Complexation of Manidipine with Cyclodextrins and their Derivatives.

Autor: Csabai, Katalin, Vikmon, Maria, Szejtli, József, Redenti, Enrico, Poli, Gianluigi, Ventura, Paolo
Zdroj: Journal of Inclusion Phenomena & Molecular Recognition in Chemistry; Jun1998, Vol. 31 Issue 2, p169-178, 10p
Abstrakt: Manidipine (MDP,(±)-2-[-(diphenylmethyl)-1-piperazinyl]ethylmethyl-1,4-dihydro-2,6-dimethyl-4(m-nitrophenyl)-3,5-pyridinedicarboxylate methyl-ester) is a poorlysoluble (<1 μg/mL) long acting antihypertensive drug. Salt formingwith citric or tartaric acid results in a 400 to 600 fold solubilityenhancement, respectively, which can be further increased by an order ofmagnitude with cyclodextrins. Dimethyl-βCD alone results in a more than8000 fold solubility enhancement. Besides the strongly enhanced solubility1HNMR spectroscopy also proves the inclusion-type interactionbetween Manidipine and cyclodextrins. From the attained 5-8 mg/mL solubilityof the drug in water an improved bioavailability and pharmacokinetics isexpected. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index
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