Abstract
Purpose: Kojic acid (KA) a natural metabolite and its dipalmitate ester, kojic acid dipalmitate(Kadp) are both prescribed to treat skin hyperpigmentation. Stress test reveals the intrinsicstability of active ingredients and leads to selection of the suitable formulations. This researchevaluates the comparative stability of KA and its di-palmitate ester under liquid oxidative stress. Methods: The HPLC-UV/PDA method with a C18 column was utilized. Liquid oxidative stresswas induced using hydrogen peroxide (H2O2). Degradation was separately induced for eachdrug, and they were compared to each other. Results: Kadp degraded more rapidly in similar liquid oxidative stress conditions than KA did.The superior degradation model was the first order for both drugs based on the mean percentage error (MPE) values, indicating the dependency of the reaction rate on the initial concentrationof the reactive substance. Ring opening was proposed as the most possible theory for KA andKadp oxidative degradation. Conclusion: It is suggested to use KA instead of Kadp in less stable formulations, such asextemporaneous preparations. The incorporation of antioxidant excipients in Kadp formulationsis recommended for yielding better stability results. Formulating Kadp in the internal phase ofo/w emulsion formulations may protect this susceptive molecule from oxidative degradationduring the shelf life of the pharmaceutical preparation. Further studies are required to study theexact mechanism of the degradation process.
Highlights
Stability is a crucial factor in manufacturing new formulations in the pharmaceutical market.u Pharmaceutical formulators attempt to reach the most stable formulations, which are costeffective and can gain customer acceptance.[1,2,3] n Kojic acid (Ka) is a metabolite derived from the activity of various species of Aspergillus and Penicillium fungi
The incorporation of antioxidant excipients in kojic acid dipalmitate p (Kadp) formulations is recommended for yielding better stability results
Formulating Kadp in the internal phase of o/w emulsion formulations may protect this susceptive molecule from 1|Page oxidative degradation during the shelf life of the pharmaceutical preparation
Summary
The melting peak of the pure standard powders of KA and Kadp was determined using the DSC analysis. In developing stress tests, the researcher should specify suitable parameters such as concentration of the oxidant (H2O2), temperature, a sampling time intervals, and suitable stability indicating the HPLC method for quantitative purposes. Oxidative stress test performed on acyclovir as an antiviral drug was conducted by 1.5% H2O2 at room temperature, which was performed at 30 minutes up to 3 hours.[16] Singh et al have provided a comparative list of different approaches.[1] The selected H2O2 d concentration in the present study was kept at 1.5%. According to the results of data fitting to the first-order kinetic model for KA and Kadp n degradation under oxidative stress, KA and Kadp degrade after hours and minutes, respectively. Further research is needed to prove this mechanism in detail using mass spectrometry and NMR studies
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