Solid ganaxolone compositions and methods for the making and use thereof

A pharmaceutical composition comprising solid stabilized particles comprising ganaxolone, a hydrophilic polymer, a wetting agent, and an effective amount of a complexing agent which is a small organic molecule having a molecular weight less than 550 and containing a moiety selected from the group consisting of a phenol moiety, an aromatic ester moiety and an aromatic acid moiety, wherein the stabilized particles have a volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm, the complexing agent being present in an amount from about 0.05% to about 5% w/w, based on the weight particles of the solid;

• the pharmaceutical composition further comprising one or more pharmaceutically acceptable additives selected from the group consisting of a diluent, a binder, a disintegrant, a plasticizer, a stabilizer, and mixtures of any of the foregoing, the pharmaceutical composition being an oral solid dosage form.

The pharmaceutical composition solid stabilized particles of claim 4, wherein the wetting agent is selected from the group consisting of sodium lauryl sulfate, a pharmaceutically acceptable salt of docusate, and mixtures thereof.

A pharmaceutical composition comprising solid stabilized particles comprising ganaxolone, a hydrophilic polymer, a wetting agent, and an effective amount of a complexing agent selected from the group consisting of methyl paraben, propyl paraben, and mixtures thereof and being present in an amount from about 0.05% to about 5% w/w based on the weight particles of the solid;

• the pharmaceutical composition further comprising one or more pharmaceutically acceptable additives selected from the group consisting of a diluent, a binder, a disintegrant, a plasticizer, a stabilizer, and mixtures of any of the foregoing, wherein the stabilized particles have a volume weighted median diameter (D50) of the particles from about 50 nm to about 500 nm, the pharmaceutical composition being an oral solid dosage form and including from about 50 mg to about 800 mg ganaxolone.

A pharmaceutical composition comprising solid stabilized particles comprising ganaxolone, a hydrophilic polymer, a wetting agent, and an effective amount of a complexing agent selected from the group of small organic molecules having a molecular weight less than 550 and containing a moiety selected from the group consisting of a phenol moiety, an aromatic ester moiety and an aromatic acid moiety;

• the pharmaceutical composition further comprising one or more pharmaceutically acceptable additives selected from the group consisting of a diluent, a binder, a disintegrant, a plasticizer, a stabilizer, and mixtures of any of the foregoing, the stabilized particles having a volume weighted median diameter (D50) of the particles from about 50 nm to about 500 nm, the concentration of ganaxolone in the solid stabilized particles being at least 50% by weight and the composition including from about 50 mg to about 800 mg ganaxolone, wherein the pharmaceutical composition is an oral solid dosage form.