Antiemetic-oral contraceptive combination
The present invention relates to a method of reducing the incidence of nausea and vomiting associated with the administration of oral contraceptive formulation and a method of preparation of oral contraceptive formulation comprising progestin and/or estrogen and an antiemetic. The preferred oral contraceptive formulation comprises of levonorgestrel and an antiemetic.
1. An oral pharmaceutical formulation comprising a combination of levonorgestrel and an antiemetic selected from ondansetron or meclizine within the same formulation, wherein levonorgestrel is contained in a delayed release portion comprising at least one delayed release agent selected from the group consisting of hydrophilic or hydrophobic polymers or mixtures thereof, and the antiemetic is contained in an immediate release portion comprising at least one pharmaceutically acceptable excipients, wherein at least 80% of antiemetic is released within 30 min in 0.1 N HCl and at least 80% of levonorgestrel is released within 30 min at pH 6.8, when the dissolution is carried out for 2 hours in 0.1 N HCl followed by pH 6.8 phosphate buffer using a USP Type I apparatus at 100 rpm.
2. The oral pharmaceutical formulation according to claim 1 wherein the antiemetic is selected from ondansetron or meclizine is released at least about 30 minutes prior to the release of Levonorgestrel.
3. The oral pharmaceutical formulation according to claim 1 is selected from the group consisting of granules, sachets, capsules, matrix tablets, layered tablet or coated tablets.
4. The oral pharmaceutical formulation according to claim 1 wherein the levonorgestrel is coated with a delayed release agent selected from an enteric polymer.
5. The oral pharmaceutical formulation according to claim 1 wherein the dose of levonorgestrel is selected from 0.75 mg or 1.5 mg.
6. A method of emergency contraception comprising administering the single oral pharmaceutical formulation according to claim 1 as an emergency contraceptive.