在Sprague-Dawley大鼠中,Meloxicam皮下延长释放配方的药理动力学和初步安全性数据
Avantika Gupta1, Harshita Akkaraju1, Vignesh Vasudevan1
1Department of Pharmaceutical Sciences, University of Pittsburgh School of Pharmacy, Pittsburgh, PA, United States.
Frontiers in veterinary science
|March 9, 2026
概括
一种新的延长释放型皮下西卡姆配方在老鼠中提供了长时间的疼痛控制,维持治疗性血水平长达72小时. 这种新型的非类固醇抗炎药物 (NSAID) 输送系统显示出改善兽医疼痛控制和动物护理的希望.
科学领域:
- 兽医药理学 兽医药理学
- 药物输送系统 药物输送系统
- 疼痛管理 疼痛管理
背景情况:
- 在兽医中,非类固醇抗炎药 (NSAID) 对于控制疼痛和炎症至关重要.
- 目前的梅洛西卡姆配方 (口服,注射) 需要经常服用,因此需要更少的剂量选择.
研究的目的:
- 开发和评估一种安全的,延长释放性皮下 (SC-XR) 梅洛西卡姆配方,用于兽医.
- 评估SC-XR配方是否可以在不太频繁的服用下保持足够的血梅洛西卡姆度.
主要方法:
- 在Sprague Dawley大鼠中进行的药理动力学研究比较了SC-XR meloxicam与静脉注射 (IV),皮下注射 (SC) 和持续释放 (SC-SR) 配方.
- 进行了剂量升级和多次剂量研究,以评估SC-XR配方的药物暴露和安全性.
主要成果:
- 该SC-XR梅洛西卡姆配方实现了长时间的药物释放,维持血度超过1μg/ml长达72小时.
- 多次服用SC-XR (4,12,20毫克/公斤) 显示药物积累最小.
- 组织学,血液学和器官功能评估显示没有剂量依赖的不良影响.
结论:
- 新型梅洛西卡姆XR悬浮剂 (4mg/kg) 是安全的,并且在老鼠中耐受良好.
- 这种延长释放配方为加强疼痛管理和兽医合规性提供了一个可行的选择,使得更少的频率管理成为可能.
更多相关视频
07:49Slow-release Drug Delivery through Elvax 40W to the Rat Retina: Implications for the Treatment of Chronic Conditions
Published on: September 17, 2014
12.0K
12:57X-Ray Visualization of Intraductal Ethanol-Based Ablative Treatment for Prevention of Breast Cancer in Rat Models
Published on: December 9, 2022
2.8K
相关概念视频
Modified-Release Drug Delivery Systems: Bioavailability
70
Modified-release (MR) dosage forms are designed to extend drug release over time, thereby maintaining stable plasma concentrations and reducing dosing frequency. However, their bioavailability is typically below 100% due to incomplete drug release and presystemic metabolism, and limitations in drug permeability across the gastrointestinal epithelium, all of which can restrict the fraction of the drug reaching systemic circulation. Consequently, studying the in vivo bioavailability of MR...
70
Pharmacokinetic–Pharmacodynamic Relationship: Duration of Dose-Effect Relationship
73
For drugs producing a quantal response, onset occurs when plasma concentration reaches a minimum effective level (Cmin). The drug's action duration depends on how long the plasma concentration remains above Cmin.Two primary factors influence this duration: dose size and the rate of drug removal from the action site. Both depend on the drug's redistribution to poorly perfused tissues and elimination processes. A larger dose promotes rapid onset and prolongs the effect's duration.Consider a...
73
