Claims
- 1. A unit formulation which comprises a compound of formula whereinX represents SO2 or CO; R1 represents phenyl, carboxymethylphenyl or —R2Y; R2 represents (CH2)n or benzyl-(CH2)n wherein one or more of the hydrogen atoms of the alkylene moiety may be replaced by a C1-6-alkyl, NH2, NH(C1-6-alkyl) or N(C1-6-alkyl)2 group; Y represents COOH, SO3H, OH, NH2, NHR3 or N(R3)2; R3 represents C1-6-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/mm3.
- 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/mm3.
- 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; wherein X represents SO2 or CO; R1 represents phenyl, carboxymethylphenyl or —R2Y; R2 represents (CH2)n or benzyl-(CH2)n wherein one or more of the hydrogen atoms of the alkylene moiety may be replaced by a C1-6-alkyl, NH2, NH(C1-6-alkyl) or N(C1-6-alkyl)2 group; Y represents COOH, SO3H, OH, NH2, NHR3 or N(R3)2; R3 represents C1-6-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/mm3.
- 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/mm3.
- 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; wherein X represents SO2 or CO; R1 represents phenyl, carboxymethylphenyl or —R2Y; R2 represents (CH2)n or benzyl-(CH2)nwherein one or more of the hydrogen atoms of the alkylene moiety may be replaced by a C1-6-alkyl, NH2, NH(C1-6-alkyl) or N(C1-6-alkyl)2 group; Y represents COOH, SO3H, OH, NH2, NHR3 or N(R3)2; R3 represents C1-6-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/mm3.
- 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/mm3.
- 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/mm3.
- 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.
Priority Claims (1)
Number |
Date |
Country |
Kind |
9700934-4 |
Mar 1997 |
SE |
|
Parent Case Info
This is a continuation of International Patent Application No. PCT/SE98/00455, with an international filing date of Mar. 13, 1998, now pending.
US Referenced Citations (5)
Foreign Referenced Citations (4)
Number |
Date |
Country |
2 080 796 |
Feb 1982 |
GB |
8102671 |
Oct 1981 |
WO |
9206679 |
Apr 1992 |
WO |
9518622 |
Jul 1995 |
WO |
Continuations (1)
|
Number |
Date |
Country |
Parent |
PCT/SE98/00455 |
Mar 1998 |
US |
Child |
09/068823 |
|
US |