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Merck

Lactic acid oligomers (OLAs) as prodrug moieties.

Die Pharmazie (2013-03-09)
J Kruse, B Lachmann, R Lauer, S Eppacher, C R Noe
ABSTRACT

In this paper we propose the use of lactic acid oligomers (OLAs) as prodrug moieties. Two synthetic approaches are presented, on the one hand a non selective oligomerisation of lactic acid and on the other hand a block synthesis to tetramers of lactic acid. Dimers of lactic acid were investigated with respect to their plasma stability and their adsorption to albumine. Ibuprofen was chosen as the first drug for OLAylation. The ester 19 of LA(1)-ibuprofen was evaluated with respect to the degradation to human plasma and the adsorption to albumine. All results indicate that lactic acid oligomers are promising prodrug moieties.

MATERIALI
N° Catalogo
Marchio
Descrizione del prodotto

Sigma-Aldrich
Ibuprofene, ≥98% (GC)
Sigma-Aldrich
(S)-(+)-Ibuprofen, ReagentPlus®, 99%
Supelco
Ibuprofene, Pharmaceutical Secondary Standard; Certified Reference Material
Supelco
Ibuprofene
Supelco
Ibuprofen solution, 1.0 mg/mL in methanol, ampule of 1 mL, certified reference material, Cerilliant®
Supelco
Ibuprofen sodium salt, ≥98% (GC)
Ibuprofene, European Pharmacopoeia (EP) Reference Standard
Ibuprofene, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
Ibuprofene, meets USP testing specifications