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

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The inclusion ability of triacetyl-β-cyclodextrin (TAβCD), a hydrophobic cyclodextrin (CD) derivative was examined, using nicardipine hydrochloride (NC) as model drug. The binary compounds were prepared in a 1:1 molar ratio by the kneading and the spray-drying techniques. In order to confirm the complexation between NC and TAβCD in the solid state, differential scanning calorimetry, X-ray diffractometry, Fourier transformation-infrared spectroscopy and scanning electron microscopy were carried out and the results were compared with the corresponding physical mixture in the same molar ratio. The kneaded product presented only slight modifications on the drug physicochemical and morphological properties, which could mean that no complex formation occurred during this process. In contrast, spray-drying was found to produce inclusion complexes with amorphous nature. In vitro dissolution studies were carried out in simulated gastric (pH 1.2) and intestinal (pH 6.8) fluids, according to the United States Pharmacopoeia (USP) basket method. The NC in vitro release from the kneaded and spray-dried products was markedly retarded in both dissolution media. However, this retarding effect was significantly more evident for the spray-dried compound. It was concluded that the formation of real inclusion complexes could only be achieved by the spray-drying method.
公益社団法人日本薬学会の論文
2002-12-01