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Chitosan microsphere simultaneously containing 5-fluorouracil and oleanolic acid derivative and preparation method of chitosan microsphere

A technology of chitosan microspheres and oleanolic acid, which is applied in the field of medicine, can solve problems such as drug combination and synergistic effects that have not been considered, and achieve increased passive targeting performance, good encapsulation efficiency, and improved bioavailability Effect

Active Publication Date: 2015-06-03
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of the existing technologies only study the preparation of 5-fluorouracil into a suitable dosage form, without considering the combination and synergistic effects of drugs

Method used

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  • Chitosan microsphere simultaneously containing 5-fluorouracil and oleanolic acid derivative and preparation method of chitosan microsphere
  • Chitosan microsphere simultaneously containing 5-fluorouracil and oleanolic acid derivative and preparation method of chitosan microsphere
  • Chitosan microsphere simultaneously containing 5-fluorouracil and oleanolic acid derivative and preparation method of chitosan microsphere

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 Preparation of oleanolic acid succinate monoester (butylene oleate)

[0019] Add 1.14g (2.5mmol) of oleanolic acid and 1.25g (12.5mmol) of succinic anhydride into a three-necked flask, dissolve completely in toluene, and then add 1.53g (12.5mmol) of DMAP. Keep warm at 65°C, stir and react for 3 hours, expand the silica gel plate to detect the disappearance of raw material points (mobile phase: ethyl acetate:petroleum ether=3:1), stop the reaction. After the solvent was evaporated, ethyl acetate was dissolved, washed with hydrochloric acid solution at pH 1, and then washed with distilled water until neutral, and the ethyl acetate layer was spin-dried to obtain a white powder product with a yield of 95.0%.

Embodiment 2

[0020] Example 2 Optimization of the preparation process conditions of chitosan microspheres

[0021] Method: Dissolve chitosan in 1% (v / v) acetic acid solution to obtain chitosan acetic acid solution; dissolve butyl ester in ethanol to obtain 0.5% (m / m) butyl ester concentration Solution A; 5-fluorouracil was dissolved in distilled water to obtain solution B with a concentration of 5-fluorouracil (5-Fu) of 200 mg / ml; under rapid stirring conditions, solution A and solution B were added to chitosan acetate in proportion In the solution, stir and emulsify to obtain solution C; dropwise add sodium tripolyphosphate (TPP) solution, the volume ratio of sodium tripolyphosphate solution to solution C is 1:100, after the dropwise addition, continue to stir for 30 minutes to obtain the target Microspheres. G-50 gel chromatography: the encapsulation efficiency of 5-fluorouracil.

[0022] (1) The influence of chitosan concentration

[0023] The mass ratio of butyl butyl ester to chito...

Embodiment 3

[0052] Example 3 Chitosan Microspheres Containing 5-Fluorouracil and Zibutyl Ester

[0053] (1) Preparation method

[0054] Chitosan is dissolved in the acetic acid solution of 1.0% (v / v), obtains the chitosan acetic acid solution that concentration is 2.00% (m / m); Dissolves butyl ester in ethanol, obtains the concentration of butyl ester of 0.5% (m / m) solution A; 5-fluorouracil was dissolved in distilled water to obtain solution B with a 5-fluorouracil concentration of 200 mg / ml; in proportion, the mass ratio of SOA to chitosan was 1:20, 5- The mass ratio of fluorouracil to chitosan is 1:10. Take solution A and solution B. Under rapid stirring conditions, add solution A and solution B to chitosan acetic acid solution, and stir and emulsify for 30 minutes to obtain solution C; 0.20% sodium tripolyphosphate (TPP) solution, the volume ratio of sodium tripolyphosphate solution to solution C is 1:50, after the dropwise addition, continue to stir for 30 minutes to obtain the targe...

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Abstract

The invention discloses a chitosan microsphere simultaneously containing 5-fluorouracil and an oleanolic acid derivative and a preparation method of the chitosan microsphere. The preparation method comprises the following steps: firstly adopting an ionic crosslinking method to prepare a chitosan microsphere simultaneously coating 5-fluorouracil and succinyl oleanolate, wherein the obtained microsphere is round in form, smooth in surface and uniform in particle size; the encapsulation efficiency of 5-fluorouracil is 52.23+ / -1.76%; the average particle size is 563+ / -101 nm. The preparation method disclosed by the invention is stable and reliable in process; the obtained chitosan microsphere is good in slow release effect and meanwhile can play the synergetic anti-tumor function of 5-fluorouracil and the oleanolic acid derivative.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to chitosan microspheres containing 5-fluorouracil and oleanolic acid derivatives and a preparation method thereof. Background technique [0002] Cancer is one of the diseases with the highest morbidity and mortality in my country, which seriously threatens people's health. Currently, the treatment methods for cancer are mainly limited to three methods: surgery, radiation therapy and chemotherapy. Tumor chemotherapy plays an important role in the treatment of tumors due to its wide applicability and relatively low toxicity and side effects. 5-fluorouracil (5-fluorouracil, 5-FU) is an important anti-metabolite anti-tumor drug commonly used in clinic, which is widely used in the treatment of digestive tract cancer, breast cancer and various solid tumors. Studies have shown that the half-life of 5-fluorouracil (5-FU) in the body is about 10-20 minutes, the oral absorption is irregul...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61K9/16A61K47/36A61P35/00A61K31/513
Inventor 郝爱军孙乐郭兴家赵世钰佟健张龙杰
Owner LIAONING UNIVERSITY
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