Preparation and Characterization of Solid Complexes of Naphtoquinone and Hydroxypropyl-b-Cyclodextrin 英文参考文献.docVIP

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Preparation and Characterization of Solid Complexes of Naphtoquinone and Hydroxypropyl-b-Cyclodextrin 英文参考文献.doc

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Preparation and Characterization of Solid Complexes of Naphtoquinone and Hydroxypropyl-b-Cyclodextrin 英文参考文献

342 Molecules 2000, 5 Preparation and Characterization of Solid Complexes of Naphtoquinone and Hydroxypropyl-β-Cyclodextrin Marcela Linares, María Martínez de Bertorello and Marcela Longhi* Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba. Ciudad Universitaria , 5000 Córdoba, Argentina Fax: 54-351-433-4163, E-mail: mrlcor@dqo.fcq.unc.edu.ar * Author to whom correspondence should be addressed. Abstract: The formation of an inclusion compound between a naphthoquinone derivative (I) and HP-?-CD was studied in solid state by X-ray diffractometry, DSC, and IR. Introduction The formation of inclusion complexes with cyclodextrins constitutes a widely used strategy to in- crease the aqueous solubility and to decrease the countereffects of many drugs. Isoxazolylnaphthoqui- nones belong to a family of compounds with bacterial and tripanocidal activity [1,2], as well as with very low solubility in water. In previous studies in our laboratory, we demonstrated that their hydro- philic capacity increases markedly through complexation with hydroxypropyl-?-cyclodextrin (HP-?- CD) in aqueous solution [3]. In this study we investigate the formation of complexes between 2-hydroxy-N-(3,4-dimethyl-5- isoxazolyl)-1,4-naphthoquinone-4-imine (I) and HP-?-CD in solid state. Thermoanalytic techniques, X-ray diffraction and IR spectroscopy were performed [4]. Experimental 1. Materials The synthesis and identification procedures for I have been described previously. HP-β-CD (MW = 1326 - 1400; degree of molar substitution, 7.0) was a gift from CERESTAR USA Inc. (Hammond, IN). All other materials and solvents were of analytical reagent grade. 2. Methods 2.1 Preparation of inclusion complexes 343 Molecules 2000, 5 Formation of solid complexes: aqueous solutions were prepared between I and HP-?-CD in con- centrations of 1:0,5; 1:1 and 1:2, respectively. The solutions were then placed in a thermostat