Evaluation and Pharmacokinetic Study in healthy human volunteers of developed bilayer thin films containing Piroxicam and Zolmitriptan

Abstract

In the current work, sublingual bilayer thin films (SBTFs) containing piroxicam and zolmitriptan, were prepared by solvent casting technique using HPMC E15, pullulan afterwards evaluated for their physicomechanical properties, disintegration time and in-vitro drug release. A single dose of formulated SBTFs containing piroxicam (10mg) and Zolmitriptan (2.5mg) was administered to healthy volunteers and their blood samples were withdrawn at predefined time interval for in-vivo pharmacokinetic studies. Plasma concentration of drugs were analysed using a validated HPLC-MS/MS method. The pharmacokinetic parameters were obtained and compared with pharmacokinetic data of marketed formulation. The thickness, weight variation, folding endurance and pH of the films was found to be within the acceptable range. The in-vitro disintegration time varied from 27-45 sec and drug content was found to be 96.01- 100.62% for all the formulation. Formulation B3 showed drug release of 92% within 3-4.5 mins. The plasma concentration time curve helped in assessing the pharmacokinetic parameters i.e. AUC0-24, t1/2, Cmax, tmax, and Vd. The plasma concentration time profile of both drugs indicated the increase of AUC, bioavailability, elimination half-life and Vd when compared with the pharmacokinetic parameters of marketed formulation which helped in the rapid onset of action in the management of acute pain. The results suggested that plasma drug concentration of active ingredient started appearing in a significant amount within 30 minutes which indicated that the developed sublingual delivery system had effectively delivered the drug into the systemic circulation.