10-hydroxy camptothecin long cyclic liposome and its freeze aried preparation

A technology of hydroxycamptothecin and liposome preparation, which is applied in the directions of liposome delivery, medical preparations containing active ingredients, organic active ingredients, etc., can solve the difficulty of fusion and freeze-drying, and the speed of liposome removal is slowed down , large particle size of liposomes, etc., to increase blood circulation time, improve needle adaptability, and reduce toxicity

Inactive Publication Date: 2005-08-10
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention is characterized in that it uses PEGylated lipids to modify liposomes. On the one hand, it can solve the problems of traditional liposomes with large particle size, poor stability, easy leakage, fusion and freeze-drying difficulties; on the other hand, it can make lipids The surface of the plastid is modified by PEG to form a three-dimensional "conformation cloud", which prevents the recognition of opson...

Method used

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  • 10-hydroxy camptothecin long cyclic liposome and its freeze aried preparation
  • 10-hydroxy camptothecin long cyclic liposome and its freeze aried preparation
  • 10-hydroxy camptothecin long cyclic liposome and its freeze aried preparation

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Embodiment 1

[0024] 10-hydroxycamptothecin 1g, phospholipid 50g, cholesterol 15g, polyethylene glycol-distearoylphosphatidylethanolamine (PEG-DSPE) 5g, dissolved in chloroform:methanol (2:1), rotary evaporation to remove organic The solvent was vacuum-dried, added into a solution of trehalose and sucrose water (1:1) dissolved in 100 g, hydrated for 30 min, and treated with ultrasonic waves to obtain a long-circulating liposome solution of 10-HCPT.

Embodiment 2

[0026] Dissolve 2 g of 10-hydroxycamptothecin, 50 g of phospholipids, 10 g of cholesterol, and 10 g of polyethylene glycol-polycaprolactone (PEG-PCL) in chloroform:methanol (2:1), remove the organic solvent by rotary evaporation, and vacuum After drying, add 100g of trehalose solution, hydrate for 30 minutes, and process it with a high-pressure homogenizer to obtain a long-circulation liposome solution of 10-HCPT.

Embodiment 3

[0028] Dissolve 4 g of 10-hydroxycamptothecin, 50 g of phospholipids, 20 g of cholesterol, and 8 g of polyethylene glycol-polyglycolide lactide (PEG-PLGA) in dichloromethane:ethanol (2:1), and rotate to evaporate Remove the organic solvent, dry in vacuum, add 70g of mannose and sucrose in water (1:1) solution, hydrate for 30min, and process with a high-pressure homogenizer to obtain a long-circulating liposome solution of 10-HCPT.

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Abstract

A long-cycle lipoid of 10-hydroxyamptothecin and its freeze dried medicine for treating cancer are prepared from lecithin, PEG modified bipid, cholesterol, mycose or cane sugar, alcohol and dichloromethane.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to 10-hydroxycamptothecin long-circulation liposome, a freeze-dried preparation of the long-circulation liposome and a preparation method thereof. Background technique [0002] 10-hydroxycamptothecin (Hydrocamptothecin, HCPT) is a trace alkaloid with the strongest anti-cancer effect among similar anti-tumor monomers extracted from camphor tree chinensis in the 1960s and 1970s. It is an S-phase specific anti-cancer drug . Systematic pharmacological research. Its anti-cancer mechanism is to inhibit Topo I. It is mainly used clinically in ascites-type liver cancer, head and neck cancer, gastric cancer, bladder cancer and leukemia. The toxic reactions of HCPT are mainly manifested in the inhibition of urinary system, digestive system and hematopoietic function. etc., but its toxicity is significantly lower than that of camptothecin, especially the urinary system reaction is les...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/475A61P35/00
Inventor 施斌裴元英
Owner FUDAN UNIV
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