Abstract: This invention relates to new water-soluble solid pharmaceutical inclusion complexes and their aqueous solutions for oral, ophthalmic, topical or parenteral use containing a macrolide and certain cyclodextrins. More particularly the invention relates to new water-soluble solid pharmaceutical inclusion complexes and their solutions in aqueous solvents, said compositions containing a) as an active ingredient a macrolide such as Rapamycin, Pimecrolimus, Temsirolimus, Everolimus or Tacrolimus in an amorphous form and optionally in the form of their polymorphic hydrates or solvates e.g. solvates formed with acetone or ethanol. b) a large surface cyclodextrin, such as gamma cyclodextrin—whereby the weight ratio of said macrolide to said cyclodextrin ranges between 1:111 and 1:333.

Abstract: This invention relates to new water-soluble solid pharmaceutical inclusion complexes and their aqueous solutions for oral, ophthalmic, topical or parenteral use containing a macrolide and certain cyclodextrins. More particularly the invention relates to new water-soluble solid pharmaceutical inclusion complexes and their solutions in aqueous solvents, said compositions containing a) as an active ingredient a macrolide such as Rapamycin, Pimecrolimus, Temsirolimus, Everolimus or Tacrolimus in an amorphous form and optionally in the form of their polymorphic hydrates or solvates e.g. solvates formed with acetone or ethanol. b) a large surface cyclodextrin, such as gamma cyclodextrin—whereby the weight ratio of said macrolide to said cyclodextrin ranges between 1:111 and 1:333.

Abstract: Process for the preparation of compounds active in the treatment of Parkinson's disease, and such compounds, having general formula (VI) wherein R4 may be, independently, a linear, branched or cyclic, saturated or unsaturated C1-8 alkyl radical, such as, for example, the radicals methyl, ethyl, propyl, butyl, isobutyl, tert-butyl, pentyl, cyclopentyl, hexyl, cyclohexyl and octyl. The process utilizes as starting materials the compound of formula (I) wherein R1 represents a linear, branched or cyclic, saturated or unsaturated C1-8 alkyl residue.

Abstract: In the synthesis of amikacin, having the formula: ##STR1## by acylation of a diprotected derivative of kanamycin A with a reactive derivative of L-(-)-4-amino-2-hydroxybutyric acid, the selection of the reaction solvent and of the pH conditions permit the industrial economically and the synthesis yield to be improved.

Abstract: A novel process for the synthesis of amikacin starting from kanamycin A protected at the positions 3 and 6' is described comprising the reaction of kanamycin A with a salt of a bivalent metal cation selected from zinc, nickel, iron, cobalt, manganese, copper and cadmium in the presence of water as the solvent or co-solvent followed by the in situ reaction of the resulting complex with a reactive derivative of L-amino-2-hydroxy-butyric acid, removal of the metal cation of the protecting groups and purification of the thus obtained raw product. The acylation under these conditions is extremely selective.

Abstract: A process for the total or partial elimination of aspartic acid and glutamic acid from a protein hydrolyzate or a mixture of aminoacids is described, which consists of passing the hydrolyzate or mixture of aminoacids in solution on an anion exchange resin and then washing with water or eluting the aminoacids from the resin. Aspartic acid and glutamic acid are at least partially separated from the other aminoacids because of their affinity for the resin which is greater than the affinity of the other aminoacids. The resulting mixtures of aminoacids may be used as such or may be further adjusted by addition of valine, leucine, isoleucine, and arginine to give products valuable in clinical nutrition.

Abstract: A process for the preparation of the anhydride of N-formyl-L-aspartic acid by reacting L-aspartic acid with nearly stoichiometric amounts of formic acid and acetic anhydride, under controlled conditions of temperature, reaction and addition times. The product is a known intermediate in the synthesis of .alpha.-L-aspartyl-L-phenylalanine methyl ester, a known sweetening agent.

Abstract: A process for the removal of the formyl group in N-formylated peptides or their esters is described. The N-formyl compound is reacted with hydrazine or a substituted hydrazine of formula I: ##STR1## at a pH between 1 and 3.5, keeping the pH constant during the reaction. The process is particularly useful for the preparation of aspartam.