Formulation, Characterization and Pharmacokinetics of Long-acting Ceftiofur Hydrochloride Suspension
| Autor: | Lingli Huang, Yanfei Tao, Kuiyu Meng, Dongmei Chen, Xiaoqiu Zhang, Zonghui Yuan, Shuyu Xie, Yuanhu Pan, Zhenli Liu, Yulian Wang, Wanhe Luo |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
Swine
Biological Availability Pharmaceutical Science 02 engineering and technology Ceftiofur Hydrochloride medicine.disease_cause Injections Intramuscular 030226 pharmacology & pharmacy Suspension (chemistry) 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Suspensions Pharmacokinetics Pulmonary surfactant medicine Animals Ethyl oleate Chromatography Chemistry 021001 nanoscience & nanotechnology Anti-Bacterial Agents Cephalosporins Bioavailability Long acting Irritation 0210 nano-technology |
| Zdroj: | Current Drug Delivery. 18:224-233 |
| ISSN: | 1567-2018 |
| Popis: | Objectives: A ceftiofur hydrochloride long-acting oily suspension with no irritation was prepared by testing and optimizing the types and amounts of organic solvents, suspending agents, and surfactants. Methods: Its properties, stability, injection site irritation, in vitrorelease, and pharmacokinetics in pigs were evaluated. The optimum formulation was used ethyl oleate, aluminum monosterate, and span-80 as organic solvents, suspending agents, and surfactant, respectively. The drug microparticles were uniform long strip with size of 1.53 ± 0.11 μm and no agglomerations, and were evenly dispersed. The re-dispersed time, sedimentation rate and pH value of the suspension were 4 s under a magnetic shaker rotating at 20 r/min, 1 and 5.0, respectively. It could go through 7-gage needle smoothly with withdrawal volume of 9.9 mL/min. Results: The suspension showed good stability when stored away from light, no irritation at the injection site and sustained release in PBS buffer. After intramuscular administration, the drug concentration above 0.15 μg/mL was last for 120 h. Its elimination half-life (T1/2ke), mean residence time (MRT), and bioavailability were increased by 1.73, 1.62, and 2.16 times compared to Excenel®. Conclusion: The results suggested that the suspension had excellent sustained-release and will make ceftiofur hydrochloride more effective and convenient to use. |
| Databáze: | OpenAIRE |
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