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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Main Authors MUELLNER, STEFAN., 65239 HOCHHEIM, DE, SEIPKE, GERHARD., 65719 HOEIM, DE, PETRI, WALTER., 65195 WIESBADEN, DE, GEISEN, KARL., 60318 FRANKFURT, DE
Format Patent
LanguageEnglish
German
Published 21.04.1994
Edition5
Subjects
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Summary: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.
Bibliography:Application Number: DE19924234537