Formulation and evaluation of buccoadhesive quetiapine fumarate tablets

Abstract

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.Uniterms: Quetiapine Fumarate. Bioadhesion. In vivo mucoadhesive behaviour.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. Uniterms: Fumarato de quetiapina. Bioadesão. Comportamento mucoadesivo in vivo.

Effect of Polymers and Permeation Enhancers in the Release of Quetiapine Fumarate Transdermal Patch through the Dialysis Membrane

“…More than 50% of people with schizophrenia are not receiving appropriate care. A total of 90% of people with untreated schizophrenia are in developing countries [ 1 , 2 , 3 ]. Available oral dosage form has severe hepatic first-pass metabolism, resulting in much less oral bioavailability [ 4 ].…”

Formulation, Development, and Evaluation of Quetiapine Fumarate Immediate Release Tablets

“…[1,4]benzothiazepin-6-ylpiperazin-1-yl)ethoxy]ethanol;but-2-enedioic acid Immediate release formulation (API) is a form of drug delivery system used for the management of mental disorders such as schizophrenia, bipolar disorder, epilepsy, and other environments that need a quick activity commencement and drug pharmacological effects. It has been developed to be cost-effective, easy to carry, and administered to patients accurately and conveniently [16][17][18]. The main objective to formulate a generic version of the reference product is to provide cost-effective quality products to the market.…”