In vitro and in vivo study of water-soluble prodrugs of dexanabinol

Emil Pop, Stanislaw Rachwal, Jirina Vlasak, Anat Biegon, Alevtina Zharikova, Laszlo Prokai

Research output: Contribution to journalArticlepeer-review

12 Scopus citations

Abstract

Trialkylammonium acetoxymethyl esters of dexanabinol were synthesized and evaluated as water-soluble prodrugs. Syntheses were performed by conventional methods; solubility in water and stability in buffers and human plasma were determined by HPLC, and in vivo tissue distribution studies were performed in a rat model. Most of the new derivatives were soluble in water (~50 mg/mL). They were relatively stable in water, while rapidly hydrolyzed in human plasma. Distribution studies indicated that peak concentrations of drug both in blood (30 μg/mL) and brain (2 μg/mL) were rapidly (5 min) achieved after iv administration of a selected prodrug to rats. The blood concentration decreased faster than brain levels which were detectable even after 24 h. Some of the examined esters could be further developed as water soluble prodrugs of dexanabinol.

Original languageEnglish
Pages (from-to)1156-1160
Number of pages5
JournalJournal of Pharmaceutical Sciences
Volume88
Issue number11
DOIs
StatePublished - Nov 1999

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