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Modified polyhydroxyethyl methacrylate gel and preparation method thereof, drug excipient and external gel

A technology of poly(hydroxyethyl methacrylate) and excipient, which is applied in the field of colloid gel and medicine, can solve the problems of application limitation, bleeding water, poor water retention performance, easy shrinkage of colloid, etc., and achieves an increase in the pore volume of the gel , good bioadhesion, enhance the effect of stimulation

Pending Publication Date: 2021-03-16
瑞希(重庆)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

[0003] Due to its unique thermoreversible gel properties and anti-protein coagulation properties, polyhydroxyethyl methacrylate is currently the most widely used gel material, but in practical applications, the colloid is easy to shrink and has bleeding properties. , Poor water retention performance, resulting in limited application

Method used

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  • Modified polyhydroxyethyl methacrylate gel and preparation method thereof, drug excipient and external gel
  • Modified polyhydroxyethyl methacrylate gel and preparation method thereof, drug excipient and external gel
  • Modified polyhydroxyethyl methacrylate gel and preparation method thereof, drug excipient and external gel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1 prepares pharmaceutical excipient

[0026] The preparation of the pharmaceutical excipient of the present invention is carried out according to the following steps: Weigh each component according to the weight percentage of each component, add carboxymethylated modified polyhydroxyethyl methacrylate and initiator in the container, stir, Fully swell the carboxymethylated poly(hydroxyethyl methacrylate), then add λ-type carrageenan, osmotic pressure regulator, humectant, and preservative to mix, add water and stir well, and adjust the pH to 6-8 with a pH regulator , stirred for 30-45 minutes, that is.

[0027] Prepare the pharmaceutical excipient gel samples of Experimental Examples 1, 2, and 3 according to this method, and prepare Comparative Examples 1 and 2 according to this method, and the specific components and proportioning of each sample are as shown in Table 1 (each component in the table The content is mass percent, and the balance is water). The ...

Embodiment 2

[0034] Embodiment 2 Determination of gel water separation rate

[0035] Accurately weigh 5 g of the pharmaceutical excipients just prepared in Experimental Examples 1-3 respectively, blot the water droplets on the surface of the gel with filter paper, and then accurately weigh again.

[0036] Calculation formula of water analysis rate:

[0037]

[0038] In the formula, K is the water separation rate of the gel;

[0039] m 1 is the initial gel mass;

[0040] m 2 is the gel mass after removal of surface moisture.

[0041] The results of the calculated water separation rate are shown in Table 2: the gel obtained in Experimental Example 1-3 does not have a water separation rate, indicating that the gel will not shrink in size due to dehydration, and the gel has better stability; , the water absorption rate of Comparative Example 1 was too high.

[0042] Table 2 Water analysis rate

[0043]

Embodiment 3

[0044] Embodiment 3 texture property analysis

[0045] The gel strength and cohesiveness of pharmaceutical excipients were investigated by Brookfield CT3 texture analyzer. Select the cylindrical P / 0.5 probe, set the test to the push-down mode, lower the probe at a speed of 1mm / s, and the trigger force is 5g. When the probe touches the surface of the sample, the probe is pressed down to 10mm at 2mm / s, and then rises at a speed of 10mm / s. Record the stress-time curve and process the graph to obtain the maximum value of the positive peak of gel strength and the area of ​​negative peak of adhesiveness.

[0046] The gel strength and adhesiveness test results of Experimental Examples 1-3 are shown in Table 3: the pharmaceutical excipient gel of the present invention has a softer texture and higher gel strength and adhesiveness. The strength and adhesion of the gel in Comparative Example 1 are relatively weak, which affects the quality of the gel and the use effect.

[0047] Table...

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PUM

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Abstract

The invention discloses a carboxymethylation modification method of polyhydroxyethyl methacrylate. The method comprises the following steps: adding polyhydroxyethyl methacrylate into an organic solvent, fully stirring to enable polyhydroxyethyl methacrylate to be in a dispersed state, dropwise adding an aqueous alkali solution, carrying out an alkalization reaction at a constant temperature of 35-40 DEG C, adding sodium chloroacetate after the reaction is finished, heating the reaction system to 50-60 DEG C, carrying out etherification reaction under the condition of constant-temperature stirring, cooling a reactant to room temperature after the reaction is finished, regulating the pH value of the reactant to 6.8-7.2, carrying out suction filtration on the product, washing the filtrate, and drying to obtain the carboxymethylated modified polyhydroxyethyl methacrylate. The invention also discloses a modified polyhydroxyethyl methacrylate gel, which comprises the following components inpercentage by weight: 5 to 15 percent of carboxymethylated modified polyhydroxyethyl methacrylate , 0.5 to 0.7 percent of an initiator, 0.005 to 0.1 percent of lambda-type carrageenan and the balanceof water. The invention also discloses a drug excipient containing the modified polyhydroxyethyl methacrylate gel and an external gel.

Description

technical field [0001] The invention relates to the technical fields of colloid gel and medicine, in particular to a modified polyhydroxyethyl methacrylate gel, a preparation method, a pharmaceutical excipient and an external gel. Background technique [0002] Poly(hydroxyethyl methacrylate) (PHEMA) is obtained by polymerizing hydroxyethyl methacrylate, usually adding a multifunctional cross-linking agent to prepare PHEMA hydrogel. PHEMA was first synthesized by O.Wichterle in 1960. PHEMA It is hydrophilic, expands to a certain volume after absorbing water, is elastic, flexible, chemically inert, and biologically inert. It has good affinity to the body, and its elastic modulus can be changed by adjusting the degree of cross-linking. PHEMA hydrogels have since been proposed as a biomaterial, and have since been widely used as soft tissue substitutes and drug delivery systems. [0003] Due to its unique thermoreversible gel properties and anti-protein coagulation properties, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F8/00C08F120/20A61K47/32A61K9/06C08J3/075C08L33/14C08L5/00
CPCC08F8/00C08J3/075A61K47/32A61K9/06A61K9/0014A61K9/0043C08J2333/14C08J2405/00C08F120/20
Inventor 冯文学李杨洪
Owner 瑞希(重庆)生物科技有限公司
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