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Fluorouracil medicine carrier microsphere and production thereof

A technology of drug-loaded microspheres and fluorouracil is applied in the directions of pharmaceutical formulations, medical preparations containing active ingredients, and bulk delivery, which can solve the problems of low drug-loading capacity of microspheres and high requirements for preparation conditions, and achieve uniform diameter distribution. , the surface is smooth, the effect of drug loading is improved

Inactive Publication Date: 2007-02-14
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

[0014] Example 1: Dissolve 0.4g of PLA (Mn=67,000g / mol) in 10ml of dichloromethane, and 0.02g of 10nm nano-SiO under ultrasonic vibration 2 Uniformly dispersed in PLA solution. The solution was injected into 75ml 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 obtained suspension were collected by centrifugation, washed with twice distilled water and dried under vacuum at 37 °C to obtain SiO 2 - PLA microspheres. Accurately weigh 50 mg of the prepared SiO 2 - The PLA microspheres were soaked in 20ml of 4g / L fluorouracil hydrochloric acid solution, and after one hour, the microspheres in the suspension were centrifuged, collected, washed with twice distilled water, and freeze-dried. The content of fluorouracil in the microspheres is 27.54%, and the average particle size of the microspheres is 21.59 μm.

Embodiment 2

[0015] Embodiment 2: This embodiment is basically the same as Embodiment 1, the difference is the SiO used 2 The particle size is 30nm, the fluorouracil content in the obtained drug-loaded microspheres is 30.9%, and the average particle size is 30.42 μm.

Embodiment 3

[0016] Embodiment 3: This embodiment is basically the same as Embodiment 1, the difference is the SiO used 2 Mesoporous SiO 2 , the content of fluorouracil in the obtained drug-loaded microspheres is 29.58%, and the average particle diameter is 40.01 μm.

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PUM

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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-wrapped fluorouracil drug-loaded microsphere and a preparation method thereof. Background technique [0002] Fluorouracil is a pyrimidine anti-metabolite, which mainly inhibits the formation of thymine nucleotides and DNA biosynthesis through the competition of enzymes, thereby inhibiting tumor growth. It has a wide anti-cancer spectrum and is effective against colon cancer, rectal cancer, gastric cancer and breast cancer, and is the drug of choice for the treatment of solid tumors. Although the curative effect of fluorouracil is good, it is also highly toxic, and can cause side effects such as severe gastrointestinal reactions and bone marrow suppression, and it disappears from the plasma soon after intravenous injection. 1 / 2 About 10 to 20 minutes. In order to reduce the toxic and side effects of fluoro...

Claims

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Application Information

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