Physicochemical characterization, the Hirshfeld surface, and biological evaluation of two meloxicam compounding pharmacy samples  

作　　者：Luciana F.A.Romani Maria I.Yoshida Elionai C.L.Gomes Renes R.Machado Felipe F.Rodrigues Marcio M.Coelho Marcelo A.Oliveira Maria B.Freitas-Marques Rosane A.S.San Gil Wagner N.Mussel 

机构地区：[1]Department of Chemistry, Institute of Exact Sciences, Federal University of Minas Gerais [2]Department of Pharmaceutical Products, Faculty of Pharmacy, Federal University of Minas Gerais [3]Health Science Department, Federal University of Espírito Santo, Campus Sao Mateus [4]Institute of Chemistry, Federal University of Rio de Janeiro, Campus Fundao

出　　处：《Journal of Pharmaceutical Analysis》2018年第2期103-108,共6页药物分析学报（英文版）

基　　金：Fundacao de Amparo a Pesquisa do Estado de Minas Gerais project APQ-01083-11;Conselho Nacional de Desenvolvimento Cientifico e Tecnologico grant 245914/2012-9;Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior grant PNPD 1648694;Pro-Reitoria de Pesquisa/UFMG IE 27/2010 for financial support

摘　　要：Meloxicam(MLX) is an anti-inflammatory drug susceptible to variations and crystalline transitions. In compounding pharmacies, the complete crystallographic evaluation of the raw material is not a routine procedure. We performed a complete crystallographic characterization of aleatory raw MLX samples from compounding pharmacies. X-ray diffraction indicated the presence of two crystalline forms in one sample. DSC experiments suggested that crystallization, or a crystal transition, occurred differently between samples. The FTIR and ~1H NMR spectra showed characteristic assignments.^(13)C solid-state NMR spectroscopy indicated the presence of more than one phase in a sample from pharmacy B. The Hirshfeld surface analysis, with electrostatic potential projection, allowed complete assignment of the UV spectra in ethanol solution. The polymorph I of meloxicam was more active than polymorph III in an experimental model of acute inflammation in mice. Our results highlighted the need for complete crystallographic characterization and the separation of freely used raw materials in compounding pharmacies,as a routine procedure, to ensure the desired dose/effect.Meloxicam(MLX) is an anti-inflammatory drug susceptible to variations and crystalline transitions. In compounding pharmacies, the complete crystallographic evaluation of the raw material is not a routine procedure. We performed a complete crystallographic characterization of aleatory raw MLX samples from compounding pharmacies. X-ray diffraction indicated the presence of two crystalline forms in one sample. DSC experiments suggested that crystallization, or a crystal transition, occurred differently between samples. The FTIR and ~1H NMR spectra showed characteristic assignments.^(13)C solid-state NMR spectroscopy indicated the presence of more than one phase in a sample from pharmacy B. The Hirshfeld surface analysis, with electrostatic potential projection, allowed complete assignment of the UV spectra in ethanol solution. The polymorph I of meloxicam was more active than polymorph III in an experimental model of acute inflammation in mice. Our results highlighted the need for complete crystallographic characterization and the separation of freely used raw materials in compounding pharmacies,as a routine procedure, to ensure the desired dose/effect.

关 键 词：MELOXICAM POLYMORPHISM Hirshfeld surface Anti-inflammatory activity 

分 类 号：R[医药卫生]