Fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol

1. A solid pharmaceutical composition comprising a pharmaceutically acceptable carrier and as active ingredient a therapeutically effective amount of the Fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol, and further comprising a wetting agent, said wetting agent being a polyethylene glycol sorbitan fatty acid ester.

2. A pharmaceutical composition according to claim 1 wherein the composition is suitable for oral administration.

3. A pharmaceutical composition according to claim 1 comprising by weight based on the total weight of the composition:

(a) from 5 to 50% of active ingredient;

(b) from 0.01 to 5% of a said wetting agent;

(c) from 40 to 92% of a diluent;

(d) from 0.1 to 5% of a glidant.

4. A pharmaceutical composition according to claim 1 wherein the composition is in the form of a tablet.

5. A pharmaceutical composition according to claim 4 comprising by weight based on the total weight of the tablet core

(a) from 5 to 50% of active ingredient;

(b) from 0.01 to 5% of a wetting agent;

(c) from 40 to 92% of a diluent;

(d) from 0 to 10% of a polymer;

(e) from 2 to 10% of a disintegrant;

(f) from 0.1 to 5% of a glidant;

(g) from 0.1 to 1.5% of a lubricant.

6. A pharmaceutical composition according to claim 5 having the following composition

Active ingredient

120.89

mg (i.e. 100 mg base

equivalent)

Lactose monohydrate (200 mesh)

152.91

mg

Maize starch

66

mg

Hypromellose 2910 15 mPa · s

8

mg

Polysorbate 20

1

mg

Microcrystalline cellulose

82.2

mg

Croscarmellose sodium

23

mg

Colloidal silicon dioxide

1.4

mg

Magnesium stearate

4.6

mg.

7. A pharmaceutical composition according to claim 4 which is film-coated.

8. A process for preparing a pharmaceutical composition according to claim 4 comprising the following steps:

(i) dry blending the active ingredient and part of the diluent;

(ii) preparing a binder solution by dissolving the binder and the wetting agent in the binder solution solvent;

(iii) spraying the binder solution obtained in step (ii) on the mixture obtained in step (i);

(iv) drying the wet powder obtained in step (iii) followed by sieving and optionally mixing;

(v) mixing the remaining part of the diluent, the disintegrant and the optional glidant in the mixture obtained in step (iv);

(vi) optionally adding the lubricant to the mixture obtained in step (v);

(vii) compressing the mixture obtained in step (vi) into a tablet;

(viii) optionally film-coating the tablet obtained in step (vii).

9. A process for preparing a pharmaceutical composition according to claim 4 comprising the following steps:

(i) dry blending the active ingredient and part of the diluent;

(ii) preparing a granulation solution optionally containing the binder and wetting agent;

(iii) spraying the granulation solution obtained in step (ii) on the mixture obtained in step (i);

(iv) drying the wet granulate obtained in step (iii) followed by sieving and optionally mixing;

(v) mixing the remaining part of the diluent, the disintegrant, the optional glidant and optionally the binder and wetting agent in the mixture obtained in step (iv);

(vi) optionally adding the lubricant to the mixture obtained in step (v);

(vii) compressing the mixture obtained in step (vi) into a tablet;

(viii) optionally film-coating the tablet obtained in step (vii).

10. Process for the preparation of a compound as claimed in claim 1 characterized by reacting the corresponding free base with fumaric acid in the presence of a suitable solvent.

11. A method for treating a patient suffering from a mycobacterial infection, said method comprising administering to said patient a therapeutically effective amount of the composition of claim 1 .

12. The method of claim 11 wherein the Patient is suffering from tuberculosis.