Preparation Method of Sustained-Release Microcapsules Having Good Initial Burst Inhibiting Property and the Microcapsules Thereby

• US 20100272820A1
• Filed: 11/21/2007
• Published: 10/28/2010
• 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, Se-Yeon, Park, Mork-Soon, Cha, Kyung-Hoi, Jung, Hyung-Joon, Jung, Goo-Young, Kim, Jung-Kwoun
• Granted Patent: US 8,541,030 B2
• Time in Patent Office: Days
• 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 a bioactive substance, a biocompatible polymer and polyvinylpyrrolidone to an aqueous solution to provide the sustained-release microcapsules.

2. The method of claim 1, wherein the emulsion is prepared by

mixing a first non-aqueous solution containing a bioactive substance and a second non-aqueous solution containing a biocompatible polymer and polyvinylpyrrolidone.

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

4. The method of claim 1, wherein the biocompatible polymer has a molecular weight of about 60,000 or less.

5. The method of claim 1, wherein the aqueous solution includes a salt.

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

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

8. The method of claim 1, wherein the bioactive substance comprises octreotide or a salt thereof.

17. The method of claim 2, wherein the bioactive substance comprises octreotide or a salt thereof.

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

adding an emulsion containing a bioactive substance and a biocompatible polymer to an aqueous solution containing a salt to provide the sustained-release microcapsules.

10. The method of claim 9, wherein the emulsion is prepared by mixing a first non-aqueous solution containing a bioactive substance and a second non-aqueous solution containing a biocompatible polymer.

11. The method of claim 9, wherein the biocompatible polymer is polylactide-co-glycolide or poly(lactide-co-glycolide)glucose.

12. The method of claim 9, wherein the biocompatible polymer has a molecular weight of about 60,000 or less.

13. The method of claim 9, wherein the salt is sodium chloride.

14. The method of claim 10, wherein the first non-aqueous solution contains methanol.

15. The method of claim 10, wherein the second non-aqueous solution contains methylene chloride.

16. The method of claim 9, wherein the bioactive substance comprises octreotide or a salt thereof.

18. The method of claim 10, wherein the bioactive substance comprises octreotide or a salt thereof.

19. A method for preparing sustained-release octreotide microcapsules comprising:

mixing a first non-aqueous solution containing octreotide and methanol and a second non-aqueous solution containing a biocompatible polymer having a molecular weight of about 60,000 or less, polyvinylpyrrolidone and methylene chloride, to provide an emulsion; and

adding the emulsion to an aqueous solution to provide the sustained-release octreotide microcapsules,

wherein the biocompatible polymer is selected from;

polylactide-co-glycolide and poly(lactide-co-glycolide)glucose.

20. The method of claim 19, wherein the aqueous solution contains a salt.