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Injectio natarii norcantharidatis freeze-dried powder for injection and preparing method thereof

A technology of sodium demethylcantharidinate and sodium cantharidinate, which is applied in the field of medicine, can solve problems such as irrationality of freeze-drying curves, difficult removal of water, and shortened storage period, so as to ensure drug safety, good shape and appearance, and improve The effect of product quality

Active Publication Date: 2008-07-30
SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, sodium norcantharidinate is relatively unstable under the acid-base condition, and the moisture is difficult to remove in the drying process after preparing the aqueous solution, and the method provided by the present invention still does not solve this problem. A temperature of 70°C, which will accelerate the decomposition of sodium norcantharidate
Moreover, the freeze-drying procedure is too simple to effectively remove excess water from the product, which affects the effect of the drug.
[0010] In summary, the sodium norcantharidate freeze-dried powder provided by the prior art does not overcome the defects caused by the instability of its raw material itself, and tests have proved that the freeze-dried powder made by its freeze-drying process has a higher water content, making Its shelf life is greatly shortened, limiting the long-term storage of drugs
This defect may be caused by the irrationality of the freeze-drying curve. For example, if the cooling rate in the pre-freezing stage is too fast, the drug particles will be too fine and dense, which will hinder the rise of water vapor in the sublimation stage and cause the sample to collapse.
However, the physical and chemical properties of the drug itself determine the suitable cooling speed of different drugs. In order to find a suitable freeze-drying process for sodium norcantharidate, a lot of experimental work is still needed.

Method used

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  • Injectio natarii norcantharidatis freeze-dried powder for injection and preparing method thereof
  • Injectio natarii norcantharidatis freeze-dried powder for injection and preparing method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0040] Add 5 g of sodium hydroxide to 1500 ml of water for injection to prepare a solution, add 10 g of norcantharidin and 100 g of mannitol, stir to dissolve, adjust the pH to 9.1 to 9.5 with hydrochloric acid or sodium hydroxide, add water for injection until the volume of the solution is 2000 ml, and add to the Add 0.01% medical activated carbon to the prepared solution, stir at room temperature for 20 minutes, filter to remove carbon, and then fine filter the filtrate through a 0.22 μm microporous filter membrane. 57°C, the cooling rate is 17°C / min, heat preservation and freezing for 3 hours, vacuumize the pre-frozen medicinal solution to 10Pa, then slowly and uniformly heat up to 0°C at a speed of 3.2°C / hour, and keep warm for 3 hours, sublimation The finished drug is heated to 25°C at a uniform speed, the heating time is 4 hours, and then heat-preserved and dried for 5 hours, tested, pressed and packed, and packed into the warehouse.

Embodiment 2

[0042] Add 5 g of sodium hydroxide to 1500 ml of water for injection to prepare a solution, add 10 g of norcantharidin and 100 g of mannitol, stir to dissolve, adjust the pH to 9.3 with hydrochloric acid or potassium hydroxide, add water for injection until the volume of the solution is 2000 ml, and add to the prepared solution Add 0.01% medical activated carbon, stir at room temperature for 20 minutes, filter to remove carbon, and then filter the filtrate through a 0.22μm microporous filter membrane. After the fine filter filtrate is tested and qualified, it will be subpackaged, and the subpackaged drug solution will be quickly cooled to -60°C , the cooling rate is 25°C / min, heat preservation and freezing for 3 hours, vacuumize the pre-frozen medicinal solution to 15Pa, then slowly and uniformly heat up to -5°C at a speed of 3°C / hour, and keep warm for 5 hours, and the sublimation is completed The drug is heated to 20°C at a uniform speed, the heating time is 5 hours, and then...

Embodiment 3

[0044] Add 5g of sodium hydroxide to 1500ml of water for injection to prepare a solution, add 10g of norcantharidin and 100g of mannitol, stir to dissolve, adjust the pH to 9.5 with hydrochloric acid or sodium hydroxide, add water for injection until the volume of the solution is 2000ml, add to the prepared solution Add 0.01% medical activated carbon to the solution, stir at room temperature for 20 minutes, filter to remove carbon, and then filter the filtrate through a 0.22μm microporous membrane. After the fine filter filtrate passes the test, it will be subpackaged, and the subpackaged drug solution will be quickly cooled to -55°C. , the cooling rate is 15°C / min, heat preservation and freezing for 3 hours, vacuumize the pre-frozen medicinal solution to 5Pa, then slowly and uniformly heat up to 5°C at a speed of 3.5°C / hour, keep warm for 2 hours, and sublimate the liquid The medicine is heated to 30°C at a uniform speed, and the heating time is 3 hours, and then it is kept wa...

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Abstract

The invention relates to a freeze-dried powder of sodium norcantharidin for injection and a preparation method for the freeze-dried powder: adding the norcantharidin and mannitol into well prepared sodium hydroxide solutions and adjusting the ph; adding activated carbon and removing colors, filtering and removing the carbon and finely filtering through a 0.22Mu m filtering film and making loading separately; cooling the separately loaded medical solution rapidly to minus 60 to minus 55 DEG C with the speed of 15 to 25 DEG C per minute; preserving heat and freezing for 3 hours and pumping the vacuum of 5 to 15 Pa; heating slowly and uniformly to minus 5 to 5 DEG C with the speed of 3 to 3.5 DEG C per hour and preserving the heat for 2 to 5 hours and then heating with a uniform speed to 20 to 30 DEG C with 3 to 6 heating hours; preserving heat and drying for 5 hours and detecting, pressing a whole cover and packaging and warehousing. The freeze-dried powder obtained by the method is high in purity, beautiful in appearance and low in water content and the proportion of the nor cantharidin, the sodium hydroxide and the mannitol is provided as 2 to 1 to 20.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a drug for treating tumors and a preparation method thereof, more specifically to a freeze-dried sodium norcantharidate powder for injection and a preparation method thereof. Background technique [0002] Cantharidin is an anti-tumor active ingredient extracted from the traditional Chinese medicine Mylabris. It was tried for primary liver cancer in the 1970s, but its application was limited due to its strong stimulating effect on the urinary system. Sodium norcantharidinate is a derivative of cantharidin, which is a sodium salt formed by removing two methyl groups of cantharidin and hydrolyzing it. [0003] [0004] Cantharidin Norcantharidin Sodium norcantharidinate [0005] Sodium demethylcantharidinate, as an antineoplastic drug, has significant curative effect, less toxic and side effects and has certain characteristics of promoting bone marrow cells. Compared with current...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/365A61K47/10A61K47/02A61P35/00
Inventor 刘保起李明华陈雨
Owner SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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