Solid dispersion pharamaceutical formulations

• US 7,364,752 B1
• Filed: 11/10/2000
• Issued: 04/29/2008
• Est. Priority Date: 11/12/1999
• Status: Expired due to Term

• Current Assignee: Abbvie Incorporated
• Original Assignee: Abbott Laboratories Incorporated
• Inventors: Qiu, Yihong, Krill, Steven L., Schmitt, Eric A., Fort, James J., Law, Devalina, Porter, William R.
• Primary Examiner(s): RUSSEL, JEFFREY E
• Application Number:
  US09/709,829
• Time in Patent Office: 2,727 Days
• Field of Search: 424/455, 424/464, 424/484, 424/486, 514/274, 514/365, 514/772, 514/772.3, 514/937
• US Class Current: 424/455
• CPC Class Codes: A61K 31/425 Thiazoles
• CPC Class Codes: A61K 31/505 Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
• CPC Class Codes: A61K 9/1641 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
• CPC Class Codes: A61K 9/167 with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface with further drug-free outer coating A61K9/5073
• CPC Class Codes: A61K 9/2072 characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms A61K9/0004, A61K9/0056, A61K9/0065 take precedence

Abstract

A pharmaceutical composition is disclosed which comprises a solid dispersion of an HIV protease inhibitor in a water soluble carrier, such as PEG, having enhanced bioavailability and improved dissolution properties. The solid dispersion may optionally be encapsulated in hard gelatin capsules, compressed into a tablet, or may be granulated with a pharmaceutically acceptable granulating agent. Also disclosed are methods of making said solid dispersion and methods of treating an HIV infection employing said solid dispersion.

Claims

1. A pharmaceutical composition comprising ritonavir, wherein ritonavir in said composition is formulated as a solid dispersion of amorphous ritonavir in a matrix including a water soluble polymer.

2. A pharmaceutical composition of claim 1, comprising a gelatin capsule which encapsulates said solid dispersion.

3. A pharmaceutical composition of claim 1 which is a tablet comprising said solid dispersion.

4. The pharmaceutical composition of claim 1, wherein said water soluble polymer is PEG.

5. The pharmaceutical composition of claim 1, wherein said water soluble polymer is PEG 8000.

6. The pharmaceutical composition of claim 1, wherein said solid dispersion further comprises (2S,3S,5S)-2-(2,6-dimethylphenoxyacetyl)amino-3-hydroxy-5-[2S-(1-tetrahydro-pyrimid-2-onyl)-3-methylbutanoyl]amino-1,6-diphenylhexane (ABT-378).

7. The pharmaceutical composition of claim 1, further comprising a pharmaceutically-acceptable filler, diluent, lubricant or disintegrant.

8. The pharmaceutical composition of claim 1, wherein said solid dispersion is ground and formulated into a delivery system.

9. A method of treating an HIV infection comprising administering a pharmaceutical composition of claim 1 to a mammal in need of such treatment.

10. A method of treating an HIV infection comprising administering the pharmaceutical composition of claim 6 to a mammal in need of such treatment.