局部输送系统通过直接扩散有效地将止痛药运送到局部疼痛区域
Thomas Birngruber1, Kip Vought2, Simon Schwingenschuh1
1HEALTH-Institute for Biomedical Research and Technologies, Joanneum Research Forschungsgesellschaft mbH, 8010 Graz, Austria.
Pharmaceutics
|November 25, 2023
概括
新的局部利多卡因配方将药物直接输送到肌肉组织,以缓解局部疼痛. 与现有的选择相比,在肌肉中使用新的5.4%利多卡因配方实现了更高的度.
科学领域:
- 药理学和药物输送 药理学和药物输送
- 肌肉骨疼痛管理 肌肉骨疼痛管理
- 皮肤病学 皮肤病学
背景情况:
- 局部输送系统 (TDS) 为肌肉骨疾病提供有针对性的缓解疼痛,最大限度地减少全身副作用.
- 利多卡因和迪克洛菲纳克是常见的局部止痛药.
- 了解主要的传输机制 (扩散与系统性) 对于优化TDS有效性至关重要.
研究的目的:
- 要确定药物从TDS传递到肌肉组织主要是通过直接扩散或全身传输.
- 为了比较试验性利多卡因TDS (SP-103,5.4%) 与商业利多卡因TDS (ZTlido®,1.8%) 和双烯酸凝 (Pennsaid®,2%) 的肌肉组织透率.
主要方法:
- 利用开放式流量微 perfusion (OFM) 来从皮肤,皮下脂肪组织 (SAT) 和肌肉中取样间歇性液体.
- 进行了ex vivo和in vivo实验,以评估药物通过所有组织层的透率.
- 在不同组织部位的量化利多卡因和二甲度.
主要成果:
- 与狄克洛菲纳克相比,利多卡因在组织层中传播的转移率更高.
- 已证实扩散运输对肌肉组织中利多卡因度的显著贡献.
- SP-103 5.4%的肌肉组织里多卡因度明显高于ZTlido® 1.8% (p = 0.008).
结论:
- SP-103 5.4%通过扩散有效地将利多卡因输送到肌肉组织中,用于局部疼痛.
- 与现有的局部利多卡因产品相比,正在研究中的SP-103配方显示出优越的肌肉透能力.
- 这些发现支持SP-103的5.4%作为肌肉骨疼痛障碍的有希望的治疗方法,包括腰部疼痛.
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