Preparation method of sustained-release microcapsules having initial burst inhibiting property and the microcapsules thereby

• US 8,541,030 B2
• Filed: 11/21/2007
• Issued: 09/24/2013
• Est. Priority Date: 11/27/2006
• Status: Active Grant

• Current Assignee: Dongkook Pharmaceutical Co., Ltd.
• Original Assignee: Dongkook Pharmaceutical Co., Ltd.
• Inventors: Lim, Nak-Hyun, Kim, Jung-Kwoun, Jung, Hyung-Joon, Kim, Se-Yeon, Jung, Goo-Young, Cha, Kyung-Hoi, Park, Mork-Soon
• Primary Examiner(s): Wax, Robert A
• Assistant Examiner(s): Tcherkasskaya, Olga V
• Application Number:
  US12/516,275
• Publication Number:
  US 20100272820A1
• Time in Patent Office: 2,134 Days
• Field of Search: None
• US Class Current: 424/497
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 5/02 of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
• CPC Class Codes: B01J 13/02 Making microcapsules or microballoons for medical preparations A61K9/50

Abstract

Disclosed is a method for preparing a longer sustained-release formulation containing bioactive substances. More particularly, the present invention provides a method for preparing longer sustained-release microcapsules comprising: adding an emulsion including bioactive substances, biocompatible polymer and polyvinylpyrrolidone to an aqueous solution.

Claims

1. A method for preparing sustained-release microcapsules comprising:

adding an emulsion containing octreotide or a salt thereof as a bioactive substance, a bio-compatible polymer and polyvinylpyrrolidone to an aqueous solution containing a salt in an amount of 0.02 to 0.15 M to provide the sustained-release microcapsules, wherein the salt is sodium chloride, and wherein the drug encapsulation efficacy of the sustained-release microcapsules is increased in an amount of 15.6% to 40.5% compared to that of a sustained-release microcapsules prepared by an aqueous solution not containing salt.

2. The method of claim 1, wherein the emulsion is prepared by mixing a first non-aqueous solution containing the octreotide or a salt thereof and a second non-aqueous solution containing a bio-compatible polymer and polyvinylpyrrolidone.

3. The method of claim 1, wherein the bio-compatible polymer is polylactide-co-glycolide or poly(lactide-co-glycolide)glucose.

4. The method of claim 1, wherein the bio-compatible polymer has an average molecular weight of 60,000 or less.

5. The method of claim 2, wherein the first non-aqueous solution contains methanol.

6. The method of claim 2, wherein the second non-aqueous solution contains methylene chloride.