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Claims for Patent: 6,730,679

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Claims for Patent: 6,730,679

Title: Pharmaceutical formulations
Abstract:Pharmaceutical formulations containing HIV protease inhibitors, specifically including 3S-[3R*(1R*,2S*)]-[3-[[(4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2- hydroxy-1-phenylmethyl)propyl]carbamic acid, tetrahydro-3-furanyl ester (alternatively known as VX 478 or 141W94), and a tocopherol, and their use in medical therapy are described.
Inventor(s): Roy; Arup K. (Greenville, NC), Tillman; Lloyd Gary (Carlsbad, CA)
Assignee: SmithKline Beecham Corporation (Philadelphia, PA)
Application Number:08/820,848
Patent Claims: 1. A pharmaceutical formulation possessing unexpectedly enhanced bio-availability, comprising: a) 3S-[3R*(1R*,2S*)]-[3-[[4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-h ydroxy-1-phenylmethyl)propyl]carbamic acid, tetrahydro-3-furanyl ester, b) a water soluble tocopherol derivative, and (c) a hydrophilic non-aqueous solvent miscible with said water soluble tocopherol derivative.

2. A pharmaceutical formulation as claimed in claim 1, comprising at least 20% of the water soluble tocopherol derivative.

3. A pharmaceutical formulation as claimed in claim 1, wherein the ratio of (a) to (b) is from about 1:0.5 to about 1:3 w/w.

4. A pharmaceutical formulation as claimed in claim 1, wherein the water soluble tocopherol derivative is Vitamin E-TPGS.

5. A pharmaceutical formulation as claimed in claim 1, in the form of a capsule.

6. A pharmaceutical formulation as claimed in claim 1, comprising 3S-[3R*(1R*, 2S*)]-[3-[[4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-hydroxy-1-phe nylmethyl)propyl]carbamic acid, tetrahydro-3-furanyl ester in an amount of about 10 to about 1500 mg.

7. A pharmaceutical formulation as claimed in claim 1, wherein the hydrophillic non-aqueous solvent is a mixture of a polyethylene glycol and propylene glycol.

8. A pharmaceutical formulation as claimed in claim 1, in the form of a solution.

9. A pharmaceutical formulation as claimed in claim 1, comprising 3S-[3R*(1R*, 2S*)]-[3-[[4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-hydroxy-1-phe nylmethyl)propyl]carbamic acid, tetrahydro-3-furanyl ester in an amount of about 10 to about 1500 mg.

10. The pharmaceutical formulation of claim 1, wherein the water soluble tocopherol derivative is Vitamin E-TPGS.

11. A pharmaceutical formulation, comprising: a) 3S-[3R*(1R*,2S*)]-[3-[[4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-h ydroxy-1-phenylmethyl) propyl]carbamic acid, tetrahydro-3-furanyl ester, b) from about 10% to about 60% w/w of a water soluble tocopherol derivative, and (c) a hydrophilic non-aqueous solvent miscible with said water soluble tocopherol derivative,

wherein the ratio of (a) to (b) is from about 1:0.5 to about 1:10 w/w, and wherein said formulation possesses unexpectedly enhanced bioavailability.

12. A pharmaceutical formulation as claimed in claim 11, in the form of a soft gelatin capsule.

13. A pharmaceutical formulation, comprising: (a) 3S-[3R*(1R*,2S*)]-[3-[[4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-h ydroxy-1-phenylmethyl)propyl]carbamic acid, tetrahydro-3-furanyl ester, (b) Vitamin E-TPGS, (c) polyethylene glycol, and (d) propylene glycol, and

wherein said formulation possesses unexpectedly enhanced bioavailability.

14. A pharmaceutical formulation as claimed in claim 13, in the form of a soft gelatin capsule.

15. The pharmaceutical formulation according to claim 13, which comprises from about 10% to about 60% w/w of Vitamin E-TPGS.

16. The pharmaceutical formulation according to claim 13, wherein said formulation is a flowable liquid.

17. The pharmaceutical formulation according to claim 13, wherein said formulation is formulated for oral administration.

18. A pharmaceutical formulation, comprising: (a) 3S-[3R*(1R*,2S*)]-[3-[[4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-h ydroxy-1-phenylmethyl)propyl]carbamic acid, tetrahydro-3-furanyl ester in an amount from 1% to 50% w/w; (b) a water soluble tocopherol derivative in an amount from about 10% to about 60% w/w; and (c) a hydrophilic non-aqueous solvent miscible with the water soluble tocopherol derivative in an amount from about 15% to about 95%, wherein, the hydrophilic non-aqueous solvent is a polyethylene glycol, propylene glycol, polyvinyl pyrrolidone, or a combination thereof; and

wherein said formulation possesses unexpectedly enhanced bioavailability.

19. A pharmaceutical formulation according to claim 18, wherein the water soluble tocopherol derivative is Vitamin E-TPGS.

20. The pharmaceutical formulation according to claim 18, wherein said formulation is in the form of a soft gelatin capsule.

21. A pharmaceutical formulation for oral administration, comprising: (a) about 19% w/w of 3S-[3R*(1R*,2S*)]-[3-[[4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-h ydroxy-1-phenylmethyl)propyl]carbamic acid, tetrahydro-3-furanyl ester, (b) about 51% w/w of Vitamin E-TPGS, (c) about 25% w/w of polyethylene glycol, and (d) about 5% w/w of propylene glycol, and

wherein said formulation possesses unexpectedly enhanced bioavailability.
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