engleski

Influence of β-cyclodextrin and its various derivatives on cinnarizine solubility in water

Cinnarizine (CIN) is a piperazine derivative with antihistaminic and calcium channel blocking activity which is widely used for the treatment of vertigo and prevention of motion sickness. Due to its extremely poor aqueous solubility, CIN is classified as a Class 2 drug substance according to The Biopharmaceutical Classification System [1]. β-Cyclodextrins (β-CDs) are cyclic oligosaccharides consisting of seven D- glucopyranose units which are α-(1, 4)-linked in a ring formation. It is already well known that β- CDs can interact with poorly soluble drugs by taking up lipophilic drug moieties into their central cavity hence forming inclusion complexes and thus enhancing drug aqueous solubility and bioavailability [2]. Our study aimed to evaluate the influence of β-CD and its randomly methylated (RMβCD), sulfobutylether (SBEβCD), and hydroxypropyl (HPβCD) derivatives on intrinsic solubility of CIN in water through phase- solubility studies according to existing Higuchi- Connors method [2]. To evaluate total drug solubility changes in the presence of increasing CD concentration phase- solubility diagrams were constructed. Quantitative determination of CIN was performed by developed and validated UV/Vis spectrophotometric and spectrofluorimetric methods. [1] S. Raghuvanshi, K. Pathak, J. Drug Delivery 2014, 2014, 479246. [2] P. Jansook, N. Ogawa, T. Loftsson, Int. J. Pharm. 2018, 535, 272– 284.

cinnarizine ; cyclodextrin ; inclusion complex

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