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Microparticle and pharmaceutical composition

A technology of microparticles and polymers, which is applied in the direction of pharmaceutical formulations, microcapsules, and medical preparations of non-active ingredients, etc., and can solve the problems of non-biodegradable and inapplicable administration of microparticles

Inactive Publication Date: 2008-03-05
TORAY IND INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since amphiphilic block copolymers of vinyl ethers are not biodegradable, the microparticles are not suitable for in vivo administration by injection or oral administration.
In addition, since the microparticles are microparticles with a hydrophobic outer layer, it is difficult to prepare the microparticles into an aqueous dispersion suitable for in vivo administration.

Method used

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  • Microparticle and pharmaceutical composition
  • Microparticle and pharmaceutical composition
  • Microparticle and pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0129] Microparticle preparation:

[0130] 10 mg of polyethylene glycol-poly(ε-caprolactone) (molecular weight of polyethylene glycol: 5,000, molecular weight of poly(ε-caprolactone): 10,000) which is an amphiphilic polymer was dissolved in 500 μL of chloroform. This solution was added to 2 mL of a mixed solvent of hexane and chloroform (1.6 mL of hexane, 0.4 mL) to prepare a polymer solution. While stirring the polymer solution at a stirring rate of 1,600 rpm, 10-100 μL of a 25 wt % bovine serum albumin solution was added dropwise. Stirring was further performed for 5 minutes, thereby preparing microparticles. After spreading this fine particle dispersion on a silicon wafer, it was fully dried under vacuum, and platinum was vapor-deposited, and observed with a scanning electron microscope (HITACHS-4800).

[0131]

[0132] Microparticles with a diameter of several micrometers to hundreds of micrometers were observed. The particle shape observed after drying is not inconsi...

Embodiment 2

[0134] Microparticle preparation:

[0135] 10 mg of polyethylene glycol-poly(ε-caprolactone) (molecular weight of polyethylene glycol 5,000, molecular weight of poly(ε-caprolactone) 10,000 or 37,000) which is an amphiphilic polymer was dissolved by heating in 2 mL of acetic acid in ethyl ester. While stirring the polymer solution at a stirring rate of 1,600 rpm, 50-200 µL of a horseradish peroxidase aqueous solution (1 wt% horseradish peroxidase, 9 wt% sucrose, 10 mM Tris-HCl pH 7.4) was added dropwise. Stirring was further carried out for 1 hour, whereby microparticles were prepared. The particle size measurement of the fine particles was carried out by a dynamic light scattering method using an apparatus Zetasizer 3000HSA (MALVERN INSTRUMENTS). The obtained data was analyzed by the CONTIN method and the histogram method, and the particle diameter was calculated.

[0136]

[0137] Microparticles with a minimum number-average particle diameter of 25.1 nm were formed (Fig....

Embodiment 3

[0139] Microparticle preparation:

[0140] Dissolve 10 mg of polyethylene glycol-poly(ε-caprolactone) (molecular weight of polyethylene glycol 5,000, molecular weight of poly(ε-caprolactone) 37,000) which is an amphiphilic polymer in 2 mL of ethyl acetate , to prepare a polymer solution. While stirring the polymer solution at a stirring rate of 1,600 rpm, 100 μL of a 1 wt % horseradish peroxidase solution was added dropwise. After further stirring for 1 hour, it was added to 10 times the amount of dioxane. After evaporating the solvent and concentrating to about 2 mL, the particle dispersion was added to a phosphate buffer solution (10 mL) containing various concentrations of Pluronic (registered trademark of BASF) F68 (PEO-PPO-PEO block polymer). The particle size measurement of the fine particles was carried out by a dynamic light scattering method using an apparatus Zetasizer 3000HSA (Malvern Instruments). The obtained data was analyzed by the CONTIN method and the histo...

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Abstract

A fine particle comprising an amphiphilic polymer, further comprising an inner nucleus of hydrophilic segment of amphiphilic polymer, and a hydrophobic outer layer of hydrophobic segment of amphiphilic polymer, and having a surface modifier bonded to the hydrophobic outer layer. A fine particle of the invention effectively enclose protein, peptide drug, nucleic acid medicine of hydrophilic property and large molecular weight in the inner nucleus of hydrophilic segment of amphiphilic polymer, and are preferable for stabilizing in the body and promoting absorption.

Description

technical field [0001] The present invention relates to microparticles and pharmaceutical compositions for effectively delivering physiologically active substances, drugs, contrast agents, genes, and the like. The present invention relates to microparticles and pharmaceutical compositions as so-called drug delivery systems. More specifically, the present invention relates to microparticles and pharmaceutical compositions that effectively encapsulate, for example, hydrophilic and large molecular weight protein / peptide drugs, nucleic acid drugs, and the like. Background technique [0002] Microparticle formulations, in which drugs are encapsulated in microparticles, are being developed and investigated for use as drug carriers. The microparticles are called microparticles, microspheres, microcapsules, nanoparticles, or nanospheres. [0003] However, in commonly used microparticles, that is, microparticles or polymer micelles formed of biodegradable polymers, the compartment ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00A61K9/14A61K9/50A61K31/7105A61K31/711A61K38/00A61K47/32A61K47/34
CPCA61K9/146A61K31/711A61K38/28A61K31/7105C08J3/12C08J2323/06C08G81/00A61K9/14
Inventor 柿泽资训青木孝夫井田伸夫西尾玲士
Owner TORAY IND INC
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