Cefquinome sulfate: Clinical treatment, Solubility and Preparation

What is Cefquinome sulfate?

Cefquinome Sulfate (CS) is a fourth-generation cephalosporin, which has been developed solely for veterinary use. It shows potent antibacterial activity against a broad spectrum of bacterial species, such as a large number of Gram–positive bacterium, some Gram–negative bacterium, vibrios, spirochete, mycoplasma, etc. The antibiotic has been extensive use for treatment of cattle and pig against bacterial infections of respiratory tract and the udder.

However, like other β-lactam compounds, CS is chemically unstable. This is due to susceptibility of β-lactam ring to acidic or alkaline catalyzed hydrolysis. In addition, the short elimination half–life, wide tissue distribution, large dosage, frequent drug administration, comparatively evident hormesis and animal’s stress reaction after intramuscular injection of commercial preparations have restricted the therapeutic use of CS.

Clinical treatment of Cefquinome sulfate

The clinical treatment of dairy cow mastitis during the lactation period plays a significant role in dairy manufacture. In this work, 3 groups of lactating dairy cows with clinical mastitis were selected, for the first time, to explore the treatment effects using cefquinome sulfate and lincomycin hydrochloride through the udder injection. Methods: The treatment effects with the udder injection of cefquinome sulfate and lincomycin hydrochloride were compared based on effective rate, cure rate, somatic cell reduction in the milk, decrease of cow body temperature and recovery of milk yield. Result: Both cefquinome sulfate and lincomycin hydrochloride showed effective treatment on the dairy cow mastitis during the lactation period. The effective rate and the cure rate obtained with cefquinome sulfate were 88% and 80%, which were higher than those treated with lincomycin hydrochloride (effective rate: 72% and cure rate: 64%). Furthermore, the cefquinome sulfate test group seemed to display a better role in the reduction of somatic cells in milk, a decrease of cow body temperature and the recovery of milk yield.

Solubility of Cefquinome sulfate

Solid-liquid equilibrium data of cefquinome sulfate is important to develop industrial crystallization processes for cefquinome sulfate. The solubilities of cefquinome sulfate in five pure solvents (methanol, ethanol, ethylene glycol, acetic acid and water) from 277.15 to 305.15 K and in a binary acetone-water solvent from 278.15 to 293.15 K were measured at atmospheric pressure. The pure-solvent solubility data was correlated to the modified Apelblat and Van’t Hoff equations whereas the mixed-solvent system data was correlated to the modified Apelblat, Van’t Hoff, CNIBS/R-K and Jouyban- Acree models. It was found that the solubilities of cefquinome sulfate in all tested solvents decreased with the increasing of temperature. In addition, the thermodynamic properties of the dissolution processes, including standard Gibbs free energy, enthalpy and entropy changes, were calculated using the Van’t Hoff equation. It was found that the dissolution of cefquinome sulfate is exothermic.

Preparation of Cefquinome Sulfate Proliposome

The CSLS prepared by the method of solid dispersion and effervescent techniques was milky white suspension. The shape observed by TEM was spherical or ellipsoidal. In the light of DLS detection, the particle size was 203 ± 5 nm and more than 90% of the amount was in the range of 100-1000 nm. PDI was found to be lower than 0.132 ± 0.02, indicating that the liposome populations were homogeneous in size. The entrapment efficiency of CSLS was 53.5 ± 0.16% with RSD of lower than 2%.

References

[1] ZHICHUN GU. A Comparison of Cefquinome Sulfate and Lincomycin Hydrochloride in the Treatment of Mastitis for Lactating Cows[J]. Indian Journal of Animal Research, 2022. DOI:10.18805/ijar.bf-1454.

[2] FU Q, LIN HUA-FU, HUAN L, et al. Preparation of Cefquinome Sulfate Proliposome and its Pharmacokinetics in Rabbit[J]. Iranian Journal of Pharmaceutical Research : IJPR, 2013. DOI:10.22037/IJPR.2013.1392.

[3] RONGBAO QI. The solubility of cefquinome sulfate in pure and mixed solvents[J]. Frontiers of Chemical Science and Engineering, 2016. DOI:10.1007/s11705-016-1569-z.

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