# US 8,772,353 B2 · Method for enhancing the bioavalability of ospemifene

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- Number: US 8,772,353 B2
- Document ID: US8772353B2
- Status: Granted
- Kind: B2
- Application number: 13/904,818
- Filed: 2013-05-29
- Published: 2013-12-05
- Granted: 2014-07-08
- Earliest claimed: 2004-02-13
- Assignees: Hormos Medical Corporation
- Applicants: Hormos Medical Ltd.
- Inventors: Markku Anttila
- Web page: https://patentgrep.com/patent/US8772353B2

## CPC

- A61K 31/085: having an ether linkage to aromatic ring nuclear carbon
- A23L 33/30: {Dietetic or nutritional methods, e.g. for losing weight (A23L33/10 takes precedence)}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 31/075: Ethers or acetals
- A61P 5/30: Oestrogens
- A61P 13/00: Drugs for disorders of the urinary system
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 15/02: for disorders of the vagina
- A61P 17/00: Drugs for dermatological disorders
- A61P 19/10: for osteoporosis
- A23V 2002/00: Food compositions, function of food ingredients or processes for food or foodstuffs
- 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)
- A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A23V: INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION

## Abstract

This invention relates to a method for enhancing the bioavailability of a therapeutically active compound of the formula (I) or a geometric isomer, a stereoisomer, a pharmaceutically acceptable salt, an ester thereof or a metabolite thereof, wherein said compound is administered orally to the individual in connection with the intake of food.

## Claims

### Claim 1

A method of treating sexual dysfunction comprising orally administering a therapeutically effective amount of ospemifene or a pharmaceutically acceptable salt thereof to a patient in need thereof in connection with the intake of a foodstuff having nutritional value and causing secretion of bile acids to enhance bioavailability of the ospemifene or pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method according to claim 1 wherein the ospemifene or pharmaceutically acceptable salt thereof is administered at a time point which is in the range defined by 1 hour before starting the food intake and 2 hours after starting the food intake.

### Claim 3 (depends on 2)

The method according to claim 2 wherein the ospemifene or pharmaceutically acceptable salt thereof is administered at a time point which is in the range defined to begin at a time point during the food intake and to end 1 hour after the food intake was started.

### Claim 4 (depends on 3)

The method according to claim 3 wherein the ospemifene or pharmaceutically acceptable salt thereof is administered at a time point which is no later than 0.5 hours after starting the food intake.

### Claim 5 (depends on 2)

The method according to claim 2 wherein the ospemifene or pharmaceutically acceptable salt thereof is administered in oral dosage form and wherein the dosage amount is from 30 to 90 mg/day.

### Claim 6 (depends on 5)

The method according to claim 5 wherein the dosage amount is 60 mg.

### Claim 7 (depends on 2)

The method of claim 2 wherein said patient is a perimenopausal or postmenopausal woman.

### Claim 8 (depends on 1)

The method according to claim 1 wherein said sexual dysfunction is dyspareunia.

### Claim 9 (depends on 8)

The method according to claim 8 wherein the ospemifene or pharmaceutically acceptable salt thereof is administered in oral dosage form and wherein the dosage amount is from 30 to 90 mg/day.

### Claim 10 (depends on 9)

The method according to claim 9 wherein the dosage amount is 60 mg.

### Claim 11 (depends on 10)

The method of claim 10 where said patient is a perimenopausal or postmenopausal woman.

### Claim 12 (depends on 1)

The method according to claim 1 wherein the ospemifene or pharmaceutically acceptable salt thereof is administered in oral dosage form and wherein the dosage amount is from 30 to 90 mg/day.

### Claim 13 (depends on 12)

The method according to claim 12 wherein the dosage amount is 60 mg.

### Claim 14 (depends on 1)

The method of claim 1 wherein said patient is a perimenopausal or a postmenopausal woman.

### Claim 15

A method of treating sexual dysfunction comprising orally administering a therapeutically effective amount of ospemifene to a patient in need thereof in connection with the intake of a foodstuff having nutritional value and causing secretion of bile acids to enhance bioavailability of the ospemifene or pharmaceutically acceptable salt thereof.

### Claim 16 (depends on 15)

The method according to claim 15, wherein the ospemifene is administered at a time point which is in the range defined by 1 hour before starting the food intake and 2 hours after starting the food intake.

### Claim 17 (depends on 15)

The method according to claim 15, wherein said sexual dysfunction is dyspareunia.

### Claim 18 (depends on 17)

The method according to claim 17, wherein the dosage amount is 60 mg.

### Claim 19 (depends on 17)

The method of claim 17, wherein said patient is a perimenopausal or a postmenopausal woman.
