Method of grinding pharmaceutical substances

• US 5,518,187 A
• Filed: 01/12/1994
• Issued: 05/21/1996
• Est. Priority Date: 11/25/1992
• Status: Expired due to Term

• Current Assignee: Alkermes Pharma Ireland Limited (Alkermes plc)
• Original Assignee: Nano Systems, Inc.
• Inventors: Doty, Brian D., Gustow, Evan, Bruno, Joseph A., Rajagopalan, Nats, Sarpotdar, Pramod, Illig, Kathleen J.
• Primary Examiner(s): Eley, Timothy V.
• Application Number:
  US08/180,827
• Time in Patent Office: 860 Days
• Field of Search: 241/5, 241/21, 241/22, 241/30, 241/170-184, 424/63, 424/165.1, 424/489
• US Class Current: 241/5
• CPC Class Codes: A61K 9/14 Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51
• CPC Class Codes: A61K 9/146 with organic macromolecular compounds
• CPC Class Codes: A61K 9/1688 resulting in pure drug agglomerate optionally containing up to 5% of excipient
• CPC Class Codes: G03C 1/005 Silver halide emulsions; Preparation thereof; Physical treatment thereof; Incorporation of additives therein catalytic amounts of silver halide in dry silver systems or thermographic systems using noble metal compounds G03C1/494
• CPC Class Codes: Y10S 977/775 Nanosized powder or flake, e.g. nanosized catalyst
• CPC Class Codes: Y10S 977/788 Of specified organic or carbon-based composition
• CPC Class Codes: Y10S 977/90 having step or means utilizing mechanical or thermal property, e.g. pressure, heat
• CPC Class Codes: Y10S 977/928 X-ray agent

Abstract

A method of preparing particles of a drug substance or diagnostic imaging agent which comprises grinding the drug substance or imaging agent in the presence of grinding media comprising a polymeric resin. The method provides particles exhibiting reduced contamination.

Claims

1. A method of preparing particles of a diagnostic imaging agent by grinding said agent with rigid grinding media to reduce said particles to submicron size, wherein said grinding media has a substantially spherical shape, has a particle size range of 0.1 to 3 mm and comprises a polymeric resin.

2. The method of claim 1 wherein said grinding media comprises particles containing a core having adhered thereon a coating of said polymeric resin.

3. The method of claim 1 wherein said polymer is polystyrene crosslinked with divinyl benzene.

4. The method of claim 1 wherein said polymer is polycarbonate.

5. The method of claim 1 wherein said method is a wet grinding process.

6. The method of claim 1 wherein said method is a dry grinding process.

7. The method of claim 1 wherein said grinding takes place in a mill selected from an airjet mill, a roller mill, a ball mill, an attritor mill, a vibratory mill, a planetary mill, a sand mill, and a bead mill.

8. The method of claim 1 wherein said imaging agent is WIN 8883.

9. A method of preparing particles of a drug substance by grinding said substance with rigid grinding media to reduce said particles to submicron size, wherein said grinding media has a substantially spherical shape, has a particle size range of 0.1 to 3 mm and comprises a polymeric resin.

10. The method of claim 9 wherein said grinding media comprises particles containing a core having adhered thereon a coating of said polymeric resin.

11. The method of claim 9 wherein said polymer is polystyrene crosslinked with divinyl benzene.

12. The method of claim 9 wherein said polymer is polycarbonate.

13. The method of claim 9 wherein said method is a wet grinding process.

14. The method of claim 9 wherein said method is a dry grinding process.

15. The method of claim 9 wherein said grinding takes place in a mill selected from an airjet mill, a roller mill, a ball mill, an attritor mill, a vibratory mill, a planetary mill, a sand mill, and a bead mill.

16. The method of claim 9 wherein said drug substance is naproxen.