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Hydroxy camptothecin emulsion and its preparation method

A technology of hydroxycamptothecin and emulsion, applied in the field of medicine, can solve the problems of reduced activity, low water solubility, increased side reactions, etc., and achieves the effects of easy productization, changing distribution, and improving curative effect

Inactive Publication Date: 2004-05-05
曹永强 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its water solubility is small, and the process of dissolving in the lye to form sodium salt will cause the cracking of the E ring of hydroxycamptothecin, thereby reducing the activity and increasing the side reaction.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] As shown in the first column of Table 1, weigh 0.05 grams of hydroxycamptothecin (being 0.005% of the total weight of the emulsion) according to the weight percentage of the emulsion, add 1.0 grams (1%) of polyethylene glycol, add an appropriate amount of ethanol, and ultrasonically dissolve , made into a drug-containing solution.

[0075] Weigh 10 grams (10%) of soybean oil and MCT, 0.6 grams (0.6%) of soybean lecithin, and 0.4 grams (0.4%) of cholesterol to form an oil phase.

[0076] The drug-containing solution is added into the oil phase, the phospholipid is dissolved by ultrasonic waves, and the drug is dispersed in the oil phase. The organic solvent was removed by rotary evaporation under reduced pressure.

[0077] Weigh 2.5 grams (2.5%) of glycerin, 4 grams (4%) of PVP, add water for injection to 100g

[0078] The water phase and the oil phase are mixed to form colostrum, which is ultrasonically emulsified according to the routine of the preparation to form an...

Embodiment 2

[0082] As shown in the second column of Table 1, weigh 0.05 grams of hydroxycamptothecin by weight percentage, add 2 grams of soybean oil, 4 grams of MCT, 1.2 grams of soybean lecithin, and 3 grams of cholesterol, heat and melt, and control the temperature at 80 ° C to form oil Mutually.

[0083] Weigh 2.5 grams of glycerin and add water for injection to 100 grams.

[0084] The water phase and the oil phase are mixed to form colostrum, which is pulverized by ultrasonic waves or a homogenizer to form an emulsion.

Embodiment 3

[0086] As shown in the third column of Table 1, take hydroxycamptothecin 0.05g by weight percentage, add polyethylene glycol 6g, soybean oil 2.5g, MCT 2.5g, soybean lecithin 1.2g, cholesterol 4g, grind, make the main drug dispersed in the oil phase.

[0087] Weigh 2.2g of glycerin and add water for injection to 100g.

[0088] The water phase and the oil phase are mixed to form colostrum, which is pulverized by ultrasonic waves or a homogenizer to form an emulsion.

[0089] Method of use: the emulsions of the second and third examples are diluted to 500 ml with 5% glucose or 0.9% sodium chloride and injected intravenously with 10 mg / d for 5 consecutive days as a course of treatment.

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Abstract

A hydroxycamptothecin emulsion is prepared from hydroxycamptothecin 0.01-2.2 %, emulsifier 0.3-8%, triglyceride 2-30%, glycerine for injection 2.0-3.0 % and water for injection through dissolving the 10-hydroxycamptothecin in the oil phase containing triglyceride and emulsifier, adding water phase, mixing, and ultrasonic or homogeneous emulsifying. Its advantages are high curative effect and stability, and good target to tissue.

Description

technical field [0001] The invention relates to an emulsion and a preparation method thereof, in particular to a hydroxycamptothecin emulsion and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Studies have found that 10-hydroxycamptothecin (10-HCPT) isolated from camptothecin is the most active compound among all natural or synthetic camptothecin analogs. [0003] Since HCPT can selectively inhibit the activity of DNA topoisomerase I, interfere with the DNA cleavage link reaction catalyzed by topoisomerase, stabilize the complex of the enzyme and the DNA chain scission, and inhibit the rejoining at the nick, so it has the potential to cause DNA chain scission. , interfere with DNA replication, and have anti-tumor effects. In medicine, HCPT, as a cell cycle-specific drug, mainly acts on the S 2 -M boundary also has a delaying effect, and the effective rate for primary liver cancer is 56.2%, the effective rate for he...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/475A61P35/00
Inventor 曹永强熊俊袁建华
Owner 曹永强
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