Stable shaped particles of crystalline organic compounds

• US 6,663,895 B2
• Filed: 05/29/2002
• Issued: 12/16/2003
• Est. Priority Date: 02/25/1998
• Status: Expired due to Term

• Current Assignee: Skendi Finance, Ltd.
• Original Assignee: John-Claude Savoir
• Inventors: Savoir, John-Claude, Gomez, Abraham, Angeles, Juan, De Gyves, Aurelio
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Pulliam, Amy E
• Application Number:
  US10/156,079
• Publication Number:
  US 20020168395A1
• Time in Patent Office: 566 Days
• Field of Search: 424/408, 424/439, 424/451, 424/457, 424/458, 424/465, 424/469, 424/470, 424/489, 428/402
• US Class Current: 424/489
• 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 and size consisting essentially of an allotropic organic compound wherein said allotropic organic compound consists of a uniform crystalline character and a plurality of crystalline domains;

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

2. The particles of claim 1, wherein the desired crystalline form of the allotropic organic compound is a hydrate.

3. The particles of claim 1, wherein the allotropic organic compound is a steroid or sterol.

4. The particles of claim 3, wherein said steroid or sterol is selected from the group consisting of 17β

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

5. The particles of claim 1, wherein said allotropic organic compound is selected from the group consisting of oxatomide, nifedipine, astemizole, and cisapride.

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

7. 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.

8. The particles of claim 1, wherein said particles are in the shape of a sphere, spheroid, rod, or cube.