A compound a polymeric bile acid and insulin - useful in the prodn. of a medicament for diabetes mellitus, for nasal admin

A prepn. contg. at least one polymeric bile acid and insulin is new. The bile acids are produced by (i) polymerisation of a monomeric bile acid of the formula G-X-A; G = a bile acid residue or deriv. thereof, X = bridging gp. and A = a polymerisable, ethylenic unsatd. gp., (ii) copolymerisation of m...

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Hauptverfasser: MUELLNER, STEFAN., 65239 HOCHHEIM, DE, SEIPKE, GERHARD., 65719 HOEIM, DE, PETRI, WALTER., 65195 WIESBADEN, DE, GEISEN, KARL., 60318 FRANKFURT, DE
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Sprache:eng ; ger
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Zusammenfassung:A prepn. contg. at least one polymeric bile acid and insulin is new. The bile acids are produced by (i) polymerisation of a monomeric bile acid of the formula G-X-A; G = a bile acid residue or deriv. thereof, X = bridging gp. and A = a polymerisable, ethylenic unsatd. gp., (ii) copolymerisation of monomeric bile acids with monomers of the given formula (I) R9 = H or methyl and R10 = C(O)OR11, C(O)NR12R13, OC(O)R14,CN, OR15, H, halogen, esp. chlorine, bromine or iodine, SO3H or O(CH2CH2O)nR16; R11 = H, C1-10 alkyl, C1-10 mono-hydroxyalkyl or CH2CH2O)nR16; R12, R13, R15, R16 = C1-10 alkyl; R14 = C1-18 alkyl; n = 1-50, (ii) copolymerisation of a monomeric bile acid with N-vinyl pyrrolidone or a deriv. thereof, (iv) copolymerisation of a monomeric bile acid with an ethylenic unsatd. dicarbonic acid anhydride and an ethylenic-unsatd. dicarbonic acid having 2 to 6 C-atoms, their esters or semiesters and human or animal insulin of the formula (II), R30 = a genetically encodable L-amino acid, R31 = OH, a gp. comprising up to 50 C atoms or a genetically encodable L- amino acid not contg. an amido gp.. USE/ADVANTAGE - The prepn. is used for the prodn. of a medicament for Diabetes mellitus and pref. is given nasally (claimed). Compared to prior art prods., the new prepn. can be applied non-parenterally without causing irritation of mucous membranes or cytotoxic reactions. They form clear solns. or dispersions, solubilise insulin, and show membrane transport by the formation of reversed micelles.