Department of Pharmaceutics, Pacific Academy of Higher Education and Research University, Udaipur, Rajasthan, India.
Formulation and Development, Sinomune Pharmaceutical Co. Ltd., Wuxi, China.
AAPS PharmSciTech. 2024 Jul 11;25(6):159. doi: 10.1208/s12249-024-02882-y.
Vitamin C is extensively used in cosmetic formulation, howbeit stability is the supreme demerit that limits its use in beautifying products. Numerous techniques are being employed to inhibit the degradation of vitamin C caused by formulation components to facilitate the use in skin rejuvenating products. Diverse materials are being exercised in formulation to stabilize the ascorbic acid and ingredients selected in this formulation composition help for stabilization. The initial stable prototype is developed and further optimization is accomplished by applying the design of experiment tools. The stable pharmaceutical formulations were evaluated for the evaluation parameters and designated as two optimized formulations. The analytical method for the assay of ascorbic acid from the United States pharmacopeia and the related substance method from European pharmacopeia has been modified to be used for cream formulation. The DoE design exhibited that the stability of formulation is impacted by citric acid and tartaric acid but not by propylene glycol and glycerin. The analysis results of topical formulations for the evaluation parameter exhibited satisfactory results. The in-vitro release study method has been developed, optimized, and validated to fit the analysis. The in-vitro studies have been performed for selected compositions and both the formulation has similar kinds of release patterns. The stability study as per ICH guidelines exhibited that the product is stable for accelerated, intermediate, and room-temperature storage conditions. The optimized formulation shows constant release and permeation of ascorbic acid through the skin. The formulation with the combinations of citric acid, tartaric acid, and tocopherol is more stable and the degradation of vitamin C has been reduced significantly. The beaucoup strategies in the unique composition help to protect the degradation by inhibiting the multitudinous degradation pathways.
维生素 C 在化妆品配方中被广泛应用,但其稳定性是限制其在美容产品中使用的最大缺点。为了抑制配方成分对维生素 C 降解的影响,促进其在皮肤焕新产品中的应用,人们采用了许多技术。在配方中使用了各种材料来稳定抗坏血酸,并且在这种配方成分中选择的成分有助于稳定。最初的稳定原型是通过应用实验设计工具开发的,然后通过进一步优化来实现。对稳定的药物制剂进行了评估,以评估参数,并指定了两种优化的制剂。对美国药典中的抗坏血酸测定分析方法和欧洲药典中的有关物质方法进行了修改,以用于乳膏制剂。设计实验表明,配方的稳定性受柠檬酸和酒石酸的影响,但不受丙二醇和甘油的影响。局部制剂的分析结果显示出令人满意的结果。已经开发、优化和验证了药物释放度研究方法,以适应分析。已经对选定的组合物进行了体外释放研究,两种制剂都具有相似的释放模式。根据 ICH 指南进行的稳定性研究表明,该产品在加速、中间和室温储存条件下稳定。优化的制剂表现出抗坏血酸的恒定释放和透过皮肤的渗透。含有柠檬酸、酒石酸和生育酚的配方更稳定,维生素 C 的降解明显减少。独特配方中的大量策略有助于通过抑制多种降解途径来保护降解。