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A kind of preparation method containing quaternary ammonium group (meth)acrylate copolymer aqueous dispersion

A technology of acrylates and copolymers, which is applied in the field of preparation of aqueous dispersions of quaternary ammonium-based (meth)acrylate copolymers, can solve the problems of subsequent release of drugs, change retardation and slow release performance, and accelerate drug release, etc., to achieve Reduce the crushing process, speed up the preparation, good dispersion effect

Active Publication Date: 2021-11-12
英德茂丰药业有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Dissolve polyammonium methacrylate I or II with a large amount of ethanol to obtain a copolymer ethanol solution, and then add the obtained solution into hot water containing poloxamer, sorbic acid, sodium hydroxide and sodium stearate In the process, disperse and emulsify synchronously evaporate to remove ethanol to obtain quaternary ammonium methacrylate water dispersion, the preparation time is 6-10h, a large amount of ethanol used needs to be removed by distillation, high energy consumption and low production efficiency
[0009] Both CN102665695A and CN106883429A patent applications have used water-soluble surfactants, but the addition of known surfactants or water-soluble plasticizers and carboxylic acids in the industry will usually change the quaternary ammonium-containing (meth)acrylate copolymer as a drug. Retarding release properties in coatings or matrices, which can lead to undesired pore formation and accelerated drug release
Similarly, water-soluble polyvinyl alcohol and alkyl glycosides in the formulation may also have other effects on the subsequent release of the drug product

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Attempt to add water-soluble plasticizer and ethanol to prepare larger molecular weight aqueous dispersion containing quaternary ammonium (meth)acrylate copolymer:

[0079] (1) Add 576g of water into the reactor, stir at 350rpm, and set the temperature of the water bath to 96°C;

[0080] (2) When the internal temperature rises above 90°C, add 400g of polyammonium methacrylate II particles (by 65% ​​by weight of methyl methacrylate, 30% by weight of ethyl acrylate and 5% by weight of methyl Copolymer composed of trimethylammonium ethyl acrylate chloride, developed by Guangzhou Maofeng Pharmaceutical Co., Ltd., relatively large molecular weight, viscosity: 15.0mPa·s), stirring;

[0081] (3) Add triethyl citrate ethanol solution (80g triethyl citrate dissolved in 160g ethanol) into the reaction kettle, after stirring for 5min, the polymer particles become smaller obviously, and begin to form a blue water dispersion body;

[0082] (4) Stir until the polymer particles swel...

Embodiment 2

[0120] Attempt to add fat-soluble plasticizer and ethanol to prepare larger molecular weight water dispersion containing quaternary ammonium (meth)acrylate copolymer:

[0121] (1) Add 500g of water into the reactor, stir at 350rpm, and set the temperature of the water bath to 96°C;

[0122] (2) When the internal temperature rises above 90°C, add 200g of polyammonium methacrylate I powder (by 60% by weight of methyl methacrylate, 30% by weight of ethyl acrylate and 10% by weight of methyl A copolymer composed of trimethylammonium ethyl acrylate chloride, small particles less than 14 mesh, developed by Guangzhou Maofeng Pharmaceutical Co., Ltd., viscosity: 6.8mPa s), stirring;

[0123] (3) Add the ethanolic solution of dibutyl sebacate (20g dibutyl sebacate is dissolved in 70g ethanol) in the reactor several times, immediately begin to pan blue after adding, polymer particle obviously becomes smaller, and A bluish aqueous dispersion begins to form;

[0124] (3) After about 60 ...

Embodiment 3

[0142] Attempt to add water-soluble plasticizer, ethanol, sorbic acid to prepare larger molecular weight aqueous dispersion containing quaternary ammonium group (meth)acrylate copolymer:

[0143] (1) Add 630g of water into the reactor, stir at 200rpm, and set the temperature of the water bath to 90°C;

[0144] (2) When the internal temperature rises above 80°C, add 2.1g sorbic acid first, and then add 100g polyammonium methacrylate I particles (by 60% by weight of methyl methacrylate, 30% A copolymer composed of ethyl acrylate and 10% by weight of trimethylammonium ethyl methacrylate by weight, developed by Guangzhou Maofeng Pharmaceutical Co., Ltd., relatively large molecular weight, viscosity: 15mPa·s), stirring;

[0145] (3) Stir for about 5 minutes, add 8 g of triethyl citrate ethanol solution (10 g of triethyl citrate dissolved in 6 g of ethanol), after 5 minutes, it becomes sticky and difficult to stir; after 15 minutes, almost all the polymer particles swell;

[0146] ...

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Abstract

The invention relates to a preparation method of an aqueous dispersion containing a quaternary ammonium group (meth)acrylate copolymer. The steps include: maintaining stirring in hot water at 50-100°C, adding a quaternary ammonium-based (meth)acrylate copolymer, a small amount of plasticizer combined with a solvent, and stirring for 2-24 hours to produce an aqueous dispersion; then, According to the follow-up application of the preparation, it is necessary to choose whether to recover the solvent by distillation and add other additives suitable for pharmaceutical use; after cooling to room temperature, use a fine sieve to filter out the possible undispersed complete solids. The inventive method is suitable for water-soluble and fat-soluble plasticizers simultaneously, avoids using the tensio-active agent that does not expect to add, has porosity effect to influence drug release, makes the preparation of this quaternary ammonium-containing (meth)acrylate copolymer aqueous dispersion more efficient Efficient and more widely used.

Description

technical field [0001] The invention belongs to the technical field of functional polymer applications such as pharmaceutical excipients, and specifically relates to a method for converting a solid quaternary ammonium group-containing (meth)acrylate copolymer into an aqueous dispersion. The aqueous dispersion does not contain surfactant, and has no adverse effect on the application of sustained and controlled release of medicines or health product preparations. Background technique [0002] Quaternary ammonium group-containing (meth)acrylate copolymers and aqueous dispersions are used in the field of sustained and controlled release of pharmaceutical preparations, and have been recognized by drug regulatory agencies in various countries and recorded in national pharmacopoeias. [0003] Especially the well-known type of pharmaceutical excipients polyammonium methacrylate I (also known as quaternary ammonium methacrylate copolymer type A, Ammonio Methacrylate Copolymer, Type A...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08J3/05C08J5/18C08L33/12C08K5/11A61K47/32
CPCA61K47/32C08J3/05C08J5/18C08J2333/12C08K5/11
Inventor 杨海峰郭雪静李姗
Owner 英德茂丰药业有限公司
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