Rapidly-dissolving pharmaceutical composition for inhibiting ovulation
A rapidly-dissolving oral dosage pharmaceutical composition for inhibiting ovulation in a mammal, said composition comprising drospirenone or a pharmaceutically acceptable salt or ester thereof, optionally ethinyl estradiol or a pharmaceutically acceptable salt, ester or ether thereof, a surfactant and at least one pharmaceutically acceptable excipient, wherein the drospirenone has a surface area of less than 10,000 cm 2 /g.
1. A rapidly-dissolving oral dosage pharmaceutical composition for inhibiting ovulation in a mammal, said composition comprising drospirenone or a pharmaceutically acceptable salt or ester thereof, a polyoxyethylene-sorbitan-fatty acid ester surfactant and at least one pharmaceutically acceptable excipient, wherein the drospirenone is in the form of solid particles having a surface area of less than 10,000 cm 2 /g and greater than 2% of said particles have a diameter of at least 30 μm, and wherein the surfactant is present in an amount of from about 0.01 wt % to about 20 wt %, based on the total weight of the composition.
2. The composition according to claim 1 , wherein the drospirenone is present in an amount of from about 2 mg to about 4 mg.
3. The composition according to claim 1 , wherein the polyoxyethylene-sorbitan-fatty acid ester is selected from the group consisting of polyoxyethylene(20)sorbitanmonolaurate, polyoxyethylene(4)sorbitanmonolaurate, polyoxyethylene(20)sorbitanmonopalmitate, polyoxyethylene(20)sorbitanmonostearate, polyoxyethylene(20)sorbitantristearate, polyoxyethylene(20)sorbitanmonooleate, polyoxyethylene(5)sorbitanmonooleate and polyoxyethylene(20)sorbitantrioleate.
4. The composition according to claim 3 , wherein the polyoxyethylene-sorbitan-fatty acid ester is polyoxyethylene(20)sorbitanmonooleate.
5. The composition according to claim 1 , further comprising a second surfactant selected from the group consisting of sodium lauryl sulfate, ammonium lauryl sulfate, ammonium stearate, alpha olefin sulfonate, ammonium laureth sulfate, ammonium laureth ether sulfate, ammonium stearate, sodium laureth sulfate, sodium octyl sulfate, sodium sulfonate, sodium sulfosuccinamate, sodium tridecyl ether sulfate and triethanolamine lauryl sulfate.
6. The composition according to claim 5 , wherein the second surfactant is sodium lauryl sulfate.
7. The composition according to claim 1 , wherein the polyoxyethylene-sorbitan-fatty acid ester surfactant is present in an amount of from about 1 wt % to about 10 wt %, based on the total weight of the composition.
8. The composition according to claim 1 , wherein the excipient is selected from the group consisting of diluents, binders, anti-caking agents, amino acids, fibers, solubilizers, disintegrants, fillers, lubricants, emulsifiers, flavorants, solvents, buffers, stabilizers, colorants, dyes, anti-oxidants, anti-adherents, preservatives, electrolytes, glidants, carrier materials and mixtures thereof.
9. The composition according to claim 1 , wherein the excipient is polyvinylpyrrolidone.
10. The composition of claim 1 in the form of an uncoated tablet.