United States Patent:  5,948,436

Assignee:  Abbott Laboratories (Abbott Park, IL)

Filed:  March 13, 1995

A pharmaceutical composition is disclosed which comprises a solution of an HIV protease inhibiting compound in a pharmaceutically acceptable organic solvent comprising a pharmaceutically acceptable alcohol. The composition can optionally comprise a pharmaceutically acceptable acid or a combination of pharmaceutically acceptable acids. The solution can optionally be encapsulated in hard gelatin capsules or soft elastic gelatin capsules. The solution can optionally be granulated with a pharmaceutically acceptable granulating agent.

Abstract of Disclosure of the Invention

"In accordance with the present invention, there is a pharmaceutical composition comprising a solution of an HIV protease inhibiting compound in a pharmaceutically acceptable organic solvent or a mixture of pharmaceutically acceptable organic solvents, the solvent comprising a pharmaceutically acceptable alcohol.

Also in accordance with the present invention, there is a pharmaceutical composition comprising a solution of an HIV protease inhibiting compound  in a pharmaceutically acceptable organic solvent or a mixture of pharmaceutically acceptable organic solvents, the solvent comprising a pharmaceutically acceptable alcohol, wherein the solution is encapsulated in a soft elastic gelatin capsule (SEC) or a hard gelatin capsule.

The solution composition of the invention can also comprise from about 0 to about 3 molar equivalents (based on the amount of the HIV protease inhibiting compound in the composition) of a pharmaceutically acceptable acid or a mixture of pharmaceutically acceptable acids. Preferably, the pharmaceutically acceptable acid or mixture of pharmaceutically acceptable acids is present in a total amount of from about 0.2 to about 2.0 molar equivalents (based on the amount of the HIV protease inhibiting compound in the composition).

The solution composition of the invention can also comprise from about 0% to about 10% (by weight of the total solution) of water. In addition, the solution composition of the invention can comprise a pharmaceutically acceptable surfactant or a mixture of pharmaceutically acceptable surfactants. In addition, the solution composition of the invention can comprise an antioxidant (for example, ascorbic acid, BHA (butylated hydroxyanisole), BHT (butylated hydroxytoluene), vitamin E, vitamin E PEG 1000 succinate and the like) for chemical stability. Solutions encapsulated in a SEC may also comprise glycerin for physical stability."

"A preferred composition of the invention comprises a solution of (1) an HIV protease inhibiting compound; and (2) a pharmaceutically acceptable acid or a mixture of pharmaceutically acceptable acids in a pharmaceutically acceptable organic solvent or a mixture of pharmaceutically acceptable organic solvents, the solvent comprising a pharmaceutically acceptable alcohol.

Another preferred composition of the invention comprises a solution of (1)an HIV protease inhibiting compound  in the amount of from about 2% to about 30% (preferably, from about 4% to about 30%) by weight of the total solution; and (2) a total of from about 0.2 molar equivalent to about 3 molar equivalents (based on compound II) of (i) a pharmaceutically acceptable acid or (ii) a mixture of pharmaceutically acceptable acids in a pharmaceutically acceptable organic solvent or a mixture of pharmaceutically acceptable organic solvents, the solvent comprising a pharmaceutically acceptable alcohol.

Yet another preferred composition of the invention comprises a solution of (1) an HIV protease inhibiting compound; and (2) a pharmaceutically acceptable acid or a mixture of pharmaceutically acceptable acids in a pharmaceutically acceptable organic solvent or a mixture of pharmaceutically acceptable organic solvents, the solvent comprising a pharmaceutically acceptable alcohol, wherein the solution is encapsulated in a soft elastic gelatin capsule (SEC) or a hard gelatin capsule.

Yet another preferred composition of the invention comprises a solution of (1) an HIV protease inhibiting compound  in the amount of from about 2% to about 30% (preferably, from about 4% to about 30%) by weight of the total solution; and (2) a total of from about 0.2 molar equivalent to about 3 molar equivalents of (i) a pharmaceutically acceptable acid or (ii) a mixture of pharmaceutically acceptable acids in a pharmaceutically acceptable organic solvent or a mixture of pharmaceutically acceptable organic solvents, the solvent comprising a pharmaceutically acceptable alcohol, wherein the solution is encapsulated in a soft elastic gelatin capsule (SEC) or a hard gelatin capsule."

Claim 1 of 44 Claims

1. A pharmaceutical composition comprising a solution of a compound of the formula: 

in (i) a pharmaceutically acceptable organic solvent which is a pharmaceutically acceptable alcohol or (ii) a mixture of pharmaceutically acceptable organic solvents wherein the mixture comprises a pharmaceutically acceptable alcohol.

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