Formulation of Gel Containing Phenylbutenoid Extract for Pain Relief

Thidaporn Gundom, Thanaporn Amnuaikit, Pharkphoom Panichayupakaranant
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Abstract

Objective: A phenylbutenoid extract (PE) was obtained from Zingiber cassumunar rhizomes. Phenylbutenoids; namely DMPBD, compound D, and compound D acetate, have been identified as major anti-inflammatory and analgesic constituents. This present study aimed to formulate a gel containing PE that could be used as an alternative ultrasound gel for acute or chronic inflammatory treatment. Material and Methods: Gel formulations containing 0.5, 1, and 2% w/w PE were prepared using Carbopol 934 and hydroxyethylcellulose (HEC 4,000) as gelling agents. The contents of phenylbutenoids were quantified by a high-performance liquid chromatography (HPLC). PE gels were studied on physicochemical properties and accelerated stability tests. The PE gels, F2 and F5, were used to evaluate the release of phenylbutenoids using a modified Franz diffusion cell. In the skin permeation study, the 2% PE gels were applied either with or without a 0.8 W/cm2 intensity ultrasound for 2, 5, and 10 min. Results: Based on physicochemical properties and accelerated stability tests, F2 and F5 formulations showed good stability. The release kinetics of 0.5% and 1% and 2% w/w PE of both formulations were best fit to Higuchi’s model and zero-order model, respectively. In the skin permeation study, PE gel combined with ultrasound application for 2 min exhibited higher phenylbutenoids in the skin and also a shorter lag time than PE gel application alone. Conclusion: The gel containing 2% w/w phenylbutenoid extract was suggested as an alternative ultrasound gel containing an anti-inflammatory agent for the treatment of musculoskeletal disorders in phonophoresis.
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含有苯丁烯类提取物的凝胶配方,用于缓解疼痛
目的:从香姜根茎中提取苯丁烯类提取物(PE)。Phenylbutenoids;即DMPBD,化合物D和化合物D醋酸酯,已被确定为主要的抗炎和镇痛成分。本研究旨在研制一种含有PE的凝胶,可作为急性或慢性炎症治疗的替代超声凝胶。材料与方法:以卡波波尔934和羟乙基纤维素(HEC 4000)为胶凝剂,制备含有0.5、1和2% w/w聚乙烯的凝胶配方。采用高效液相色谱法对苯丁烯类进行含量测定。研究了PE凝胶的理化性质和加速稳定性。在改良的Franz扩散池中,使用PE凝胶F2和F5来评价苯基类丁烯酮的释放。在皮肤渗透研究中,2% PE凝胶分别在0.8 W/cm2强度的超声下或不加超声作用2、5和10分钟。结果:基于物理化学性质和加速稳定性测试,F2和F5配方表现出良好的稳定性。在0.5%、1%和2% w/w PE时,两种配方的释放动力学分别最符合Higuchi模型和零级模型。在皮肤渗透研究中,PE凝胶联合超声应用2分钟,皮肤中的类苯丁烯含量更高,延迟时间也比单独应用PE凝胶更短。结论:含2% w/w苯丁烯类提取物的超声凝胶可作为抗炎剂替代超声凝胶治疗音泳症所致的肌肉骨骼疾病。
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