# US 10,500,215 B2 · Formulations and methods for providing progestin-only contraception while minimizing adverse side effects associated therewith > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,500,215 B2 - Document ID: US10500215B2 - Status: Granted - Kind: B2 - Application number: 16/162,670 - Filed: 2018-10-17 - Published: 2019-04-18 - Granted: 2019-12-10 - Earliest claimed: 2005-08-15 - Assignees: Allergan Sales, Inc. - Applicants: Allergan Sales, LLC - Inventors: Charles Ebert; Gary Hoel; Angela Anigbogu; Samir Roy - Web page: https://patentgrep.com/patent/US10500215B2 ## CPC - A61K 31/57: substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone - A61K 9/7061: {Polyacrylates} - A61K 31/565: not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol - A61P 15/18: Feminine contraceptives - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract Formulations and methods for providing progestin-only contraception to a woman while minimizing various side effects, such as breakthrough bleeding, that are normally associated with progestin-only contraception are disclosed and described. In one aspect, the method can include transdermally administering a formulation having a contraceptively effective amount of a single progestin as the sole active hormonal agent to the woman as part of a contraceptive regimen. ## Claims ### Claim 1 A transdermal patch comprising: a) norethindrone as the sole hormonal active agent or a combination of norethindrone and norethindrone acetate as the sole hormonal active agents in an amount of from 1% to 15% w/w; and b) a permeation enhancer comprising (i) isopropyl myristate and (ii) lauryl alcohol, wherein the transdermal patch is formulated to minimize adverse side effects associated with progestin-only contraception by providing: a) a minimum norethindrone serum level of at least 300 pg/ml from 24 hours to 168 hours following application of the patch to an outer skin surface; and b) a maximum norethindrone serum level of less than 2400 pg/ml from about 24 to 96 hours following application of the patch to the outer skin surface, wherein the side effects are selected from the group consisting of strokes, myocardial infarctions, embolisms, breakthrough bleeding and combinations thereof. ### Claim 2 (depends on 1) The transdermal patch of claim 1 wherein the permeation enhancer is present in an amount of from 0.01% to 50% w/w. ### Claim 3 (depends on 2) The transdermal patch of claim 2 wherein the permeation enhancer is present in an amount of from 3% to 15% w/w. ### Claim 4 (depends on 1) The transdermal patch of claim 1, wherein the sole hormonal active agents are present in an amount of from 2.5% to 12% w/w. ### Claim 5 (depends on 4) The transdermal patch of claim 4, wherein the sole hormonal active agents are present in an amount of from 5% to 10% w/w. ### Claim 6 (depends on 1) The transdermal patch of claim 1, wherein the sole hormonal active agents are present in an amount of 10% w/w. ### Claim 7 (depends on 1) The transdermal patch of claim 1, wherein the permeation enhancer is present in an amount of 5% w/w. ### Claim 8 (depends on 1) The transdermal patch of claim 1, wherein the permeation enhancer is present in an amount of 10% w/w. ### Claim 9 (depends on 1) The transdermal patch of claim 1, wherein the sole active hormonal agent is norethindrone. ### Claim 10 (depends on 1) The transdermal patch of claim 1, wherein the sole active hormonal agent is a combination of norethindrone and norethindrone acetate. ### Claim 11 (depends on 1) The transdermal patch of claim 1, wherein the transdermal patch is formulated to deliver the sole active hormonal agent in an amount of 0.2 mg/day. ### Claim 12 (depends on 1) The transdermal patch of claim 1, wherein the transdermal patch is formulated to deliver the sole active hormonal agent in an amount of 0.25 mg/day. ### Claim 13 (depends on 1) The transdermal patch of claim 1, wherein the transdermal patch is formulated to deliver the sole active hormonal agent in an amount of 0.3 mg/day. ### Claim 14 (depends on 1) The transdermal patch of claim 1, wherein the transdermal patch is formulated to deliver the sole active hormonal agent in an amount of 0.35 mg/day. ### Claim 15 (depends on 1) The transdermal patch of claim 1, wherein the transdermal patch is a matrix patch. ### Claim 16 (depends on 15) The transdermal patch of claim 15, wherein the matrix patch comprises an acrylic polymer adhesive. ### Claim 17 (depends on 1) The transdermal patch of claim 1, wherein the transdermal patch is a transdermal liquid system patch. ### Claim 18 (depends on 1) The transdermal patch of claim 1, wherein the transdermal patch further comprises diluents, emollients, plasticizers, skin irritation reducing agents, or a mixture thereof. ### Claim 19 (depends on 18) The transdermal patch of claim 18, wherein the transdermal patch includes a skin irritation reducing agent and wherein the skin irritation reducing agent is glycerin. ### Claim 20 (depends on 1) The transdermal patch of claim 1, wherein the sole active hormonal agent is a combination of norethindrone and norethindrone acetate, which are present in an amount of from 2.5% to 12% w/w; the permeation enhancer is present an amount of from 3% to 15% w/w; and the patch further comprises a diluent, an emollient, a plasticizer, a skin irritation reducing agent, or a mixture thereof. ### Claim 21 (depends on 20) The transdermal patch of claim 20, wherein the patch is a matrix patch and comprises an acrylic polymer adhesive.