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Combretastatin nanometer polymer micelle freeze-dried preparation and preparation method thereof

A technology of nano-polymer and compretidine, which is applied in the field of compretidine nano-polymer micelle freeze-dried preparations and its preparation, can solve the problems of poor stability, poor water solubility and low bioavailability, and achieve stability High, reduced toxicity, good compatibility

Inactive Publication Date: 2016-01-20
SUZHOU HAITE BIAO BIOLOGICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, CA-4 has many defects, such as poor water solubility, no activity in the trans configuration, and the extremely poor water solubility makes the oral bioavailability of CA4 low, and the aqueous solution of its phosphorylated drug CA4P is unstable to light and heat. , after intravenous injection in rats, the elimination half-life is only a few minutes, the elimination in the body is fast, and the stability is poor, which limits clinical use

Method used

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  • Combretastatin nanometer polymer micelle freeze-dried preparation and preparation method thereof
  • Combretastatin nanometer polymer micelle freeze-dried preparation and preparation method thereof
  • Combretastatin nanometer polymer micelle freeze-dried preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027] Example 1 Preparation of amphiphilic biodegradable diblock copolymer carrier material.

[0028] Formula dosage: D, L-lactide 150g, polyethylene glycol monomethyl ether 100g.

[0029] Weigh the formulated amount of D, L-lactide and polyethylene glycol monomethyl ether for later use, vacuum-dry the formulated amount of polyethylene glycol monomethyl ether in the reactor at 110°C for 2 hours, replace with nitrogen, and then add The D of formula quantity, L-lactide, drop into catalyst stannous octoate again, the amount of stannous octoate accounts for D, 0.2% of the total mass of L-lactide and polyethylene glycol monomethyl ether, then vacuumize, wait D, After L-lactide is completely melted, replace with nitrogen three times, then vacuumize the reactor to ensure negative pressure, airtight or nitrogen protection, then raise the temperature to 140°C, react for 6 hours, and after the reaction is completed, a light yellow clear viscous Thick liquid; add 60ml of dichloromethan...

Embodiment 2

[0034] Formula dosage: D, L-lactide 100g, glycolide 100g, polyethylene glycol monomethyl ether 100g.

[0035]Weigh the formulated amount of D, L-lactide, glycolide, and polyethylene glycol monomethyl ether for later use, dry the formulated amount of polyethylene glycol monomethyl ether in a reactor at 100°C for 3 hours under vacuum, nitrogen Replacement, then add the D of formula quantity, L-lactide, glycolide, put into catalyst stannous octoate again, the amount of stannous octoate accounts for D, L-lactide, glycolide and polyethylene glycol monomethyl 0.3% of the total mass of ether, then vacuumize, after D, L-lactide and glycolide are all melted, replace with nitrogen three times, and then vacuumize again to ensure negative pressure in the reactor, airtight or nitrogen protection, and then Raise the temperature to 120°C, react for 8 hours, and after the reaction is completed, a light yellow, clear and viscous liquid is obtained; add 50 ml of dichloromethane to the light yel...

Embodiment 3

[0037] Formula dosage: ε-caprolactone 80g, polyethylene glycol monomethyl ether 100g.

[0038] Weigh the formulated amount of ε- and lactone and polyethylene glycol monomethyl ether for later use, dry the formulated amount of polyethylene glycol monomethyl ether in the reactor at 120°C for 4 hours in vacuum, replace with nitrogen, and then add the formulated amount ε- and lactone, and then put into the catalyst stannous octoate, the amount of stannous octoate accounts for 0.1% of the total mass of ε-caprolactone and polyethylene glycol monomethyl ether, then vacuumize, until ε- and lactone are all After melting, replace with nitrogen for three times, and then vacuumize to ensure negative pressure in the reactor, airtight or nitrogen protection, then raise the temperature to 130°C, react for 10 hours, after the reaction is completed, a light yellow, clear and viscous liquid is obtained; Add 40ml of dichloromethane to the yellow clear viscous liquid to dissolve, stir for 30min, ...

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Abstract

The invention discloses a combretastatin nanometer polymer micelle freeze-dried preparation. The combretastatin nanometer polymer micelle freeze-dried preparation comprises a methoxy polyethylene glycol-polyester block copolymer carrier material and combretastatin. Combretastatin is wrapped by the copolymer carrier material. A mass ratio of combretastatin to the copolymer carrier material is 0.01-0.15. The copolymer carrier material is a block copolymer prepared from a mixture of one or more polyester monomers and methoxy polyethylene glycol by ring opening polymerization. A mass ratio of methoxy polyethylene glycol to polyester is 1: 0.55-2. The polyester monomer is one of D, L-lactide, glycolide, caprolactone and trimethylcarbonate. Through optimization of a mass ratio of polyester to polyether of the block copolymer, a mass ratio of combretastatin to the carrier is further optimized. After water redissolution, greater than 90% entrapment rate lasting time of the combretastatin micelle preparation is 12h or more, accords with clinical medicine application physical truth and satisfies clinical requirements.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a compretidine nano polymer micelle freeze-dried preparation and a preparation method thereof. Background technique [0002] Combretastatin A-4 (CA-4) is a natural and powerful small molecule anti-mitotic agent isolated from the bark of willow shrub in South Africa. It is a polyhydroxy stilbene natural compound with a chemical name of cis-1-(3, 4,5-Trimethoxyphenyl)-2-(3′-hydroxy-4′-methoxyphenyl)ethylene, its action site is the same as that of colchicine, it can inhibit the polymerization of tubulin and at the same time inhibit the cell Depolymerization of tubulin and accumulation of mitogens in medium. CA-4 can specifically target and destroy the tumor blood vessels that have been formed, so that the tumor cannot receive oxygen and nutrients until the tumor is "starved to death", thereby achieving the effect of killing tumor cells. It is expected to be developed i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K9/51A61K31/09A61K47/34A61P35/00
Inventor 不公告发明人
Owner SUZHOU HAITE BIAO BIOLOGICAL TECH
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