Formulation optimization, in vitro characterization and stability studies of sustain release tablets of Ketoprofen.

The aim of the current study was to formulate sustain release (SR) tablets of ketoprofen. Five batches (batch I -V) of matrix based ketoprofen tablet were prepared by dry granulation method using hydroxyl propyl methyl cellulose (15000cps). Compatibility of formulation excipients with drug was explored through FT-IR technique. Various physical and chemical parameters of all tablet batches were evaluated with multi-point dissolution profile (for 24hrs) for formulation optimization. Release kinetics of trials was estimated by model dependent and independent methods. Formulations having excellent quality attributes were then compared with marketed ketoprofen SR tablets. Accelerated stability study was also conducted to compute the shelf life of the optimized formulation. FT-IR scans illustrated the compatibility of ketoprofen with all tablet excipients. On the basis of testing results and controlled release pattern batch II was set to be an optimized trial having shelf life of 37 months. All trial batches (batch I-V) and the marketed brand exhibited highest linearity towards zero order and Korsmeyer-Peppas model with non-fickian anomalous transport (n=0.541-0.655).

Pharmacokinetics of diclofenac sodium in normal man.

Diclofenac sodium was administered as 50 mg tablets to four healthy male volunteers in a two-way randomized crossover study in which volunteers were either fasted or were given a standard breakfast immediately prior to dosing. Blood samples were obtained upto 9 hours period and drug concentration were determined by HPLC method. Besides a significantly delayed (at p > 0.1) peak in fed state; an increase in absorption rate constant was observed as the only significant (at p > 0.05) effect of food on biopharmaceutic characteristic of diclofenac sodium. However, the intrinsic absorption of diclofenac sodium is also fast and it is not being the rate limiting factor in the bioavailability of diclofenac sodium, its decrease upto about 18 minutes (0.31 +/- 0.05 hr) from 11 minutes (0.19 +/- 0.02 hr) produces a null difference as the net effect on bioavailability, particularly when the drug is to be used in multiple dosage regimen.