Topotecan liposome and preparation method therefor

A technology of topotecan and topotecan hydrochloride, which is applied in liposome delivery, pharmaceutical formula, liquid delivery, etc., can solve the problems affecting the treatment effect of topotecan, patient pain, no improvement, etc., and improve the drug therapy index , relieve pain, reduce the effect of thrombocytopenia

A technology of topotecan and topotecan hydrochloride, which is applied in liposome delivery, pharmaceutical formula, liquid delivery, etc., can solve the problems affecting the treatment effect of topotecan, patient pain, no improvement, etc., and improve the drug therapy index , relieve pain, reduce the effect of thrombocytopenia

CN101015526AInactive Publication Date: 2007-08-15JIANGSU AOSAIKANG PHARMA CO LTD
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  • Topotecan liposome and preparation method therefor
  • Topotecan liposome and preparation method therefor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Take topotecan hydrochloride and prepare 1 mg / ml topotecan hydrochloride solution with phosphate buffer. Another 2 g of hydrogenated soybean lecithin was dissolved in ethanol, slowly dripped in 50 ml of topotecan hydrochloride solution kept at 55-65° C. under stirring (the weight ratio of topotecan and soybean lecithin was 1: 40), Ethanol was evaporated, and stirring was continued for 2h to obtain topotecan liposomes.

Embodiment 2

[0026] Take topotecan hydrochloride and prepare 1 mg / ml topotecan hydrochloride solution with phosphate buffer. Put 1g of soybean lecithin and 0.3g of cholesterol into a round-bottomed flask, add 20ml of absolute ethanol, heat in a water bath at 65-70°C, stir, fully dissolve, then rotate on a rotary evaporator to form a film, remove the ethanol under reduced pressure to obtain a phospholipid film . Get 50ml of topotecan hydrochloride solution (the weight ratio of topotecan and soybean lecithin is 1: 20), pour it into the above-mentioned flask, heat and stir in a water bath at 65~70° C. Stir for 60 minutes to obtain topotecan liposomes.

Embodiment 3

[0028] Get topotecan hydrochloride, and make 2 mg / ml topotecan hydrochloride solution with phosphate buffer. Put 1g of soybean lecithin and 0.3g of cholesterol into a round-bottomed flask, add 20ml of absolute ethanol, heat in a water bath at 65-70°C, stir, fully dissolve, then rotate on a rotary evaporator to form a film, remove the ethanol under reduced pressure to obtain a phospholipid film . Get 50ml of topotecan hydrochloride solution (the weight ratio of topotecan and soybean lecithin is 1: 10), pour it into the above-mentioned flask, heat and stir in a water bath at 65~70° C. Stir for 60 minutes to obtain topotecan liposomes.

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Abstract

This invention relates to a topotecan liposome and its preparation method. The preparation can be used as therapeutic drug of multiple tumours such as non-small cell lung cancer, liver cancer, stomach cancer, hematopathy, and lymphomata. The topotecan liposome is characterised in containing topotecan and at least one biologic receivable phospholipid at a weight ratio of 1:0.5. The phospholipid is selected from one of natural phospholipid, hydrogenated soybean phosphatide, and synthesized phospholipid. The liposome can also contain cholesterol and supported reagent. The supported reagent is selected from one of glucose, mannit, sucrose, sorbitol, dextran, lactose, and trehalose. The weight ratio of phospholipid and supported agent is 1:0.01-500. The preparation method comprise film dispersion, injection, ultrasonic dispersion, lyophilization, freeze thawing, forceful discharging, preparing with a viscolizer, and preparing through microjet under high pressure.

Description

technical field [0001] The invention relates to a topotecan liposome and a preparation method thereof. The preparation can be used as a therapeutic drug for various tumors, such as non-small cell lung cancer, liver cancer, gastric cancer, blood diseases, lymphoma and the like. Background technique [0002] Topotecan (Topotecan, TPT) is a new semi-synthetic derivative of camptothecin, which has therapeutic effects on a variety of tumors, such as non-small cell lung cancer, liver cancer, gastric cancer, blood diseases, and lymphoma. Camptothecin drugs achieve their cytotoxic effect by inhibiting an essential enzyme in cell survival, DNA Topoisomerase I (DNATopo I). Topo exists widely in organisms and participates in key nuclear processes such as DNA replication, transcription, recombination, and repair. Topo is divided into two types in complex nuclear cells, Topo I and Topo II, which mainly solve the inherent topological constraints of DNA molecules. Topo I unwinds the supe...

Claims

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Application Information

Patent Timeline
15 Aug 2007
Publication
CN101015526A
IPC
A61K9/127; A61K9/08; A61K9/10; A61K9/19; A61K31/4745; A61K47/24; A61K47/26; A61K47/36; A61P35/00
Inventors
叶东; 宗在伟