FORMULATION, PHARMACOKINETIC AND PHARMACODYNAMIC EVALUATION OF FAST RELEASING COMPRESSED PROPRANOLOL - HCL SUPPOSITORIES

Fast releasing compressed propranolol HCl suppositories were developed and evaluated for their pharmacokinetic and pharmacodynamic performan ces and compared the results with those obtained after oral administra tion of a commercial tablet in rabbits. Two disintegrants, microcrysta lline cellulose and primogel had significantly influenced the in vitro drug release from suppositories without affecting the in vivo profile s. The differences in various pharmacokinetic parameters were signific ant (p < 0.01) for oral and rectal administration and were insignifica nt (p > 0.05) among the three suppository formulations evaluated. Drug was rapidly absorbed from the suppositories with more than 3 fold inc rease in bioavailability following rectal administration. C(max) of ab out 140 ng/ml and 49 ng/ml was observed after rectal and oral administ rations with the corresponding beta-blockade of more than 95% and abou t 58% respectively. A relationship for log plasma concentration vs %be ta-blockade was established for orally and rectally administered propr anolol HCl.