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Medicinal Chemistry Course

Medicinal Chemistry Course

Plasma concentration vs

Plasma concentration vs time after7 µmol/kg orally to ratsPlasma concentration (nmol/L)25002000R-omeprazole1500omeprazole1000S-omeprazole50000 30 60 90Andersson et alTime min

Isomers of omeprazole- after 1990• Gram quantities prepared (and subsequently Kg´s)• Enough quantities to identify possible differences inpharmacokinetic and metabolic profile• Alkaline salts crystalline (as opposed to neutral form)• Salts stable against racemisation• A clear pharmacokinetic difference identified in rats• Opportunity to go quickly to human Phase ILindberg / von Unge

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