Pharmacokinetic study of mucoadhesive metformin pellets in rats

다국어 초록 (Multilingual Abstract)

Previously, we have reported the preparation and characterization of mucoadhesive pellets of metformin hydrochloride using four high-viscosity polymers including hydroxymethylcellulose (HPMC), HPMC/carbopol, sodium carboxylmethylcellulose (Na-CMC) and sodium alginate (Na-Alg) (Piao et al., Arch Pharm Res 32:391–397, 2009).
Here, pharmacokinetic and pharmacodynamic evaluation of these metformin pellets was performed. Metformin pellets were administered orally to normal and streptozotocininduced diabetic rats at 100 mg/kg dose and the blood concentration of metformin and blood glucose levels were determined. The area under the plasma concentration versus time curve from the Na-Alg-coated metformin pellets in normal rats was 69.93 ± 39.63 lg h/mL and it was the highest among tested, followed by Na-CMC-coated pellets (58.38 ± 5.19), HPMC/carbopol-coated pellets (52.24 ±5.29), HPMC-coated pellets (42.70 ± 14.29) and metformin aqueous solution (33.49 ± 2.04). The Cmax from the Na-Alg-coated metformin pellets in normal rats was 29.47 ±10.74 lg/mLand itwas the highest among tested, followed by Na-CMC-coated pellets (15.10 ± 2.73), HPMC/carbopolcoated pellets (11.38 ± 3.04), HPMC-coated pellets (11.29 ± 3.85) and metformin aqueous solution (6.92 ±0.83). The area under the effect versus time curve of the Na-Alg-coated pellets in diabetic rats was the highest as 670.01 ± 211.20 lg h/mL, followed by CMC-coated pellets (542.42 ± 116.93), HPMC-coated pellets (539.46 ±189.91), HPMC/carbopol-coated pellets (444.03 ± 90.30),and metformin aqueous solution (199.28 ± 31.07). These data show that the Na-Alg-coated pellets were found to be the best among tested as a new mucoadhesive formulation for metformin hydrochloride prepared by the powder layering technique with a centrifugal fluidizing-granulator.

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