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Colon-targeted sinomenine hydrochloride slow-release nanofiber membrane and preparation method and application thereof

A technology of sinomenine hydrochloride and nanofiber membrane, applied in nanotechnology, nanomedicine, nanotechnology and other directions, can solve the problems of reducing the sudden release of water-soluble drugs and side effects of the digestive tract, so as to reduce the sudden release phenomenon and maintain the efficacy of the drug , reducing the effect of irritation

Inactive Publication Date: 2020-04-17
GUANGXI UNIV FOR NATITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to provide a colon-targeted sinomenine hydrochloride slow-release nanofibrous membrane and its preparation method and application. The destruction of gastric acid, small intestine, and large intestine environment enables sustained release in the colon, reduces the burst release of water-soluble drugs, and prolongs the release of water-soluble drugs

Method used

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  • Colon-targeted sinomenine hydrochloride slow-release nanofiber membrane and preparation method and application thereof
  • Colon-targeted sinomenine hydrochloride slow-release nanofiber membrane and preparation method and application thereof
  • Colon-targeted sinomenine hydrochloride slow-release nanofiber membrane and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] A method for preparing a colon-targeted sinomenine hydrochloride slow-release nanofibrous membrane, comprising:

[0035] (1) Weigh 2.2508g of polyacrylic resin Eudragit S100 with an analytical balance, add it to a mixed solution of 3.6430g N,N-dimethylacetamide and 9.110g of absolute ethanol, heat and stir to obtain a shell spinning solution . Wherein, the concentration of absolute ethanol is ≥99.7%, the concentration of N,N-dimethylacetamide is ≥99.5%, the heating temperature is 50°C, and the stirring time is 8h;

[0036] (2) Weigh 0.2503g of polyacrylic acid resin Eudragit RS100 and 0.3003g of sinomenine hydrochloride with an analytical balance, add them together to a mixed solution of 1.2720g of chloroform and 3.1781g of absolute ethanol, stir at room temperature to obtain a nuclear layer spinning solution. Wherein, the concentration of absolute ethanol is ≥99.7%, the concentration of chloroform is ≥99.0%; the stirring time is 4h;

[0037] (3) Spin the spinning sol...

Embodiment 2

[0046] A method for preparing a colon-targeted sinomenine hydrochloride slow-release nanofibrous membrane is basically the same as the method in Example 1, the difference being:

[0047] In step (1), the amount of polyacrylic resin Eudragit S100 is 2.2501 g; the solution is mixed with 6.3750 g of N,N-dimethylacetamide and 6.3750 g of absolute ethanol. The rest of the steps are the same.

[0048] In step (3), the positive electrode of the voltage in the electrospinning process is +17KV, the ambient temperature is 26° C., and the drug-loaded nanofiber membrane obtained has a drug-loading capacity of 20% to 30%.

[0049] The same method as in Example 1 was used to measure the in vitro release of the coaxial drug-loaded sustained-release nanofiber membrane of Example 2. The nanofibrous membrane prepared in Example 2 of the present invention released only about 5% in two hours in a simulated stomach environment with a pH of 1.2, and only released about 4% in two hours in a simulat...

Embodiment 3

[0051] A method for preparing a colon-targeted sinomenine hydrochloride slow-release nanofibrous membrane is basically the same as the method in Example 1, the difference being:

[0052] In step (1), the amount of polyacrylic resin Eudragit S100 is 2.2498g; the solution is mixed with 6.3750g N,N-dimethylacetamide and 6.3750g absolute ethanol. The rest of the steps are the same.

[0053] In step (2), weigh the polyacrylic acid resin Eudragit RS100 of 0.2503g and 0.3003g sinomenine hydrochloride; add together in the mixed solution of 1.0556g chloroform and 3.6944g dehydrated alcohol, stir at room temperature to obtain the nuclear layer spinning solution . Wherein, the concentration of absolute ethanol is ≥99.7%, the concentration of chloroform is ≥99.0%; the stirring time is 4h;

[0054] In step (3), the positive electrode of the voltage in the electrospinning process is +17KV, the ambient temperature is 26° C., and the drug-loaded nanofiber membrane obtained has a drug-loadin...

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Abstract

The invention discloses a colon-targeted sinomenine hydrochloride slow-release nanofiber membrane and a preparation method and application thereof. The nanofiber membrane comprises a shell layer and acore layer coated in the shell layer, wherein the shell layer comprises the following components: Eudragit S100 or Eudragit RS100; the core layer comprises the following components: any one or more than two of Eudragit S100, Eudragit RS100, polycaprolactone and polyvinylpyrrolidone, and sinomenine hydrochloride. The drug loading capacity of sinomenine hydrochloride in the nanofiber membrane is 10%-30%. According to the sinomenine hydrochloride slow-release nanofiber membrane with the shell-core structure, slow release and targeting of the drug are realized and the membrane has good biocompatibility.

Description

technical field [0001] The invention relates to a colon-targeting sinomenine hydrochloride preparation, in particular to a colon-targeting sinomenine hydrochloride slow-release nanofibrous film and its preparation method and application. Background technique [0002] Sinomenine hydrochloride is a non-steroidal anti-inflammatory analgesic with good anti-inflammatory and analgesic effects and few side effects. It is an effective alkaloid monomer extracted from the dry rhizomes of the plants of the family Fangeaceae. Modern pharmacological studies have shown that it has significant anti-inflammatory, analgesic, immunosuppressive, sedative, and histamine-inhibiting effects, and has been widely used in the treatment of rheumatism, rheumatoid arthritis, and antiarrhythmic diseases with definite curative effects. However, sinomenine hydrochloride has side effects of the digestive tract, and is relatively irritating to the gastrointestinal tract, and sinomenine hydrochloride is a wa...

Claims

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Application Information

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IPC IPC(8): D04H1/728D04H1/4382D01D5/00D01D5/34A61K9/70A61K47/32A61K47/34A61K31/485A61P29/00A61P19/02A61P9/06B82Y5/00
CPCA61K9/7007A61K31/485A61K47/32A61K47/34A61P9/06A61P19/02A61P29/00B82Y5/00D01D5/003D01D5/0069D01D5/0092D01D5/34D04H1/4382D04H1/728
Inventor 赵彦芝邹梦君周菊英廖华珍
Owner GUANGXI UNIV FOR NATITIES
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