# US 10,369,158 B2 · Pharmaceutical packaging for estriol therapy

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- Number: US 10,369,158 B2
- Document ID: US10369158B2
- Status: Granted
- Kind: B2
- Application number: 15/307,198
- Filed: 2015-04-27
- Published: 2017-02-16
- Granted: 2019-08-06
- Earliest claimed: 2014-04-28
- Assignees: The Regents of the University of California
- Applicants: The Regents of the University of California
- Inventors: Rhonda R. Voskuhl
- Web page: https://patentgrep.com/patent/US10369158B2

## CPC

- A61K 31/566: having an oxo group in position 17, e.g. estrone
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 31/57: substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 37/00: Drugs for immunological or allergic disorders
- 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

This invention relates to novel packaged pharmaceutical products for the treatment of neurodegenerative diseases, such as multiple sclerosis, and methods of using these products.

## Claims

### Claim 1

A packaged pharmaceutical product, comprising:
a first region comprising a first series of doses of estriol, wherein each dose of the estriol is co-located with a dose of a progestogen; and
a second region comprising a second series of doses of the estriol that are not co-located with doses of the progestogen; wherein
each dose of estriol comprises about 8 mg of estriol.

### Claim 2 (depends on 1)

The packaged pharmaceutical product of claim 1, wherein each dose of the estriol in the second region is co-located with a dose of placebo.

### Claim 3 (depends on 1)

The packaged pharmaceutical product of claim 1, wherein each dose of progestogen is co-formulated with a dose of estriol.

### Claim 4 (depends on 1)

The packaged pharmaceutical product of claim 1, wherein the progestogen is a progestin.

### Claim 5 (depends on 1)

The packaged pharmaceutical product of claim 1, wherein the progestogen is progesterone, 17-hydroxyprogesterone, 5α-dihydroprogesterone, norethindrone, norethindrone acetate, desogestrel, levonorgestrel, medroxyprogesterone acetate, megestrol, chlormadinone acetate, cyproterone acetate, norethynodrel, ethynodiol diacetate, norgestrel, gestodene, norgestimate, dienogest, drospirenone, etonogestrel, nestorone, nomegestrol acetate, trimegestone, tanaproget, or a pharmaceutically acceptable salt of any of the foregoing, or any combination thereof.

### Claim 6 (depends on 1)

The packaged pharmaceutical product of claim 1, wherein a dose of the progestogen comprises a dose equal or equivalent to about 100 μg to 1 mg of norethindrone.

### Claim 7 (depends on 6)

The packaged pharmaceutical product of claim 6, wherein a dose of the progestogen comprises a dose equal or equivalent to about 700 μg of norethindrone.

### Claim 8 (depends on 1)

The packaged pharmaceutical product of claim 1, wherein successive doses of the estriol in each series are associated with successive days of an administration cycle, and the administration cycle consists of 28-365 consecutive calendar days.

### Claim 9 (depends on 8)

The packaged pharmaceutical product of claim 8, wherein the administration cycle consists of 4 weeks.

### Claim 10 (depends on 8)

The packaged pharmaceutical product of claim 8, wherein the administration cycle consists of 1 month.

### Claim 11 (depends on 1)

The packaged pharmaceutical product of claim 1, wherein:
the administration cycle consists of 84 consecutive calendar days;
the first region comprises 14 doses each of the estriol and the progestogen; and
the second region comprises 70 doses of the estriol.

### Claim 12 (depends on 11)

The packaged pharmaceutical product of claim 11, wherein the second region comprises a number of doses of the placebo that is equal to the number of doses of the estriol within the second region.

### Claim 13 (depends on 2)

The packaged pharmaceutical product of claim 2, wherein the doses are adapted for oral administration.

### Claim 14 (depends on 13)

The packaged pharmaceutical product of claim 13, wherein the doses of estriol, progestogen, or placebo are provided in a tablet, pill, capsule, or gelcap.

### Claim 15

A method of treating multiple sclerosis using a packaged pharmaceutical product, the method comprising:
ingesting one dose of an estriol and one dose of a progestogen daily from a first region of the product; and
when the doses in the first region are exhausted, ingesting one dose of estriol daily from a second region of the product;
wherein the product comprises:
a first region comprising a first series of doses of an estriol, wherein each dose of the estriol is co-located with a dose of a progestogen; and
a second region comprising a second series of doses of the estriol that are not co-located with doses of the progestogen; wherein
each dose of estriol comprises about 8 mg of estriol.

### Claim 16 (depends on 11)

The packaged pharmaceutical product of claim 11, wherein the dose of the progestogen comprises a dose equal or equivalent to about 100 μg to 1 mg of norethindrone.

### Claim 17 (depends on 11)

The packaged pharmaceutical product of claim 11, wherein the dose of the progestogen comprises a dose equal or equivalent to about 700 μg of norethindrone.

### Claim 18 (depends on 15)

The method of claim 15, wherein the first series of doses comprises 14 doses each of the estriol and the progestogen; and the second region comprises 70 doses of the estriol.

### Claim 19 (depends on 15)

The method of claim 15, wherein the dose of the progestogen comprises a dose equal or equivalent to about 700 μg of norethindrone.

### Claim 20 (depends on 18)

The method of claim 18, wherein the dose of the progestogen comprises a dose equal or equivalent to about 700 μg of norethindrone.