Introduction: Cefquinome sulfate (CS) is the first fourth-generation antibiotic for animals, which has a wide antibacterial spectrum, strong antibacterial activity and low drug resistance. However, it is accompanied by problems of poor therapeutic efficacy. In this context, the use of nanosuspensions have been found to be an attractive strategy. The main objective of this work is to develop a new oily nanosuspension to improve bioavailability and stability of CS formulations.
Methods: After screening the formulations, cefquinome sulfate oily nanosuspension (CS-NSP) was prepared by mortar grinding, using propylene glycol dicaprolate/dicaprate (Labrafac™ PG) as oil medium and caprylocaproyl polyoxyl-8 glycerides (Labrasol®) as stabilizer. The properties of CS-NSP were investigated by testing its physicochemical characteristics, stability, in vitro release, hemolysis, and muscle irritation. The in vivo pharmacokinetics of CS-NSP was studied using rats.
Results: Results show that CS-NSP presents suitable stability, physicochemical properties and safety. Moreover, a rapid release and high bioavailability of CS-NSP have also been verified in the study. Pharmacokinetic experiments in vivo showed that the bioavailability of CS-NSP was about 1.6 times that of commercial cefquinome sulfate injection (CS-INJ, Chuangdao®) (p< 0.01). These advantages of CS-NSP were carried out by small particle size and low viscosity, being associated with the use of Labrafac PG and stabilizer Labrasol.
Conclusion: The results proved that the new preparation is safe and effective and is expected to become a promising veterinary nanodelivery system.

Keywords: cefquinome sulfate, oily nanosuspension, Labrafac PG, labrasol, pharmacokinetics


中文翻译：

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旨在提高其在兽医感染治疗中的生物利用度的硫酸头孢喹啉油性纳米混悬剂

简介：硫酸头孢喹啉（CS）是第一个用于动物的第四代抗生素，具有抗菌谱广、抗菌活性强、耐药性低等特点。然而，它伴随着治疗效果差的问题。在这种情况下，已发现使用纳米混悬剂是一种有吸引力的策略。这项工作的主要目的是开发一种新的油性纳米混悬剂，以提高 CS 制剂的生物利用度和稳定性。
方法：筛选配方后，通过研钵研磨制备硫酸头孢喹啉油性纳米混悬剂（CS-NSP），使用丙二醇二己酸酯/二癸酸酯（Labrafac™ PG）作为油介质，辛癸酰聚氧-8甘油酯（Labrasol®）作为稳定剂。通过测试其理化特性、稳定性、体外释放、溶血和肌肉刺激性来研究CS-NSP的性质。使用大鼠研究了 CS-NSP 的体内药代动力学。
结果：结果表明，CS-NSP具有适宜的稳定性、理化性质和安全性。此外，该研究还验证了 CS-NSP 的快速释放和高生物利用度。体内药代动力学实验表明，CS-NSP的生物利用度约为市售硫酸头孢喹啉注射液（CS-INJ，创道®）的1.6倍（p < 0.01）。CS-NSP 的这些优点是通过小粒径和低粘度实现的，这与使用 Labrafac PG 和稳定剂 Labrasol 相关。
结论：结果证明该新制剂安全有效，有望成为一种很有前景的兽用纳米递送系统。

关键词：硫酸头孢喹啉，油性纳米混悬剂，Labrafac PG，labrasol，药代动力学