Avtor/Urednik     Planinšek, Odon; Pišek, Robert; Kristl, Albin; Schmidt, Peter C; Srčić, Stanko
Naslov     Increased aqueous solubility of N-(7-oxododecanoyl)-L-alanyl-D-isoglutamine by coprecipitating with various pharmaceutical carriers
Prevedeni naslov     Povečana topnost N-(7-oksododekanoil)-L-alanil-D-izoglutamina v vodi z izdelavo koprecipitatov z različnimi pomožnimi snovmi
Tip     članek
Vir     Acta Pharm Zagreb
Vol. in št.     Letnik 49, št. 2
Leto izdaje     1999
Obseg     str. 89-98
Jezik     eng
Abstrakt     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.
Izvleček     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.
Deskriptorji     ACETYLMURAMYL-ALANYL-ISOGLUTAMINE
SOLUTIONS
DRUG CARRIERS
SOLUBILITY
NIACINAMIDE
SODIUM SALICYLATE
CYCLODEXTRINS
DIFFERENTIAL THERMAL ANALYSIS