Improved Oral Pharmacokinetics of Diclofenac Sodium from SNEDDS in Human Volunteers
DOI:
https://doi.org/10.12974/2311-8792.2015.03.01.2Keywords:
SNEDDS, tablet, diclofenac sodium, pharmacokinetics, absorptionAbstract
The pharmacokinetics of diclofenac sodium in SNEDDS formulation and tablet were compared in healthy human volunteers. In this, randomized study with a cross over design, diclofenac sodium was administered as a single dose to subjects before food. Blood samples were obtained before dosing as a control and at 0.5, 1, 1.5, 2, 4, 8, 12 and 24 hours after dosing. The serum concentrations were determined by high performance liquid chromatography. Possible adverse events were monitored during the entire study. After log-transformation of the comparable variables, statistically significant differences were found between the two formulations with respect to the time between dosing and the appearance of the drug in serum, time to reach maximum concentration, elimination half-life, absorption rate constant and mean residence time. The extent of absorption was assessed by estimating the area under the serum concentration-time curve (AUC). AUC0-8hr and AUMC0-24hr was statistically significantly higher for diclofenac sodium (DFS) self nanoemulsifying drug delivery systems (SNEDDS) (6.428mcg.hr/ml, 218.83mcg.hr/ml) than for voveran tablet (5.869mcg.hr/ml, 52.19mcg.hr/ml). No significant differences were found in AUC0-24hr. SNEDDS of diclofenac sodium showed a statistically significant higher maximum serum concentration than voveran tablet (2.289mcg/ml and 1.375mcg/ml for SNEDDS and tablet, respectively). The results of the present study suggest that SNEDDS of diclofenac sodium could be a clinically useful rapid release formulation for immediate relief without causing gastric ulcers.
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