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A kind of preparation method of ibuprofen colon-targeted slow-release microspheres

A slow-release microsphere and colon-targeting technology, which is applied to non-active ingredient medical preparations, active ingredient-containing medical preparations, microcapsules, etc., can solve the problem that the microsphere structure is not dense enough and colon-targeted drug delivery is not possible and other issues, to achieve good biocompatibility and degradability, improve drug efficacy, and reduce production costs

Active Publication Date: 2020-09-22
HUAZHONG AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there have been literature reports on ibuprofen sustained-release microspheres, but sodium alginate, gelatin, chitosan, etc. are mostly used as capsule materials, and microspheres are prepared by water-in-oil emulsion-solvent evaporation method, ion cross-linking method, etc. , most of the prepared microspheres have a single-layer membrane structure, the microsphere structure is not dense enough, it is easy to release in the stomach, and cannot be colon-targeted drug delivery

Method used

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  • A kind of preparation method of ibuprofen colon-targeted slow-release microspheres
  • A kind of preparation method of ibuprofen colon-targeted slow-release microspheres
  • A kind of preparation method of ibuprofen colon-targeted slow-release microspheres

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Embodiment 1

[0031] The preparation method of ibuprofen colon-targeted slow-release microspheres, the steps are as follows:

[0032] (1) Dissolve chitosan in 1% (v / v) acetic acid solution, adjust pH to 3.5, then add ibuprofen, vortex and ultrasonic, disperse evenly, prepare chitosan concentration as 30mg / mL, The ibuprofen concentration was 50 mg / mL in the inner mixed phase.

[0033] (2) Dissolve carboxymethyl konjac glucomannan and sodium tripolyphosphate in water to prepare an external mixture with carboxymethyl konjac glucomannan concentration of 7.5 mg / mL and sodium tripolyphosphate concentration of 2.5 mg / mL Mutually.

[0034] (3) Under magnetic stirring (500-600r / min), add the inner water phase to the outer water phase drop by drop with a syringe, the volume ratio of the inner mixed phase to the outer mixed phase is 1:10, continue to stir and solidify for 15 minutes, The precipitate was washed three times with deionized water, and then freeze-dried for 2 hours to obtain ibuprofen dr...

Embodiment 2

[0041] (1) Dissolve chitosan in an acetic acid solution with a pH of 4.5, then add ibuprofen, vortex and ultrasonically disperse evenly, and prepare chitosan with a concentration of 20 mg / mL and ibuprofen with a concentration of 75 mg / mL internal mixed phase.

[0042] (2) Sodium alginate and sodium tripolyphosphate were dissolved in water respectively to prepare an external mixed phase with a sodium alginate concentration of 12.5 mg / mL and a sodium tripolyphosphate concentration of 5 mg / mL.

[0043] (3) Under magnetic stirring, use a syringe to add the inner water phase to the outer water phase drop by drop, the volume ratio of the inner mixed phase to the outer mixed phase is 1:8, continue to stir and solidify for 30 minutes, and then use deionized water to dissolve the precipitate Washed three times, and then freeze-dried for 3 hours to obtain ibuprofen drug-loaded microspheres.

[0044] The drug encapsulation efficiency of the drug-loaded microspheres was 64.24%, and the d...

Embodiment 3

[0048] (1) Dissolve chitosan in an acetic acid solution with a pH of 5.5, then add ibuprofen, vortex and ultrasonically disperse evenly, and prepare chitosan with a concentration of 45 mg / mL and ibuprofen with a concentration of 125 mg / mL internal mixed phase.

[0049] (2) Dissolving chondroitin sulfate and sodium tripolyphosphate in water respectively to prepare an external mixed phase with a concentration of chondroitin sulfate of 5 mg / mL and a concentration of sodium tripolyphosphate of 10 mg / mL.

[0050] (3) Under magnetic stirring, use a syringe to add the inner mixed phase to the outer mixed phase drop by drop, the volume ratio of the inner mixed phase to the outer mixed phase is 1:20, continue to stir and solidify for 15 minutes, and then use deionized water to dissolve the precipitate Washed 3 times, and then freeze-dried for 2 hours to obtain ibuprofen drug-loaded microspheres.

[0051] The drug encapsulation efficiency of the drug-loaded microspheres was 53.12%, and...

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Abstract

The invention discloses a preparation method for a colon-targeted slow-release Ibuprofen microsphere. By adopting a polyelectrolyte complexation-ionic crosslinking combined technique, chitosan and water-soluble polysaccharide with anions on the surface are formed into a double-layered composite film with a dense structure, an insoluble drug, i.e. Ibuprofen, is wrapped in the core of the microsphere, moreover, an acid-resistant material is also adopted to coat the microsphere, consequently, the release of the drug in the gastrointestinal tract is reduced, and the colon-targeted delivery of Ibuprofen is realized. According to the method, not only is the side effect of Ibuprofen in the gastrointestinal tract effectively reduced, but also the half-life of the drug in the body is prolonged, sothat the drug can more sufficiently exert effect. The method further has the advantages of simple preparation process, mild condition, environment-friendliness, high drug safety and the like.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a preparation method of ibuprofen colon-targeting slow-release microspheres. Background technique [0002] Oral administration is the most important way to administer drugs. It has the advantages of easy administration, high flexibility, and good compliance, but there are also some defects, such as the first-pass effect that reduces the bioavailability of drugs. For proteins and peptides Drugs like these are not effectively utilized because they are easily degraded in the stomach and small intestine. [0003] The Oral Colon Targeted Drug Delivery System (OCDDS) uses certain pharmacy methods to prevent the drug from being released at the upper end of the gastrointestinal tract after oral administration, and only begins to disintegrate or erode to release the drug at the colon, which can not only increase the drug in the target The concentration to the site can exert local or s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K47/36A61K47/32A61K31/192A61P29/00
CPCA61K9/5026A61K9/5036A61K31/192A61P29/00
Inventor 王运陈娜胡珊方秋杰叶小舟
Owner HUAZHONG AGRI UNIV
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