Methyl cantharis amine injection and its prepn. method

A methylcantharidin injection and the technology of methylcantharidin, which are applied in the field of pharmaceutical preparations, can solve the problems of affecting clinical treatment effects, large local irritation, and high risk of clinical use, so as to facilitate clinical treatment monitoring and reduce drug toxicity. Effects of side effects and cost reduction of drug raw materials

Inactive Publication Date: 2006-11-29
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the solubility of methylcantharidinamine in water is small, the bioavailability of oral drugs is low, and the individual differences in patients' use are large, which affects the clinical treatment effect
[0003] CN1679543A discloses a kind of injection preparation of methylcantharidamine, increases the dissolubility of methylcantharidin by adding ethanol, PEG, acid, the mode of alkali, thereby develops methylcantharidin injection, but contains ethanol in

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] 0.3 g of methylcantharidin and 1 g of β-cyclodextrin are ground at room temperature for 1 hour to prepare the β-cyclodextrin inclusion compound of methylcantharidin, and the obtained inclusion compound is calculated by methylcantharidin per 1 hour. Dissolve 0.3g in 5ml of water for injection, filter, fill, seal, and sterilize to obtain the injection of methylcantharidamine, and each ampoule is calculated as 0.3g / carriage of methylcantharidamine.

Embodiment 2

[0030] Dissolve 0.3 g of methylcantharidin and 5 ml of propylene glycol in 250 ml of normal saline, filter, fill, seal, and sterilize to obtain the infusion of methylcantharidin.

Embodiment 3

[0032] Methylcantharidin and Pluronic F-68 are made into Pluronic F-68 solid dispersion of methylcantharidin by melting method: methylcantharidin 0.3g and 2g Pluronic F-68 are weighed respectively , and mixed evenly at room temperature, heated to 85°C, stirred at a constant temperature of 85°C for 30 minutes, cooled to room temperature, and airflow pulverized to obtain methylcantharidamine pluronic solid dispersion powder, which can be obtained by aseptic subpackaging The powder injection can be dissolved in normal saline or glucose infusion.

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PUM

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Abstract

An injection of methyl cantharidamine is prepared from methyl cantharidamine, phosphatide, cyclodextrin, Pulangnike, polyvinyl pyrrolidone and urea. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a methylcantharidin injection preparation and a preparation method thereof. Background technique [0002] Methylcantharidimide (Methylcantharidimide) is a derivative of cantharidin, an effective anticancer ingredient isolated from the Coleoptera biliary insect Mylabris. Methylcantharidinine can inhibit the synthesis of protein and nucleic acid in cancer cells, and has inhibitory and killing effects on tumor cells. It is mainly used for the treatment of primary liver cancer, and also has good curative effects on lung cancer, esophageal cancer, colon cancer and breast cancer. In addition, methylcantharidinine has a good inhibitory effect on HBV replication, thereby improving liver function; in addition, methylcantharidinium also has the effect of increasing white blood cells and stimulating bone marrow cell DNA synthesis, which is an important role in anticancer drugs. R...

Claims

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Application Information

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IPC IPC(8): A61K31/407A61K9/08A61K9/19A61K47/40A61K47/18A61K47/10A61P35/00
Inventor 宋赟梅齐雪飞平其能庄捷
Owner CHINA PHARM UNIV
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