APPROACHES TO THE SELECTION OF EXCIPIENTS FOR DENTAL GEL WITH CETYLPYRIDINIUM CHLORIDE

E. Y. Zagorulko, A. Karavaeva
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Abstract

The aim of the study was to determine the excipients influence on the characteristics of gels with cetylpyridinium chloride and to select the dental gel formulation gelation agents promising for the development of dental gel compositions. Hereby, the properties of the active pharmaceutical ingredient, characteristics of the specific gelation agents, as well as their influence on stability, biopharmaceutical and application properties of gels, were taken into account. Materials and methods. In this study, polymers with various gelation mechanisms were considered. Their compatibility with cetylpyridinium chloride as well as storing kinetic and colloid kinds of stability, pH of aqueous solutions, spreadability and textural properties, a penetration ability by the agar diffusion method, an osmotic activity and rheological properties of the gels, were examined. For a complex evaluation of gel compositions study results, a desirability function was used.Results. Stable homogenous dental gels with cetylpyridinium chloride can be obtained by using 25% poloxamer 407 and 5.0% high molecular weight chitosan as the basis.The addition of poloxamer 188 to high molecular weight chitosan gels can produce stable systems with improved textural characteristics as well as increase their osmotic activity. Agar and low molecular weight chitosan addition significantly decrease, whereas poloxamer188 and various molecular weight polyethyleneglycol increase the osmotic activity of 25 % poloxamer 407 gels which are also characterized by a high penetration ability.Conclusion. A complex evaluation of biopharmaceutical, physicochemical and application properties of the gels made it possible to establish that combinations of poloxamer 407 with polyvinylpyrrolidone, agar, and low molecular weight chitosan, can be recommended as a base for a dental gel with cetylpyridinium chloride.
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十六烷基吡啶氯化牙凝胶辅料选择的探讨
研究辅料对十六烷基氯吡啶凝胶特性的影响,为牙科凝胶配方的开发选择有前景的凝胶剂。因此,考虑了活性药物成分的性质,特定凝胶剂的特性,以及它们对凝胶稳定性、生物制药和应用性能的影响。材料和方法。在本研究中,考虑了不同凝胶机制的聚合物。考察了其与十六烷基氯化吡啶的相容性、存储动力学和胶体种类的稳定性、水溶液pH、涂涂性和结构性能、琼脂扩散法渗透能力、渗透活性和凝胶的流变性能。为了对凝胶组成的研究结果进行复杂的评价,使用了可取函数。以25%的波洛沙姆407和5.0%的高分子量壳聚糖为基料,可制得稳定的十六烷基氯化吡啶牙凝胶。在高分子量壳聚糖凝胶中加入波洛沙姆188可以制备稳定的体系,改善其结构特性并提高其渗透活性。琼脂和低分子量壳聚糖的加入显著降低了25%波洛沙姆407凝胶的渗透活性,而poloxamer188和不同分子量的聚乙二醇的加入则提高了25%波洛沙姆407凝胶的渗透活性,并具有较高的渗透能力。通过对凝胶的生物制药、物理化学和应用性能的复杂评估,可以确定poloxomer 407与聚乙烯吡咯烷酮、琼脂和低分子量壳聚糖的组合可以推荐作为十六烷基吡啶氯化牙凝胶的基础。
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