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Stable polymer micelle medicine carrging system

A technology of mixing polymers and micelles, which is applied in the fields of cardiovascular system diseases, antipyretics, antineoplastic drugs, etc., can solve the problem of low drug loading, and achieve the effect of large drug loading and high stability

Inactive Publication Date: 2007-07-18
涂家生 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] In recent years, drug-loaded phospholipid micelles have been prepared by PEGylation of phospholipids, but the drug loading is low

Method used

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  • Stable polymer micelle medicine carrging system
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  • Stable polymer micelle medicine carrging system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The synthesis of embodiment 1 amphiphilic block copolymer mPEG-PDLLA

[0038] Weigh 16g of methyl polyethylene glycol and 24g of lactide, place in a closed reactor, add 50mg of stannous octoate toluene solution (2mL), raise the temperature to 120-140°C under nitrogen flow to melt the solid and remove the toluene , raising the temperature to 150-180° C. for 6 hours. After cooling, a white solid crude product was obtained. After the crude product was dissolved in 1ml of dichloromethane, it was added into 100ml of diethyl ether under stirring, filtered, washed with diethyl ether three times, and the product was vacuum-dried for 24 hours.

[0039] The NMR (D-chloroform as solvent) spectrum of the product confirmed the mass ratio and molecular weight of methylpolyethylene glycol and polylactic acid in the polymer with the peak area ratio of 5.2ppm (PLA) and 3.6ppm (PEG) (Figure 1).

Embodiment 2

[0040] Embodiment 2 Preparation and particle size determination of etoposide mixed polymer micelles

[0041] Weigh 1 g of etoposide, 2 g of mPEG-PDLLA, and 100 mg of lecithin into a flask, add 200 ml of acetonitrile, and stir until dissolved. Slowly evaporate acetonitrile under vacuum at 60°C (rotary evaporator). After no obvious acetonitrile evaporates, increase the temperature and vacuum to continue removing acetonitrile to obtain a colorless gel. Add water for injection at 60°C to 150ml, and hydrate to obtain a mixed polymer micelle solution with light blue opalescence. The product is sterilized by filtration with a 0.22 mm microporous membrane and then freeze-dried to obtain etoposide mixed polymer micelles (etoposide, mPEG-PDLLA and lecithin, 30 mg etoposide per bottle).

[0042] Weigh 400mg of etoposide and 1gmPEG-PDLLA respectively into a flask, add 200ml of acetonitrile, and stir until dissolved. Slowly evaporate acetonitrile under vacuum at 60°C (rotary evaporator)....

Embodiment 3

[0044] The preparation of embodiment 3 paclitaxel mixed polymer micelles

[0045] Weigh 300mg of paclitaxel, 1g of mPEG-PDLLA and 100mg of lecithin into a flask, add 150ml of acetonitrile, and stir until dissolved. Slowly evaporate acetonitrile under vacuum at 60°C (rotary evaporator). After no obvious acetonitrile evaporates, increase the temperature and vacuum to continue removing acetonitrile to obtain a colorless gel. Add water for injection at 60°C to 150ml, hydrate to obtain a mixture with light blue opalescence, and homogenize with a high-speed homogenizer at 12000rpm for 30 seconds to obtain a mixed polymer micelle solution. The product is sterilized by filtration with a 0.22mm microporous membrane and then freeze-dried to obtain paclitaxel mixed polymer micelles (paclitaxel, mPEG-PDLLA and lecithin, 30mg paclitaxel per bottle).

[0046] Weigh 300mg of paclitaxel and 1gmPEG-PDLLA respectively into a flask, add 150ml of acetonitrile, and stir until dissolved. Slowly e...

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Abstract

A stable polymer micella carrier system for medicines is composed of an amphipathic block copolymer including diblock copolymer and triblock copolymer and a phosphatide chosen from glyceryl phosphatide, sphingomyelin, and their derivatives.

Description

Technical field: [0001] The invention relates to a stable mixed polymer micelle drug loading system and its preparation. Background technique: [0002] Polymer micelle is a drug-loading system developed in recent years for insoluble drugs. It has a core-shell structure, in which the core is the hydrophobic part and the shell is the hydrophilic part. Polymer micelles can encapsulate poorly soluble drugs in the core part to solubilize poorly soluble drugs. Compared with commonly used solubilizers and latent solvents, the polymer micellar drug-loading system is made of biodegradable materials, and its safety is higher. [0003] Drug-loaded polymer micelles often choose biodegradable amphiphilic polymers as materials. This type of amphiphilic polymer can be diblock A-B type or triblock A-B-A, B-A-B type. For the structure, see reference Torchilin , V.P., Structure and design of polymeric surfactant-based drug delivery systems. J Control Release, 2001.73(2-3): p.137-72. Block c...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K47/36A61K47/32A61K9/00A61K45/00A61P35/00A61P31/00A61P29/00A61P9/00A61P3/10A61K47/10
Inventor 涂家生吴建梅
Owner 涂家生
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