Preparation of medicinal poly(methyl acrylamide) with low film forming temperature and medium permeability

A technology of polymethacrylate and film-forming temperature, applied to the application of water-soluble drug sustained-release coating, in the field of osmotic polymethacrylate, can solve the problems of limited promotion, complicated formulation, etc. The effect of easy industrialization, reduced equipment investment, and reduced energy consumption

Inactive Publication Date: 2009-07-08
广州华博生物制药研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because the permeability is located at both ends, only one of them is used. Generally, a large amount of EC or lactose is required to achieve the expected sustained release effect. This property complicates the formula and limits its application.

Method used

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  • Preparation of medicinal poly(methyl acrylamide) with low film forming temperature and medium permeability
  • Preparation of medicinal poly(methyl acrylamide) with low film forming temperature and medium permeability
  • Preparation of medicinal poly(methyl acrylamide) with low film forming temperature and medium permeability

Examples

Experimental program
Comparison scheme
Effect test

no. 1 approach

[0040] Take 0.33ml of ethyl acrylate, 4.36ml of butyl acrylate, 3.4ml of methyl methacrylate, 0.96g of trimethylammonium ethyl methacrylate chloride, first use 1ml of anhydrous Dissolve ethanol, and then add it to a four-neck flask equipped with an electric stirrer, reflux condenser, and thermometer, add 0.02g AIBN, turn on the electric stirrer, and control the speed at 100r~200r / min, without pre-reaction, directly dissolve the polymer The temperature was continuously raised from 30 to 110°C for 8 hours, and the temperature was continuously raised for 5 hours before 65°C to ensure that the monomer reaction was complete, and the reaction was completed. The product was a light yellow translucent solid. The Tg of the obtained polymer was 28.3°C, the number average molecular weight was 45012, and the base value was 3.83 mg / g.

no. 2 approach

[0042] Take 16.6ml of ethyl acrylate, 21.8ml of butyl acrylate, 17ml of methyl methacrylate, 4.82g of trimethylammonium ethyl methacrylate chloride, first use 5ml of absolute ethanol Dissolve, then add to the four-necked bottle equipped with electric stirrer, reflux condenser, and thermometer, add 0.1gAIBN, turn on the electric stirrer, control the speed at 100r~200r / min, do not carry out pre-reaction, directly polymer from 30-110°C was continuously heated for 8 hours, and the temperature was continuously raised for 5h before 65°C to ensure that the monomer reaction was complete, and the reaction was completed. The product was a light yellow translucent solid. The Tg of the obtained polymer was 28.3°C, the number average molecular weight was 45012, and the base value was 19.15 mg / g.

no. 3 approach

[0044] Take 8.3ml of ethyl acrylate, 10.9ml of butyl acrylate, 34ml of methyl methacrylate, 5.43g of trimethylammonium ethyl methacrylate chloride, first use 10ml of absolute ethanol Dissolve, then add to a four-neck flask equipped with an electric stirrer, reflux condenser, and thermometer, add 0.15g AIBN, turn on the electric stirrer, control the speed at 100r~200r / min, slowly raise the temperature to 55°C, and pre-react for 0.5h , stop heating, cool to room temperature, and then continuously raise the temperature of the polymer from 30 to 110°C for 8 hours, and continue to raise the temperature for 3 hours before 65°C to ensure that the monomer reaction is complete, and the reaction is completed. The product is a light yellow translucent solid. The Tg of the obtained polymer was 29.4°C, the number average molecular weight was 40719, and the base value was 22.19 mg / g.

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Abstract

The invention relates to a synthesis method for a low MFT moderate permeability polymethyl acrylamide ester for drug use and application thereof, which belongs to the technical field of sustained release coating material for drug use. The synthesis method comprises the following steps: adopting the body-solution polymerization, introducing a butyl acrylate monomer to obtain the low MFT polymethyl acrylamide ester, and carrying out coating and film forming without adding a plasticizer; regulating the proportion of methylacrylic acid chlorinated trimethylamine ethyl ester in the polymer monomer to obtain the polyacrylic acid resin with moderate permeability. The polymer is mainly applied to the water soluble drug sustained release coating, and can reach a satisfied sustained release effect by adding a few insoluble components or pore-forming agents.

Description

technical field [0001] The invention relates to a synthetic polymer slow-release material and a preparation method, mainly relating to a low film-forming temperature, medium-permeability polymethacryloyl ammonium ester and a preparation method using bulk-solution polymerization synthesis and slow release of water-soluble drugs. Coating application. Background technique [0002] At present, polymer materials that can be used as sustained-release films for medicine can be divided into two categories: natural polymer sustained-release materials and synthetic polymer sustained-release materials. Sustained-release preparations prepared from natural polymer materials are unstable, prone to changes during storage, and poor reproducibility in production, so they are rarely used in industrial production. Polyoxyethylene, a synthetic polymer material, is used in the preparation of paracetamol sustained-release tablets. Polyethylene glycol and povidone are sometimes used as sustained-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F220/14C08F220/18C08F220/34A61K47/32
Inventor 蒋琳兰詹外华
Owner 广州华博生物制药研究所
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