Microsphere preparation encapsulating hydrophilic medicine and preparation method thereof

A hydrophilic drug and a hydrophilic technology are applied in the field of microsphere preparations encapsulating hydrophilic drugs and the preparation thereof, and can solve the problems of inability to maintain long-term drug release, increase drug toxicity and side effects, and low encapsulation efficiency. Achieve controllable drug release behavior, improve hydrophilicity, and avoid sudden release effects

Active Publication Date: 2012-12-05
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the preparation process of superparamagnetic streptomycin sulfate PLA-PEG microspheres, hydrophilic drugs are easy to diffuse into the external water phase, resulting in low encapsulation efficiency and obvious burst release effect, thus increasing the toxic and side effects of drugs , causing waste of drugs and unable to maintain long-term release of drugs, there are still technical defects

Method used

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  • Microsphere preparation encapsulating hydrophilic medicine and preparation method thereof
  • Microsphere preparation encapsulating hydrophilic medicine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Weigh 4.5g of D, L-lactide and 0.5g of polyethylene glycol 5000 monomethyl ether and dissolve in 100ml of anhydrous toluene, add 25mg of stannous octoate as a catalyst, and reflux in an oil bath at 130°C under nitrogen protection After reacting for 24 hours, part of the toluene was distilled off under reduced pressure, the concentrated solution was poured into anhydrous ether to precipitate, the product was collected by filtration, and vacuum-dried for 24 hours to obtain a mass ratio of polylactic acid to polyethylene glycol 5000 monomethyl ether of 90:10. PLA-mPEG with a number average molecular weight of 50,000.

[0041] Weigh 20 mg of the above-mentioned PLA-mPEG, 80 mg of PLGA (the number-average molecular weight is 60,000, and the mass ratio of lactic acid to glycolic acid is 50:50) and dissolve in a mixed solvent of 0.8 ml ethyl acetate and 0.2 ml acetonitrile to prepare an organic solution. Dissolve 15 mg of leuprolide in 0.2 ml of water to prepare a hydrophilic ...

Embodiment 2

[0043] Weigh 3.5g of D, L-lactide and 1.5g of polyethylene glycol 5000 monomethyl ether and dissolve in 100ml of anhydrous toluene, add 20mg of stannous octoate as catalyst, and reflux in an oil bath at 130°C under nitrogen protection After reacting for 24 hours, part of the toluene was distilled off under reduced pressure, the concentrated solution was poured into anhydrous ether to precipitate, the product was collected by filtration, and dried in vacuum for 24 hours to obtain a mass ratio of polylactic acid to polyethylene glycol 5000 monomethyl ether of 70:30, PLA-mPEG with a number average molecular weight of 17,000.

[0044] Weigh the above-mentioned PLA-mPEG 40mg, PLGA (the number average molecular weight is 50,000, the mass ratio of lactic acid and glycolic acid is 75:25), and the mass ratio of lactic acid and glycolic acid is 75:25) 60mg is dissolved in 1.5ml ethyl acetate The mixed solvent of 0.3ml acetonitrile makes organic solution, and doxorubicin hydrochloride 20...

Embodiment 3

[0046] Weigh 3.0g of D, L-lactide and 2.0g of polyethylene glycol 5000 monomethyl ether and dissolve in 100ml of anhydrous toluene, add 20mg of stannous octoate as a catalyst, and reflux in an oil bath at 130°C under nitrogen protection After reacting for 24 hours, part of the toluene was distilled off under reduced pressure, the concentrated solution was poured into anhydrous ether to precipitate, the product was collected by filtration, and vacuum-dried for 24 hours to obtain a mass ratio of polylactic acid to polyethylene glycol 5000 monomethyl ether of 60:40. PLA-mPEG with a number average molecular weight of 13,000.

[0047] Weigh 50 mg of the above PLA-mPEG, 50 mg of PLGA (the number average molecular weight is 20,000, and the mass ratio of lactic acid to glycolic acid is 80:20) dissolved in a mixed solvent of 2 ml of ethyl acetate and 0.5 ml of acetonitrile to prepare an organic solution, rice hydrochloride Toxantrone 10mg was dissolved in 0.5ml 0.1M phosphate buffered ...

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Abstract

The invention discloses a microsphere preparation encapsulating a hydrophilic medicine, and the microsphere preparation comprises the following components in percentage by weight: a hydrophilic medicine 0.1-40%, methoxy poly(ethylene glycol)-poly(lactic acid) block copolymers 0.1-99%, and poly(lactic acid) or poly(lactic acid-glycollic acid) copolymers 0.1-99%. The microsphere preparation has round and intact surface, uniform and controllable particle diameter, high encapsulation rate, and controllable drug release behaviors. The invention also discloses a preparation method of the microsphere preparation encapsulating the hydrophilic medicine, and the preparation method has simple process and good controllability and comprises the following steps: adding a water solution of the hydrophilic medicine into an organic solution of the methoxy poly(ethylene glycol)-poly(lactic acid) block copolymers, and vortexing to form water-in-oil type primary emulsion; adding the primary emulsion intoliquid paraffin containing emulsifier I, and vortexing to form water-in-oil type multiple emulsion; and adding the multiple emulsion into liquid paraffin containing emulsifier II, continuing stirringfor 4-24 h, centrifuging, collecting pellets, washing, and drying to obtain the microsphere preparation encapsulating the hydrophilic medicine.

Description

technical field [0001] The invention relates to the field of drug microsphere preparations and preparation thereof, in particular to a microsphere preparation carrying hydrophilic drugs and a preparation method thereof. Background technique [0002] Microspheres are tiny spherical entities formed by dissolving or dispersing drugs in a polymer matrix. They belong to matrix-type skeleton particles, and their diameters are generally in the micron or even nanometer range. After the drug is made into microspheres, the drug can be concentrated in the target area, the drug can be released slowly or controlled, and the toxic and side effects of the drug can be reduced. [0003] In microsphere drug delivery systems, the nature of the carrier material is the main factor determining drug release. Polyester polymer materials are the most researched and widely used biodegradable synthetic polymer materials at home and abroad so far. They are basically polymers of lactic acid or its lact...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K9/16
Inventor 邱利焱于洋朱金芳
Owner ZHEJIANG UNIV
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