Effect of mixed film coating on pharmacokinetics of paracetamol tablets

Abstract

This study was carried out to evaluate the effect of mixed film coating on pharmacokinetics of paracetamol tablets. The tablet cores were prepared and film-coated with a mixture of pectin (0.98%w/w), chitosan (0.16%w/w), HPMC (0.06%w/w), glycerol (0.24%w/w) and 0.1M HCl (98.55%w/w). A single oral dose (1200 mg) of the coated tablets having a coat weight gain of 9%w/w was administered to 5 healthy male volunteers under fasting conditions. Saliva samples were collected at regular time intervals over a 16h period and analysed for paracetamol by reverse phase HPLC. The main pharmacokinetic parameters were determined using non-compartmental analysis. The parameters for the uncoated tablets were similar to published values while wide variations were observed for the coated tablets. The mean lag time (T_lag) was higher in the coated tablets (2.14 ± 1.21h) than the uncoated tablets (0.15 ± 0.05h). The mean AUC_{0- α} (16.92 ± 9.84µg/ml^-1h^-1) and mean C_max (3.15 ± 2.10µg/ml^-1) of the coated tablets were 47% and 25%, respectively of the corresponding values of the uncoated tablets. There was a 9-fold increase in the mean T_max (8.40 ± 2.88h) of the coated tablets as compared to the uncoated tablets. The rate and extent of drug absorption was low in the film-coated tablets compared to the uncoated tablets, demonstrating the ability of the mixed films to modulate drug release. The mixed pectin/chitosan/HPMC film coating has the potential for use in the design of controlled release dosage forms.


Keywords: mixed films, controlled drug delivery, pharmacokinetics, chitosan


Journal Of Science And Technology Vol. 25 (1) 2005: 25-32