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KMID : 0617220030140010193
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Duksung Bulletin Phamaceutical Sciences
2003 Volume.14 No. 1 p.193 ~ p.199
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Characterization of Physicochemical Properties of Ferulic Acid
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Sohn Young-Taek
Oh Jin-Hee
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Abstract
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Ferulic acid (3-methoxy, 4-hydroxy cinnamic acid) is a flavoid component possessing antioxidant property. The compound is currently under development as a new drug candidate for the treatment of the dementia. The objective of this preformulation study was to determine the physicochemical properties of ferulic acid. The n-octanol to water partition coefficients of ferulic acid were 0.375 and 0.489 at the pHs of 3 and 10, respectively. Accelerated stability study for ferulic acid indicated that the t90 value for the drug was estimated to be 459 days at 25℃. Ferulic acid was also found to be unstable under the relative humidity of more than 76％, probably because of the hygroscopic nature of the drug. In order to study compatibility of ferulic acid with typical excipients, potential change in differential scanning calorimetry spectrum was studied in 1:1 binary mixtures of ferulic acid and typical pharmaceutical excipients (e.g., Aerosil, Avicel, CMC, Eudragit, lactose, PEG, PVP, starch and talc). Avicel, CMC, PVP and starch were found to be incompatible with ferulic acid, indicating the addition of these excipients may complicate the manufacturing of the formulation for the drug. Particle size distribution of ferulic aicd powder was in the size range of 10-190μm with the mean particle size of 61μm. The flowability of ferulic acid was apparently inadequate, indicating the granulation may be necessary for the processing of the drug to solid dosage forms. Two polymorphic forms were obtained by recrystallization from various solvents used in formulation. New polymorphic form of ferulic acid, Form Ⅱ, was obtained by recrystallization from 1,4-dioxane. The equilibrium solubility for FormⅡ. The dissolution rate of FormⅡ was higher than that of Form I in the early phase (＜6min). Therefore, these physicochemical information has to be taken in the consideration for the formulation of ferulic acid.
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