PROCESS FOR PRODUCING BILE-ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

Bile acid derivatives of the formula I W-X-G in which G is a bile acid residue, W is an active substance portion of a medicament and X is a linker between bile acid residue and active substance portion, are outstandingly suitable for introducing active substances into the enterohepatic circulation....

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Hauptverfasser: KRAMER,WERNER, WESS,GUENTHER
Format: Patent
Sprache:eng
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Zusammenfassung:Bile acid derivatives of the formula I W-X-G in which G is a bile acid residue, W is an active substance portion of a medicament and X is a linker between bile acid residue and active substance portion, are outstandingly suitable for introducing active substances into the enterohepatic circulation. The compounds I are absorbed and enter the bloodstream. This makes it possible by utilising the natural reabsorption of the bile acids to improve the absorption of drugs which are absorbed with difficulty, if at all. W can be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a liver protective, an antihyperlipidaemic, a diuretic, an agent to lower blood pressure, a renin inhibitor, a substance to treat cirrhosis of the liver or a substance for treating diabetes. G is a bile acid residue in the form of the free, natural or chemically modified acids, the esters and amides, the salt forms and forms derivatised on alcohol groups. X is a large number of intermediate members or else a bond.