Use of flibanserin for the treatment of post-menopausal Sexual Desire Disorders

Abstract

The invention relates to the use of flibanserin for the preparation of a medicament for the treatment of post-menopausal Sexual Desire Disorders.

Description

The Examples which follow illustrate the present invention without restricting its scope:

Examples of Pharmaceutical Formulations

	A)	Tablets	per tablet
	flibanserin	100 mg
	lactose	240 mg
	corn starch	340 mg
	polyvinylpyrrolidone	45 mg
	magnesium stearate	15 mg
		740 mg

The finely ground active substance, lactose and some of the corn starch are mixed together. The mixture is screened, then moistened with a solution of polyvinylpyrrolidone in water, kneaded, wet-granulated and dried. The granules, the remaining corn starch and the magnesium stearate are screened and mixed together. The mixture is compressed to produce tablets of suitable shape and size.

	B)	Tablets	per tablet
	flibanserin	80 mg
	corn starch	190 mg
	lactose	55 mg
	microcrystalline cellulose	35 mg
	polyvinylpyrrolidone	15 mg
	sodium-carboxymethyl starch	23 mg
	magnesium stearate	2 mg
		400 mg

The finely ground active substance, some of the corn starch, lactose, microcrystalline cellulose and polyvinylpyrrolidone are mixed together, the mixture is screened and worked with the remaining corn starch and water to form a granulate which is dried and screened. The sodium-carboxymethyl starch and the magnesium stearate are added and mixed in and the mixture is compressed to form tablets of a suitable size.

	C)	Coated tablets	per coated tablet
	flibanserin	5 mg
	corn starch	41.5 mg
	lactose	30 mg
	polyvinylpyrrolidone	3 mg
	magnesium stearate	0.5 mg
		80 mg

The active substance, corn starch, lactose and polyvinylpyrrolidone are thoroughly mixed and moistened with water. The moist mass is pushed through a screen with a 1 mm mesh size, dried at about 45° C. and the granules are then passed through the same screen. After the magnesium stearate has been mixed in, convex tablet cores with a diameter of 6 mm are compressed in a tablet-making machine. The tablet cores thus produced are coated in known manner with a covering consisting essentially of sugar and talc. The finished coated tablets are polished with wax.

	D)	Capsules	per capsule
	flibanserin	150 mg
	Corn starch	268.5 mg
	Magnesium stearate	1.5 mg
		420 mg

The substance and corn starch are mixed and moistened with water. The moist mass is screened and dried. The dry granules are screened and mixed with magnesium stearate. The finished mixture is packed into size 1 hard gelatine capsules.

E)              Ampoule solution
flibanserin     50 mg
sodium chloride 50 mg
water for inj.  5 ml

The active substance is dissolved in water at its own pH or optionally at pH 5.5 to 6.5 and sodium chloride is added to make it isotonic. The solution obtained is filtered free from pyrogens and the filtrate is transferred under aseptic conditions into ampoules which are then sterilised and sealed by fusion.

F)          Suppositories
flibanserin 50 mg
solid fat   1650 mg
            1700 mg

The hard fat is melted. At 40° C. the ground active substance is homogeneously dispersed. It is cooled to 38° C. and poured into slightly chilled suppository moulds.

Claims

1) A method of treating post-menopausal Sexual Desire Disorders (lifelong or acquired) in a woman comprising administering an effective amount of flibanserin, optionally in form of the free base or a pharmacologically acceptable acid addition salt, to a woman in need thereof.

2) The method according to claim 1 wherein the flibanserin is in the form of a hydrate and/or solvate thereof.

3) The method according to claim 1, wherein the post-menopausal Sexual Desire Disorder is selected from the group consisting of lifelong post-menopausal Hypoactive Sexual Desire Disorder, lifelong post-menopausal Sexual Aversion Disorder, lifelong post-menopausal loss of sexual desire, lifelong post-menopausal lack of sexual desire, lifelong post-menopausal decreased sexual desire, lifelong post-menopausal inhibited sexual desire, lifelong post-menopausal loss of libido, lifelong post-menopausal libido disturbance, and lifelong post-menopausal frigidity.

4) The method according to claim 1, wherein the post-menopausal Sexual Desire Disorder is selected from the group consisting of lifelong post-menopausal Hypoactive Sexual Desire Disorder, lifelong post-menopausal Sexual Aversion Disorder, lifelong post-menopausal loss of sexual desire, lifelong post-menopausal lack of sexual desire, lifelong post-menopausal decreased sexual desire, and lifelong post-menopausal inhibited sexual desire.

5) The method according to claim 1, wherein the post-menopausal Sexual Desire Disorder is selected from the group consisting of acquired post-menopausal Hypoactive Sexual Desire Disorder, acquired post-menopausal Sexual Aversion Disorder, acquired post-menopausal loss of sexual desire, acquired post-menopausal lack of sexual desire, acquired post-menopausal decreased sexual desire, acquired post-menopausal inhibited sexual desire, acquired post-menopausal loss of libido, acquired post-menopausal libido disturbance, and acquired post-menopausal frigidity.

6) The method according to claim 1, wherein the post-menopausal Sexual Desire Disorder is selected from the group consisting of acquired post-menopausal Hypoactive Sexual Desire Disorder, acquired post-menopausal Sexual Aversion Disorder, acquired post-menopausal loss of sexual desire, acquired post-menopausal lack of sexual desire, acquired post-menopausal decreased sexual desire, acquired post-menopausal inhibited sexual desire.

7) The method according claim 1, wherein the post-menopausal Sexual Desire Disorders is of the generalized subtype.

8) The method according to claim 1, wherein the post-menopausal Sexual Desire Disorders is of the situational subtype.

9) The method according to claim 1, wherein the post-menopausal Sexual Desire Disorders is due to psychological factors.

10) The method according to claim 1, wherein the post-menopausal Sexual Desire Disorders is due to combined factors.

11) The method according to claim 1, wherein flibanserin is administered in form of a pharmaceutically acceptable acid addition salt wherein the salt is formed from an acid selected from the group consisting of succinic acid, hydrobromic acid, acetic acid, fumaric acid, maleic acid, methanesulphonic acid, lactic acid, phosphoric acid, hydrochloric acid, sulphuric acid, tartaric acid, citric acid, and mixtures thereof.

12) The method according to claim 1, wherein flibanserin is administered in form of the free base.

13) The method according to claim 12, wherein flibanserin is administered in form of a polymorph A of the free base, having a melting point of about 161° C. as measured using DSC.

14) The method according to claim 1, characterized in that flibanserin is administered in a dosage range between 0.1 to 400 mg per day.

15) The method according to claim 1, wherein flibanserin is administered once daily.

16) The method of claim 15, wherein flibanserin is adminstered in the evening (50 or 100 mg of flibanserin).

17) The method according to claim 1, wherein flibanserin is administered twice daily.

18) The method of claim 17, wherein flibanserin is adminstered once in the morning (25 or 50 mg of flibanserin) and once in the evening (25 or 50 mg of flibanserin).