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Lorenzo Drago - One of the best experts on this subject based on the ideXlab platform.
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antimicrobial activity of Thiamphenicol glycinate acetylcysteinate and other drugs against chlamydia pneumoniae
Drug Research, 2011Co-Authors: Alessandra Lombardi, Lorenzo Drago, Elena De Vecchi, B Mombelli, M R GismondoAbstract:Chlamydia pneumoniae is responsible for respiratory tract infections of both upper and lower respiratory tract. Although this bacterium is one of the most wide-spread pathogens of man, there are limited data on the antibiotic treatment of C. pneumoniae infections. The aim of this study has been to evaluate the in vitro activity of Thiamphenicol glycinate acetylcysteinate (TGA, CAS 20192-91-0) in comparison with molecules with established activity against C. pneumoniae, as well as macrolides and quinolones. The results have shown that TGA and clarithromycin (CAS 81103-11-9) are the most active drugs tested, but it is important to underline that the minimal inhibitory concentration (MIC) ranges of TGA are very much lower than the breakpoint of thlamphenicol for the respiratory pathogens. In conclusion, the good antimicrobial in vitro activity of TGA against C. pneumoniae together with its in vivo characteristics, in particular the high concentration reached in lung and the combination with the mucolytic agent N-acetylcysteine (NAC, CAS 616-91-1), can make a valid choice in the treatment of respiratory tract infections caused by C. pneumoniae. These findings need further evaluation by clinical studies.
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Comparative effect of Thiamphenicol glycinate, Thiamphenicol glycinate N-acetylcysteinate, amoxicillin plus clavulanic acid, ceftriaxone and clarithromycin on pulmonary clearance of Haemophilus influenzae in an animal model.
Chemotherapy, 2000Co-Authors: Lorenzo Drago, Alessandra Lombardi, B Mombelli, M.c. Fassina, E. De Vecchi, Maria Rita GismondoAbstract:Background: Thiamphenicol glycinate (TG) and its derivative Thiamphenicol glycinate N-acetylcysteinate (TGA) could be a valid therapeutic option in the treatment of respiratory trac
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serum and lung levels of Thiamphenicol after administration of its glycinate n acetylcysteinate ester in experimentally infected guinea pigs
International Journal of Antimicrobial Agents, 2000Co-Authors: Lorenzo Drago, Elena De Vecchi, B Mombelli, M.c. Fassina, M R GismondoAbstract:Abstract Thiamphenicol is an analogue of chloramphenicol and is characterised by a broad spectrum of action. In this study, serum and lung levels of Thiamphenicol (TAP) were studied in infected guinea pigs after the administration of Thiamphenicol glycinate N -acetylcysteinate (TGA). Animals received a single dose of TGA (15 mg/kg, subcutaneously) immediately after intra-tracheal infection with Haemophilus influenzae (about 10 7 CFU/animal). Serum and lung concentrations of TAP were determined at 0, 1, 3, 6, 12 and 24 h after drug administration by means of HPLC. TAP serum levels were elevated at 1 h and remained detectable for 24 h after drug administration. Tissue lung levels were comparable to peak serum concentrations but remained higher and decreased more slowly than serum concentrations.
M R Gismondo - One of the best experts on this subject based on the ideXlab platform.
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antimicrobial activity of Thiamphenicol glycinate acetylcysteinate and other drugs against chlamydia pneumoniae
Drug Research, 2011Co-Authors: Alessandra Lombardi, Lorenzo Drago, Elena De Vecchi, B Mombelli, M R GismondoAbstract:Chlamydia pneumoniae is responsible for respiratory tract infections of both upper and lower respiratory tract. Although this bacterium is one of the most wide-spread pathogens of man, there are limited data on the antibiotic treatment of C. pneumoniae infections. The aim of this study has been to evaluate the in vitro activity of Thiamphenicol glycinate acetylcysteinate (TGA, CAS 20192-91-0) in comparison with molecules with established activity against C. pneumoniae, as well as macrolides and quinolones. The results have shown that TGA and clarithromycin (CAS 81103-11-9) are the most active drugs tested, but it is important to underline that the minimal inhibitory concentration (MIC) ranges of TGA are very much lower than the breakpoint of thlamphenicol for the respiratory pathogens. In conclusion, the good antimicrobial in vitro activity of TGA against C. pneumoniae together with its in vivo characteristics, in particular the high concentration reached in lung and the combination with the mucolytic agent N-acetylcysteine (NAC, CAS 616-91-1), can make a valid choice in the treatment of respiratory tract infections caused by C. pneumoniae. These findings need further evaluation by clinical studies.
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serum and lung levels of Thiamphenicol after administration of its glycinate n acetylcysteinate ester in experimentally infected guinea pigs
International Journal of Antimicrobial Agents, 2000Co-Authors: Lorenzo Drago, Elena De Vecchi, B Mombelli, M.c. Fassina, M R GismondoAbstract:Abstract Thiamphenicol is an analogue of chloramphenicol and is characterised by a broad spectrum of action. In this study, serum and lung levels of Thiamphenicol (TAP) were studied in infected guinea pigs after the administration of Thiamphenicol glycinate N -acetylcysteinate (TGA). Animals received a single dose of TGA (15 mg/kg, subcutaneously) immediately after intra-tracheal infection with Haemophilus influenzae (about 10 7 CFU/animal). Serum and lung concentrations of TAP were determined at 0, 1, 3, 6, 12 and 24 h after drug administration by means of HPLC. TAP serum levels were elevated at 1 h and remained detectable for 24 h after drug administration. Tissue lung levels were comparable to peak serum concentrations but remained higher and decreased more slowly than serum concentrations.
Domenico Ungheri - One of the best experts on this subject based on the ideXlab platform.
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In vitro antibacterial activity of Thiamphenicol glycinate acetylcysteinate against respiratory pathogens.
Arzneimittel-Forschung, 2011Co-Authors: Enrico Albini, Giuliano Belluco, Mauro Berton, Giovanna Schioppacassi, Domenico UngheriAbstract:After 30 years of therapeutic use, Thiamphenicol glycinate acetylcysteinate (CAS 20192-91-0) is still widely employed in the treatment of upper and lower respiratory tract infections. This is due to its particular characteristic to exert at pulmonary level, either the antibacterial activity of Thiamphenicol (CAS 15318-45-3) and the mucolytic activity of N-acetylcysteine (CAS 616-91-1). The aim of this study was to evaluate the present pattern of susceptibility of several clinical isolates to Thiamphenicol and the interference of N-acetylcysteine on this parameter. The studies have been performed in vitro. Equimolar concentrations of N-acetylcysteine and even higher concentrations did not interfere with the antibacterial activity of Thiamphenicol against Streptococcus pneumoniae, Streptococcus pyogenes and Haemophilus influenzae. The spectrum of activity of Thiamphenicol was similar to that observed in the past and was superior to that of erythromycin and amoxicillin. The activity of Thiamphenicol was greater than that of erythromycin against H. influenzae and streptococci and equivalent versus Branhamella catarrhalis. In comparison with amoxicillin the activity of Thiamphenicol was higher against H. influenzae and B. catarrhalis and slightly lower against streptococci. The results demonstrate that Thiamphenicol maintains its therapeutic value confirming the importance of Thiamphenicol glycinate acetylcysteinate in the treatment of respiratory tract infections.
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Influence of Thiamphenicol on the primary functions of human polymorphonuclear leucocytes against Streptococcus pyogenes
International journal of antimicrobial agents, 2004Co-Authors: Vivian Tullio, Domenico Ungheri, Annamaria Cuffini, Narcisa Mandras, Janira Roana, Giuliana Banche, Nicola CarloneAbstract:Current antibiotic therapy encourages the use of antibiotics that may potentiate the host’s immune defences. We therefore investigated the effect of Thiamphenicol (TAP), the active principle of Thiamphenicol glycinate acetylcysteinate (TGA), on human granulocyte functions, mainly phagocytosis and intracellular killing of Streptococcus pyogenes. Our findings support the use of Thiamphenicol in the treatment of respiratory tract infections caused by S. pyogenes as it acts directly against the pathogen as well as in cooperation with PMNs by eliciting their intracellular killing.
Hongkun Zhao - One of the best experts on this subject based on the ideXlab platform.
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solubility modeling solvent effect and preferential solvation of Thiamphenicol in cosolvent mixtures of methanol ethanol n n dimethylformamide and 1 4 dioxane with water
Journal of Chemical & Engineering Data, 2018Co-Authors: Yu Liu, Yong Cao, Yang Cong, Ali Farajtabar, Hongkun ZhaoAbstract:The Thiamphenicol solubility in aqueous cosolvent solutions of ethanol (1), methanol (1), 1,4-dioxane (1), and N,N-dimethylformamide (DMF, 1) was measured via the isothermal dissolution equilibrium method at temperatures ranging from 278.15 to 318.15 K under local pressure (101.1 kPa). At fixed composition of ethanol (methanol, 1,4-dioxane, or DMF) and temperature, the solubility of Thiamphenicol was larger in DMF + water mixtures than in the ethanol/methanol/1,4-dioxane mixtures. The local solvent proportions were acquired with the method of inverse Kirkwood–Buff integrals. The absolute value of these preferential solvation parameters were all lower than 1.0 × 10–2 for ethanol (1) + water (2) and 1,4-dioxane (1) + water (2) solutions in water-rich compositions and for methanol (1) + water (2) solutions in whole compositions. In the former two cosolvent mixtures in intermediate compositions and cosolvent-rich regions, Thiamphenicol was preferentially solvated by cosolvent. However, for the DMF (1) + water...
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Solubility Modeling, Solvent Effect, and Preferential Solvation of Thiamphenicol in Cosolvent Mixtures of Methanol, Ethanol, N,N-Dimethylformamide, and 1,4-Dioxane with Water
2018Co-Authors: Yu Liu, Yong Cao, Yang Cong, Ali Farajtabar, Hongkun ZhaoAbstract:The Thiamphenicol solubility in aqueous cosolvent solutions of ethanol (1), methanol (1), 1,4-dioxane (1), and N,N-dimethylformamide (DMF, 1) was measured via the isothermal dissolution equilibrium method at temperatures ranging from 278.15 to 318.15 K under local pressure (101.1 kPa). At fixed composition of ethanol (methanol, 1,4-dioxane, or DMF) and temperature, the solubility of Thiamphenicol was larger in DMF + water mixtures than in the ethanol/methanol/1,4-dioxane mixtures. The local solvent proportions were acquired with the method of inverse Kirkwood–Buff integrals. The absolute value of these preferential solvation parameters were all lower than 1.0 × 10–2 for ethanol (1) + water (2) and 1,4-dioxane (1) + water (2) solutions in water-rich compositions and for methanol (1) + water (2) solutions in whole compositions. In the former two cosolvent mixtures in intermediate compositions and cosolvent-rich regions, Thiamphenicol was preferentially solvated by cosolvent. However, for the DMF (1) + water (2) solutions, water solvated preferentially Thiamphenicol in water-rich compositions and by DMF in intermediate and DMF-rich compositions. This case by cosolvent might be illustrated based on higher basic behavior of water, which interacted with Lewis acidic groups of Thiamphenicol. In addition, the solubility of Thiamphenicol was described with the van’t Hoff–Jouyban–Acree, Jouyban–Acree, and Apelblat–Jouyban–Acree models. The obtained average relative deviations were no greater than 1.85%. Furthermore, the solvent effect treatment through the KAT-LSER model indicated that the solubility variation was significantly affected by the cavity term
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Solubility Modeling and Mixing Thermodynamics of Thiamphenicol in Water and Twelve Neat Organic Solvents from T = (278.15 to 318.15) K
2017Co-Authors: Yang Cong, Hongkun ZhaoAbstract:The solid–liquid equilibrium for Thiamphenicol in 13 neat solvents (ethanol, methanol, n-propanol, isopropyl alcohol, n-butanol, acetone, acetonitrile, ethyl acetate, 2-butanone, toluene, water, N,N-dimethylformamide, and 1,4-dioxane) was built with the static method at temperatures T = (278.15 to 318.15) K under pressure of 101.2 kPa, and the Thiamphenicol solubilities in the selected solvents were measured by using high-performance liquid chromatography. Generally, the solubility data in mole fraction in the selected solvents ranked as N,N-dimethylformamide > acetone > methanol >1,4-dioxane >2-butanone > ethanol > acetonitrile > ethyl acetate > n-propanol > isopropyl alcohol > water > n-butanol > toluene. The nonrandom two-liquid model, Wilson model, modified Apelblat equation, and λh equation were employed to describe the solubility behavior of Thiamphenicol in theses solvents. The maximum values of the RMSD and RAD were 4.08 × 10–4 and 2.02%, respectively, and the correlation results by using the modified Apelblat equation were best among the studied models. Additionally, the mixing properties, activity coefficient at infinitesimal concentration and reduced excess enthalpy were derived
Yongning Wu - One of the best experts on this subject based on the ideXlab platform.
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technical note development of an enzyme linked immunosorbent assay for the determination of florfenicol and Thiamphenicol in swine feed
Journal of Animal Science, 2011Co-Authors: Wenxiao Jiang, J Z Shen, Xia Chen, Yongning WuAbstract:: One polyclonal antibody against florfenicol and Thiamphenicol was produced and a competitive ELISA was developed for the detection of florfenicol and Thiamphenicol in swine feed. The ELISA gave a 50% inhibiting concentration of 1.02 ng/mL for florfenicol. For swine feed fortified with 0.05 to 3.0 mg/kg, the interassay recoveries of florfenicol and Thiamphenicol ranged from 86.4 to 118.6%, whereas intraassay recoveries of both drug ranged from 90.1 to 126.5% with less than 15% CV. Results obtained from HPLC-tandem mass spectrometry indicated this ELISA procedure could be used as a convenient method for rapid screening of florfenicol and Thiamphenicol in swine feed.
