Preparation method of 5-fluorouracil-carried pH-sensitive drug-bearing microsphere

A kind of technology of fluorouracil and drug-loaded microspheres

Inactive Publication Date: 2012-07-18
ZHONGBEI UNIV
View PDF2 Cites 7 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the drug-loaded microspheres in the above method do not have pH sensit

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0010] Example 1:

[0011] In a four-necked flask, soak 0.2g of cross-linked polyvinyl alcohol microsphere CPVA in 25mL of distilled water for 4 hours, then add 2.8g of sodium p-styrene sulfonate monomer, pass N 2 30min to remove air. Add 0.1g of cerium ammonium sulfate and 0.25mL of concentrated sulfuric acid into the above four-neck flask, heat to 45℃, stir and 2 The graft polymerization reaction was carried out under protective conditions; the reaction was terminated after 6h, filtered, washed with water, and dried to obtain grafted microsphere CPVA- g -PSSS, the grafting degree is 16.1mg / g.

[0012] Dissolve 5-fluorouracil in 0.1 mol / L hydrochloric acid to prepare a concentration of 1.8 mg / mL, adjust its pH to 1, take 25 mL and place it in an Erlenmeyer flask, and add 0.05 g grafted microsphere CPVA- g -In PSSS, oscillate at 25°C for 5 hours and filter with a 0.45μm microporous filter to obtain 5-fluorouracil-loaded pH-sensitive drug-loaded microspheres. After dilution, the drug...

Example Embodiment

[0014] Example 2:

[0015] In a four-neck bottle, soak 0.2g of cross-linked polyvinyl alcohol microsphere CPVA in 25mL distillation for 4 hours, then add 4.5g of sodium p-styrene sulfonate monomer, pass N 2 30min to remove air. Add 0.13g of ceric ammonium sulfate and 0.625mL of concentrated sulfuric acid into the above four-necked flask, heat up to 55℃, stir and 2 The graft polymerization reaction was carried out under protective conditions; the reaction was terminated after 8h, filtered, washed with water, and dried to obtain grafted microsphere CPVA- g -PSSS, the grafting degree is 11.3mg / g.

[0016] Dissolve 5-fluorouracil in 0.1 mol / L hydrochloric acid, prepare a concentration of 1.0 mg / mL, adjust its pH to 8, take 25 mL and place it in an Erlenmeyer flask, add 0.05 g grafted microsphere CPVA- g -In PSSS, vibrate at 30°C for 4 hours and filter with a 0.45μm microporous membrane to obtain 5-fluorouracil-loaded pH-sensitive drug-loaded microspheres. After dilution, the drug-loadin...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
Degree of graftingaaaaaaaaaa
Degree of graftingaaaaaaaaaa
Login to view more

Abstract

The invention relates to a preparation method of a 5-fluorouracil-carried pH-sensitive drug-bearing microsphere, which is characterized in that: monomer sodium styrene sulfonate is put into a cross-linked polyvinyl alcohol microsphere after being soaked, then ceric ammonium sulfate and concentrated sulfuric acid are added to obtain a grafted microsphere CPVA-g-PSSS, 5-fluorouracil is dissolved inhydrochloric acid, and the grafted microsphere CPVA-g-PSSS prepared in the previous step is added to obtain the 5-fluorouracil-carried pH-sensitive drug-bearing microsphere. The drug-bearing microsphere has pH sensitivity, is basically not released in stomach and small intestines and is greatly released in colon. Due to adoption of the preparation method, the treatment effect of the 5-fluorouracil can be improved, the selectivity is improved, the dosage can be reduced, and the toxic side effect can be reduced.

Description

technical field [0001] The invention belongs to the technical field of drugs and polymer materials for localized treatment of colon cancer, and in particular relates to a preparation method of pH-sensitive drug-loaded microspheres loaded with 5-fluorouracil. Background technique [0002] 5-Fluorouracil is a star drug for the treatment of colon cancer, but the concentration of intravenous administration reaches the colon is low, and the toxicity and side effects are large, which is difficult for patients to tolerate. Oral colon cancer chemotherapeutic drug 5-fluorouracil has high curative effect in clinical application. The drug can be released in the colon and rectum to increase the local concentration of the drug in the lesion, reduce the dosage of the drug, and reduce systemic side effects, thereby improving the effectiveness and safety of chemotherapy. It can be treated as an outpatient, suitable for elderly cancer patients and home chemotherapy, and has become a ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K9/16A61K47/32A61K31/513A61P35/00
Inventor 门吉英高保娇王蕊欣陈建军
Owner ZHONGBEI UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap