IP Library Patent Application 11189139
Patent Application
App. No. 11/189,139

Applicatin of a bioactive agent in a solvent composition to produce a target particle morphology

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Quick Facts
Patent No.
US None
App. No.
11/189,139
Abstract

A selected morphology for a deposited bioactive agent can be obtained by selecting solvent composition, preparing a solution of the bioactive agent in the solvent composition, and applying the bioactive agent to a substrate as a plurality of droplets so that evaporation of the applied solution produces particles having the target particle morphology.

Claims (45)

1 . A method of preparing a deposited bioactive agent having a selected morphology, the method comprising:

selecting a solvent composition based on a target particle morphology;

preparing a solution of the bioactive agent in the selected solvent composition;

applying the bioactive agent solution to a substrate as a plurality of droplets;

wherein evaporation of the applied bioactive agent solution produces particles of the bioactive agent having the target morphology.

2 . The method of claim 1 , wherein the selected solvent composition includes at least two solvent components.

3 . The method of claim 2 , wherein the at least two solvent components are selected so that the bioactive agent has differential solubility in the solvent components.

4 . The method of claim 2 , wherein the at least two solvent components are miscible in the solvent composition.

5 . The method of claim 2 , wherein the two solvent components each have a boiling point below 90° C.

6 . The method of claim 1 , wherein the solvent composition includes at least one solvent selected from the group consisting of chloroform, tetrabromoethane, tetrachloroethylene, trichlorethylene, trichloroacetic acid, trichloroethane, 1,2-dichloroethane, trichloroethylene, bromoform, tetrahydrofuran, and toluene; and at least one solvent selected from the group consisting of ethanol, propanol, isopropanol, butanol, and isobutanol.

7 . The method of claim 1 , wherein the solvent composition includes at least one solvent selected from the group consisting of ethanol, propanol, isopropanol, butanol, and isobutanol.

8 . The method of claim 1 , wherein the solvent composition includes ethanol and chloroform.

9 . The method of claim 8 , wherein the solvent composition includes ethanol and chloroform in a ratio of between about 70:30 and 90:10.

10 . The method of claim 8 , wherein the solvent composition includes ethanol and chloroform in a ratio of about 80:20.

11 . The method of claim 1 , wherein preparing a solution of the bioactive agent includes preparing a solution of the bioactive agent and an additive in the solvent composition.

12 . The method of claim 11 , wherein the additive is a polymer additive.

13 . The method of claim 1 , wherein the substrate is selected to have a substantially impermeant surface character.

14 . The method of claim 1 , wherein applying the bioactive agent to the substrate includes applying the solution with a thermal ejection element or piezoelectric ejection element.

15 . The method of claim 1 , wherein the target particle morphology includes a desired crystalline form.

16 . The method of claim 1 , wherein the target particle morphology includes an amorphous form.

17 . The method of claim 1 , wherein the target particle morphology includes a target particle size.

18 . The method of claim 17 , wherein the target particle size is less than about 1 μm.

19 . A method of preparing nanoparticles of a bioactive agent, the method comprising:

preparing a solution of the bioactive agent in a solvent composition having at least two solvents; and

applying the solution to a substrate as a plurality of droplets;

wherein evaporation of the applied solution produces nanoparticles of the bioactive agent.

20 . The method of claim 19 , wherein the solvent composition includes a halocarbon solvent and an alcohol.

21 . The method of claim 19 , where the solution includes a polymer additive.

22 . The method of claim 19 , wherein applying the solution to a substrate includes applying the solution to a polyfluorinated polymer substrate, a paraffin substrate, or a glass substrate.

23 . The method of claim 19 , wherein the substrate is a nonpolar substrate, and a drop of the solution exhibits a contact angle of less than about 90 degrees on the substrate.

24 . The method of claim 19 , wherein the bioactive agent is a medicament.

25 . The method of claim 24 , wherein the bioactive agent is selected from a group consisting of glyburide, digoxin, prednisolone, lovastatin, and indomethacin.

26 . A method of preparing amorphous nanoparticles of a bioactive agent, the method comprising:

preparing a solution of the bioactive agent in a composition of ethanol and chloroform; and

applying the solution to a substantially impermeant substrate as a plurality of droplets;

wherein evaporation of the applied bioactive agent solution produces at least substantially amorphous nanoparticles of the bioactive agent.

27 . The method of claim 26 , wherein the solution of the bioactive agent includes a polymer additive, and evaporation of the applied solution produces nanoparticles in which the polymer additive and the bioactive agent are dispersed throughout the nanoparticle volume.

28 . The method of claim 26 , wherein the bioactive agent is selected from a group consisting of glyburide, digoxin, prednisolone, lovastatin, and indomethacin.

29 . A method of preparing particles of a bioactive agent, the method comprising:

selecting a target particle morphology;

preparing a first solution of the bioactive agent in a first solvent composition;

applying the solution to a substrate as a plurality of droplets to create particles of the bioactive agent having the target particle morphology;

preparing a second solution of the bioactive agent in a second solvent composition;

applying the second solution to the particles.

30 . The method of claim 29 wherein the first solvent composition and the second solvent composition are different.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 25, 2005
From: CHINEA, VANESSA I.; KANE, KEVIN MICHAEL; RUIZ, ORLANDO
To: HEWLETT-PACKARD DEVELOPMENT COMPANY, L.P.
Reel/Frame 016818/0515 →