Method for preparing nano particles

• US 9,439,871 B2
• Filed: 09/21/2012
• Issued: 09/13/2016
• Est. Priority Date: 09/21/2011
• Status: Active Grant

• Current Assignee: Bio-Synectics, Inc.
• Original Assignee: Bio-Synectics, Inc.
• Inventors: Kim, Kab Sig, Park, Joo Won
• Primary Examiner(s): Palenik, Jeffrey T
• Application Number:
  US14/344,256
• Publication Number:
  US 20150031707A1
• Time in Patent Office: 1,453 Days
• Field of Search: None
• US Class Current: 1/1
• CPC Class Codes: A61K 31/122 having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
• CPC Class Codes: A61K 31/443 containing a five-membered ring with oxygen as a ring hetero atom
• CPC Class Codes: A61K 31/496 Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• CPC Class Codes: A61K 9/145 with organic compounds
• CPC Class Codes: A61K 9/146 with organic macromolecular compounds
• CPC Class Codes: A61K 9/5123 Organic compounds, e.g. fats, sugars
• CPC Class Codes: A61K 9/5138 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/5146 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides
• CPC Class Codes: A61K 9/5192 Processes

Abstract

The present invention relates to a method for manufacturing nano-scale particles of an active material. More particularly, the present invention relates to a method which uniformly mixes a surfactant having an HLB value of 8 or more and a melting point or glass transition temperature of 80° C. or lower and an active material, and mills the mixture using a roller mill, to thereby prepare nanoparticle powder from the active material.

Claims

1. A method for preparing nanoparticle powder of an active ingredient, comprising:

(1) uniformly mixing an active ingredient with a surfactant having an HLB value of 8 or more and a melting point or a glass transition temperature of 80°

C. or lower; and

(2) grinding the mixture obtained in step (1) by using a roller mill,

wherein water is added to the mixture in step (1) or step (2) and the amount of water is 1% to 5% by weight, based on the total weight of the mixture obtained in step (1).

2. The method for preparing nanoparticle powder of an active ingredient according to claim 1, wherein the mixture obtained in step (1) further comprises a biocompatible polymer.

3. The method according to claim 2, wherein the biocompatible polymer is selected from the group consisting of gelatin, casein, dextran, gum arabic, tragacanth, polyethyleneglycols, carboxymethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, methylcellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose phthalate, noncrystalline cellulose, polyvinylalcohol, polyvinylpyrrolidone, poloxamers, eudragit, lysozyme, albumin and mixtures thereof.

4. The method according to claim 2, wherein the active ingredient is one or more selected from the group consisting of physiologically active organic compounds, organometallic compounds, natural extracts, peptides, proteins and polysaccharides, and wherein the surfactant is selected from the group consisting of phospholipids, benzalkonium chloride, glycerin esters of fatty acid, cetomacrogol, polyoxyethylene alkyl ethers, polyoxyethylene stearate, polyoxyethylene fatty acid esters, sorbitan esters, polyoxyethylene castor oil derivatives, polyoxyethylene sorbitan fatty acid esters, sucrose fatty acid esters, PEG-cholesterol, PEG-vitamin E and mixtures thereof, and wherein the biocompatible polymer is selected from the group consisting of gelatin, casein, dextran, gum arabic, tragacanth, polyethyleneglycols, carboxymethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, methylcellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose phthalate, noncrystalline cellulose, polyvinylalcohol, polyvinylpyrrolidone, poloxamers, eudragit, lysozyme, albumin and mixtures thereof.

5. The method according to claim 1, wherein the mixture obtained in step (1) further comprises a saccharide or a salt.

6. The method according to claim 5, wherein the saccharide is glucose, lactose, mannitol, sucrose, xylitol, chitosan, starch, fiber or a mixture thereof.

7. The method according to claim 5, wherein the salt is sodium chloride, calcium chloride or calcium carbonate, or a mixture thereof.

8. The method according to claim 5, wherein the active ingredient is one or more selected from the group consisting of physiologically active organic compounds, organometallic compounds, natural extracts, peptides, proteins and polysaccharides, and wherein the surfactant is selected from the group consisting of phospholipids, benzalkonium chloride, glycerin esters of fatty acid, cetomacrogol, polyoxyethylene alkyl ethers, polyoxyethylene stearate, polyoxyethylene fatty acid esters, sorbitan esters, polyoxyethylene castor oil derivatives, polyoxyethylene sorbitan fatty acid esters, sucrose fatty acid esters, PEG-cholesterol, PEG-vitamin E and mixtures thereof, and wherein the saccharide is glucose, lactose, mannitol, sucrose, xylitol, chitosan, starch, fiber or a mixture thereof.

9. The method according to claim 5, wherein the active ingredient is one or more selected from the group consisting of physiologically active organic compounds, organometallic compounds, natural extracts, peptides, proteins and polysaccharides, and wherein the surfactant is selected from the group consisting of phospholipids, benzalkonium chloride, glycerin esters of fatty acid, cetomacrogol, polyoxyethylene alkyl ethers, polyoxyethylene stearate, polyoxyethylene fatty acid esters, sorbitan esters, polyoxyethylene castor oil derivatives, polyoxyethylene sorbitan fatty acid esters, sucrose fatty acid esters, PEG-cholesterol, PEG-vitamin E and mixtures thereof, and wherein the salt is sodium chloride, calcium chloride or calcium carbonate, or a mixtures thereof.

10. The method according to claim 1, wherein the active ingredient is one or more selected from the group consisting of physiologically active organic compounds, organometallic compounds, natural extracts, peptides, proteins and polysaccharides.

11. The method according to claim 1, wherein the surfactant is selected from the group consisting of phospholipids, benzalkonium chloride, glycerin esters of fatty acid, cetomacrogol, polyoxyethylene alkyl ethers, polyoxyethylene stearate, polyoxyethylene fatty acid esters, sorbitan esters, polyoxyethylene castor oil derivatives, polyoxyethylene sorbitan fatty acid esters, sucrose fatty acid esters, PEG-cholesterol, PEG-vitamin E and mixtures thereof.

12. The method according to claim 1, wherein the grinding in step (2) is performed continuously 20 or more times.

13. The method according to claim 1, wherein the temperature of the roller of the roller mill is 40°

C. or lower.

14. The method according to claim 1, wherein the active ingredient is one or more selected from the group consisting of physiologically active organic compounds, organometallic compounds, natural extracts, peptides, proteins and polysaccharides, and wherein the surfactant is selected from the group consisting of phospholipids, benzalkonium chloride, glycerin esters of fatty acid, cetomacrogol, polyoxyethylene alkyl ethers, polyoxyethylene stearate, polyoxyethylene fatty acid esters, sorbitan esters, polyoxyethylene castor oil derivatives, polyoxyethylene sorbitan fatty acid esters, sucrose fatty acid esters, PEG-cholesterol, PEG-vitamin E and mixtures thereof.