Medicine containing active components of methylcantharidimide and its preparing method and use

A technology containing cantharidin methyl and cantharidin methyl, which is used in pharmaceutical applications, a new medicinal dosage form containing cantharidin methyl active ingredients and the field of preparation thereof, can solve the problem of restricting the application of cantharidin methyl and being unable to manufacture It can avoid the first-pass effect of the liver, prolong the survival time, and inhibit the DNA synthesis of cancer cells.

Inactive Publication Date: 2005-10-12
CHANGZHOU FANGYUAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But because the nature of methylcantharidin is slightly soluble in water, conventional methods can not be made into injections with water as a solvent. So far, only methylcantharidin tablets (oral solid preparation) have been placed on the market, which limits methylcantharidin Amine application

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] 2ml: 20mg methylcantharidin injection preparation.

[0049] prescription:

[0050] Methylcantharidin 20.0g

[0051] 95% ethanol 100ml

[0052] Sodium sulfite 2g

[0053] Activated carbon 1g

[0054] Add water for injection to 2000ml

[0055] Make 1000 sticks (2ml: 20mg)

[0056] Add the prescribed amount of methylcantharidamine into about 1500ml of water for injection, add ethanol and sodium sulfite, stir to dissolve, add water to the full amount, heat to 80°C, add activated carbon, stir and absorb for 15 minutes, decarbonize, filter through a 0.22μm membrane, potting, Sterilize at 100°C for 30 minutes.

Embodiment 2

[0058] 100ml: 20mg Methylcantharidin Sodium Chloride Injection is prepared.

[0059] prescription:

[0060] Methylcantharidin 20.0g

[0061] 95% ethanol 200ml

[0062] Sodium sulfite 4g

[0063] Sodium chloride 900g

[0064] Add water for injection to 100000ml

[0065] Make 1000 bottles (100ml: 20mg)

[0066] Add the prescribed amount of methylcantharidamine into about 80L water for injection, add ethanol, sodium sulfite, and sodium chloride, stir to dissolve, add water to the full amount, heat to 80°C, add an appropriate amount of activated carbon, stir and absorb for 15 minutes, decarbonize, 0.22μm Membrane filtration, potting, sterilizing at 121°C for 20 minutes.

Embodiment 3

[0068] 20mg of methylcantharidin lyophilized powder preparation.

[0069] prescription:

[0070] Methylcantharidin 20.0g

[0071] Hydrochloric acid amount

[0072] Sodium sulfite 2g

[0073] Sorbitol 70g

[0074] Add water for injection to 1500ml

[0075] Made 1000 pieces

[0076] Add the prescribed amount of methylcantharidamine into about 1200ml of water for injection, add hydrochloric acid, sodium sulfite and sorbitol, stir to dissolve, add water to the full amount, heat to 80°C, add an appropriate amount of activated carbon, stir and absorb for 15 minutes, decarbonize, 0.22μm membrane Filter, fill (1.5ml / bottle), freeze-dry, cap and pack.

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PUM

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Abstract

An injection containing methylcantharidimide for treating primary liver cancer and chronic viral hepatitis B is prepared through dissolving methylcantharidimide in solvent, decarbonizing, filtering, freeze drying and sterilizing.

Description

technical field [0001] The invention relates to a preparation of methylcantharidin, in particular to a new medicinal dosage form containing an active ingredient of methylcantharidin, a preparation method thereof and an application in pharmacy. Background technique [0002] Methyl cantharidinimide is a derivative of cantharidin, an effective anti-cancer ingredient isolated from mylabris. According to literature reports, cantharidin can inhibit the synthesis of cancer cell protein nucleic acid and enhance the phagocytosis of macrophages; methylcantharidin can remove HBV in the body by inhibiting the synthesis of HBV nucleic acid and enhancing the function of macrophages. Cantharidin has the functions of attacking toughness and dispelling stagnation, promoting blood circulation and removing blood stasis, can dredge the microcirculation of the liver, and has a certain protective effect on the mitochondria of liver cells, so it has a certain effect on improving liver function. B...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/365A61K47/10A61P1/16A61P31/12A61P35/00
Inventor 蒋维平
Owner CHANGZHOU FANGYUAN PHARMA
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