Abstract
AbstractThe effect of water-soluble polymers and ionization of the drug molecules on the cyclodextrin, mainly 2-hydroxypropyl-β-cyclodextrin (HPβCD), solubilization of drugs was investigated. HPβCD has significant solubilizing effect on acetazolamide, prazepam, and sulfamethoxazole in aqueous solutions. All three polymers tested-i.e., hydroxypropyl methylcellulose (HPMC), polyvinylpyrrolidone (PVP), and carboxymethylcellulose-increase the solubilizing effect of HPβCD. The polymers increase the solubilization by increasing the apparent stability constant (Kc of the drug-HPβCD complex. Thus, addition of 0.10% (w/v) HPMC to the aqueous complexation medium results in a 56% increase in K, for the acetazolamide-HPβCD complex and a 200% increase in Kc for the prazepam-HPβCD complex. Addition of 0.25% (w/v) PVP to the complexation medium results in a 138% increase in K for the sulfamethoxazole-HPβCD complex. The HPβCD solubilization of the drugs can also be improved by ionization of the drug molecule through pH a...
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