Abstract:Cefquinome sulfate is a veterinary, parenteral, fourth-generation cephalosporin with a methoxyimino-aminothiazolyl moiety into the acyl side chain and the quaternary quinoline group at position 3 of the cefem ring. Cefquinome sulfate is known to undergo degradation, which could be additionally increased by the presence of some critical factors such as temperature, relative air humidity, buffer components as well as hydrogen and hydroxide ions. The aim of this study was to evaluate the factors underlying the st… Show more
“…However, some drugs are inherently hard-to-crystallize drugs and used only in the amorphous form. There are no reports about crystalline CFQ in the literature, and only several crystalline salt forms of CFQ were reported. , …”
Section: Resultsmentioning
confidence: 99%
“…There are no reports about crystalline CFQ in the literature, and only several crystalline salt forms of CFQ were reported. 20,21 To produce a higher quality crystal product of CFQ, selecting the appropriate solvent as antisolvent is of importance. The solvents must meet two basic principles:…”
In
the pharmaceutical industry, crystalline products are preferred
because of their higher purity, chemical and physical stability, as
well as tunability through crystal engineering. In this study, a crystalline
cefquinome (CFQ) product was prepared for the first time. A reverse
antisolvent crystallization (RAC) recipe was proposed to avoid the
formation of a jelly-like phase (JLP) during the solution crystallization
process. A comprehensive characterization and analysis were conducted
for the undesirable JLP by using thermogravimetric analysis and rotational
rheometry. The results show that the JLP is a semisolid fluid, and
it hinders nucleation and growth of crystals. The formation of JLP
should be considered as an important factor of lacking crystalline
CFQ products in past decades. In this work, the ternary phase diagram
was determined to study the mechanism of the RAC process and analyze
it for further optimization. The optimized crystallization process
was monitored and analyzed by powder X-ray diffraction, in situ Raman
spectroscopy, and in situ focused beam reflectance measurement, and
produced a higher crystallinity product. In addition, the solubility
of the crystalline product and the commercial product was measured
in three solvents. The results indicate a higher solubility of the
crystalline CFQ product compared to the commercial product which shows
great potential for further application.
“…However, some drugs are inherently hard-to-crystallize drugs and used only in the amorphous form. There are no reports about crystalline CFQ in the literature, and only several crystalline salt forms of CFQ were reported. , …”
Section: Resultsmentioning
confidence: 99%
“…There are no reports about crystalline CFQ in the literature, and only several crystalline salt forms of CFQ were reported. 20,21 To produce a higher quality crystal product of CFQ, selecting the appropriate solvent as antisolvent is of importance. The solvents must meet two basic principles:…”
In
the pharmaceutical industry, crystalline products are preferred
because of their higher purity, chemical and physical stability, as
well as tunability through crystal engineering. In this study, a crystalline
cefquinome (CFQ) product was prepared for the first time. A reverse
antisolvent crystallization (RAC) recipe was proposed to avoid the
formation of a jelly-like phase (JLP) during the solution crystallization
process. A comprehensive characterization and analysis were conducted
for the undesirable JLP by using thermogravimetric analysis and rotational
rheometry. The results show that the JLP is a semisolid fluid, and
it hinders nucleation and growth of crystals. The formation of JLP
should be considered as an important factor of lacking crystalline
CFQ products in past decades. In this work, the ternary phase diagram
was determined to study the mechanism of the RAC process and analyze
it for further optimization. The optimized crystallization process
was monitored and analyzed by powder X-ray diffraction, in situ Raman
spectroscopy, and in situ focused beam reflectance measurement, and
produced a higher crystallinity product. In addition, the solubility
of the crystalline product and the commercial product was measured
in three solvents. The results indicate a higher solubility of the
crystalline CFQ product compared to the commercial product which shows
great potential for further application.
“…Stability study and kinetic monitoring of cefquinome sulfate using cyclodextrin-based ion-selective electrode were developed by Yehia AM, et al, 38 . Shantier SW et al and Dołhań A et al, 39,40 developed chromatographic and spectrophotometric methods for the analysis and stability studies of cefquinome sulphate in bulk and pharmaceutical dosage forms.…”
Drugs have been used for the treatment of infectious diseases since the 17 th century. However, chemotherapy as a science began in the first decade of the 20 th century with understanding of the principles of selective toxicity, the specific chemical relationships between microbial pathogens and drugs, the development of drug resistance and the role of combined therapy. Analysis of such drugs, whether used for treatment of human or animal illness, is essential in understanding the bioavailability and therapeutic control which will ensure their activity and safety. Thus, this review aims to highlight the characteristics, specifically the pharmacokinetic parameters and the analytical methods reported in literature for cefquinome, a fourth generation cephalosporine used to treat infections caused by gram-positive and gram-negative microorganisms.
“…Generally, cephalosporin has been susceptible to degradation even in solution (12,13) or in solid states (14). CFQ, without exception, shows low stability toward acidic and alkaline hydrolysis, along with its susceptibility to photodegradation and thermal decomposition (15). In this work, stability study of CFQ was performed using two membrane-selective electrodes, one without ionophore (sensor 1) and the other with ionophore (sensor 2).…”
Two novel cefquinome sulfate (CFQ)-selective electrodes were performed with dibutyl sebacate as a plasticizer using a polymeric matrix of polyvinyl chloride. Sensor 1 was prepared using sodium tetraphenylborate as a cation exchanger without incorporation of ionophore, whereas 2-hydroxy propyl β-cyclodextrin was used as ionophore in sensor 2. A stable, reliable, and linear response was obtained in concentration ranges 3.2 × 10(-5) to 1 × 10(-2) mol/L and 1 × 10(-5) to 1 × 10(-2) mol/L for sensors 1 and 2, respectively. Both sensors could be sufficiently applied for quantitative determination of CFQ in the presence of degradation products either in bulk powder or in pharmaceutical formulations. Sensor 2 provided better selectivity and sensitivity, wider linearity range, and higher performance. Therefore it was used successfully for accurate determination of CFQ in biological fluids such as spiked plasma and milk samples. Furthermore, an online kinetic study was applied to the CFQ alkaline degradation process to estimate the reaction rate and half-life with feasible real-time monitoring. The developed sensors were found to be fast, accurate, sensitive, and precise compared with the manufacturer's reversed-phase chromatographic method.
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