The aim of the study was to assess the bioequivalence of two different diclofenac (CAS 15307-86-5) formulations (diclofenac free acid suspension as test formulation and diclofenac resinate suspension, Cataflam, as reference formulation) in 24 healthy volunteers. After an overnight fast, the volunteers received a single oral dose (50 mg) of each formulation, following an open, randomized, two-period crossover design, with a fourteen-day washout interval between doses. Serum samples were obtained over a 24-h interval post-dosing, and were analysed for their diclofenac content by HPLC-UV. No adverse effect was reported for any of the formulations administered. Geometric mean test/reference individual ratios were: 92.8% for AUC(0-24 h), 93.2% for AUC(0-infinity), 117.2% for Cmax, 131.0% for Ke and 76.2% for T1/2. The variability of Cmax parameter expressed as CV was greater than 25%. Since the 90% CI for AUC(0-24 h) mean ratio were within the 80-125% interval proposed by the Food and Drug Administration, it can be concluded that diclofenac free acid formulation is bioequivalent to diclofenac resinate formulation for the extent of absorption. Since the European Community Agency accepts a 90% CI for Cmax of 70-143%, it can be concluded that diclofenac free acid formulation is bioequivalent to diclofenac resinate formulation for both the rate and the extent of absorption after single dose administration.
Isosorbide 5-mononitrate (5-ISMN) is an organic nitrate widely used for its vasodilating properties in the treatment of angina pectoris. In the present study, a new method was developed for the determination and quantification of 5-ISMN, in human plasma, by liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS), using photospray ionization. 5-ISMN was extracted from 0.5 mL human plasma by liquid-liquid extraction (LLE). The method had a chromatographic run of 2.0 min using a C8 analytical column (100 mm ×2.1 mm i.d.). Although the method showed a non linear calibration curve response (20 to 2000 ng mL-1), the analytical methodology was fully validated (r 2 > 0.995).The assay performance results indicate that the method is efficient, robust and sufficiently precise and accurate for the routine determination of the 5-ISMN in human plasma.The method herein developed was employed in a bioequivalence study of two tablet formulations of 5-ISMN 40 mg. The bioequivalence study was conducted open, randomized, two-period, crossover, one-week washout period. Both formulations was well tolerated. Pharmacokinetic parameters of 5-ISMN was similar those described in the literature. The 90% confidence interval (CI) for the geometric mean of AUC 0-t and C max were included into the bioequivalence range. Based on FDA and Anvisa rules for human bioequivalence trial, can be concluded bioequivalence for both, rate and extent of absorption between both formulations after single oral dose administration (5-ISMN 40 mg).
Objective: The aim was to assess the comparative bioavailability of two formulations (200 mg tablet) of amiodarone (CAS 19774-82-4) in healthy volunteers of both sexes, with and without food. Methods: The study was conducted using an open, randomized, two-period crossover design with a 3-week washout interval, in two groups, with and without food. Plasma samples were obtained for up to 240 h post dose. Plasma amiodarone concentrations were analyzed by liquid chro-matography coupled to tandem mass spectrometry (LC-MS-MS) with positive ion electrospray ionization using multiple reactions monitoring (MRM). From the amiodarone plasma concentration vs. time curves, the following pharmacoki-netic parameters were obtained, with and without food: AUClast, AUCinf, AU C0-240h, AUC0-72h and Cmax. Results: The limit of quantification was 1 ng/mL for plasma amiodarone analysis. The geometric mean and 90 % confidence interval CI of Test/Reference percent ratios were, without and with food, respectively: 107.61 (92.73?124.89) and 100.6 (94.1?107.5) for Cmax, 107.05 (95.88?119.51) and 100.2 (96.0?104.7) for AUClast, 107.27 (95.78?120.15) and 100.8 (97.0?104.8) for AUC0-72h , 106.76 (95.84? 118.94) and 100.2 (96.0?104.7) for AUC0-240h and AUCinf 105.15 (94.18?117.41) and 100.7 (96.6?105.0). Conclusion: Since the 90 % CI for AUC0-72, and Cmax ratios were within the 80?125 % interval proposed by the US FDA, it was concluded that the amio-darone 200 mg tablet (test formulation) with and without food was bioequivalent to the reference 200 mg tablet for both the rate and extent of absorption.
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