Pharmacokinetics of pentoxifylline after oral administration of a sustained release tablet at two different times of the day.
The pharmacokinetics of pentoxifylline (CAS-6493-05-6) was studied in healthy subjects by orally administering a 400 mg sustained release tablet (Trental) at two different times (10:00 or 22:00 h) of the day in a crossover design. Pentoxifylline concentrations in serum samples were estimated by using high performance liquid chromatography. The mean values of Cmax (326.38 +/- 39.77 vs 266.35 +/- 36.0 ng/ml, p < 0.01, n = 8), AUC0-t (2424 +/- 382 vs 2141 +/- 300 ng/ml/h, p < 0.05, n = 8) were significantly higher and Vss/f (16537 +/- 2869 vs 20136 +/- 5006 ml/kg), Vd/f (11807 +/- 2704 vs 15801 +/- 5960 ml/kg) were significantly (p < 0.05, n = 8) lower following morning (10:00 h) administration than in the night (22:00 h). These variations should be considered while designing sustained release dosage forms.
Srinivasu
P
P
University College of Pharmaceutical Sciences, Kakatiya University, Warangal, India.
Rambhau
D
D
Rao
B R
BR
Rao
Y M
YM
D000328:Adult; D019540:Area Under Curve; D002851:Chromatography, High Pressure Liquid; D002940:Circadian Rhythm / Q000502:physiology; D003692:Delayed-Action Preparations; D006207:Half-Life; D006801:Humans; D008297:Male; D010431:Pentoxifylline / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*
D003692:Delayed-Action Preparations; D014665:Vasodilator Agents; D010431:Pentoxifylline