Characterization of lidocaine:hydroxypropyl-β-cyclodextrin inclusion complex

Journal of inclusion phenomena - Tập 57 - Trang 313-316 - 2007
Carolina Morales Moraes1, Priscila Abrami1, Daniele Riberio de Araujo2, Angélica F. A. Braga3, Michelle Georges Issa4, Humberto G. Ferraz4, Eneida de Paula2, Leonardo Fernandes Fraceto1,2
1Departamento de Farmácia, Universidade de Sorocaba, Sorocaba, Brazil
2Departamento de Bioquímica, Instituto de Biologia, Universidade Estadual de Campinas (UNICAMP), Campinas, Brazil
3Departamento de Anestesiologia, F.C. Médicas, UNICAMP, Campinas, Brazil
4Departamento de Farmácia, F.C. Farmacêuticas, Universidade de São Paulo (USP), Sao Paulo, Brazil

Tóm tắt

An inclusion complex was prepared between the local anesthetic lidocaine (LDC) and hydroxypropyl-β-CD (HP-β-CD). The complex was characterized by thermal analysis (differential scanning calorimetry, DSC), UV absorption and high-pressure liquid chromatography (HPLC). DSC results were indicative of complexation, due to the loss of the characteristic endothermic peak of LDC (77 °C). Phase-solubility diagrams allowed the determination of the association constant between LDC and HP-β-CD (35.7 ± 4.7 M−1). The rate of LDC release decreased after complexation and thermodynamic parameters from the HPLC studies (ΔG° = −2.65 kJ/mol) revealed that a stable complex was formed.

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