Vaginal delivery for physiologic follicular-luteal steroid treatment

• US 4,372,951 A
• Filed: 07/21/1981
• Issued: 02/08/1983
• Est. Priority Date: 10/11/1979
• Status: Expired due to Fees

• Current Assignee: Nichols Vorys
• Original Assignee: Nichols Vorys
• Inventors: Vorys, Nichols
• Primary Examiner(s): Roberts, Elbert L.
• Application Number:
  US06/285,590
• Time in Patent Office: 567 Days
• Field of Search: 424/238, 424/241, 424/243, 424/239
• US Class Current: 514/170
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 9/0036 Devices retained in the vagina or cervix for a prolonged period, e.g. intravaginal rings, medicated tampons, medicated diaphragms

Abstract

A vaginal delivery system which provides an effective concurrent dosage of combined exogenous estrogenic active steroid and exogenous progestational active steroid during the corpus luteum phase of a follicular-luteal drug administration cycle to provide predictable physiologic levels of such steroids for the finite period of time of the corpus luteum phase of the drug administration cycle.

Claims

1. A method of regulation of the menstrual cycle in which effective dosages of pharmacologically active steroid compositions selected from the group of estrogenic active steroids and progestational active steroids are administered in a temporal succession in a correspondence with a first follicular phase and a following luteal phase in an approximately 28 day menstrual cycle, in which, dosage of the follicular phase is dependent upon the presenting endogenous estrogen characteristic of the patient, and the luteal phase includes:

a vaginal delivery system which provides effective concurrent dosages of (1) a pharmacologically active steroid selected from the group of estrogen active steroids and (2) a pharmacologically active steroid selected from the group of progestational active steroids, administered together, for a finite period of time of approximately 14 days during the luteal phase of the drug administration cycle, whereby predictable physiologic levels of activity of each steroid administered are provided during the luteal phase of the drug administration cycle.

2. The follicular-luteal method in accord with claim 1 in which the concurrent vaginal delivery of an estrogen active steroid with a progestational active steroid during the luteal phase provides a standardized level of pharmacological activity which mimics the physiological activity of an optimum predetermined normal menstrual cycle.

3. The method of claim 2 in which the standardized level of steroid activity provided in a system is a level of activity which is the same for euestrogen, hyperestrogen and hypoestrogen presenting endogenous estrogen conditions.

4. The system of claim 1 or claim 2 or claim 3 for treatment of a menstrual dysfunction condition in a patient of one of an (1) euestrogen and (2) hyperestrogen presenting condition.

5. A delivery system in accord with claim 1 or claim 2 or claim 3 which provides by vaginal delivery an effective dosage, related to the presenting endogenous estrogen characteristic of the patient, of one of (1) an estrogenic active steroid and (2) a progestational active steroid, during the later portion of the follicular phase of the drug administration cycle, preceding the administration of steroids in the luteal phase of the drug administration cycle.

12. A follicular-luteal method in accord with claim 1 or claim 2 or claim 3 in which a pharmacologically active steroid composition related to the presenting endogenous estrogen characteristic of the patient is one of (1) an estrogenic active steroid and (2) a progestational active steroid administered by means other than vaginal delivery.

13. The delivery system of claim 1 or claim 6 in which the steroid having an estrogenic activity is 17 beta estradiol.

14. The delivery system of claim 1 or claim 6 in which the steroid having a progestational activity is progesterone.

15. The delivery system of claim 1 or claim 6 in which the steroid having an estrogenic activity is 17 beta estradiol and the steroid having a progestational activity is progesterone.

6. A vaginal delivery system for providing pharmacologically active exogenous steroids with respect to a predetermined first follicular phase and a following luteal phase according to a temporal relationship in a single menstrual cycle having a duration of approximately 28 days in which

a first steroid, having one of (1) estrogenic activity and (2) progestational activity, is administered, beginning with the later part of the follicular phase, for a period of about 21 days during the menstrual cycle;

and for the last approximately 14 days of the 21 day administration of the first steroid, a second steroid, having the other of (1) estrogenic activity and (2) progestational activity, is concurrently administered therewith during the luteal phase.

7. The system of claim 6 in which the presenting endogenous estrogen state of the patient is one of euestrogenic and hyperestrogenic and the first steroid administered is a progestational active steroid.

8. The system of claim 6 in which the presenting endogenous estrogen state of the patient is hypoestrogenic and the first steroid administered is an estrogenic active steroid.

9. The system of claim 8 for treatment of a menopause condition.

10. The system of claim 7 for contraception.

11. The system of claim 8 for contraception.