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Methylcantharidimide injection and freeze-dried powder injection for treating tumor and preparation method thereof

A methylcantharidin injection and technology of methylcantharidin, applied in the field of intravenous drip injection, can solve the problems of high drug toxicity and irritation, and achieve the goal of improving clinical symptoms, prolonging survival time, and alleviating cancer pain Effect

Inactive Publication Date: 2008-02-13
JIANGSU SIHUAN BIOENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Although ethanol is still listed among the solubilizers in the Pharmacopoeia, as a solubilizer, the injection of ethanol is more toxic (the half-lethal dose of mice LD 50 Intravenous injection is 1.973g / kg), when the concentration exceeds 10%, the muscle or subcutaneous injection is more irritating, and it is easy to penetrate the human red blood cell membrane to cause red blood cell denaturation or hemolysis (refer to the edited by the Pharmacy Teaching and Research Group of Nanjing Pharmaceutical University, "Pharmacy" , People's Medical Publishing House, 1984, p. 435)

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Example 1 : 2ml: 10mg methylcantharidin injection preparation

[0055] formula:

[0056] Methylcantharidinamine: 5g

[0057] Sodium bisulfite: 3g

[0058] Propylene glycol: 150ml

[0059] Add water for injection to: 1000ml

[0060] Take 150ml of propylene glycol, add appropriate amount of water for injection, stir and heat to 50℃~60℃, first add 3g of sodium bisulfite, then add 5g of methylcantharidinium to dissolve it, and adjust the pH value with 0.1mol / L sodium hydroxide solution to Add water for injection to 1000ml at about 7.0, add gac, stir, decarbonize, filter to clarification after passing the test, potting, sterilizing at 100°C for 30 minutes to obtain methylcantharidin injection of the present invention.

Embodiment 2

[0061] Example 2 : 2ml: 20mg methylcantharidin injection preparation

[0062] formula:

[0063] Methylcantharidin: 10g

[0064] Sodium bisulfite: 3g

[0065] Propylene glycol: 300ml

[0066] Add water for injection to: 1000ml

[0067] Take 300ml of propylene glycol, add appropriate amount of water for injection, stir and heat to 50℃~60℃, first add 3g of sodium bisulfite, then add 10g of methylcantharidinium to dissolve it, and adjust the pH value with 0.1mol / L sodium hydroxide solution to About 7.0, add water for injection to 1000ml, add gac, stir, decarbonize, filter to clarification after testing qualified, potting, 100 ℃ of sterilizing 30 minutes promptly get methylcantharidamine injection of the present invention.

Embodiment 3

[0068] Example 3 : 100ml: 20mg or 10mg methylcantharidin injection preparation

[0069] formula:

[0070] Methylcantharidin: 20g or 10g

[0071] Sodium bisulfite: 6g

[0072] Propylene glycol: 1000ml

[0073] Sodium chloride: 900g

[0074] Add water for injection to: 100000ml

[0075] According to the method similar to above-mentioned embodiment, prepare the injection that total amount is 100000ml with the above prescription, steam sterilization at 100 ℃ for 30 minutes after potting, obtain the methylcantharidamine injection of the present invention.

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PUM

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Abstract

The present invention is an intravenous infusion-typed methyl mylabris amine injection for the tumor treatment. The present invention is a new generation injection preparation for tumor treatment, which has very good therapy function in antitumor and leukocyte rising. The injection preparation comprises the injection liquid and the freezing dry powder preparation. The propanediol or one kind or a plurality of kinds of the propanediol with the ethanol, the glycerol and the polyethylene glycol are taken as the solubilizer. The double solvents composed by the water and the injection are taken as the solvent in order to enhance solubility and stability of the solute. The methyl mylabris amine injection of the present invention can be prepared in conventional method. The injection preparation of The present invention is wide spectrum antineoplastic agents, which is applicable for treatment of a plurality of tumor comprising primary liver cancer, lung cancer, esophagus cancer, nasopharynx cancer, malignant lymphoma, bladder cancer, malignant tumor. The present invention is also applicable for hepatitis, liver cirrhosis and HBV carriers.

Description

technical field [0001] The invention relates to a methylcantharidin injection, especially an intravenous drip injection of methylcantharidin. The injection is a new generation of tumor-treating drug that has good therapeutic effects in both anticancer and whitening. Injection, the injection may be injection or freeze-dried powder preparation. Background technique [0002] Methyleantharidinimide is a derivative of cantharidin, which has a great effect on both anti-cancer and whitening, and has a direct killing and inhibiting effect on cancer cells; it stimulates the bone marrow hematopoietic system, and increases blood leukocytes. . [0003] More than 2,000 years ago, Chinese medicine in my country began to use mylabris to treat tumors. The medicine is pungent and cold in nature, poisonous, can attack toxins and erode sores, break blood and dissipate stagnation, and is a traditional Chinese medicine with obvious effects. However, the side effects are very serious. After ta...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61K9/08A61K9/19A61K47/10A61P35/00A61P1/16
Inventor 濮毅华孙国建任丽源张品芳尤正一江永红徐益明俞锋
Owner JIANGSU SIHUAN BIOENG
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