CN112957265B - Hydrophilic gel with good permeability and controllable permeation time and preparation method thereof - Google Patents

Hydrophilic gel with good permeability and controllable permeation time and preparation method thereof Download PDF

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Publication number
CN112957265B
CN112957265B CN202110212334.5A CN202110212334A CN112957265B CN 112957265 B CN112957265 B CN 112957265B CN 202110212334 A CN202110212334 A CN 202110212334A CN 112957265 B CN112957265 B CN 112957265B
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mixed solution
regulator
hydrophilic gel
carboxymethyl cellulose
uniformly mixing
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CN112957265A (en
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石磊
颜慧
纪晓宁
王涌
布洛丹
陈瑞
丁玉萱
李冬梅
韩聪慧
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Zhengzhou Elaine Biotechnology Co ltd
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Zhengzhou Elaine Biotechnology Co ltd
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    • A61K8/042Gels
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    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
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Abstract

The invention discloses a hydrophilic gel with good permeability and controllable permeation time and a preparation method thereof, wherein the hydrophilic gel comprises the following components in percentage by weight: 3-8% of sodium polyacrylate, 0.5-2.5% of polyvinylpyrrolidone, 0.2-2% of carboxymethyl cellulose alkali metal salt, 2-5% of thickener, 0.01-0.5% of cross-linking agent, 25-35% of humectant, 0.01-0.18% of regulator, 0.5-1% of preservative, 2-5% of functional component and the balance of deionized water; the preparation method comprises the following steps: and (3) placing the cross-linking agent, the regulator and the humectant into a stirring device, uniformly mixing, adding sodium polyacrylate, polyvinylpyrrolidone and carboxymethyl cellulose alkali metal salt, uniformly mixing to obtain a mixed solution B, placing the thickener, the functional components, the preservative and deionized water into the stirring device, uniformly mixing to obtain a mixed solution C, and uniformly mixing the mixed solution B and the mixed solution C to obtain the hydrophilic gel. The three-dimensional structure formed by the hydrophilic gel has strong bearing capacity on moisture and functional components, improves the control of the release rate of the functional components, and improves the permeability of the functional components.

Description

Hydrophilic gel with good permeability and controllable permeation time and preparation method thereof
Technical Field
The invention relates to the field of hydrophilic gel, in particular to hydrophilic gel with good permeability and controllable permeation time and a preparation method thereof.
Background
The gel is polymer solution or sol with certain concentration, and under proper condition, the viscosity gradually increases, and finally the fluidity is lost, so that the whole system becomes an elastic semisolid with uniform appearance and certain shape. Hydrophilic gels are a class of gels of three-dimensional network structure that are extremely hydrophilic, and are widely used in a variety of fields, such as: the pharmaceutical field, the cosmetic field, the food field, the industrial field, etc.
The hydrophilic gel applied to the medicine field and the cosmetic field needs to permeate the functional components in the gel into the skin to exert the action effect of the functional components, but the functional components in the gel are released too quickly, part of the functional components can remain on the surface of the skin, and the functional components are released too slowly and cannot exert the action well. In order to ensure that the hydrophilic gel can slowly and continuously release the functional components, the hydrophilic gel with good permeability and controllable permeation time needs to be developed.
Disclosure of Invention
In order to solve the technical problems, the first aspect of the invention provides a hydrophilic gel with good permeability and controllable permeation time, which comprises the following components in percentage by weight: 3-8% of sodium polyacrylate, 0.5-2.5% of polyvinylpyrrolidone, 0.2-2% of carboxymethyl cellulose alkali metal salt, 2-5% of thickener, 0.01-0.5% of cross-linking agent, 25-35% of humectant, 0.01-0.18% of regulator, 0.5-1% of preservative, 2-5% of functional component and the balance of deionized water.
Further, the components comprise the following components in percentage by weight: 3-6% of sodium polyacrylate, 0.5-2% of polyvinylpyrrolidone, 0.2-2% of carboxymethyl cellulose alkali metal salt, 2-5% of thickening agent, 0.01-0.3% of cross-linking agent, 25-35% of humectant, 0.01-0.14% of regulator, 0.5-1% of preservative, 2-5% of functional component and the balance of deionized water.
Further, the components comprise the following components in percentage by weight: 3-6% of sodium polyacrylate, 0.5-1.5% of polyvinylpyrrolidone, 0.2-1.5% of carboxymethyl cellulose alkali metal salt, 2-5% of thickener, 0.01-0.3% of cross-linking agent, 25-35% of humectant, 0.01-0.14% of regulator, 0.5-1% of preservative, 2-5% of functional component and the balance of deionized water.
Further, the carboxymethyl cellulose alkali metal salt comprises one or more of carboxymethyl cellulose calcium, sodium carboxymethyl cellulose and potassium carboxymethyl cellulose.
Further, the carboxymethyl cellulose alkali metal salt comprises one or more of carboxymethyl cellulose calcium and carboxymethyl cellulose sodium.
Further, the thickener comprises one or more of xanthan gum, sodium alginate, gelatin and polyvinyl alcohol.
Further, the cross-linking agent comprises one or more of aluminum glycinate, aluminum hydroxide, aluminum oxide and aluminum chloride.
Further, the regulator includes a crosslinking regulator and a pH regulator.
Further, the preservative comprises one or more of benzyl alcohol, phenoxyethanol, sodium benzoate and potassium sorbate.
Further, the functional components comprise one or more of nicotinamide, magnolol, salicylic acid, arbutin, glutathione, hyaluronic acid, tea polyphenol and oligopeptide.
The second aspect of the invention provides a preparation method of hydrophilic gel with good permeability and controllable permeation time, comprising the following steps:
s1, placing a cross-linking agent, a cross-linking regulator and a humectant into a stirring device, and uniformly mixing to obtain a mixed solution A;
s2, adding sodium polyacrylate, polyvinylpyrrolidone and carboxymethyl cellulose alkali metal salt into the mixed solution A, and uniformly mixing to obtain a mixed solution B;
s3, placing the thickener, the functional components, the preservative, the pH regulator and the deionized water into a stirring device, and uniformly mixing to obtain a mixed solution C;
s4, placing the mixed solution B into a stirring device, stirring for 10-20min, adding the mixed solution C, and stirring for 10-20min to obtain hydrophilic gel.
Further, the preparation method is performed at room temperature.
Compared with the prior art, the invention has the following beneficial effects:
1. the hydrophilic gel prepared by the method has rich components, the preparation method is simple and easy to produce, the network structure of the hydrophilic gel is adjusted by changing the addition amount of each component in the hydrophilic gel, the bearing capacity of the network structure on the functional components is improved, and the purpose of controlling the permeation time of the functional components is further achieved.
2. The hydrophilic gel prepared by the invention is comfortable to apply, the functional components are slowly released layer by layer in the release and permeation processes, the effect is durable, the permeation capacity of the functional components is improved, and the transdermal absorption effect of the functional components is enhanced.
Detailed Description
In order to solve the technical problems, the first aspect of the invention provides a hydrophilic gel with good permeability and controllable permeation time, which comprises the following components in percentage by weight: 3-8% of sodium polyacrylate, 0.5-2.5% of polyvinylpyrrolidone, 0.2-2% of carboxymethyl cellulose alkali metal salt, 2-5% of thickener, 0.01-0.5% of cross-linking agent, 25-35% of humectant, 0.01-0.18% of regulator, 0.5-1% of preservative, 2-5% of functional component and the balance of deionized water.
Further, the components comprise the following components in percentage by weight: 3-6% of sodium polyacrylate, 0.5-2% of polyvinylpyrrolidone, 0.2-2% of carboxymethyl cellulose alkali metal salt, 2-5% of thickening agent, 0.01-0.3% of cross-linking agent, 25-35% of humectant, 0.01-0.14% of regulator, 0.5-1% of preservative, 2-5% of functional component and the balance of deionized water.
Further, the components comprise the following components in percentage by weight: 3-6% of sodium polyacrylate, 0.5-1.5% of polyvinylpyrrolidone, 0.2-1.5% of carboxymethyl cellulose alkali metal salt, 2-5% of thickener, 0.01-0.3% of cross-linking agent, 25-35% of humectant, 0.01-0.14% of regulator, 0.5-1% of preservative, 2-5% of functional component and the balance of deionized water.
Still further, the components comprise, in weight percent: 5% of sodium polyacrylate, 0.5-1.5% of polyvinylpyrrolidone, 0.2-1.5% of carboxymethyl cellulose alkali metal salt, 2-5% of thickener, 0.15-0.5% of cross-linking agent, 30% of humectant, 0.01-0.14% of regulator, 0.5-1% of preservative, 2-5% of functional component and the balance of deionized water.
Further, the weight ratio of polyvinylpyrrolidone to carboxymethyl cellulose alkali metal salt is 1: (1-3).
Further, the weight ratio of polyvinylpyrrolidone to carboxymethyl cellulose alkali metal salt is 1: (1-2).
Further, the carboxymethyl cellulose alkali metal salt comprises one or more of carboxymethyl cellulose calcium, sodium carboxymethyl cellulose and potassium carboxymethyl cellulose.
Further, the carboxymethyl cellulose alkali metal salt comprises one or more of carboxymethyl cellulose calcium and carboxymethyl cellulose sodium.
Further, the thickener comprises one or more of xanthan gum, sodium alginate, gelatin and polyvinyl alcohol.
Further, the thickener is sodium alginate.
Further, the cross-linking agent comprises one or more of aluminum glycinate, aluminum hydroxide, aluminum oxide and aluminum chloride.
Further, the cross-linking agent is aluminum glycinate.
Further, the regulator includes a crosslinking regulator and a pH regulator.
Further, the crosslinking regulator comprises one or a combination of ethylene diamine tetraacetic acid and disodium ethylene diamine tetraacetate.
Further, the crosslinking regulator is disodium ethylenediamine tetraacetate, and the weight percentage is 0-0.05%.
Further, the pH regulator comprises one or more of tartaric acid, citric acid and lactic acid.
Further, the pH regulator is tartaric acid, and the weight percentage is 0-0.09%.
Further, the weight percentage of the tartaric acid is 0.03-0.09%.
Further, the preservative comprises one or more of benzyl alcohol, phenoxyethanol, sodium benzoate and potassium sorbate.
Further, the preservative is phenoxyethanol.
Further, the functional components comprise one or more of nicotinamide, magnolol, salicylic acid, arbutin, glutathione, hyaluronic acid, tea polyphenol and oligopeptide.
The second aspect of the invention provides a preparation method of hydrophilic gel with good permeability and controllable permeation time, comprising the following steps:
s1, placing a cross-linking agent, a cross-linking regulator and a humectant into a stirring device, and uniformly mixing to obtain a mixed solution A;
s2, adding sodium polyacrylate, polyvinylpyrrolidone and carboxymethyl cellulose alkali metal salt into the mixed solution A, and uniformly mixing to obtain a mixed solution B;
s3, placing the thickener, the functional components, the preservative, the pH regulator and the deionized water into a stirring device, and uniformly mixing to obtain a mixed solution C;
s4, placing the mixed solution B into a stirring device, stirring for 10-20min, adding the mixed solution C, and stirring for 10-20min to obtain hydrophilic gel.
Further, the preparation method is performed at room temperature.
In the hydrophilic gel prepared by the invention, components such as sodium polyacrylate, polyvinylpyrrolidone and the like form a three-dimensional structure with water cube characteristics under the action of a cross-linking agent and a regulator, moisture and functional components are effectively coated in the three-dimensional structure, and the carboxymethyl cellulose alkali metal salt has rapid water absorption expansion capacity, and simultaneously has a chelating effect with other components in the hydrophilic gel prepared by the invention, so that the carrying capacity and the control capacity of the moisture and the functional components are improved, the control of the release speed of the functional components is enhanced, and the purpose of controlling the permeation time of the functional components is further achieved. Meanwhile, the combined action of the components in the hydrophilic gel ensures that the functional components are slowly released layer by layer in the release and permeation processes, the action is lasting, and the permeation capacity of the functional components is enhanced.
The present invention will be specifically described below by way of examples. It is noted herein that the following examples are given solely for the purpose of further illustration and are not to be construed as limitations on the scope of the invention, as will be apparent to those skilled in the art in light of the foregoing disclosure.
In addition, the raw materials used are commercially available unless otherwise indicated.
Sodium polyacrylate, CAS number: 9003-04-7, model number purchased from Australian biotechnology Co., ltd., guangzhou: viscomate NP700.
Polyvinylpyrrolidone, CAS number: 9003-39-8 purchased from Kayinji chemical Co., ltd., model: plasdone K90.
Carboxymethylcellulose calcium, CAS number: 9050-04-8.
Example 1
A hydrophilic gel with good permeability and controllable permeation time comprises the following components in percentage by weight: sodium polyacrylate 5%, polyvinylpyrrolidone 0.5%, carboxymethylcellulose calcium 1%, sodium alginate 3%, phenoxyethanol 1%, aluminum glycinate 0.25%, glycerol 30%, disodium edetate 0.03%, tartaric acid 0.07%, nicotinamide 3%, and deionized water to supplement the rest.
A preparation method of hydrophilic gel with good permeability and controllable permeation time comprises the following steps:
(1) Putting aluminum glycinate, disodium ethylenediamine tetraacetate and glycerol into a stirring device, and uniformly mixing at room temperature to obtain a mixed solution A;
(2) Adding sodium polyacrylate, polyvinylpyrrolidone and carboxymethylcellulose calcium into the mixed solution A, and uniformly mixing at room temperature to obtain a mixed solution B;
(3) Placing phenoxyethanol, sodium alginate, nicotinamide, tartaric acid and deionized water into a stirring device, and uniformly mixing at room temperature to obtain a mixed solution C;
(4) And (3) placing the mixed solution B into a stirring device, stirring for 10min, adding the mixed solution C, and stirring for 10min to obtain the hydrophilic gel.
Example 2
A hydrophilic gel with good permeability and controllable permeation time comprises the following components in percentage by weight: sodium polyacrylate 5%, polyvinylpyrrolidone 1%, carboxymethylcellulose calcium 1.5%, sodium alginate 4%, phenoxyethanol 1%, aluminum glycinate 0.15%, glycerol 30%, disodium edetate 0.01%, tartaric acid 0.04%, nicotinamide 3%, and deionized water to supplement the rest.
A preparation method of hydrophilic gel with good permeability and controllable permeation time comprises the following steps:
(1) Putting aluminum glycinate, disodium ethylenediamine tetraacetate and glycerol into a stirring device, and uniformly mixing at room temperature to obtain a mixed solution A;
(2) Adding sodium polyacrylate, polyvinylpyrrolidone and carboxymethylcellulose calcium into the mixed solution A, and uniformly mixing at room temperature to obtain a mixed solution B;
(3) Placing phenoxyethanol, sodium alginate, nicotinamide, tartaric acid and deionized water into a stirring device, and uniformly mixing at room temperature to obtain a mixed solution C;
(4) And (3) placing the mixed solution B into a stirring device, stirring for 10min, adding the mixed solution C, and stirring for 10min to obtain the hydrophilic gel.
Comparative example 1
A hydrophilic gel with good permeability and controllable permeation time comprises the following components in percentage by weight: sodium polyacrylate 5%, polyvinylpyrrolidone 0.5%, sodium alginate 3%, phenoxyethanol 1%, aluminum glycinate 0.25%, glycerol 30%, disodium ethylenediamine tetraacetate 0.03%, tartaric acid 0.07%, nicotinamide 3%, and deionized water to supplement the balance.
A preparation method of hydrophilic gel with good permeability and controllable permeation time comprises the following steps:
(1) Putting aluminum glycinate, disodium ethylenediamine tetraacetate and glycerol into a stirring device, and uniformly mixing at room temperature to obtain a mixed solution A;
(2) Adding sodium polyacrylate and polyvinylpyrrolidone into the mixed solution A, and uniformly mixing at room temperature to obtain a mixed solution B;
(3) Placing phenoxyethanol, sodium alginate, nicotinamide, tartaric acid and deionized water into a stirring device, and uniformly mixing at room temperature to obtain a mixed solution C;
(4) And (3) placing the mixed solution B into a stirring device, stirring for 10min, adding the mixed solution C, and stirring for 10min to obtain the hydrophilic gel.
Comparative example 2
A hydrophilic gel with good permeability and controllable permeation time comprises the following components in percentage by weight: sodium polyacrylate 5%, sodium alginate 3%, phenoxyethanol 1%, aluminum glycinate 0.25%, glycerol 30%, disodium edetate 0.03%, tartaric acid 0.07%, nicotinamide 3%, and deionized water for the rest.
A preparation method of hydrophilic gel with good permeability and controllable permeation time comprises the following steps:
(1) Putting aluminum glycinate, disodium ethylenediamine tetraacetate and glycerol into a stirring device, and uniformly mixing at room temperature to obtain a mixed solution A;
(2) Adding sodium polyacrylate into the mixed solution A, and uniformly mixing at room temperature to obtain a mixed solution B;
(3) Placing phenoxyethanol, sodium alginate, nicotinamide, tartaric acid and deionized water into a stirring device, and uniformly mixing at room temperature to obtain a mixed solution C;
(4) And (3) placing the mixed solution B into a stirring device, stirring for 10min, adding the mixed solution C, and stirring for 10min to obtain the hydrophilic gel.
Comparative example 3
A hydrophilic gel with good permeability and controllable permeation time comprises the following components in percentage by weight: sodium polyacrylate 5%, sodium alginate 3%, phenoxyethanol 1%, aluminum glycinate 0.25%, glycerol 30%, tartaric acid 0.07%, nicotinamide 3%, and deionized water in balance.
A preparation method of hydrophilic gel with good permeability and controllable permeation time comprises the following steps:
(1) Putting aluminum glycinate and glycerol into a stirring device, and uniformly mixing at room temperature to obtain a mixed solution A;
(2) Adding sodium polyacrylate into the mixed solution A, and uniformly mixing at room temperature to obtain a mixed solution B;
(3) Placing phenoxyethanol, sodium alginate, nicotinamide, tartaric acid and deionized water into a stirring device, and uniformly mixing at room temperature to obtain a mixed solution C;
(4) And (3) placing the mixed solution B into a stirring device, stirring for 10min, adding the mixed solution C, and stirring for 10min to obtain the hydrophilic gel.
Performance testing
The hydrophilic gel prepared in the example and the comparative example are respectively added with a carrier to prepare gel patches, a vertical Franz diffusion method is adopted to carry out transdermal experiments of the isolated mouse skin, a certain amount of receiving liquid is respectively taken at 1h, 2h, 4h, 6h and 8h, the content of nicotinamide in the receiving liquid is measured, and the cumulative penetration (mug/cm) is calculated 2 ). Cumulative transmission is the total amount of nicotinamide that permeated through the skin of the isolated mice over a period of time and the data are recorded in table 1.
TABLE 1
Examples 1h 2h 4h 6h 8h
Example 1 12.5 26 38 48 79
Example 2 14 27 37 50 76
Comparative example 1 25 43 67 72 73
Comparative example 2 18 45 66 74 74
Comparative example 3 8 12 21 28 36
As can be seen from Table 1, the nicotinamide in the hydrophilic gels prepared in examples 1 and 2 was gradually released from the hydrophilic gel within 8 hours, and a sustained and stable permeation was maintained. The hydrophilic gels prepared in comparative examples 1 and 2 have high release rate of nicotinamide, and the nicotinamide has a large amount of residues on the skin surface, which is unfavorable for absorption. In comparative example 3, the release rate of nicotinamide from the hydrophilic gel was slow, resulting in a large amount of nicotinamide remaining in the gel after 8 hours.
The above description is only a preferred embodiment of the present invention, and is not intended to limit the invention in any way, and any person skilled in the art may make modifications or alterations to the disclosed technical content to equivalent embodiments without departing from the technical content of the present invention, and any simple modification, equivalent changes and alterations to the above embodiments according to the technical substance of the present invention still fall within the scope of the technical solution of the present invention.

Claims (1)

1. A hydrophilic gel with good permeability and controllable permeation time is characterized by comprising the following components in percentage by weight: sodium polyacrylate 5%, polyvinylpyrrolidone 0.5%, carboxymethyl cellulose alkali metal salt 1%, thickener 3%, crosslinking agent 0.25%, humectant 30%, regulator 0.1%, preservative 1%, effective component 3%, and deionized water for balancing;
the weight ratio of polyvinylpyrrolidone to carboxymethyl cellulose alkali metal salt is 1:2;
the carboxymethyl cellulose alkali metal salt is carboxymethyl cellulose calcium, and the humectant is glycerin;
the thickening agent is sodium alginate; the cross-linking agent is aluminum glycinate;
the regulator comprises a crosslinking regulator and a pH regulator;
the crosslinking regulator is disodium ethylenediamine tetraacetate, and the weight percentage is 0.03%;
the pH regulator is tartaric acid, and the weight percentage is 0.07%;
the preservative is phenoxyethanol; the functional component is nicotinamide;
the preparation method of the hydrophilic gel with good permeability and controllable permeation time comprises the following steps:
s1, placing a cross-linking agent, a cross-linking regulator and a humectant into a stirring device, and uniformly mixing to obtain a mixed solution A;
s2, adding sodium polyacrylate, polyvinylpyrrolidone and carboxymethyl cellulose alkali metal salt into the mixed solution A, and uniformly mixing to obtain a mixed solution B;
s3, placing the thickener, the functional components, the preservative, the pH regulator and the deionized water into a stirring device, and uniformly mixing to obtain a mixed solution C;
s4, placing the mixed solution B into a stirring device, stirring for 10-20min, adding the mixed solution C, and stirring for 10-20min to obtain hydrophilic gel;
the preparation process is carried out at room temperature.
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