Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.
Pharm Dev Technol. 2024 Oct;29(8):805-813. doi: 10.1080/10837450.2024.2393729. Epub 2024 Aug 27.
The utilization of pharmaceutical products in pediatric medicine, while established for use in adults, often presents uncertainties due to differences in application for children. The FDA discourages the use of local anesthetic gels, notably lidocaine, for teething pain in pediatrics due to concerns regarding potential adverse effects if inadvertently swallowed excessively. Therefore, significant attention is being directed towards modifying available marketed products to make them suitable for pediatric use. Here, we introduce mucoadhesive patches that not only have an adjusted dose of lidocaine but also feature a controlled release profile to manage teething pain with prolonged effect. This design helps to prevent issues related to gel liquefaction and swallowing, thereby reducing the potential hazardous side effects of lidocaine in the pediatric population.
The study involved the development of controlled-release lidocaine HCl-loaded pellets forming a matrix for inclusion in mucoadhesive patches. Characterization was performed to ensure prolonged drug release, particularly during overnight use, aiming to improve pediatric patient compliance and enable precise dosing.
The mucoadhesive patches exhibited sustained lidocaine release lasting 24 h, potentially offering overnight relief suitable for pediatric application. The analysis of lidocaine content revealed that the developed patches maintained stable levels compared to doses obtained from commercially available oral gels. This finding implies effective pain control without the need for frequent reapplications, alongside controlled doses that decrease the likelihood of side effects.
The formulated medicated patches demonstrated consistent lidocaine content, effectively controlled drug release, and consequently, reduced the likelihood of undesired side effects when compared to oral gel administration.
在儿科医学中,虽然某些药物在成人中已有应用,但由于儿童应用的差异,其使用仍存在不确定性。由于担心如果不慎过量吞咽,可能会产生潜在的不良反应,FDA 不鼓励在儿科中使用局部麻醉凝胶,特别是利多卡因,用于缓解出牙疼痛。因此,人们高度关注对现有市售产品进行改良,使其适用于儿科使用。在这里,我们介绍一种具有粘弹性的贴片,它不仅具有调整后的利多卡因剂量,而且具有控释特性,可实现长时间缓解出牙疼痛的效果。这种设计有助于防止与凝胶液化和吞咽相关的问题,从而降低利多卡因在儿科人群中潜在的有害副作用。
本研究涉及开发控释盐酸利多卡因载药微丸,形成包含在粘弹性贴片基质中的载药微丸。对其进行了特性研究,以确保药物的释放时间延长,特别是在夜间使用时,旨在提高儿科患者的依从性并实现精确的剂量控制。
粘弹性贴片显示出持续 24 小时的利多卡因释放,可能提供适合儿科应用的夜间缓解。对利多卡因含量的分析表明,与市售口腔凝胶获得的剂量相比,所开发的贴片保持了稳定的水平。这一发现意味着可以在无需频繁重新应用的情况下,进行有效的疼痛控制,同时控制剂量,减少副作用的可能性。
与口腔凝胶给药相比,所制备的贴剂具有一致的利多卡因含量、有效的药物控释,因此减少了不良副作用的发生。