Investigation and Physicochemical Characterization of Vinpocetine-Sulfobutyl Ether β-Cyclodextrin Binary and Ternary Complexes

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概要

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• The purpose of this study was to investigate the interactions between vinpocetine (VP), sulfobutyl ether beta-cyclodextrin (SBEβCD) and the water-soluble polymers polyvinylpyrrolidone (PVP) and hydroxypropyl methylcellulose (HPMC). The water-soluble polymers were shown to improve the complexation efficiency of SBEβCD, and thus less SBEβCD was needed to prepare solid VP-SBEβCD complexes in the presence of the polymers. The interactions between VP and SBEβCD, with or without PVP or HPMC, were thoroughly investigated in aqueous solutions using the phase-solubility method as well as in the solid state. The amount of VP solubilized in water or aqueous polymer solution increased linearly with increasing SBEβCD concentration, demonstrating A_L-type plots. We estimated the apparent stability constant (K_c) at room temperature of VP-SBEβCD binary complex to be 340 _M^<-1> and this value increased to 490_M^<-1> or 390 _M^<-1>, respectively, with the addition of PVP and HPMC, assuming a 1:1 VP-SBEβCD molar ratio. Improvement in the K_c values for ternary complexes clearly confirmed the benefit of the addition of water-soluble polymers to promote higher complexation efficiency. Solid VP-SBEβCD binary and ternary systems were prepared by physical mixing, kneading, coevaporation, and lyophilization methods and fully characterized by scanning electron microscopy, differential scanning calorimetry, and X-ray diffractometry. The results obtained suggest that coevaporation and lyophilization methods yield a higher degree of amorphous entities and indicated formation of VP-SBEβCD binary and ternary complexes.

• 公益社団法人日本薬学会の論文
• 2003-08-01

著者

• Veiga Francisco

  Laboratory Of Pharmaceutical Technology Faculty Of Pharmacy University Of Coimbra

• Ribeiro Laura

  Laboratory of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra

• Loftsson Thorsteinn

  Department of Pharmacy, University of Iceland

• Ferreira Domingos

  Laboratory of Pharmaceutical Technology, Faculty of Pharmacy, University of Porto

• Ribeiro Laura

  Laboratory Of Pharmaceutical Technology Faculty Of Pharmacy University Of Coimbra

• Loftsson T

  Department Of Pharmacy University Of Iceland

• Ferreira Domingos

  Laboratory Of Pharmaceutical Technology Faculty Of Pharmacy University Of Porto

関連論文

• Effect of the Hydrophobic Nature of Triacetyl-β-cyclodextrin on the Complexation with Nicardipine Hydrochloride : Physicochemical and Dissolution Properties of the Kneaded and Spray-dried Complexes
• Molecular Modelling and ^1H-NMR:Ultimate Tools for the Investigation of Tolbutamide : β-Cyclodextrin and Tolbutamide : Hydroxypropyl-β-Cyclodextrin Complexes
• Investigation and Physicochemical Characterization of Vinpocetine-Sulfobutyl Ether β-Cyclodextrin Binary and Ternary Complexes

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