A new rapidly absorbed paediatric paracetamol suspension. A six-way crossover pharmacokinetic study comparing the rate and extent of paracetamol absorption from a new paracetamol suspension with two marketed paediatric formulations

作者：Smith Stephen; Collaku Agron; Heaslip Louise; Yue Yong; Starkey Yan Yan; Clarke Geoffrey; Kronfeld Nick^*

来源：Drug Development and Industrial Pharmacy, 2012, 38(3): 372-379.

DOI：10.3109/03639045.2011.605141

• Paracetamol pediatric suspensions
• rate of absorption
• minimum effective concentration
• bioequivalence
• early paracetamol exposure

The objective of this study was to compare the rate and extent of paracetamol absorption from the new Paracetamol pediatric suspension (PPS) with two marketed paracetamol suspensions: Children's panadol (CP) and Panodil baby & infant (PBI). The study also assessed the effect on paracetamol absorption of light-calorie, low-fat food consumed 2 h before dosing. Twenty eight male adult volunteers received a single oral dose of 1000 mg of paracetamol from each of three treatments, in both fasted and fed states according to a randomized, single-center, open-label, six-way crossover study design. PPS was bioequivalent to both CP and PBI for AUC(0-10 h), AUC(0-inf) and C-max in both fasted and fed state. However, PPS had greater rate of paracetamol absorption and a faster speed of onset. T-max for PPS was significantly shorter than for PBI in both fasted (p = 0.0005) and fed state (p = 0.0001). Median T-max for PPS was also 10 min shorter than CP in fasted state. Time to reach minimum effective concentration (MEC) for PPS was significantly shorter than CP and PBI. Early paracetamol exposure of PPS was significantly higher than that of the two existing paracetamol products. Food had a significant effect in the early exposure and onset of therapeutic level of paracetamol from PPS. AUC(0-30 min) was significantly higher and time to reach plasma paracetamol at MEC level was significantly shorter than in the fasted state.

• 出版日期2012-3