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Claims for Patent: 6,197,341

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Claims for Patent: 6,197,341

Title: Formulations of balsalazide and its derivatives
Abstract:The invention provides a unit formulation which comprises a 2-hydroxy-5-phenylazobenzoic acid derivative which is particularly sodium balsalazide dihydrate which formulation has a density of at least 0.9 mg/mm.sup.3 and its use in the treatment of gastrointestinal diseases.
Inventor(s): Friess; Stefan (S-22587 Hamburg, DE), Heckenmuller; Harald (D-22559 Hamburg, DE), Szambien; Oliver (D-23611 Bad Schwartau, DE)
Assignee:
Application Number:09/068,823
Patent Claims: 1. A unit formulation which comprises a compound of formula ##STR2##

wherein

X represents SO.sub.2 or CO;

R.sup.1 represents phenyl, carboxymethylphenyl or --R.sup.2 Y;

R.sup.2 represents (CH.sub.2).sub.n or benzyl-(CH.sub.2).sub.n wherein one or more of the hydrogen atoms of the alkylene moiety may be replaced by a C.sub.1-6 -alkyl, NH.sub.2, NH(C.sub.1-6 -alkyl) or N(C.sub.1-6 -alkyl).sub.2 group;

Y represents COOH, SO.sub.3 H, OH, NH.sub.2, NHR.sup.3 or N(R.sup.3).sub.2 ;

R.sup.3 represents C.sub.1-6 -alkyl optionally substituted by a carboxylic or sulphonic acid group; and

n is an integer from 1 to 6;

or an ester thereof; or an active metabolite thereof; or a non-toxic pharmaceutically acceptable salt thereof;

in association with one or more pharmaceutically acceptable excipients or binding agents;

which formulation is in the form of a tablet having a density of at least 0.9 mg/mm.sup.3.

2. A formulation according to claim 1 wherein the compound of formula (I) is sodium balsalazide dihydrate.

3. A formulation according to claim 1 wherein the density of the formulation is from 1.1 to 1.7 mg/mm.sup.3.

4. A method of treating a patient suffering from a gastrointestinal disease, which method comprises administering to the patient a therapeutically effective amount of a formulation comprising:

a compound of formula I or a derivative thereof; ##STR3##

wherein

X represents SO.sub.2 or CO;

R.sup.1 represents phenyl, carboxymethylphenyl or --R.sup.2 Y;

R.sup.2 represents (CH.sub.2).sub.n or benzyl-(CH.sub.2).sub.n wherein one or more of the hydrogen atoms of the alkylene moiety may be replaced by a C.sub.1-6 -alkyl, NH.sub.2, NH(C.sub.1-6 -alkyl) or N(C.sub.1-6 -alkyl).sub.2 group;

Y represents COOH, SO.sub.3 H, OH, NH.sub.2, NHR.sup.3 or N(R.sup.3).sub.2 ;

R.sup.3 represents C.sub.1-6 -alkyl optionally substituted by a carboxylic or sulphonic acid group; and

n is an integer from 1 to 6;

and wherein the derivative is selected from the group consisting of esters, active metabolites, and non-toxic pharmaceutically acceptable salts;

in association with one or more pharmaceutically acceptable excipients or binding agents;

wherein the formulation is in the form of a tablet having a density of at least 0.9 mg/mm.sup.3.

5. The method according to claim 4, wherein the compound of formula I is sodium balsalazide dihydrate.

6. The method according to claim 4, wherein the density of the formulation is from 1.1 to 1.7 mg/mm.sup.3.

7. The method according to claim 4, wherein the gastrointestinal disease is active ulcerative colitis.

8. The method according to claim 4, wherein the gastrointestinal disease is colon cancer.

9. A method of manufacturing a tablet, said method comprising the steps of:

granulating a compound of formula I or a derivative thereof; ##STR4##

wherein

X represents SO.sub.2 or CO;

R.sup.1 represents phenyl, carboxymethylphenyl or --R.sup.2 Y;

R.sup.2 represents (CH.sub.2).sub.n or benzyl-(CH.sub.2).sub.n wherein one or more of the hydrogen atoms of the alkylene moiety may be replaced by a C.sub.1-6 -alkyl, NH.sub.2, NH(C.sub.1-6 -alkyl) or N(C.sub.1-6 -alkyl).sub.2 group;

Y represents COOH, SO.sub.3 H, OH, NH.sub.2, NHR.sup.3 or N(R.sup.3).sub.2 ;

R.sup.3 represents C.sub.1-6 -alkyl optionally substituted by a carboxylic or sulphonic acid group; and

n is an integer from 1 to 6;

and wherein the derivative is selected from the group consisting of esters, active metabolites, and non-toxic pharmaceutically acceptable salts;

in association with one or more pharmaceutically acceptable excipients or binding agents;

and compressing the granulate to form a tablet having a density of at least 0.9 mg/mm.sup.3.

10. The method according to claim 9, wherein the formulation is granulated with a binding agent in the granulating step.

11. The method according to claim 9, wherein the granulate is compressed with an excipient in the compressing step.

12. The method according to claim 9, further comprising the step of coating the tablet with a coating dispersion, wherein the compressing step precedes the step of coating.

13. A formulation according to claim 2, wherein the density of the formulation is from 1.1. to 1.7 mg/mm.sup.3.

14. A method of manufacturing a tablet, said method comprising the steps of:

granulating sodium balsalazide dihydrate; and

compressing the granulate to form a tablet having a density of at least 0.9 mg/mm.sup.3.

15. The method according to claim 14, wherein the sodium balsalazide dihydrate is granulated with a binding agent in the granulating step.

16. The method according to claim 14, wherein the granulate is compressed with an excipient in the compressing step.

17. The method according to claim 14, further comprising the step of coating the tablet with a coating dispersion, wherein the compressing step precedes the step of coating.

18. The method according to claim 4, wherein the therapeutically effective amount is a dosage regimen of three tablets of the formulation, each tablet weighing about 750 mg, three times each day.

19. The method according to claim 4, wherein the therapeutically effective amount is a dosage regimen of two tablets of the formulation, each tablet weighing about 1125 mg, three times each day.

20. The method according to claim 4, wherein the therapeutically effective amount is a dosage regimen of one tablet of the formulation, each tablet weighing about 2250 mg, three times each day.
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