Contraceptive method and composition

Abstract

The present invention relates to a method of achieving contraception in a woman, comprising daily administering to said woman, from the first day of her cycle, a pharmaceutical composition comprising (i) estradiol, an ester thereof or an equine conjugated estrogen and (ii) nomegestrol acetate. The invention further relates to a contraceptive product comprising 21 to 28 dosage forms containing (i) estradiol, an ester thereof or an equine conjugated estrogen and (ii) nomegestrol acetate, and 0 to 7 dosage forms containing a placebo.

We claim:  
     
         1 . A method of achieving contraception in a woman comprising daily administering to said woman, from the first day of her cycle and for at least 21 days, a pharmaceutical composition comprising (i) about 0.3 mg to about 3 mg of estradiol, an ester thereof or an equine conjugated estrogen and (ii) about 1.5 mg to about 3.75 mg of nomegestrol acetate.  
     
     
         2 . The method of  claim 1 , wherein the composition comprises 1.5 mg of estradiol.  
     
     
         3 . The method of  claim 1 , wherein the composition comprises 2 mg of ester of estradiol.  
     
     
         4 . The method of  claim 3 , wherein the ester of estradiol is estradiol valerate.  
     
     
         5 . The method of  claim 1 , wherein the composition comprises 0.625 mg of equine conjugated estrogen.  
     
     
         6 . The method of  claim 1 , wherein the composition comprises 2.5 mg of nomegestrol acetate.  
     
     
         7 . The method of  claim 2 , wherein the composition comprises 2.5 mg of nomegestrol acetate.  
     
     
         8 . The method of  claim 3 , wherein the composition comprises 2.5 mg of nomegestrol acetate.  
     
     
         9 . The method of  claim 4 , wherein the composition comprises 2.5 mg of nomegestrol acetate.  
     
     
         10 . The method of  claim 5 , wherein the composition comprises 2.5 mg of nomegestrol acetate.  
     
     
         11 . The method of  claim 1 , wherein the composition is administered orally.  
     
     
         12 . The method of  claim 1 , wherein the composition is administered for up to 25 days.  
     
     
         13 . A contraceptive product comprising at least 21 and up to 25 dosage forms comprising (i) about 0.3 mg to about 3 mg of estradiol, an ester thereof or an equine conjugated estrogen and (ii) about 1.5 mg to about 3.75 mg of nomegestrol acetate.  
     
     
         14 . The product of  claim 13 , wherein the dosage forms comprise 1.5 mg of estradiol and 2.5 mg of nomegestrol acetate.  
     
     
         15 . The product of  claim 13 , wherein the dosage forms are tablets.  
     
     
         16 . The product of  claim 14 , wherein the dosage forms are tablets.  
     
     
         17 . A method of achieving contraception in a woman comprising daily administering to said woman, from the first day of her cycle and for 21 days to 28 days, a composition comprising (i) about 0.3 mg to about 3 mg of estradiol, an ester thereof or an equine conjugated estrogen and (ii) about 0.1 mg to about 2.5 mg of nomegestrol acetate.  
     
     
         18 . The method of  claim 17 , wherein the composition comprises about 0.5 mg to about 2 mg of estradiol, an ester thereof or an equine conjugated estrogen.  
     
     
         19 . The method of  claim 17 , wherein the composition comprises about 0.1 mg to about 1.25 mg of nomegestrol acetate.  
     
     
         20 . The method of  claim 19 , wherein the composition comprises about 0.3 mg to about 1.25 mg of nomegestrol acetate.  
     
     
         21 . The method of  claim 18 , wherein the composition comprises about 0.1 mg to about 1.25 mg of nomegestrol acetate.  
     
     
         22 . The method of  claim 21 , wherein the composition comprises about 0.3 mg to about 1.25 mg of nomegestrol acetate.  
     
     
         23 . The method of  claim 22 , wherein the composition comprises 1 mg of estradiol and 0.312 mg of nomegestrol acetate.  
     
     
         24 . The method of  claim 22 , wherein the composition comprises 1 mg of estradiol and 0.625 mg of nomegestrol acetate.  
     
     
         25 . The method of  claim 22 , wherein the composition comprises 1.5 mg of estradiol and 0.625 mg of nomegestrol acetate.  
     
     
         26 . The method of  claim 22 , wherein the composition comprises 2 mg of estradiol and 0.625 mg of nomegestrol acetate.  
     
     
         27 . The method of  claim 17 , which further comprises administering to the woman a placebo for the balance of the 28 day cycle whereby an effective control of the menstrual cycle is ensured.  
     
     
         28 . The method of  claim 17 , wherein the composition is administered orally.  
     
     
         29 . A contraceptive product comprising 21 to 28 dosage forms comprising (i) about 0.3 mg to about 3 mg of estradiol, an ester thereof or an equine conjugated estrogen and (ii) about 0.1 mg to about 2.5 mg of nomegestrol acetate.  
     
     
         30 . The product of  claim 29 , wherein the dosage forms comprise about 0.5 mg to about 2 mg of estradiol, an ester thereof or an equine conjugated estrogen.  
     
     
         31 . The product of  claim 30 , wherein the dosage forms comprise about 2.5 mg of nomegestrol acetate.  
     
     
         32 . The product of  claim 29 , wherein the dosage forms are tablets.  
     
     
         33 . The product of  claim 29 , further comprising 1 to 7 dosage forms comprising a placebo.