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Method for preparing monodisperse nanosphere medicine carrier

A nano-microsphere and monodisperse technology, which is applied in the direction of non-active ingredient medical preparations, pharmaceutical formulations, powder delivery, etc., can solve the problems that affect the overall uniformity of drug carriers, difficult precise control, cumbersome washing process, etc., and achieve good results. Biocompatibility, high emulsification efficiency, and good size uniformity

Active Publication Date: 2013-01-09
广州智焜生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although polyvinyl alcohol has a good ball-forming effect, it has certain toxicity; and if it is necessary to prepare microsphere carriers with a diameter of less than 500nm, it is necessary to use high-concentration polyvinyl alcohol, which has a high viscosity and is difficult to prepare. The middle washing process is cumbersome and easy to remain; in addition, the distribution of nano-microspheres prepared by high-viscosity polyvinyl alcohol as an emulsifier is wide, and it is easy to form larger-sized microspheres, which affects the overall uniformity of the drug carrier, resulting in the slow-control of the drug. Difficult to precisely control during the release phase

Method used

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  • Method for preparing monodisperse nanosphere medicine carrier
  • Method for preparing monodisperse nanosphere medicine carrier
  • Method for preparing monodisperse nanosphere medicine carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] (1) 60mg poly(lactic acid-glycolic acid) copolymer (molecular weight 30000, LA:GA=50:50) was dissolved in 1ml N'N'-dimethylformamide to form an organic phase;

[0032] (2) 0.004mg polyethylene glycol 1000 vitamin E succinate was dissolved in 200ml distilled water to form the water phase;

[0033] (3) Under the synergistic effect of 100W ultrasonic and 1000rpm stirring, the organic phase is added dropwise to the aqueous phase at a rate of 0.5 drops per second under an ice-water bath, and the addition is completed after 1 minute, and the ultrasonic wave is stopped;

[0034] (4) Continue to stir for 6 hours at room temperature, and volatilize on the rotary evaporator to remove the organic solvent as much as possible;

[0035] (5) Centrifuge at 1000rpm to remove the aggregates, and the supernatant is subjected to ultrafiltration and refrigerated centrifugation at 3000rpm for 10 minutes, and washed 3 times with water to obtain the monodisperse nano-microsphere drug carrier. ...

Embodiment 2

[0038] (1) 250mg poly(lactic acid-glycolic acid) copolymer (molecular weight 30000, LA:GA=50:50) is dissolved in 5ml N'N'-dimethylformamide to form an organic phase;

[0039] (2) 0.05 mg polyethylene glycol 1000 vitamin E succinate was dissolved in 100 ml distilled water to form the water phase;

[0040] (3) Under the synergistic effect of 200W ultrasonic and 600rpm stirring, the organic phase was added dropwise to the aqueous phase at a rate of 2 drops per second under an ice-water bath, and the addition was completed after 5 minutes, and the ultrasonic wave was stopped;

[0041] (4) Continue to stir for 6 hours at room temperature, and volatilize on the rotary evaporator to remove the organic solvent as much as possible;

[0042] (5) Centrifuge at 2000rpm to remove aggregates, then supernatant is subjected to ultrafiltration and refrigerated centrifugation at 5000rpm for 8 minutes, and washed with water for 3 times to obtain monodisperse nano-microsphere drug carrier.

[00...

Embodiment 3

[0045] (1) 100mg poly(lactic acid-glycolic acid) copolymer (molecular weight 25000, LA:GA=75:25) is dissolved in 2ml N'N'-dimethylformamide to form an organic phase;

[0046] (2) 0.2 mg polyethylene glycol 1000 vitamin E succinate was dissolved in 200 ml distilled water to form the water phase;

[0047] (3) Under the synergy of 40W ultrasonic and 400rpm stirring, the organic phase is added dropwise to the aqueous phase at a rate of 4 drops per second under an ice-water bath, and the addition is completed after 10 minutes, and the ultrasonic wave is stopped;

[0048] (4) Continue to stir for 6 hours at room temperature, and volatilize on the rotary evaporator to remove the organic solvent as much as possible;

[0049] (5) Centrifuge at 2000rpm to remove aggregates, and the supernatant is subjected to ultrafiltration and refrigerated centrifugation at 8000rpm for 6 minutes, and washed 4 times with water to obtain monodisperse nano-microsphere drug carriers.

[0050] The nano-mi...

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Abstract

The invention discloses a method for preparing a monodisperse nanosphere medicine carrier, which comprises the following steps: dissolving poly(lactic-co-glycolic acid) in organic solvent to form an organic phase; dissolving emulsifier in distilled water to form a water phase; under the synergistic effect of ultrasound and stirring and in an ice water bath, adding an organic phase into a water phase according to a volume ratio to obtain oil-in-water emulsion; continuously stirring the emulsion at normal temperature for 4 to 20 hours, and removing organic solvent; and performing low-speed centrifugation to remove aggregate, subjecting supernate to ultrafiltration, refrigeration, centrifugation and washing to obtain the monodisperse nanosphere medicine carrier. In the monodisperse nanospheres, the spherical shape is regular, the particle size is between 100 and 500 nanometers, the size is controllable and the specifications are uniform. The monodisperse nanospheres are suitable for coating and carrying various water soluble or liposoluble medicines and have the advantages of biodegradability, controlled medicine release and the like.

Description

technical field [0001] The invention belongs to the field of preparation of medicinal nano-microsphere materials, and in particular relates to a preparation method of a monodisperse nano-microsphere drug carrier. Background technique [0002] Nanospheres refer to polymer materials or polymer composite materials with diameters ranging from nanometers to micrometers, spherical or other geometric shapes, and their shapes can include solid, hollow, porous, etc. Due to their unique shape and morphology, monodisperse nano-scale and micron-scale polymer particles have special functions that other materials do not have, and have been widely used in nanotechnology, particle adsorption, biochemistry, polymer fillers, catalysts, Electronic information, drug controlled release and other fields. [0003] Poly(lactic-co-glycolic acid) copolymer (Poly Lactic-co-Glycolic Acid, referred to as: PLGA) is randomly polymerized from two monomers of lactic acid and glycolic acid. It is a biodegra...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K9/14A61K47/22
Inventor 魏坤凌友
Owner 广州智焜生物科技有限公司