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Method of preparing superfie fiber formulation for carmustine

A technology of ultrafine fiber and carmustine, which is applied in fiber treatment, filament/thread forming, single-component polyester artificial filament, etc., can solve the problems of poor clinical effect and achieve stable drug release behavior and residual low volume effect

Inactive Publication Date: 2005-10-26
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these methods have various deficiencies, and the clinical effect is not good.

Method used

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  • Method of preparing superfie fiber formulation for carmustine
  • Method of preparing superfie fiber formulation for carmustine
  • Method of preparing superfie fiber formulation for carmustine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1. 0.7768g of L-polylactic acid PLLA (number average molecular weight 86400) is dissolved in the mixed solvent of 4ml chloroform and 1ml acetone, after fully dissolving, add 39mg carmustine again, stir to make it fully dissolve, form uniform mixing solution. Then the mixed solution was added to a 10ml syringe, and a right-angled flat-mouthed spinneret made of No. 8 needle was adopted. The spinning flow rate was 2ml / h, the applied voltage was 35kV, and the distance between the two poles was 24cm.

[0020] The mean diameter 500nm of gained drug-loaded fiber, carmustine content 5%, see figure 1 .

Embodiment 2

[0021] Embodiment 2. is dissolved in 5ml chloroform with the random copolymer PLGA (wherein mass composition lactide 80%, glycolide 20%, number average molecular weight 79500) of 0.9616g lactide and glycolide, after fully dissolving , then add 96mg carmustine, stir to make it fully dissolved, and form a uniform mixed solution. Then the mixed solution was electrospun, using a right-angle flat nozzle made of No. 8 needle, the spinning flow rate was 1.5ml / h, the applied voltage was 33kV, and the distance between the two poles was 18cm.

[0022] The average diameter of the obtained drug-loaded fiber is 1.8 μm, and the carmustine content is 10%, see figure 2 .

Embodiment 3

[0023] Embodiment 3. 0.6874g PLLA-PEG block copolymer (number-average molecular weight is 97600, and wherein PEG section number-average molecular weight is 5000) is dissolved in 5ml chloroform, after fully dissolving, add 0.1375g carmustine again, stir to make it Fully dissolved to form a uniform mixed solution. Then the mixed solution was electrospun, using a right-angle flat nozzle made of No. 8 needle, the spinning flow rate was 1.8ml / h, the applied voltage was 35kV, and the distance between the two poles was 24cm.

[0024] The average diameter of the obtained drug-loaded fiber is 800nm, and the content of carmustine is 20%.

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Abstract

The present invention relates to a method of preparing BCNU which has the biodegradation high polymer ultra-thin fiber form. Dissolve the BCNU into the solution of high polymer which can be biodegraded, electrospinning, so non-woven fabrics or felt of ultra-thin fiber wrapped with BCNU. The preparation is simple and cheap, the diameter of drug loading fiber can be controlled at the dimension of 0.2 - 2 ª–m, drug loading can be controlled at the range of 0.1 - 100%. The release of drug is study. It has high speed of drug releasing and can also release BCNU steadily for a long time. The fiber itself can biodegrades completely so it has little poisonous side effect. On the other hand, because BCNU is wrapped in the fiber and released slowly, so it conquers the disadvantage of short half-life, and also reduces its poisonous side effect. This trademark is suitable for part chemotherapy after the operation of tumour.

Description

technical field [0001] The invention relates to a preparation method of a biodegradable polymer ultrafine fiber dosage form of carmustine. technical background [0002] Carmustine (BCNU) is an anticancer drug commonly used in clinical practice, especially for the treatment of glioma. Its mechanism of action is generally believed to be that carmustine binds to DNA in the body and also inhibits DNA polymerase, thereby preventing DNA and RNA synthesis. it to G 1 -S transition period is the strongest, it has a blocking effect on S phase, and has a blocking effect on G 2 The long-term effect is enhanced again, and the effect on G 0 Phase also has an effect, so it is a cell cycle non-specific drug. Carmustine has high fat solubility, low plasma protein binding rate, and is relatively easy to pass through the blood-brain barrier. However, it has a low melting point (30-32°C) and a short half-life. It is easy to decompose when exposed to water and light. At present, the clini...

Claims

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Application Information

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IPC IPC(8): D01F1/10
Inventor 景遐斌徐秀玲陈学思杨立新徐效义梁奇志卢天成
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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