Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, United States.
Department of Chemical Engineering, The University of Mississippi, University, MS 38677, United States.
Int J Pharm. 2021 Mar 1;596:120210. doi: 10.1016/j.ijpharm.2021.120210. Epub 2021 Jan 23.
Surfactants are the most common inactive ingredients used in topical drug products. Surfactants in topical products play many functional roles such as emulsifiers, permeation enhancers, and solubilizers. This study was aimed to evaluate the influence of incremental change in the concentration of a surfactant (tween 80) on the quality attributes and performance of semisolid topical products. Four creams were prepared using metronidazole as a model drug using the same manufacturing protocol and similar composition except for the concentration of tween 80, which was increased by 5% w/w across SF1 to SF4. The quality attributes like globule size, pH, drying rate, and in-vitro permeation profile were characterized. The critical quality attributes did not differ significantly across the products. However, there was a significant difference in the permeation profile of the products. The permeation flux (J) varied from SF1 to SF4 (51.25 ± 35.29 to 307.98 ± 138.89 ng/cm/h, respectively). The reason for the difference in the performance of products despite having consistent quality attributes was investigated. One of the major reasons was found to be the difference in the time course of degree of saturation of drug during the evaporative metamorphosis. This study confirms that the time course of degree of saturation is one of the important quality attributes of the topical product that could influence bioavailability and performance of topical products.
表面活性剂是外用药物制剂中最常用的非活性成分。外用产品中的表面活性剂具有乳化剂、渗透增强剂和增溶剂等多种功能作用。本研究旨在评估表面活性剂（吐温 80）浓度的增量变化对外用半固体制剂的质量属性和性能的影响。使用甲硝唑作为模型药物，使用相同的制造方案和相似的组成，除了吐温 80 的浓度从 SF1 到 SF4 增加 5%w/w 外，制备了四种乳膏。对粒径、pH 值、干燥速率和体外渗透特性等质量属性进行了表征。各产品的关键质量属性没有显著差异。然而，产品的渗透特性存在显著差异。渗透通量（J）从 SF1 到 SF4 分别为 51.25±35.29 至 307.98±138.89ng/cm/h。尽管具有一致的质量属性，但产品性能存在差异的原因进行了调查。发现一个主要原因是在蒸发变态过程中药物饱和度的时间进程存在差异。这项研究证实，饱和度的时间进程是外用产品的一个重要质量属性，可能会影响外用产品的生物利用度和性能。
