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Method for preparing capsaicin-loaded pH sensitive gel microsphere, and gel microsphere prepared by same

The technology of gel microspheres and capsaicin is applied in the field of preparation of pH-sensitive gel microspheres, and achieves the effects of being convenient for large-scale industrial production, reducing irritation, simple and feasible formula and method

Active Publication Date: 2014-09-17
JIANGSU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no research report on the preparation of pH-sensitive carboxymethyl chitosan-sodium alginate gel microspheres using capsaicin as a raw material to improve the bioavailability of capsaicin and reduce irritation.

Method used

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  • Method for preparing capsaicin-loaded pH sensitive gel microsphere, and gel microsphere prepared by same
  • Method for preparing capsaicin-loaded pH sensitive gel microsphere, and gel microsphere prepared by same
  • Method for preparing capsaicin-loaded pH sensitive gel microsphere, and gel microsphere prepared by same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1, pH-sensitive gel microsphere loaded with capsaicin

[0029] (1) Accurately weigh 60mg of capsaicin, add 4mL mass percentage concentration of 3% sodium alginate and 2mL mass percentage concentration of 3% carboxymethyl chitosan mixed solution, at 60 ° C Make the capsaicin melt into the oil phase, vortex and homogenize to obtain the mixed liquid;

[0030] (2) The liquid is dripped into the CaCl with a mass percentage concentration of 3% by a constant flow pump at a certain speed 2 In the solution, at (37.0±0.5)°C, after magnetically stirring at a speed of 400rpm for 30min, the microspheres were collected, washed with distilled water several times, and vacuum-dried to constant weight to obtain the pH-sensitive gel microspheres loaded with capsaicin. ball.

Embodiment 2

[0031] Embodiment 2, pH sensitive gel microsphere loaded with capsaicin

[0032] (1) Accurately weigh 120mg of capsaicin, join 36mL mass percentage concentration as 1% sodium alginate and 6mL mass percentage concentration as the mixed solution of 3% carboxymethyl chitosan, at 60 ℃ Make the capsaicin melt into the oil phase, vortex and homogenize to obtain the mixed liquid;

[0033] (2) The liquid is dripped into the CaCl with a mass percentage concentration of 1% by a constant flow pump at a certain speed 2 In the solution, at (37.0±0.5)°C, after magnetically stirring at a speed of 400rpm for 30min, the microspheres were collected, washed with distilled water several times, and vacuum-dried to constant weight to obtain the pH-sensitive gel microspheres loaded with capsaicin. ball.

Embodiment 3

[0034] Example 3, pH-sensitive gel microspheres loaded with capsaicin

[0035] (1) Accurately weigh 60 mg of capsaicin, add 6 mL of 5% sodium alginate and 6 mL of 3% carboxymethyl chitosan in mass percent concentration, at 60 ° C Capsaicin is melted into an oil phase, vortexed and homogenized to obtain a mixed liquid,

[0036] (2) Make the liquid drip into CaCl with a mass percentage concentration of 10% at a certain speed through a constant flow pump 2 In the solution, at (37.0±0.5)°C, after magnetically stirring at a speed of 400rpm for 30min, the microspheres were collected, washed with distilled water several times, and vacuum-dried to constant weight to obtain the pH-sensitive gel microspheres loaded with capsaicin. ball.

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Abstract

The invention discloses a method preparing a capsaicin-loaded pH sensitive gel microsphere, and the gel microsphere prepared by the same. According to the method, the capsaicin-loaded pH sensitive gel microsphere is prepared by regulating the proportion and concentrations of capsaicin taken as a raw material medicine and carboxymethyl chitosan and sodium alginate with excellent biodegradability, biocompatibility and low toxicity as a carrier material. According to the gel microsphere, the drug loading capacity can be (18.06+ / -0.26) percent, the encapsulation efficiency is (97+ / -3.66) percent, the release of the gel microsphere in a medium with the pH value of 7.8 is remarkably superior to those in environments with pH values of 1.2, pH 4.8 and pH 6.8, and the gel microsphere has remarkable pH sensitivity and potential colonic targeting trend. Furthermore, after the gel microsphere is administrated in an oral manner, drugs can be multiply transferred step by step to the optimal absorption part along with changes of the pH value of gastrointestinal tracts, and certain characteristics of delayed release and sustained release can be reflected, so that in-vivo absorption of capsaicin can be improved, the bioavailability can be improved, and irritation of the capsaicin to gastric mucosa can be reduced.

Description

technical field [0001] The invention relates to the field of capsaicin pharmaceutical preparations, in particular to a preparation method of pH-sensitive gel microspheres loaded with capsaicin. Background technique [0002] Capsaicin (capsaicin), the molecular formula is C 18 h 27 NO 3 , the chemical name is trans-8-methyl-N-vanillyl-6-nonenylamide, which is the main capsicum element extracted and isolated from capsicum, which has a strong spicy taste and stimulation. The melting point is 55-61°C, sublimation occurs at 115°C, and the boiling point is 210-220°C. Capsaicin is easily soluble in ethanol, ether, benzene, acetone, dioxane, toluene and other organic solvents and dilute alkali solutions, slightly soluble in hot water and carbon disulfide, and easily precipitated in cold water, and prone to crystallization in petroleum ether , forming monoclinic rectangular flaky colorless crystals. [0003] Capsaicin has a wide range of pharmacological effects and has shown gre...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/165A61K47/36
Inventor 余江南孙超男朱源徐希明童珊珊
Owner JIANGSU UNIV
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