Taxol nanoparticle composition and preparation method thereof

A nanoparticle and paclitaxel technology, which is applied in drug combinations, pharmaceutical formulas, and medical preparations containing active ingredients, can solve problems such as high cost, drug residues, and increased drug toxicity, and achieve high drug loading and good mucosal tissue High adhesion and high bioavailability

Inactive Publication Date: 2010-09-15
无锡纳生生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] (1) In the production process, dichloromethane, a highly toxic organic solvent, needs to be used. Although dichloromethane has a low boiling point and is volatile, it is inevitable that there will always be residues in the drug, which will increase the toxicity of the drug;
[0006] (2) Because dichloromethane is a carcinogen, the volatilization of dichloromethane in the production process causes environmental pollution;
[0007] (3) The production process is complicated and the cost is high

Method used

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  • Taxol nanoparticle composition and preparation method thereof
  • Taxol nanoparticle composition and preparation method thereof
  • Taxol nanoparticle composition and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0081] The purpose of this example is to prepare paclitaxel nanoparticle composition injections with various surface stabilizers.

[0082] Mix 2 g of Paclitaxel with 1.25 g of at least one of the following surface stabilizers: Taboxamer, Poloxamer 188, Tween-80, Hydroxypropylmethylcellulose, Hydroxypropylcellulose, Polyvinylpyrrolidone-K30 , Sodium Lauryl Sulfate, Macrogol 400, Sodium Deoxycholate, Lecithin.

[0083] For each combination of paclitaxel and surface stabilizer, first dissolve 1.25g of surface stabilizer in 96.75g of water for injection, then add 2g of paclitaxel, ultrasonically disperse evenly, add 50mL of zirconium beads in a ball mill, and circulate condensation at 1500rpm The water temperature was controlled at 4°C, and the mixed solution of paclitaxel and surface stabilizer was added while stirring. After degassing for 10 minutes, the speed was increased to 4000 rpm, and the wet grinding was carried out for a total of 30 minutes to obtain a milky white paclit...

Embodiment 2

[0093] The purpose of this example is to prepare paclitaxel nanoparticle composition oral formulations with various surface stabilizers

[0094] Dissolve 2 g of hydroxymethylpropyl cellulose and 1 g of poloxamer 188 in 92 g of water for injection to prepare a solution, then add 5 g of paclitaxel, and disperse the above mixture solution evenly by ultrasonic, add 50 mL of zirconium beads in a ball mill, and start at 1500 rpm Under the rotating speed, the temperature of the circulating condensed water is controlled at 4°C, and the mixed solution of paclitaxel and surface stabilizer is added while stirring. After degassing for 10 minutes, the rotating speed is increased to 4000rpm, and the wet grinding is carried out for 30 minutes to obtain a milky white paclitaxel suspension, which is then freeze-dried at low temperature to obtain White solid granules, pass through 80 mesh sieve, mix the obtained granules with appropriate amount of starch, add appropriate amount of starch slurry ...

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Abstract

The invention discloses a taxol nanoparticle composition and a preparation method thereof, belonging to the technical field of taxol preparations. The invention relates to taxol nanoparticle composition and nanosuspension, the high drug-loading taxol nanoparticle composition and nanosuspension is prepared by taking a surface stabilizer as a carrier, wherein the effective average particle size of the composition is less than 1000 nm; the suspension is subjected to freeze drying or spray drying to obtain the taxol nanoparticle preparation which can be intravenously injected or taken orally. The method of the invention is reliable, easy to operate and low in energy consumption, and avoids interference of organic solvent; meanwhile, the obtained taxol nanoparticle composition has higher bioactivity and can give full play to the curative effect of taxol.

Description

technical field [0001] The present invention relates to a method for preparing paclitaxel nanoparticles or nanosuspensions. The nanoparticle composition contains paclitaxel and preferably at least one surface stabilizer, and has an effective average particle size below 1000 nm. The present invention also includes the preparation of the nanoparticle composition. method. The invention belongs to the technical field of paclitaxel preparations. Background technique [0002] Paclitaxel (trade name Taxol) is a tetracyclic diterpenoid compound with anticancer activity extracted and isolated from Taxus genus plants, and its molecular formula is C 47 h 51 NO 14 , with a molecular weight of 853.9. On December 29, 1992, the U.S. Food and Drug Administration (FDA) approved the launch of a new drug paclitaxel (trade name Taxol), which is used for the treatment of ovarian cancer where other anticancer drugs are ineffective. In 1994, the drug was released again Approved for the treatme...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/337A61K45/00A61P35/00
Inventor 吴斌
Owner 无锡纳生生物科技有限公司
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