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Gastric targeted drug carrier and preparation method thereof

The technology of a drug and a carrier is applied in the field of gastric targeted drug carrier and its preparation, which can solve the problems of losing the targeting effect, unable to satisfy the gastric targeted drug delivery carrier, unable to achieve the drug sustained-release performance, etc., and achieves stability Autofluorescence, good biocompatibility, the effect of improving the embedding rate

Inactive Publication Date: 2012-09-05
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although chitosan quaternary ammonium hydrogel microspheres have good bioadhesiveness, they disintegrate rapidly in the acidic environment of the stomach as a gastric drug delivery carrier. In the acidic release medium (pH=5.0), due to Dissociation and dissolution of chitosan quaternary ammonium salt microspheres, the drug embedded in it is also rapidly released into the surrounding medium, and all the drug embedded in it is released within 1 hour, which does not achieve good drug sustained release performance, and the shell Although polysaccharide has good pH sensitivity, it loses its targeting effect after reacting with the cross-linking agent, so chitosan and chitosan quaternary ammonium salt alone cannot meet the requirements of gastric targeted drug delivery carrier

Method used

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  • Gastric targeted drug carrier and preparation method thereof
  • Gastric targeted drug carrier and preparation method thereof
  • Gastric targeted drug carrier and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0057] Accurately weigh chitosan (molecular weight 50,000), chitosan quaternary ammonium salt (quaternary ammonium substitution degree 50%, molecular weight 50,000), sodium glycerophosphate and dissolve it in 1% acetic acid aqueous solution, and make it fully dissolve under magnetic stirring to obtain The acetic acid aqueous solution of chitosan, chitosan quaternary ammonium salt, sodium glycerophosphate, its total concentration is 2.5wt%, wherein the concentration of chitosan, chitosan quaternary ammonium salt is respectively 0.5wt%, the concentration of sodium glycerophosphate The mass ratio of chitosan and chitosan quaternary ammonium salt is 1:1, and the mass ratio of chitosan and chitosan quaternary ammonium salt to sodium glycerophosphate is 2:3. The solution was centrifuged at 8000 rpm to remove insoluble impurities, and the supernatant was retained as the aqueous phase for subsequent use. Take 400 μL of 10 mg / mL rapamycin solution O 1 (rapamycin is dissolved in chloro...

Embodiment 2

[0059] Accurately weigh chitosan (molecular weight 50,000), chitosan quaternary ammonium salt (quaternary ammonium substitution degree 50%, molecular weight 50,000), sodium glycerophosphate and dissolve it in 1% acetic acid aqueous solution, and make it fully dissolve under magnetic stirring to obtain The acetic acid aqueous solution of chitosan, chitosan quaternary ammonium salt, sodium glycerophosphate, its total concentration is 2.5wt%, wherein the concentration of chitosan, chitosan quaternary ammonium salt is respectively 0.5wt%, the concentration of sodium glycerophosphate The mass ratio of chitosan and chitosan quaternary ammonium salt is 1:1, and the mass ratio of chitosan and chitosan quaternary ammonium salt to sodium glycerophosphate is 2:3. This solution was centrifuged at 8000rpm to remove insoluble impurities, then added 20 wt% gentamicin sulfate (stomach medicine) of the total dry weight of chitosan and chitosan quaternary ammonium salt and fully dissolved for fu...

Embodiment 3

[0061] Accurately weigh chitosan (molecular weight 50,000), chitosan quaternary ammonium salt (quaternary ammonium substitution degree 70%, molecular weight 100,000), sodium glycerophosphate and dissolve it in 1% acetic acid aqueous solution, and make it fully dissolve under mechanical stirring to obtain The acetic acid aqueous solution of chitosan, chitosan quaternary ammonium salt, sodium glycerophosphate, its total concentration is 2.5wt%, wherein the concentration of chitosan, chitosan quaternary ammonium salt is respectively 0.5wt%, the concentration of sodium glycerophosphate The mass ratio of chitosan and chitosan quaternary ammonium salt is 1:1, and the mass ratio of chitosan and chitosan quaternary ammonium salt to sodium glycerophosphate is 2:3. The solution was centrifuged at 8000 rpm to remove insoluble impurities, and the supernatant was retained as the aqueous phase for subsequent use. Take 400 μL of 10 mg / mL rapamycin solution O 1 (rapamycin is dissolved in chl...

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Abstract

The invention relates to the field of drug carrier preparation, in particular to a gastric targeted drug carrier and a preparation method thereof. The gastric targeted drug carrier is prepared from the following raw materials: drug-containing emulsion and a crosslinking agent, wherein the drug-containing emulsion contains chitosan, chitosan quaternary ammonium salt and sodium glycerophosphate; and the crosslinking agent is used for crosslinking the emulsion into microspheres. The preparation method comprises the following steps: 1) preparing the drug-containing emulsion: with a aqueous solution of chitosan, chitosan quaternary ammonium salt and sodium glycerophosphate as an aqueous phase W, preparing the drug-containing emulsion with the aqueous phase, drugs and an oil phase containing anemulsifying agent; and 2) heating and stirring the drug-containing emulsion prepared in the step 1), crosslinking the chitosan quaternary ammonium salt and sodium glycerophosphate contained in the drug-containing emulsion to obtain gel microsphere suspension, heating the suspension and adding the crosslinking agent to carry out secondary crosslinking to solidify the gel microspheres. The drug carrier has the advantages of uniform and controllable grain size, high embedding rate and good dispersibility and simultaneously meets the requirements of the gastric targeted drug delivery carrier.

Description

technical field [0001] The invention relates to the field of drug carrier preparation, in particular, the invention relates to a stomach-targeting drug carrier and a preparation method thereof. Background technique [0002] Chitosan is a polysaccharide composed of glucosamine and N-acetylglucosamine copolymer, which is the product of deacetylation of chitin. Chitosan can be dissolved in dilute acid solution due to the free amino group on the molecular chain, so It has a wider range of uses than chitin. As a cationic biopolymer, chitosan has bioadhesion, biocompatibility and biodegradability, and its degradation products are non-toxic, non-immunogenic and non-carcinogenic. These unique properties of chitosan Its uniqueness makes it a biomedical carrier with broad application prospects. In the literature Chitosan-cellulose composite membrane for affinity purification of biopolymers and immunoadsorption, Journal of Membrane Science, 2002, 197: 185-197. L. Yang, W. W. Hsiao, P....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36
Inventor 王连艳马光辉宋春艳
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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