Method for preparing microsphere preparation coated with hydrophilic medicaments

A technology of hydrophilic drugs and microspheres, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, block delivery, etc., and can solve the problems of inability to maintain long-term release of drugs, increase drug toxicity and side effects, and low encapsulation efficiency , to achieve controllable drug release behavior, improve hydrophilicity, and avoid burst release

Active Publication Date: 2013-01-30
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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  • Method for preparing microsphere preparation coated with hydrophilic medicaments
  • Method for preparing microsphere preparation coated with hydrophilic medicaments

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 method for preparing microsphere preparation coated with hydrophilic medicaments. The method has simple process and good controllability, and comprises: adding hydrophilic medicament water solution into an organic solution containing a polylactic acid-polyethylene glycol monomethyl ether segmented copolymer, and carrying out vortex to form water-in-oil initial emulsion; adding the initial emulsion into liquid paraffin containing an emulsifying agent I, and carrying out the vortex to form water-in-oil compound emulsion; and adding the compound emulsion into petroleum ether containing an emulsifying agent II, continuing stirring for 10 minutes-60 minutes, collecting microspheres through centrifugation, washing and drying to obtain the microsphere preparation coated with the hydrophilic medicaments.

Description

technical field [0001] The invention relates to the field of preparation of microsphere preparations of medicines, in particular to a preparation method of microsphere preparations loaded with hydrophilic medicines. 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 lactones...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K45/00A61K47/34
Inventor 邱利焱于洋朱金芳
Owner ZHEJIANG UNIV
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