# US 8,541,030 B2 · Preparation method of sustained-release microcapsules having initial burst inhibiting property and the microcapsules thereby

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- Number: US 8,541,030 B2
- Document ID: US8541030B2
- Status: Granted
- Kind: B2
- Application number: 12/516,275
- Filed: 2007-11-21
- Published: 2010-10-28
- Granted: 2013-09-24
- Earliest claimed: 2006-11-27
- Assignees: Dongkook Pharmaceutical Co., Ltd.
- Applicants: Nak-Hyun Lim; Jung-Kwoun Kim; Hyung-Joon Jung; Se-Yeon Kim; Goo-Young Jung; Kyung-Hoi Cha; Mork-Soon Park
- Inventors: Nak-Hyun Lim; Jung-Kwoun Kim; Hyung-Joon Jung; Se-Yeon Kim; Goo-Young Jung; Kyung-Hoi Cha; Mork-Soon Park
- Web page: https://patentgrep.com/patent/US8541030B2

## CPC

- B01J 13/02: Making microcapsules or microballoons {(for medical preparations A61K9/50)}
- A61P 5/02: of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- B01J: CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## 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

### Claim 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.

### Claim 2 (depends on 1)

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.

### Claim 3 (depends on 1)

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

### Claim 4 (depends on 1)

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

### Claim 5 (depends on 2)

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

### Claim 6 (depends on 2)

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