Claims
- 1. A microparticle consisting essentially of: a molecular cluster of water-insoluble organic substance with ionizable groups capable of imparting a net charge, complexed with a layer of polyelectrolyte with ionizable groups capable of imparting a net charge opposite that of the organic substance, whereby said microparticle comprises a non-zero net charge and is stably dispersible in water.
- 2. A microparticle of claim 1, wherein the microparticle is 0.03-5 microns in size.
- 3. A microparticle of claim 2, wherein the microparticle is 0.5-2 microns in size.
- 4. A microparticle of claim 1, wherein the organic substance is a pharmaceutical.
- 5. A microparticle of claim 4, wherein the pharmaceutical is selected from the group consisting of dexiniguldipine, clofazimine and miconazole.
- 6. A microparticle of claim 1, wherein the organic substance is an organic pigment.
- 7. A microparticle of claim 1, wherein the polyelectrolyte is a polymeric acid.
- 8. A microparticle of claim 1, wherein the polyelectrolyte has a molecular weight in the range of 400 to 2,000,000 daltons.
- 9. A microparticle of claim 1, wherein the polyelectrolyte is selected from the group consisting of acidic polysaccharides, basic polysaccharides, acidic polypeptides, basic polypeptides, acidic proteins, and basic proteins.
- 10. A microparticle of claim 1, wherein the polyelectrolyte is selected from the group consisting of: polymeric carboxylic acid, polyacrylic acid, chondroitin sulfate, and dextran sulfate.
- 11. A method to make stable aqueous colloidal dispersions of ionizable, poorly-water-soluble organic substances, comprising:
- a.) dissolving a poorly-water-soluble organic substance in a suitable water-miscible organic solvent;
- b.) dissolving a polyelectrolyte of an opposite charge to that of the organic substance in a suitable aqueous solution;
- c.) mixing solutions formed from steps a.) and b.) to form a colloidal phase and a solvent phase;
- d.) separating colloidal phase of step c.) from the solvent and excess polyelectrolyte; and
- f.) resuspending the colloidal phase in a suitable aqueous solution.
- 12. A method of claim 11, which further comprises the steps of
- g.) lyophilizing the resuspended colloidal phase; and
- h.) reconstituting lyophilized colloidal phase in a suitable aqueous vehicle for medical administration.
- 13. A method of claim 12, wherein the organic substance is a pharmaceutical.
- 14. A method of claim 13, wherein the organic substance is selected from the group consisting of: dexniguldipine, clofazime, and miconazole.
- 15. A method of claim 4, wherein the polyelectrolyte is a polymeric acid.
- 16. A method of claim 15, wherein the polyelectrolyte is selected from the group consisting of: polyacrylic acid, chondroitin sulfate, and dextran sulfate.
Parent Case Info
This application claims benefit of U.S. Provisional Application Ser. No. 60/027,594, filed on Oct. 3, 1997.
US Referenced Citations (4)
Number |
Name |
Date |
Kind |
4963367 |
Ecanow |
Oct 1990 |
|
5286493 |
Oshlack et al. |
Feb 1994 |
|
5651991 |
Sugiyama et al. |
Jul 1997 |
|
5853698 |
Straub et al. |
Dec 1998 |
|
Foreign Referenced Citations (1)
Number |
Date |
Country |
0 169 618 B2 |
Nov 1993 |
EPX |