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Method for preparing oxaliplatin sustained release suppository

An oxaliplatin and sustained-release technology, applied in suppository delivery, medical preparations of non-active ingredients, pharmaceutical formulas, etc., can solve problems such as major side effects, reduce toxicity and side effects, prolong action time, and improve slow control release effect

Inactive Publication Date: 2009-09-30
WUHAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Oxaliplatin has a good therapeutic effect on various cancers, so it also brings considerable side effects

Method used

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  • Method for preparing oxaliplatin sustained release suppository
  • Method for preparing oxaliplatin sustained release suppository
  • Method for preparing oxaliplatin sustained release suppository

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] The preparation method of oxaliplatin sustained-release suppository, it comprises the steps:

[0023] 1. Preparation of Oxaliplatin Microspheres

[0024] Measure 8.33mL of 36% (mass percentage) acetic acid, dilute to 100mL to obtain a 3% (mass percentage) acetic acid solution, weigh 0.300g of oxaliplatin and dissolve it in the above acetic acid solution, and ultrasonically dissolve it to obtain 3.00 3% (mass percentage) oxaliplatin acetate solution in mg / mL. Accurately measure 10 mL of oxaliplatin acetic acid solution, weigh 0.3 g of chitosan and dissolve it in the above solution, and ultrasonically dissolve it. Get a beaker, add 30mL liquid paraffin to it, stir on a magnetic stirrer, and add about 2.4ml of Span-80 while stirring, and then add the above-mentioned oxaliplatin acetate solution containing chitosan after mixing evenly. After emulsification for 1.5 h, 0.5 ml of glutaraldehyde was added, and the pH value was adjusted to 9 with 20% (g / mL) ammonia water. 1.5...

Embodiment 2

[0050] The preparation method of oxaliplatin sustained-release suppository, it comprises the steps:

[0051] 1. Preparation of Oxaliplatin Microspheres

[0052]Measure 5.56 mL of 36% (mass percentage) acetic acid, dilute to 100 mL to obtain a 2% (mass percentage) acetic acid solution, weigh 0.200 g of oxaliplatin and dissolve it in the above acetic acid solution, and ultrasonically dissolve it to obtain 2.00 mg / mL 2% (mass percentage) oxaliplatin acetate solution. Accurately measure 10 mL of oxaliplatin acetic acid solution, weigh 0.1 g of chitosan and dissolve it in the above solution, and ultrasonically dissolve it. Take a beaker, add 20mL of liquid paraffin to it, stir on a magnetic stirrer, and add about 1.6ml of Span-80 while stirring, and then add the above-mentioned oxaliplatin acetate solution containing chitosan after mixing evenly. After emulsification for 1.0 h, 0.3 ml of glutaraldehyde was added, and the pH value was adjusted to 10 with 20% (g / mL) ammonia water. ...

Embodiment 3

[0056] 1. Preparation of Oxaliplatin Microspheres

[0057] Measure 13.89 mL of 36% (mass percentage) acetic acid, dilute it to 100 mL to obtain a 5% (mass percentage) acetic acid solution, weigh 0.500 g of oxaliplatin and dissolve it in the above acetic acid solution, and ultrasonically dissolve it to obtain 5.00 mg / mL 5% (mass percentage) oxaliplatin acetate solution. Accurately measure 10 mL of oxaliplatin acetic acid solution, weigh 0.5 g of chitosan and dissolve it in the above solution, and ultrasonically dissolve it. Take a beaker, add 40mL of liquid paraffin to it, stir on a magnetic stirrer, and add about 3ml of Tween-80 while stirring, after mixing evenly, add the above-mentioned oxaliplatin acetate solution containing chitosan, and emulsify After 2 hours, 0.5 ml of glutaraldehyde was added, and the pH value was adjusted to 9.5 with 0.5 mol / L NaOH. 2.0 h after the start of crosslinking, the stirring was stopped. At this time, the microspheres have been formed, the ...

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Abstract

The invention discloses a method for preparing an oxaliplatin sustained release suppository, which comprises the following steps of: using an acetic acid solution with a mass concentration of between 0.5 and 5 percent to prepare an oxaliplatin solution with a concentration of between 0.5 and 5 mg / mL, taking chitosan, using an oxaliplatin acetic acid solution to dissolve the chitosan, adding span-80 or tween-80 and liquid paraffin, stirring and emulsifying the mixture, adding glutaric dialdehyde into the emulsified mixture, adding NaOH or ammonia water to adjust to ensure that the pH value is more than or equal to 9, stirring the mixture, crosslinking the mixture, centrifugally separating microspheres, and drying to obtain oxaliplatin microspheres; mixing polyethyleneglycol 4000 and polyethyleneglycol 6000 according to the mass ratio of 1-7: 1, and carrying out hot melting on the mixture in water bath with constant temperature; and adding the oxaliplatin microspheres which account for 0.01 to 0.5 times of the total mass of the polyethyleneglycol 4000 and the polyethyleneglycol 6000 into the mixture after the hot melting is finished, and obtaining the oxaliplatin sustained release suppository after the model filling and cooling. The preparation method is simple, and the prepared oxaliplatin sustained release suppository has no burst effect; and the medicament has sustained release characteristics, is slowly released and has sustained release effect. The oxaliplatin sustained release suppository can well play the antitumor effect of oxaliplatin, improve the antitumor activity of the oxaliplatin, and furthest reduce the toxic side effect of the oxaliplatin at the same time.

Description

technical field [0001] The invention relates to a preparation method of a suppository containing microspheres of medicine for treating colon and rectal cancer; especially a preparation method of an oxaliplatin sustained-release suppository. Background technique [0002] According to statistics from the American Cancer Society, colorectal cancer accounts for about 10%-15% of all cancer patients and has become the second leading cause of death in the United States. About 150,000 Americans suffer from colorectal cancer every year. About 56,000 people died from the disease. [0003] Colon cancer is one of the common tumors of the digestive tract. Postoperative chemotherapy is an important step in the treatment of colon cancer. It plays an important role in prolonging the survival period and improving the quality of life of patients. Low. Finding chemotherapy drugs with good curative effect and few side effects is a clinical requirement. Because oxaliplatin has a good effect o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/02A61K31/282A61K47/44A61K47/34A61P35/00A61K47/06A61K47/10A61K47/26A61K47/36
Inventor 刘小平耿丹清吴霞
Owner WUHAN UNIV OF TECH
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