ABSTRACT
The aim of this research was to develop and validate a spectrofluorimetric method for determination of tranexamic acid in hydrogel patch formulations. Tranexamic acid (trans-4-aminomethylcyclohexanecarboxylic acid, trans-AMCHA) is an antifibrinolytic drug that recently gained attention as a skin-whitening agent due to its inhibitory effect on ultraviolet (UV)-induced pigmentation in vivo. Derivatization with naphthalene-2,3-dicarboxaldehyde (NDA) in the presence of cyanide ion (CN(-)) to produce a fluorescent 1-cyanobenz[f]isoindole (CBI) product (lambda(ex) = 420 nm, lambda(em) = 480 nm) is for the first time reported for the determination of tranexamic acid in hydrogel patch formulations. Other separation techniques were not used in the analysis of the CBI-fluorescent product as required in the previous studies. The developed method was proven to be precise and accurate with percent recoveries ranging between 98.0% and 101.8% at the concentration range of 8.4-84.0 microg/ml (R(2) > 0.999). The intra- and inter-day precisions as expressed by the relative standard deviations (RSD) were below 1.85%. Derivatization of tranexamic acid with NDA/CN(-) was completed within five minutes and was stable for at least 30 minutes. The method has been applied to the analysis of drug content and release profiles in tranexamic hydrogel patch formulations.
Subject(s)
Allergens/chemistry , Dermatitis, Allergic Contact/diagnosis , Tranexamic Acid/chemistry , Allergens/adverse effects , Chemistry, Pharmaceutical , Cyanides/adverse effects , Cyanides/chemistry , Dermatitis, Allergic Contact/etiology , Humans , Hydrogel, Polyethylene Glycol Dimethacrylate , Naphthalenes/adverse effects , Naphthalenes/chemistry , Patch Tests , Spectrometry, Fluorescence , Tranexamic Acid/adverse effectsABSTRACT
Chemical analysis on Curcuma zedoaria rhizome volatile oil, using gas chromatography-mass spectrometer techniques, demonstrated the presence of beta-tumerone (19.88%), 1,8-cineole (8.93%), and 7-zingiberene (7.84%) as major constituents. Larvicidal efficacy against Aedes aegypti mosquitoes of zedoary oil and its formulated preparation, zedoary oil-impregnated sand granules, were investigated and compared with that of Abate(R)sand (temephos). Zedoary oil exhibited pronounced potential against the fourth instar larvae of A. aegypti with an LC(50) and LC(99) of 33.45 and 83.39 ppm, respectively. Application of zedoary oil at a dosage yielding ten times that of LC(99) offered complete larval mortality (100% mortality) for a period of 3 days, and the larval mortality subsequently decreased to lower than 50% after application for more than 5 days. Zedoary oil-impregnated sand granules provided remarkably longer activity, with a larval mortality of 100% for a period of 9 days; and mortality below 50% was obtained in week 3 of application. The complete larval mortality that resulted from applying temephos at dosages of 0.1 and 1 ppm persisted for a period of 6 days and 4 weeks, respectively, and the larval mortality below 50% was reported on day 18 and week 11, respectively. Testing A. aegypti species against stored samples of zedoary oil-impregnated sand granules demonstrated that the product stored at 4 degrees C showed the longest larvicidal activity, followed by those kept at ambient temperature and 45 degrees C, yielding a complete larval mortality for 9, 8, and 6 days, respectively. Most samples of zedoary oil-impregnated sand granules stored at each temperature for 1 month showed slightly higher efficacy than those kept for 2 months. The larvicidal efficacy of samples stored at 4 degrees C seemed to be comparable to that of the fresh sample. The efficacy in killing A. aegypti larvae and good biological stability of zedoary oil-impregnated sand granules make this product promising as an alternative to essential oil in the development of new botanical natural larvicide for use in mosquito control programs.
