Stable shaped particles of crystalline organic compounds

• US 6,287,693 B1
• Filed: 02/25/1998
• Issued: 09/11/2001
• Est. Priority Date: 02/25/1998
• Status: Expired due to Term

• Current Assignee: Skendi Finance, Ltd.
• Original Assignee: John Claude Savoir
• Inventors: Gomez, Abraham, Savoir, John-Claude, Angeles, Juan, De Gyves, Aurelio
• Primary Examiner(s): LE, HOA T
• Application Number:
  US09/030,388
• Time in Patent Office: 1,294 Days
• Field of Search: 428/357, 428/402, 428/402.24, 424/401, 424/408, 424/439, 424/451, 424/455, 424/457, 424/458, 424/465, 424/469, 424/470, 424/489, 424/459
• US Class Current: 428/402
• CPC Class Codes: A61K 9/1688 resulting in pure drug agglomerate optionally containing up to 5% of excipient
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 5/30 Oestrogens
• CPC Class Codes: Y10T 428/2982 Particulate matter [e.g., sphere, flake, etc.]
• CPC Class Codes: Y10T 428/2989 Microcapsule with solid core [includes liposome]

Abstract

The present invention provides storage stable, shaped particles of allotropic organic compounds. The particles of the present invention can be shaped according to the desired application. Preferred shapes of such particles are microspheres, particularly those having diameters of about 1 to about 1,000 microns. The stable shaped particles of the present invention are particularly well-suited to the fabrication of pharmaceutical formulations, particularly where sustained release and uniform bioavailability are desired. The storage stable particles are formed by a solid state crystallization of allotropic organic compounds. The solid state crystallization process of the present invention affords a means for achieving a storage stable crystalline form of said allotropic compound without loss or deterioration of the original particle dimensions.

Claims

1. A plurality of storage stable particles of uniform shape consisting essentially of a plurality of allotropic organic compounds, wherein each of said allotropic organic compounds consists of a uniform crystalline character and a plurality of crystalline domains;

said organic compounds retaining said crystalline character, and said particles retaining said uniform shape on storage in aqueous media for at least about one month.

2. The particles of claim 1, wherein the uniform shape of the particles is selected from the group consisting of sphere, spheroid, and cylinder.

3. The particles of claim 1, wherein the particles are in the shape of a sphere of diameter of between about 1 and about 1,000 microns.

4. The particles of claim 1, wherein the particles are in the shape of a sphere of diameter of between about 10 and about 300 microns.

5. The particles of claim 1, wherein the desired crystalline form of at least one of said allotropic organic compounds is a hydrate.

6. The particles of claim 1, wherein at least one of said allotropic organic compounds is a steroid or sterol.

7. The particles of claim 6, wherein said steroid or sterol is selected from the group consisting of 17 β

-estradiol, estrogen, testosterone, progesterone, cholesterol, and mixtures thereof.

8. The particles of claim 1, wherein at least one of said allotropic organic compounds is astemizole, cisapride or oxatomide.

9. The particles of claim 1, wherein said particles are in the shape of a cylinder of length of about 1,000 to 5,000 microns and a diameter of about 500 to 1,000 microns.

10. The particles of claim 1, wherein one or more of said compounds is a steroid or sterol, and one or more of said compounds is selected from the group consisting of oxatomide, nifedipine, astemizole, and cisapride.

11. The particles of claim 1, wherein one of said allotropic organic compounds is cholesterol.