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10-hydroxy camptothecine long circulating vesica and its freeze-dried preparation

A technology of hydroxycamptothecin and freeze-dried preparations, which is applied in the direction of freeze-dried delivery, antineoplastic drugs, powder delivery, etc. It can solve the problems of increased toxicity of the reticuloendothelial system, loss of pharmacological activity, and reduced anticancer activity, and achieves increased Effects of prolonging blood circulation time, residence time, and reducing toxicity

Inactive Publication Date: 2005-10-12
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the main problems of the drug are: short half-life (5min-1h), repeated administration is required, so the side effects are relatively large; fat solubility is strong, and the anticancer activity of the water-soluble sodium salt is reduced by 90%; poor stability , the lactone ring of the drug is sensitive to light and heat, and loses its pharmacological activity after opening the lactone ring
Chinese patent 01138252.X discloses 10-hydroxycamptothecin dextran nanoparticles, 01133700.1 discloses polylactic acid nanoparticles, and 03113179.4 discloses vesicles of HCPT. Higher selectivity is good for the treatment of liver cancer, but if the lesion site is not in other tumors of the reticuloendothelial system, this type of preparation will not only have no targeting effect, but will also increase the toxicity of the drug to the reticuloendothelial system

Method used

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  • 10-hydroxy camptothecine long circulating vesica and its freeze-dried preparation
  • 10-hydroxy camptothecine long circulating vesica and its freeze-dried preparation
  • 10-hydroxy camptothecine long circulating vesica and its freeze-dried preparation

Examples

Experimental program
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Effect test

Embodiment 1

[0027] Dissolve 1 g of 10-hydroxycamptothecin, 50 g of Span, 15 g of cholesterol, and 5 g of polyethylene glycol-distearoylphosphatidylethanolamine (PEG-DSPE) in chloroform:methanol (2:1), and remove by rotary evaporation The organic solvent was vacuum-dried, added into a solution of 100 g of trehalose and sucrose in water (1:1), hydrated for 30 minutes, and treated with ultrasonic waves to obtain a long-circulating vesicle solution of 10-HCPT.

Embodiment 2

[0029] 2 g of 10-hydroxycamptothecin, 50 g of Span, 10 g of cholesterol, and 10 g of polyethylene glycol-polycaprolactone (PEG-PCL) were dissolved in chloroform:methanol (2:1), and the organic solvent was removed by rotary evaporation. Vacuum-dried, added into 100g trehalose solution, hydrated for 30 minutes, and treated with a high-pressure homogenizer to obtain a long-circulating vesicle solution of 10-HCPT.

Embodiment 3

[0031] Dissolve 4 g of 10-hydroxycamptothecin, 50 g of Span, 20 g of cholesterol, and 8 g of polyethylene glycol-polyglycolide lactide (PEG-PLGA) in dichloromethane:ethanol (2:1), and rotate Remove the organic solvent by evaporation, dry in vacuum, add 70g of mannose and sucrose in water (1:1), hydrate for 30min, and process with a high-pressure homogenizer to obtain a long-circulating vesicle solution of 10-HCPT.

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Abstract

A freeze-dried macrocyclic vesicle for preventing and treating cancer is proportionally prepared from 10-hydroxy camptothecine, PEG modified lipoid, span, cholesterol, trehalose or cane sugar, alcohol and dichloromethane. Its advantages are high water solubility and stability, and low toxin.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to 10-hydroxycamptothecin long-circulating vesicles, a freeze-dried preparation of long-circulating vesicles 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 less, a...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/475A61P35/00
Inventor 施斌裴元英
Owner FUDAN UNIV
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