpose of treating skin diseases is achieved by supplementing calcium and polypeptide to the body in a cutaneous absorption mode. By means of the way of supplementing calcium through cutaneous absorption, physiological activity ionic calcium needed by the body can be supplemented to the largest degree, particularly, calcium can be directly and rapidly supplemented to an integumentary system with no blood circulation system, and the problems that that the absorption rate of oral calcium intake is low and physiological activity ionic calcium is insufficient due to the fact that calcium is used as non-physiological activity binding calcium for skeleton forming are solved. The polypeptide chelated calcium capable of achieving transdermic absorption can be used for preparing external use medicine preparations, medical hygienic materials, external use health-care product preparations and cosmetics.

Description

technical field [0001] The invention relates to a polypeptide chelated calcium preparation for percutaneous absorption and treatment of skin diseases or systemic calcium supplementation. Background technique [0002] The common problem of calcium deficiency in the human skin system is relatively serious. Calcium deficiency in human skin can cause a variety of skin diseases, poor skin barrier function, easy infection and inflammation, fragile and long healing period after damage, dry, sensitive, watery skin. Various skin problems such as oil balance imbalance, accelerated skin aging, weak environmental tolerance, etc., especially when the facial skin is exposed and affected by adverse environments such as strong ultraviolet rays, pollution, and radiation, are more likely to cause various adverse skin conditions. The human skin system is in a state of calcium deficiency for a long time mainly due to the following reasons: [0003] 1. The calcium supplemented orally by the hum...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K38/06A61K8/64A61P3/02A61P17/00A61P17/18A61P17/02A61P37/08A61P17/10A61P31/02A61P9/14A61Q19/08A61Q19/02A61Q19/00A61Q17/00
CPCA61K8/64A61K9/0014A61K9/12A61K38/063A61K47/36A61Q17/005A61Q19/00A61Q19/008A61Q19/02A61Q19/08
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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