A pharmaceutical dosage unit for oral administration to a human female comprising a therapeutically effective amount of 17.beta.-estradiol-3-lower alkanoate, most preferably 17.beta.-estradiol-3-acetate, and a pharmaceutically acceptable carrier is disclosed. Also disclosed is a method for treating a human female in need of 17.beta.-estradiol and a contraceptive method by oral administration of the pharmaceutical dosage unit and a method of preparing a pharmaceutical composition that may be used to form the pharmaceutical dosage unit of the invention.