Physicochemical characterization, the Hirshfeld surface, and biological evaluation of two meloxicam compounding pharmacy samples
- Author:
Romani F.A. LUCIANA
1
;
Yoshida I. MARIA
;
Gomes C.L. ELIONAI
;
Machado R. RENES
;
Rodrigues F. FELIPE
;
Coelho M. MÁRCIO
;
Oliveira A. MARCELO
;
Freitas-Marques B. MARIA
;
Rosane A.S. San Gil
;
Mussel N. WAGNER
Author Information
1. Department of Chemistry
- Keywords:
Meloxicam;
Polymorphism;
Hirshfeld surface;
Anti-inflammatory activity
- From:
Journal of Pharmaceutical Analysis
2018;8(2):103-108
- CountryChina
- Language:Chinese
-
Abstract:
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 be-tween samples. The FTIR and 1H NMR spectra showed characteristic assignments. 13C 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 experi-mental model of acute inflammation in mice. Our results highlighted the need for complete crystal-lographic characterization and the separation of freely used raw materials in compounding pharmacies, as a routine procedure, to ensure the desired dose/effect.