Aminosalicylate derivatives for treatment of inflammatory...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

Reexamination Certificate

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C514S053000, C514S055000, C536S018700, C536S020000, C536S055200, C536S055300, C536S124000, C252S182270

Reexamination Certificate

active

10688585

ABSTRACT:
Therapeutic 5-aminosalicylic acid derivative compositions having general formula (I), wherein R is a 1-deoxy sugar residue or a poly(ethylene glycol) chain-containing residue, are provided. The compositions enable topical delivery of 5-aminosalicylic acid to the gastrointestinal tract following oral administration in pharmaceutical preparations. According to the invention, the compositions stabilize pharmaceutical compositions containing therapeutic 5-aminosalicylic acid derivatives in a manner that enhances the retention of said compositions in the intestine, decreases the cellular absorption thereof, and decreases the transfer of said compositions or the 5-aminosalicylic acid derived therefrom to the systemic circulation

REFERENCES:
Tjoernelund et al, Journal of Chromatography, “Stability of 5-Aminosalicylic Acid and its Metabolites in Plasma at −° C: Formation of N-β-D-Glucopyranosyl-5-Aminosalicylic Acid”, 1991, vol. 570, No. 1, pp. 224-228.
Tjoernelund et al reference, Xenobiotica, “New Metabolites of the Drug 5-Aminosalicylic Acid I: N-β-D-Glucopyranosyl-5-Aminosalicylic Acid”, 1989, vol. 19, No. 8, pp. 891-899.

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