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Fluorouracil medicine carrier microsphere and production thereof

A technology of drug-loaded microspheres and fluorouracil, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, and block delivery, which can solve the problems of high preparation conditions and low drug loading of microspheres, and achieve diameter distribution. Uniformity, smooth surface, and increased drug loading

Inactive Publication Date: 2005-10-12
SHANGHAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its disadvantage is that the microspheres prepared by O / O type and O / W type emulsification volatilization method have low drug loading, while the spray drying method requires higher preparation conditions.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1: Dissolve 0.4g of PLA (Mn=67,000g / mol) in 10ml of dichloromethane, and 0.02g of 10nm nano-SiO under ultrasonic oscillation 2 Evenly dispersed in PLA solution. This solution was poured into 75 ml of 1.5% gelatin aqueous solution under stirring, emulsified for 10 minutes to form an O / W emulsion, and then stirred for 4 hours to volatilize the dichloromethane to solidify the microspheres. The microspheres in the suspension obtained were collected by centrifugation, washed with double distilled water, and dried under vacuum at 37°C to obtain SiO 2 -PLA microspheres. Accurately weigh 50mg of the prepared SiO 2 -PLA microspheres were soaked in 20ml of 4g / L fluorouracil hydrochloric acid solution. One hour later, the microspheres in the suspension were centrifuged, collected, washed with double distilled water and freeze-dried. The content of fluorouracil in the microspheres was 27.54%, and the average particle size of the microspheres was 21.59μm.

Embodiment 2

[0016] The second embodiment: This embodiment is basically the same as the first embodiment, but the difference is the SiO 2 The particle size is 30nm, the content of fluorouracil in the obtained drug-loaded microspheres is 30.9%, and the average particle size is 30.42μm.

Embodiment 3

[0017] The third embodiment: This embodiment is basically the same as the first embodiment, the difference is the SiO 2 Mesoporous SiO 2 The content of fluorouracil in the obtained drug-loaded microspheres was 29.58%, and the average particle size was 40.01 μm.

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Abstract

A microsphere carrying fluoroplex is prepared through dissolving polylactic acid to dichloromethane, dispersing SiO2 in it to become suspension, filling it in the aqueous solution of gelatin while stirring to become oil-in-water O / W emulsion, stirring for volatilizing dichloromethane, solidifying microspheres, centrifugal collecting, washing with secondary distilled water, vacuum drying to obtain SiO2-PLA microspheres, immersing them in the solution of fluoroplex in hydrochloric acid, centrifugal collecting, washing with secondary distilled water and freeze drying. Its advantages are durable acting, slow releasing and targeting function.

Description

Technical field [0001] The invention relates to a fluorouracil drug-loaded microsphere and a preparation method thereof, in particular to a biodegradable polymer material-coated fluorouracil drug-loaded microsphere and a preparation method thereof. Background technique [0002] Fluorouracil is a pyrimidine anti-metabolite. The competition of enzymes mainly inhibits the formation of thymine nucleotides and the biosynthesis of DNA, thereby inhibiting tumor growth. It has a broad anti-cancer spectrum and is effective against colon cancer, rectal cancer, gastric cancer and breast cancer. It is the first choice for the treatment of solid tumors. Although fluorouracil has good curative effects, it is also toxic. It can cause serious gastrointestinal reactions and bone marrow suppression and other side effects. It also disappears from plasma quickly after intravenous injection. 1 / 2 About 10-20 minutes. In order to reduce the toxic and side effects of fluorouracil and improve the utiliza...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/513
Inventor 尹静波陈红丹罗坤曹田叶翠
Owner SHANGHAI UNIV
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