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N3-ortho toluene formoxyl uracil nanosuspension and lyophilized preparation thereof

A technology of benzoyluracil and nano-suspension, which is applied in the field of medicine and biology, can solve the problems of low solubility of TFu and achieve the effects of good biocompatibility, less vascular stimulation, and simple and feasible preparation process

Inactive Publication Date: 2013-07-24
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0012] For the above-mentioned prior art, the present invention provides a kind of N 3 -O-toluoyl uracil nanosuspension and its freeze-dried preparation, and its preparation method, which uses a surfactant with good physiological compatibility as a stabilizer and is prepared by a high-pressure emulsion method, which solves the problem of TFu in The problem of low solubility in water

Method used

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  • N3-ortho toluene formoxyl uracil nanosuspension and lyophilized preparation thereof
  • N3-ortho toluene formoxyl uracil nanosuspension and lyophilized preparation thereof
  • N3-ortho toluene formoxyl uracil nanosuspension and lyophilized preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042]Accurately weigh 500 mg of soybean lecithin, add it to 100 mL of double-distilled water, and disperse evenly to obtain solution A. Add 50mg TFu, ultrasonically disperse uniformly to obtain suspension B. The suspension B was sheared at a high speed of 20,000 rpm for 1 min with a high-speed shear to obtain colostrum C. Colostrum C was homogenized with a high-pressure milk homogenizer, and circulated 5 times at 200 bar, 10 times at 500 bar, and 10 times at 1000 bar to prepare a TFu nanosuspension preparation.

[0043] Take the above nanosuspension and add mannitol at a ratio of 3% (unit: g / mL), stir to dissolve, filter and sterilize, divide into vials at 2 mL / bottle, quickly put into an ultra-low temperature refrigerator, and freeze at -80°C After 24 hours, take it out and quickly place it on the shelf of a freeze dryer whose temperature has dropped to -50°C, cover with a vacuum cover, turn on the vacuum pump switch, and freeze-dry for 48 hours. After lyophilization, take...

Embodiment 2

[0047] Accurately weigh 1000 mg of soybean lecithin, add it to 100 mL of double distilled water and disperse evenly to obtain solution A. Add 100mg TFu, and ultrasonically disperse uniformly to obtain suspension B. The suspension B was sheared at a high speed of 20,000 rpm for 3 minutes with a high-speed shear to obtain colostrum C. Colostrum C was homogenized with a high-pressure milk homogenizer, and circulated 5 times at 200 bar, 10 times at 500 bar, and 10 times at 1000 bar to prepare a TFu nanosuspension preparation.

[0048] The average particle size of the prepared nanosuspension preparation is 117.9nm, such as image 3 shown.

[0049] Take the mannitol added to the above-mentioned nanosuspension in a ratio of 5% (unit: g / mL), stir and dissolve, filter and sterilize, divide into vials according to 2 mL / bottle, put it into an ultra-low temperature refrigerator quickly, and store it at -80 ° C. Freeze for 24 hours, then take it out and quickly put it on the shelf of th...

Embodiment 3

[0051] Accurately weigh 5000 mg of soybean lecithin, add it to 100 mL of double distilled water and disperse evenly to obtain solution A. Add 350mg TFu, and ultrasonically disperse uniformly to obtain suspension B. The suspension B was sheared at a high speed of 20,000 rpm for 3 minutes with a high-speed shear to obtain colostrum C. Colostrum C was homogenized with a high-pressure milk homogenizer, and circulated 5 times at 200 bar, 10 times at 500 bar, and 10 times at 1000 bar to prepare a TFu nanosuspension preparation.

[0052] The average particle size of the prepared nanosuspension preparation is 180.03nm.

[0053] Take the mannitol added to the above-mentioned nanosuspension in a ratio of 5% (unit: g / mL), stir and dissolve, filter and sterilize, divide into vials according to 2 mL / bottle, put it into an ultra-low temperature refrigerator quickly, and store it at -80 ° C. Freeze for 24 hours, then take it out and quickly put it on the shelf of the freeze dryer whose tem...

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Abstract

The invention discloses N3-ortho toluene formoxyl uracil nanosuspension and lyophilized preparation thereof, which belong to the technical field of medical drugs. The preparation method of the lyophilized preparation of the N3-ortho toluene formoxyl uracil nanosuspension comprises the steps of (1) dispersing surface active agents into water solution to obtain solution A; (2) dispersing N3-ortho toluene formoxyl uracil into the solution A to obtain injectable suspension B; (3) shearing the injectable suspension B at high speed to obtain foremilk C; (4) enabling the quality of the foremilk C tobe even through a milk evening machine to obtain the N3-ortho toluene formoxyl uracil nanosuspension; and (5) adding lyophilized protective agents into the nanosuspension, filtering and degerming, lyophilizing and drying to remove water, and obtaining the lyophilized preparation of the N3-ortho toluene formoxyl uracil nanosuspension. The nanosuspension prepared by the preparation method is uniform in appearance quality with average grain diameter of 50-200nm, high in dissolution rate and capable of being prepared into injection or oral preparation of tablets, capsules and the like in special application.

Description

technical field [0001] The present invention relates to a kind of N 3 - o-toluoyl uracil nano-suspension and its freeze-dried preparation, as well as its preparation method, belong to the field of medical biotechnology. Background technique [0002] Malignant tumor is a common and frequently-occurring disease that seriously threatens human health. The task of tumor prevention and treatment is very arduous. In recent years, with the development of tumor cell biology, molecular biology and genomics, it has provided a new direction for the research of anticancer drugs, but the research of anticancer drugs still faces severe challenges, and many anticancer drugs are in clinical application. Drug resistance develops in the process. Therefore, research on new anticancer drugs is imperative. [0003] Tofluridine (N 3 -O-toluyl-fluorouracil, TFu) that is N 3 - o-toluoyl uracil, chemical structure such as figure 1 As shown, it is a 5-fluorouracil (5-Fu) prodrug N that is being ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K9/19A61K31/513A61P35/00
Inventor 张娜张娟徐文方刘永军王丽丽
Owner SHANDONG UNIV
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