College of Animal Science and Technology, Guangxi University, Room 124, 100 Daxue Road, Xixiangtang District, Nanning, Guangxi, 530005, P. R. China.
Guangxi Key Laboratory of Animal Breeding, Disease Control and Prevention, Nanning, 530004, P. R. China.
BMC Vet Res. 2023 Sep 19;19(1):164. doi: 10.1186/s12917-023-03713-1.
A new antibacterial compound powder of amoxicillin (AMO)/Radix Scutellaria extract (RSE) was developed, and its pharmacokinetics were determined in pigs following oral administration.
The MIC ranges of AMO against Escherichia coli, Staphylococcus aureus and Streptococcus were 1-8 μg/mL, 0.5-4 μg/mL and 0.5-64 μg/mL, respectively. The MIC ranges of RSE against E. coli, S. aureus, and Streptococcus were greater than 2.5 mg/mL, 0.156-2.5 mg/mL, and greater than 2.5 mg/mL, respectively. For S. aureus, the combined drug susceptibility test showed that AMO and RSE had an additive or synergistic effect. The results of compatibility test, the excipient screening test and the drug quality control test showed that the formulation had stable quality and uniform properties under the test conditions. Two studies were conducted to investigate the pharmacokinetics of the compound product in pigs. First, the pharmacokinetics of the AMO-RSE powder were compared with those of their respective single products. The results showed no significant change in the main pharmacokinetic parameters when either component was removed from the compound formulation; thus, AMO and RSE have no pharmacokinetic interaction in pigs. Second, pigs were orally administered three different doses of AMO-RSE powder. The Cmax and AUC increased proportionally with increasing p.o. dose; thus, the λ, t, MRT, and T were unchanged for the doses of 10, 20, and 30 mg/kg AMO and the doses of 5, 10, and 15 mg/kg BCL, showing that AMO/baicalin in AMO-RSE powder showed linear pharmacokinetic characteristics in pigs.
The combined drug sensitivity test of AMO and RSE against S. aureus showed that the combination was additive or synergistic. Pharmacokinetic studies indicated that AMO and BCL do not interfere with each other in pigs when used in a compound formulation. The pharmacokinetic parameters remained unchanged regardless of the dose for p.o. administration, indicating linear pharmacokinetic properties over the tested dose range. The quality of the AMO-RSE powder was good and stable, providing a foundation for its clinical application in veterinary medicine. Further bioavailability, PK/PD and clinical trials are still needed to determine the final dosage regimen.
研制了阿莫西林（AMO）/黄芩提取物（RSE）新型抗菌复合粉剂，并对其在猪体内的药代动力学进行了研究。
AMO 对大肠杆菌、金黄色葡萄球菌和链球菌的 MIC 范围分别为 1-8μg/mL、0.5-4μg/mL 和 0.5-64μg/mL；RSE 对大肠杆菌、金黄色葡萄球菌和链球菌的 MIC 范围均大于 2.5mg/mL、0.156-2.5mg/mL 和大于 2.5mg/mL。对金黄色葡萄球菌进行的联合药敏试验表明 AMO 和 RSE 具有相加或协同作用。配伍试验、辅料筛选试验和药品质量控制试验的结果表明，在试验条件下，该制剂质量稳定，性质均匀。进行了两项研究以考察该复方制剂在猪体内的药代动力学。首先，比较了 AMO-RSE 粉剂与其各自单药产品的药代动力学。结果表明，当从复方制剂中去除任一成分时，主要药代动力学参数均无显著变化；因此，在猪体内 AMO 和 RSE 之间无药代动力学相互作用。其次，猪经口给予三种不同剂量的 AMO-RSE 粉剂。Cmax 和 AUC 随口服剂量呈比例增加；因此，当 AMO 剂量为 10、20 和 30mg/kg 以及 BCL 剂量为 5、10 和 15mg/kg 时，λ、t、MRT 和 T 不变，表明 AMO/黄芩苷在 AMO-RSE 粉中在猪体内呈线性药代动力学特征。
AMO 和 RSE 对金黄色葡萄球菌的联合药敏试验表明，两者联合具有相加或协同作用。药代动力学研究表明，在复方制剂中，AMO 和 BCL 在猪体内相互不干扰。无论口服剂量如何，药代动力学参数保持不变，表明在测试剂量范围内具有线性药代动力学特征。AMO-RSE 粉剂质量良好且稳定，为其在兽医临床的应用提供了基础。仍需要进一步的生物利用度、PK/PD 和临床试验来确定最终的剂量方案。
