Inclusion complex of the antiviral drug acyclovir with cyclodextrin in aqueous solution and in solid phase

Química Nova

Carlos Von Plessing Rossel²  Jacqueline Sepúlveda Carreño¹  Mario Rodríguez-baeza¹  Joel Bernabé Alderete¹ 

[1] ,Universidad de Concepción Facultad de Farmacia Departamento de FarmaciaConcepción,Chile

关键词: cyclodextrin;    acyclovir;    inclusion complex;   

DOI  :  10.1590/S0100-40422000000600007

来源: SciELO

【 摘 要 】

Complexation between acyclovir (ACV), an antiviral drug used for the treatment of herpes simplex virus infection, and beta-cyclodextrin (beta-CD) was studied in solution and in solid states. Complexation in solution was evaluated using solubility studies and nuclear magnetic resonance spectroscopy (¹H-NMR). In the solid state, X-ray diffraction, differential scanning calorimetry (DSC), thermal gravimetric analysis (TGA) and dissolution studies were used. Solubility studies suggested the existence of a 1:1 complex between ACV and beta-CD. ¹H-NMR spectroscopy studies showed that the complex formed occurs with a stoichiometry ratio of 1:1. Powder X-ray diffraction indicated that ACV exists in a semicrystalline state in the complexed form with beta-CD. DSC studies showed the existence of a complex of ACV with beta-CD. The TGA studies confirmed the DSC results of the complex. Solubility of ACV in solid complexes was studied by the dissolution method and it was found to be much more soluble than the uncomplexed drug.

【 授权许可】

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