Process for preparing solid formulations of lipid regulating agents with enhanced dissolution and absorption

• US 6,368,622 B2
• Filed: 01/29/1999
• Issued: 04/09/2002
• Est. Priority Date: 01/29/1999
• Status: Expired due to Term

• Current Assignee: Abbvie Incorporated
• Original Assignee: Abbott Laboratories Incorporated
• Inventors: Chen, Yisheng, Reiland, Thomas L., Engh, Kevin R., Qiu, Yihong
• Primary Examiner(s): Spear, James M.
• Application Number:
  US09/240,515
• Publication Number:
  US 20010006655A1
• Time in Patent Office: 1,166 Days
• Field of Search: 424/451, 424/452, 424/464, 424/465
• US Class Current: 424/464
• CPC Class Codes: A61K 31/216 of acids having aromatic rings, e.g. benactizyne, clofibrate
• CPC Class Codes: A61K 9/1694 resulting in granules or microspheres of the matrix type containing more than 5% of excipient
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds

Abstract

A process for preparing a solid formulation of a lipid-regulating agent comprising forming a mixture of said lipid-regulating agent with a surfactant; granulating said mixture by melting, mixing, and congealing said mixture; and optionally forming a finished dosage form.

Claims

1. A process for preparing a solid formulation of a fibrate having more rapid dissolution comprising the steps of:

forming a mixture of said fibrate with a surfactant;

granulating said mixture by melting, mixing, and congealing said fibrate and said surfactant,

optionally with one or more excipients;

and optionally forming a finished dosage form.

4. A process of claim 1 wherein said surfactant is selected from the group consisting of sodium lauryl sulfate, poloxamer polyols, block copolymers of ethylene oxide and propylene oxide, d-alpha tocopheryl polyethylene glycol succinate and polyoxyl 40 stearate.

5. The process of claim 4 wherein said surfactant is polyoxamer polyols.

6. A process of claim 1 further comprising adding one or more excipients to the granulated mixture.

7. A process of claim 6 wherein the excipient is a pharmaceutically-acceptable excipient selected from the group consisting of lactose, starch, polyvinyl pyrrolidone and magnesium stearate.

8. A process of claim 1 wherein the granulated mixture is milled.

9. A process of claim 1 further comprising preparing a finished dosage form.

11. A process of claim 9 where the finished dosage form is a capsule.

12. A composition prepared by the process of claim 1.

14. A method for treating of hyperlipidemia comprising the administration of a formulation prepared by the process of claim 1.

2. A process for preparing a solid formulation of a fibrate comprising the steps of:

forming a mixture of said fibrate with a surfactant;

granulating said mixture by melting, mixing, and congealing,

optionally with one or more excipients;

and optionally forming a finished dosage form.

3. A process of claim 2 wherein the fibrate is fenofibrate.

13. A composition prepared by the process of claim 3.

15. A method for treating of hyperlipidemia comprising the administration of a formulation prepared by the process of claim 3.

10. A process for preparing a solid formulation of a fibrate having more rapid dissolution comprising the steps of:

forming a mixture of said fibrate with a surfactant;

granulating said mixture by melting, mixing, and congealing, said fibrate and said surfactant,

optionally with one or more excipients;

and forming a tablet.