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  Česky / Czech version Čes. slov. Farm. 52, 2003, č. 1, s. 33–38
 
Dissolution of Nimodipine in Aqueous Solutions of Hydroxyethyl-β-cyclodextrin and the Survey of Nimodipine Solubilization with Cyclodextrins 
KOPECKÝ F., KOPECKÁ B.1, KACLÍK P. 

Katedra fyzikálnej chémie liečiv Farmaceutickej fakulty Univerzity Komenského, Bratislava 1Katedra farmaceutickej analýzy a nukleárnej farmácie Farmaceutickej fakulty Univerzity Komenského, Bratislava
 


Summary:

       The results of a comprehensive study of the dissolution of the calcium antagonist nimodipine in aqueous solutions of nine cyclodextrins are reported. The used cyclodextrins were native β-cyclodextrin (β-CD), its derivatives hydroxyethyl-β-CD (HE-β-CD), three hydroxypropyl-β-CD (HP-β-CD) with various degree of substitution and methyl-β-CD (M-β-CD), native α-cyclodextrin (α-CD), hydroxypropyl-α-CD (HP-α-CD) and hydroxypropyl-γ-CD (HP-γ-CD). The nimodipine dissolution was studied as a function of time (up to 14 days) and cyclodextrin concentration up to 0.07 mol/l, excepting the less soluble β-CD. In this range of cyclodextrin concentration, linear phase diagrams of nimodipine solubility in the cyclodextrin solutions were observed. From them we derived the stability constants of the inclusions complexes nimodipine – cyclodextrin (1:1) as well as the empirical linear equations for the calculation of the saturated nimodipine concentration at a given cyclodextrin concentration. The most efficient solubiliser of nimodipine was M-β-CD, a good solubilizing efficiency was also shown by HE-β-CD and HP-β-CDs (with a low degree of substitution), which may be acceptable for the preparation of parenteral nimodipine solutions.

        Key words: nimodipine – calcium antagonist – cyclodextrins – inclusion complexes – solubilization – dissolution
       

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