Author/Editor     Planinšek, Odon; Pišek, Robert; Kristl, Albin; Schmidt, Peter C; Srčić, Stanko
Title     Increased aqueous solubility of N-(7-oxododecanoyl)-L-alanyl-D-isoglutamine by coprecipitating with various pharmaceutical carriers
Translated title     Povečana topnost N-(7-oksododekanoil)-L-alanil-D-izoglutamina v vodi z izdelavo koprecipitatov z različnimi pomožnimi snovmi
Type     članek
Source     Acta Pharm Zagreb
Vol. and No.     Letnik 49, št. 2
Publication year     1999
Volume     str. 89-98
Language     eng
Abstract     N-(7-oxododecanoyl)-L-alanyl-D-isoglutamine, which is a modified N-acetylmuramyl-L-alanyl-D-isoglutamine (MDP, the smallest immunologically active glucopeptide's subunit of the bacterial cell wall), was chosen after immunorestorement tests for further preclinical testing. For the preparation of an appropriate parenteral formulation, the solubility of the compound has to be increased. For this purpose different physical mixtures and solid dispersions prepared by solvent evaporation method with different carriers were investigated. The solubility of N-(7-oxododecanoyl)-L-alanyl-D-isoglutamine increased from 0.16 g L-1 to 27 g L-1 for the dispersion with nicotinamide, to 40 g L-1 for the dispersion with sodium salicylate and to 24 g L-1 for the complex with 2-hydroxypropyl-beta-cyclodextrin.
Summary     N-(7-oksododekanoil)-L-alanil-D-izoglutamin je bil izbran po testu imunorestavracije na živalih kot ustrezna učinkovina za nadaljna testiranja. Njegova nizka vodotopnost je omejitev pri izdelavi parenteralnega pripravka. V delu smo neravnotežno topnost in hitrost raztapljanja N-(7-oksododekanoil)-L-alanil-D-izoglutamina v vodi povečali s pripravo trdnih disperzij z metodo evaporacije topila. Topnost N-(7-oksododekanoil)-L-alanil-D-izoglutamina po 24 urah smo z 0,16 g L-1 povečali na 27 g L-1 s pripravo trdnih disperzij z nikotinamidom, na 40 g L-1 z natrijevim salicilatom in na 16 g L-1 z 2-hidroksipropil-beta-ciklodekstrinom.
Descriptors     ACETYLMURAMYL-ALANYL-ISOGLUTAMINE
SOLUTIONS
DRUG CARRIERS
SOLUBILITY
NIACINAMIDE
SODIUM SALICYLATE
CYCLODEXTRINS
DIFFERENTIAL THERMAL ANALYSIS