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...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.展开更多
Recent studies have shown that Barbatimao fractions are promising for dermatological diseases treatment, due to tannins content and its strong antioxidant activity. In this study, chitosan was used as polymeric matrix...Recent studies have shown that Barbatimao fractions are promising for dermatological diseases treatment, due to tannins content and its strong antioxidant activity. In this study, chitosan was used as polymeric matrix for the development of nanoparticulated system able to deliver a Barbatimao standardized fraction. Nanoparticles were prepared by ionotropic gelation method involving the mixing of two aqueous phases at room temperature. The product was characterized by infrared absorption spectrometry, scanning electron microscopy, quantification of fraction in the formulation, in vitro release profile, size of particles and polydispersity index. The level of Barbatimao fraction obtained in the formulation was 38.23%, with 30% of encapsulated fraction released in 7 days. No chemical reaction between the fraction and the matrix could be noticed. The particles containing fraction presented an average size of 241 nm and polydispersity index of 0.484. It seems that the phytotherapic formulation could be used as drug delivery system for sustained release of Barbatimao fraction.展开更多
Sida pilosa Retz. (Malvaceae) is a medicinal plant used in Africa for the treatment of dysmenorrhea, lower abdominal pains and intestinal helminthiasis. S. pilosa aqueous extract and derived fractions were investigate...Sida pilosa Retz. (Malvaceae) is a medicinal plant used in Africa for the treatment of dysmenorrhea, lower abdominal pains and intestinal helminthiasis. S. pilosa aqueous extract and derived fractions were investigated for their bioactivity against Schistosoma mansoni. The aqueous extract from S. pilosa aerial parts (1.25 - 40 mg/mL) and derived fractions (n-hexane, DCM, EtOAc and n-BuOH: 0.25 - 8 mg/mL) were tested on adult S. mansoni maintained in a GMEN culture medium. Praziquantel was used as the reference drug. After 24 h of incubation, worms were monitored for their viability and egg output. The antioxidant activity of S. pilosa was evaluated by the ability to scavenge the 2,2-diphenyl-1-picrylhydrazyl free radicals. The chemical composition of the n-BuOH fraction was investigated by HPLC-MS analysis. S. pilosa aqueous extract and fractions significantly increased worm mortality in a concentration-dependent manner. The n-BuOH fraction was the most active with a LC50 of 1.25 mg/mL. Significant reduction of motor activity (25% to 100%) was recorded for surviving worms incubated in different concentrations of the extract and fractions. Incubation of S. mansoni in different concentrations of S. pilosa extract and fractions led to significant reduction of egg laying (52% to 100%). The aqueous extract and derived fractions exhibited antioxidant activity in a concentration-dependent manner. The highest antioxidant activity was found with the EtOAc fraction, followed by the DCM and n-BuOH fractions. HPLC-MS analysis of the n-butanol fraction revealed the presence of two indoloquinoline alkaloids. This study disclosed the schistosomicidal activity of the n-butanol fraction from S. pilosa aqueous extract. This activity is probably related to the indoloquinoline alkaloids identified in the fraction.展开更多
基金Fundacao de Amparo a Pesquisa do Estado de Minas Gerais project APQ-01083-11Conselho Nacional de Desenvolvimento Cientifico e Tecnologico grant 245914/2012-9+1 种基金Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior grant PNPD 1648694Pro-Reitoria de Pesquisa/UFMG IE 27/2010 for financial support
文摘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.
基金financial support of CNPq(577102/2008-7)and FAPEMIG.
文摘Recent studies have shown that Barbatimao fractions are promising for dermatological diseases treatment, due to tannins content and its strong antioxidant activity. In this study, chitosan was used as polymeric matrix for the development of nanoparticulated system able to deliver a Barbatimao standardized fraction. Nanoparticles were prepared by ionotropic gelation method involving the mixing of two aqueous phases at room temperature. The product was characterized by infrared absorption spectrometry, scanning electron microscopy, quantification of fraction in the formulation, in vitro release profile, size of particles and polydispersity index. The level of Barbatimao fraction obtained in the formulation was 38.23%, with 30% of encapsulated fraction released in 7 days. No chemical reaction between the fraction and the matrix could be noticed. The particles containing fraction presented an average size of 241 nm and polydispersity index of 0.484. It seems that the phytotherapic formulation could be used as drug delivery system for sustained release of Barbatimao fraction.
文摘Sida pilosa Retz. (Malvaceae) is a medicinal plant used in Africa for the treatment of dysmenorrhea, lower abdominal pains and intestinal helminthiasis. S. pilosa aqueous extract and derived fractions were investigated for their bioactivity against Schistosoma mansoni. The aqueous extract from S. pilosa aerial parts (1.25 - 40 mg/mL) and derived fractions (n-hexane, DCM, EtOAc and n-BuOH: 0.25 - 8 mg/mL) were tested on adult S. mansoni maintained in a GMEN culture medium. Praziquantel was used as the reference drug. After 24 h of incubation, worms were monitored for their viability and egg output. The antioxidant activity of S. pilosa was evaluated by the ability to scavenge the 2,2-diphenyl-1-picrylhydrazyl free radicals. The chemical composition of the n-BuOH fraction was investigated by HPLC-MS analysis. S. pilosa aqueous extract and fractions significantly increased worm mortality in a concentration-dependent manner. The n-BuOH fraction was the most active with a LC50 of 1.25 mg/mL. Significant reduction of motor activity (25% to 100%) was recorded for surviving worms incubated in different concentrations of the extract and fractions. Incubation of S. mansoni in different concentrations of S. pilosa extract and fractions led to significant reduction of egg laying (52% to 100%). The aqueous extract and derived fractions exhibited antioxidant activity in a concentration-dependent manner. The highest antioxidant activity was found with the EtOAc fraction, followed by the DCM and n-BuOH fractions. HPLC-MS analysis of the n-butanol fraction revealed the presence of two indoloquinoline alkaloids. This study disclosed the schistosomicidal activity of the n-butanol fraction from S. pilosa aqueous extract. This activity is probably related to the indoloquinoline alkaloids identified in the fraction.
