• YAKHAK HOEJI
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• v.39 no.2
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• pp.185-192
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• 1995

Flurbiprofen, one of potent nonsteroidal antiinflammatory drugs, has several systemic side effects due to dose dumping effect following oral administration of its conventional solid dosage forms. To reduce these side effects and to sustain therapeutic concentration of the drug, matrix tablets of flurbiprofen were prepared and evaluated for sustained release from the tablets. The matrix tablets of flurbiprofen were prepared with Eudragit, Pluronic, (anhydrous) lactose and colloidal silicon dioxide employing two different preparation methods, wet granulation and direct compression. The dissolution rates of the tablets were evaluated using KP 2 method. Formulation factors that affected dissolution rates of flurbiprofen were the type and content of Eudragit, the type and content of Pluronic, and the tablet preparation method. Several formulations of the matrix tablets showed dissolution patterns close to the simulated profile using pharmacokinetic parameters of flurbiprofen.

• YAKHAK HOEJI
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• v.38 no.5
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• pp.483-487
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• 1994

The pharmacokinetic characteristics of an 1% flurbiprofen gel were evaluated using rats in reference to IV bolus and oral administration of the drug using rats. Following the transdermal application of the gel at the dose of 2 mg/kg as flurbiprofen, the $C_{max}$ and $T_{max}$ of the drug were $2.14\;{\mu}g/ml$ and 2 hr, respectively, whereas those after the oral administration of the drug as a suspension were $9.90\;{\mu}g/ml$ and 0.25 hr, respectively. These results indicate that, by the transdermal administration fo flubiprofen as the gel, the absorption of the drug was much slowed down and the lower $C_{max}$ compared to the oral administration may reduce the systemic side effects of the drug. The relative bioavailability of the flurbiprofen gel in reference to the oral dose was 48.5%. Tissue levels of flurbiprofen following the application of 50 mg of the 1% flurbiprofen gel onto ventral skin of rats showed that the maximum drug concentrations in the skin $(8.52\;{\mu}g/g)$ and the muscle $(2.06\;{\mu}g/g)$ occurred at 2 hrs postdose. The drug concentration in the both tissues remained relatively constant over the next 6 hrs following the peak concentration.