Formulation, Evaluation and Pharmacokinetics of Flurbiprofen Fast Dissolving Tablets.

Aim: The intent of present study is to formulate fast dissolving tablets of flurbiprofen using different superdisintegrants to improve the dissolution and bioavailability. Place and Duration of Study: Jyothishmathi Institute of Pharmaceutical Sciences, Karimnagar, Andhra Pradesh, India, between January 2011 and December 2012. Methodology: Flurbiprofen fast dissolving tablets were prepared using different superdisintegrants and characterized for different physical parameters, DSC, FTIR studies, in vitro dissolution studies and in vivo pharmacokinetics to prove the enhancement of bioavailability. Results: From the in vitro dissolution studies, the percent drug release in 15 min (Q15) was found to be 91.46±1.42% in case of optimized formulation where as the conventional tablets prepared by similar manner showed 22.92±0.47% in 15 min. The initial dissolution rate and dissolution efficiency for optimized formulation was 6.10%/min and 53.44 but it was 1.53%/min and 10.96 in conventional tablets. They increased by 4.0 folds when compared to conventional tablets. From the pharmacokinetic evaluation, the optimized fast dissolving tablets produced peak plasma concentration (Cmax) as 11433.32 ng/ml at 2 h Tmax, but they were found to be 8792.64 ng/ml at 3 h Tmax, in case of conventional tablets. The area under the curve for the optimized fast dissolving and conventional tablets were found to be 42691.23 and 30727.14 ng-h/ml. Conclusion: In summary, formulation of fast dissolving tablets using superdisintegrants was a good approach to enhance the dissolution and absorption rates of flurbiprofen.

Formulation and evaluation of buccoadhesive quetiapine fumarate tablets

The aim of present study was to develop and evaluate buccoadhesive Quetiapine Fumarate (QF) tablets, which is extensively metabolised by liver. Buccoadhesive tablets of QF were prepared using HPMC K4M, HPMC K15M and combination of carbopol and HPC as mucoadhesive polymers by direct compression method. Sodium deoxycholate was added to formulation to improve the permeation of drug. The formulations were tested for bioadhesion strength, ex vivo residence time, swelling time and in vitro dissolution studies and ex vivo permeation studies. Optimized formulation (F3) showed 92% in vitro release in 8 h and 67% permeation of drug through porcine buccal mucosa and followed fickian release mechanism with zero order kinetics. FTIR studies of optimized formulation showed no evidence of interaction between the drug and polymers. In vivo mucoadhesive behaviour of optimized formulation was performed and subjective parameters were evaluated.

O objetivo do presente estudo foi desenvolver e avaliar os comprimidos bucoadesivos de fumarato de quetiapina (FQ), que é extensivamente metabolizada no fígado. Os comprimidos bucoadesivos de FQ foram preparados utilizando-se HPMC K4M, HPMC K15M e a combinação de carbopol e HPC como polímeros mucoadesivos pelo método de compressão direta. O desoxicolato de sódio foi adicionado à formulação para melhorar a permeação do fármaco. As formulações foram testadas quanto à força de bioadesão, tempo de residência ex vivo, tempo de inchamento, dissolução in vitro e permeação ex vivo. A formulação otimizada (F3) mostrou 92% de liberação in vivo em 8 h e 67% de permeação do fármaco através da mucosa bucal de porco e seguiu o mecanismo fickiano de liberação com cinética de ordem zero. Os estudos de FTIR da formulação otimizada não mostraram evidência da interação entre o fármaco e os polímeros. O comportamento mucoadesivo in vivo da formulação otimizada foi efetuado e avaliaram-se os parâmetros subjetivos.