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Generated: February 25, 2018

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Title: Anti-inflammatory androstane derivative compositions
Abstract:There is provided a crystalline chemical composition comprising a compound of formula (I) ##STR1## in which the crystal lattice is stabilised by the presence of a guest molecule, characterised in the crystalline composition is of space group P2.sub.1 2.sub.1 2.sub.1 having unit cell dimensions of about 7.6.+-.0.6 .ANG., 12.7.+-.0.7 .ANG., and 33.+-.3 .ANG. when determined at 120K.
Inventor(s): Biggadike; Keith (Stevenage, GB), Coote; Steven John (Stevenage, GB), Craig; Andrew (Tonbridge, GB), Jacewicz; Victor (Tonbridge, GB), Millan; Michael J. (Tonbridge, GB), Seager; John F. (Stevenage, GB), Theophilus; Andrew L. (Stevenage, GB)
Assignee: SmithKline Beecham Corporation (Philadelphia, PA)
Filing Date:Sep 11, 2002
Application Number:10/241,658
Claims:1. A crystalline chemical composition comprising a compound of formula (I) ##STR8##

in which the crystal lattice is stabilised by the presence of a guest molecule, characterised in the crystalline composition is of space group P2.sub.1 2.sub.1 2.sub.1 having unit cell dimensions of about 7.7.+-.0.6 .ANG., 13.7.+-.0.7 .ANG., and 37.+-.3 .ANG. when determined at 120K.

2. A composition according to claim 1 wherein the unit cell dimensions are 7.7.+-.0.4 .ANG., 13.8.+-.0.3 .ANG., and 36.8.+-.3 .ANG. when determined at 120K.

3. A composition according to claim 1 wherein the crystal lattice is stabilised by a hydrogen bonding interaction between the hydrogen atom of the C11 hydroxy on the compound of formula (I) with the oxygen of the C3 carbonyl on a second molecule of the compound of formula (I).

4. A composition according to claim 1 wherein the guest molecule has a relative molecular weight in the range 16 to 150.

5. A composition according to claim 1 wherein the guest molecule is toluene.

6. A composition according to claim 1 wherein the guest molecule is m-xylene.

7. A composition according to claim 1 wherein the guest molecule is o-xylene.

8. A composition according to claim 1 wherein the guest molecule is fluorobenzene.

9. A composition according to claim 1 wherein the guest molecule is chlorobenzene.

10. A composition according to claim 1 wherein the guest molecule is ethylbenzene.

11. A composition according to claim 1 wherein the ratio of compound of formula (I) to guest molecule is 1:5-0.25.

12. A pharmaceutical composition comprising a composition according to claim 1 together with a physiologically acceptable diluent or carrier.

13. A method for the treatment of a human or animal subject with an inflammatory and/or allergic condition, which method comprises administering to said human or animal subject an effective amount of the composition according to claim 1.

14. A pharmaceutical composition comprising a composition according to claim 1 in combination with another therapeutically active agent.

15. A composition according to claim 14 wherein the other therapeutically active ingredient is a long acting .beta..sub.2 -adrenoreceptor agonist.

16. A process for preparing a composition according to claim 1 which comprises (a) crystallising the composition from a solution containing a compound of formula (I) and the guest molecule; or (b) contacting the compound of formula (I) or another composition according claim 1 in solid form with a liquid containing the guest molecule and obtaining the composition therefrom; or (c) contacting a compound of formula (I) or another composition according to claim 1 in solid form with a vapour containing the guest molecule.
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