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Preparation of submicron solid particle suspensions by sonication of multiphase systems

a multi-phase system and solid particle technology, applied in the direction of microcapsules, macromolecular non-active ingredients, chemical/physical processes, etc., can solve the problems of spontaneous formation of microencapsulated products, irritation at the site of delivery, and unstable emulsions

Inactive Publication Date: 2005-02-17
BAXTER INT INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0016] The present invention provides a method for preparing submicron sized particles. The method includes the steps of: (1) providing a multiphase system having an organic phase and an aqueous phase, the organic phase having a pharmac...

Problems solved by technology

The fact that poorly soluble drugs can pose difficulties in this area has resulted in the need for new technologies that can address this obstacle.
Such emulsions, however, tend to be unstable given the predominance of the oil phase and the absence of antimicrobial agents.
In other instances, even where the pharmacological agent is successfully incorporated into an oil-free formulation, particles containing the pharmacological agent may cause irritation at the site of delivery because of their size or form.
This mixture is introduced into an effective amount of a miscible nonsolvent, thereby causing spontaneous formation of the microencapsulated product.

Method used

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  • Preparation of submicron solid particle suspensions by sonication of multiphase systems
  • Preparation of submicron solid particle suspensions by sonication of multiphase systems
  • Preparation of submicron solid particle suspensions by sonication of multiphase systems

Examples

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example 1

Preparation of a 0.5% Itraconazole Suspension Using a 1:10 Ratio of O / W

[0042] A 5% lecithin / glycocholate surfactant solution was prepared (100 mL) and combined with 10 mL of a chloroform solution containing itraconazole (0.5 grams). The resulting mixture was manually shaken to generate a crude emulsion and set in an ice bath to chill. After cooling for 5 minutes the emulsion was sonicated every other minute for 10 minutes (5 minutes total sonication time at 40% power using a ½″ probe at 20 kHz) and then rotovapped at ˜120 Torr (no heat) to remove the chloroform. The resulting solid particle dispersion was analyzed by light scattering detection (HORIBA) which revealed particles having a mean diameter of 97.78 nm.

example 2

Preparation of a 1.0% Itraconazole Suspension Using a 1:5 Ratio of O / W

[0043] A 5% lecithin / glycocholate surfactant solution was prepared (50 mL) and combined with 5 mL of a chloroform solution containing itraconazole (0.5 grams). The resulting mixture was manually shaken to generate a crude emulsion and set in an ice bath to chill. After cooling for 5 minutes the emulsion was sonicated every other minute for 10 minutes (5 minutes total sonication time) and then rotovapped at ˜100 Torr (no heat) to remove the chloroform. The resulting solid particle dispersion was analyzed by light scattering detection (HORIBA) which revealed particles having a mean diameter of 135 nm.

example 3

[0044] The process described in example 1 was repeated with the resulting particles having a mean diameter of 139 nm. This suspension was further analyzed by scanning electron microscopy to reveal solid spherical particles less than 200 nm in size. See FIG. 2.

[0045]FIG. 2 reveals the spherical nature of the particles produced. The sample was prepared by filtration of a small portion o the suspension through a 80 nm filter and using standard SEM sample preparation techniques. Analysis of particles produced by this process revealed the particles to be completely amorphous as determined by x-ray powder diffraction.

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Abstract

The present invention provides a method for preparing submicron-sized particles. The method includes the steps of: (1) providing a multiphase system having an organic phase and an aqueous phase, the organic phase having a pharmaceutically effective compound therein; and (2) sonicating the system to evaporate a portion of the organic phase to cause precipitation of the compound in the aqueous phase and having an average effective particle size of less than about 2 m.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS [0001] Not Applicable. FEDERALLY SPONSORED RESEARCH OR DEVELOPMENT [0002] Not Applicable. TECHNICAL FIELD [0003] The present invention provides a multistep process for generating submicron-sized particles of water insoluble organic compounds and more particularly a process for preparing submicron-sized particles of a pharmaceutically effective compound by sonicating a multiphase liquid. BACKGROUND OF THE INVENTION [0004] Background Art [0005] The ability to deliver pharmaceutical medications in a water-soluble formulation is a critical concern in therapeutic drug development. The fact that poorly soluble drugs can pose difficulties in this area has resulted in the need for new technologies that can address this obstacle. One solution to this problem is the production of extremely small particles of the insoluble drug candidate and the creation of a microparticulate suspension. In this way, drugs that were previously unable to be formulated in ...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K9/51A61K31/496A61K9/14A61K45/00A61K47/10A61K47/12A61K47/14A61K47/18A61K47/20A61K47/24A61K47/28A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42
CPCA61K9/5192A61K9/5169
Inventor BRYNJELSEN, SEANSTERNBERG, SHMUELDUNHAM, ANDY
Owner BAXTER INT INC
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