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Merck
CN

Drug-excipient compatibility studies in binary mixtures of avobenzone.

Journal of cosmetic science (2013-10-22)
Rita Ceresole, Yong K Han, Maria A Rosasco, Liliana R Orelli, Adriana Segall
ABSTRACT

During preformulation studies of cosmetic/pharmaceutical products, thermal analysis techniques are very useful to detect physical or chemical incompatibilities between the active and the excipients of interest that might interfere with safety and/or efficacy of the final product. Differential scanning calorimetry (DSC) was used as a screening technique for assessing the compatibility of avobenzone with some currently used cosmetic excipients. In the first phase of the study, DSC was used as a tool to detect any interaction. Based on the DSC results alone, cetearyl alcohol, isopropyl myristate, propylparaben, diethylhexyl syringylidene malonate, caprylic capric triglyceride, butylated hydroxytoluene (BHT), glycerin, cetearyl alcohol/ceteareth 20, cetearyl alcohol/sodium lauryl sulfate/sodium cetearyl sulfate, and paraffinum liquidum exhibit interaction with avobenzone. Stressed binary mixtures (stored at 50°C for 15 days) of avobenzone and excipients were evaluated by high-performance liquid chromatography. Binary mixtures were further investigated by infrared (IR) spectroscopy. Based on DSC, isothermal stress testing, and fourier transform infrared results; avobenzone is incompatible with caprylic capric triglyceride, propylparaben, and BHT.

MATERIALS
Product Number
Brand
Product Description

Propyl parahydroxybenzoate, European Pharmacopoeia (EP) Reference Standard
Supelco
Avobenzone, Pharmaceutical Secondary Standard; Certified Reference Material
Supelco
Propylparaben, Pharmaceutical Secondary Standard; Certified Reference Material
Supelco
Butylated Hydroxytoluene, Pharmaceutical Secondary Standard; Certified Reference Material
Supelco
Avobenzone, analytical standard
Sigma-Aldrich
Butylated hydroxytoluene, ≥99%, FCC, FG
Sigma-Aldrich
2,6-Di-tert-butyl-4-methylphenol, tested according to Ph. Eur.
Supelco
3,5-Di-tert-butyl-4-hydroxytoluene, analytical standard
Butylhydroxytoluene, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
2,6-Di-tert-butyl-4-methylphenol, purum, ≥99.0% (GC)
Sigma-Aldrich
2,6-Di-tert-butyl-4-methylphenol, ≥99.0% (GC), powder
Sigma-Aldrich
Propyl 4-hydroxybenzoate, ≥99%
Sigma-Aldrich
Propyl 4-hydroxybenzoate, BioXtra
Sigma-Aldrich
Propyl 4-hydroxybenzoate, tested according to Ph. Eur.