United States Patent:  5,972,381

Assignee:  Schering Corporation (Kenilworth, NJ)

Filed:  June 25, 1997

A pharmaceutical composition in the form of a substantially amorphous solid solution comprising an antifungal compound of the formula I: 

wherein: X is F; and R₁ is 

or an ester or ether of said compound of Formula I; and a soluble or insoluble polymer such as: povidone or crospovidone, wherein the ratio of said compound to said polymer is about 1:3 to about 1:6 is disclosed.

SUMMARY OF THE INVENTION

The present invention provides a pharmaceutical composition comprising a substantially amorphous solid solution, said solid solution comprising:

(a) a compound of the formula I: 

wherein: X is F; and R₁ is 

or an ester or ether of said compound of Formula I; and

(b) a polymer selected from the group consisting of:

povidone, crospovidone, hydroxypropyl methylcellulose, hydroxypropylcellulose, polyethylene oxide, gelatin, carbomer, carboxymethylcellulose, croscarmellose, methylcellulose, methacrylic acid copolymer, methacrylate copolymer, and water soluble salts such as sodium and ammonium salts of methacrylic acid and methacrylate copolymers, cellulose acetate phthalate, hydroxypropylmethylcellulose phthalate and propylene glycol alginate;

wherein the ratio of said compound to said polymer is about 1:3 to about 1:6.

This invention also provides solid dosage forms comprising the solid solution described above. Solid dosage forms include tablets, capsules and chewable tablets. Known excipients can be blended with the solid solution to provide the desired dosage form. For example, a capsule can contain the solid solution blended with (a) a disintegrant and a lubricant, or (b) a disintegrant, a lubricant and a surfactant. A tablet can contain the solid solution blended with at least one disintegrant, a lubricant, a surfactant, and a glidant. The chewable tablet can contain the solid solution blended with a bulking agent, a lubricant, and if desired an additional sweetening agent (such as an artificial sweetener), and suitable flavors.

Claim 1 of 2 Claims

1. A pharmaceutical composition comprising a substantially amorphous solid solution, said solid solution comprising:

(a) a compound of the formula: 

wherein: X is independently F; and R₁ is

and (b) the polymer selected from povidone or crospovidone;

wherein the solid solution comprises about 50 to about 70 wt % of the pharmaceutical composition and wherein the ratio of the compound to the polymer is about 1:3 to about 1:4; and

wherein the remaining about 30 to about 50% of the pharmaceutical composition further comprises:

(b) about 25 to about 30 wt % of crospovidone;

(c) about 5 to about 10 wt % of croscarmellose sodium;

(d) about 0.5 to about 2 wt % of magnesium stearate;

(e) about 2 to about 10 wt % of the compound of the formula HO(C₂ H₄ O)₈₀ (C₃ H₆ O)₂₇ (C₂ H₄ O)₈₀ H;

(f) about 1 to about 2 wt % of silicon dioxide;

such that the total wt % is 100% based on the weight of the composition.

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