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Formulation Comprising Bioactive Agents And Method Of Using Same

a technology of bioactive agents and forms, which is applied in the field of compositions containing bioactive agents, can solve the problems of affecting the development of pharmaceutical compositions containing this protein, and affecting the development of pharmaceutical compositions

Inactive Publication Date: 2012-01-05
WYETH LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The method enables the preparation of stable BMP-2 microparticles that maintain biological activity, facilitating increased BMP-2 levels in subjects, effectively treating bone-related conditions and wound healing by providing a bioactive form of the protein.

Problems solved by technology

Protein instability can be a major difficulty in preparing these pharmaceutical compositions.
Unwanted stresses on the protein during preparation of a pharmaceutical formulation can result in unwanted effects such as protein denaturation, precipitation, or adsorption to surfaces.
This limited solubility can hinder attempts to develop pharmaceutical compositions containing this protein.

Method used

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  • Formulation Comprising Bioactive Agents And Method Of Using Same
  • Formulation Comprising Bioactive Agents And Method Of Using Same
  • Formulation Comprising Bioactive Agents And Method Of Using Same

Examples

Experimental program
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Effect test

example 1

Preparation of BMP-2 Microparticles

[0073]A BMP-2 microparticle is prepared by mixing a first solution containing BMP-2 protein with a second, precipitating solution.

[0074]The first solution includes rhBMP-2 at a concentration of 0.1 to 2 mg / ml and is at pH 4.5. The second solution is formulated so that upon being added at one-tenth volume (relative to the volume of the first solution), the BMP-2 protein will precipitate and the final pH of the combined solution is pH 7.4. The second solution includes 1120 mM NaCl, 300 mM NaHCO3, 11 mM NaH2PO4, 5.5 mM Na2SO4, 40 mM NaOH and purified water.

[0075]The precipitation is performed by adding 10% (volume / volume) of a precipitating solution which contains both physiological salt and pH adjustment. The precipitation is performed in sterile tubes (15 or 50 ml), depending on the required volume. The filling of the 50 ml tube with BMP stock solution is limited to 30 ml to have enough space for the creation of a turbulent solution by using the vor...

example 2

Assessment of BMP-2 Microparticle Size

[0078]BMP-2 microparticle diameter was assessed using a MALVERN MASTERSIZER X® instrument (Malvern Instruments Ltd., Malvern, UK) with a sample cell designed for volumes of 4 to 5 ml. Mixing of a rhBMP-2 solution with a stock solution was used to generate physiologic salt concentrations.

[0079]The range in particle diameter in populations of microparticles subjected to equilibration for various lengths of time is shown in FIGS. 1-3. FIG. 1 shows the size distribution obtained in two batches microparticles equilibrated for less than ten minutes. Most particles are smaller then 10 μm in diameter, with a peak detected for microparticles of 5 μm to 6 μm in diameter.

[0080]FIG. 2 shows the size distribution obtained for three batches of microparticles equilibrated for between 10 and 110 minutes. While 6 μm to 9 μm are the most common size ranges, a higher number of microparticles with diameters greater than 10 μm are detected as compared to the distrib...

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Abstract

Disclosed are methods of making bioactive BMP-2 microparticles and methods of using the microparticles.

Description

RELATED APPLICATIONS[0001]This application is a continuation of U.S. patent application Ser. No. 10 / 361,263, filed Feb. 10, 2003, which claims priority to U.S. Provisional Patent Application Ser. No. 60 / 355,135, filed Feb. 8, 2002. The contents of this application are incorporated herein by reference in their entirety.FIELD OF THE INVENTION[0002]The invention relates generally to compositions containing bioactive agents such as bone morphogenetic protein-2 (BMP-2) and methods of making and using these compositions.BACKGROUND OF THE INVENTION[0003]Proteins used as therapeutic agents are typically provided as pharmaceutical compositions that can vary depending on, for example, the properties of the protein and the manner in which it will be introduced into a patient.[0004]Protein instability can be a major difficulty in preparing these pharmaceutical compositions. Unwanted stresses on the protein during preparation of a pharmaceutical formulation can result in unwanted effects such as...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K38/18A61P19/08A61P25/00A61P1/02A61P17/02C07K14/51A61P19/10A61K9/14A61K9/08A61K9/16A61K9/19A61K38/00A61K47/02A61K47/34A61L27/00A61P19/00
CPCA61K9/1688Y10T428/2982A61K38/1875A61K9/1694A61P1/02A61P17/02A61P19/00A61P19/08A61P19/10A61P25/00
Inventor SOFIA, SUSAN J.SCHWARTZ, DANIELFRIESS, WOLFGANG
Owner WYETH LLC