The aim of the present investigation was to develop and evaluate gastroretentive drug delivery tablets (GRDDTs) of ofloxacin using different polymers such as HPMC K4M, HPMC K15M, Polyethylene oxide WSR 303, Carbopol 971P, Xanthan Gum in different ratios for local action in gastric region to eradicate Helicobacter pylori infection. The GRDDTs were prepared by wet granulation method and evaluated for physical characteristics such as hardness, thickness, friability, drug content and floating properties. The optimized formula F4 showed better sustained drug release and which also had good floating properties and fitted best to be Korsmeyer-Peppas model with R 2 value of 0.9848. As the n value for the Korsmeyer-Peppas model was found be less than 0.45 it follows Fickian diffusion mechanism. FT-IR result showed that there is no drug excipient interaction. In vivo radiographic studies were conducted with BaSO4 loaded tablets to examine the increased gastric residence time of the prepared tablets. The study revealed that the tablet remained in the stomach for 300±10min which indicates the increase in the gastric residence time for the effective localized action of the ofloxacin in the treatment of Helicobacter pylori caused peptic ulcer.

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.

Meloxicam is a non-steroidal anti-inflammatory agent, used in the treatment of rheumatoid arthritis, osteoarthritis, joint diseases and dental pain and in the management of acute post-operative pain. It is selected as model drug candidate because of its wide spectrum of anti-inflammatory activity together with less gastric and local tissue irritation. The present study deals with the development and evaluation of a novel, stomach specific floating in situ gelling system (IGS) of MLX as a means of sustaining the drug release and improving the compliance of dysphagic and geriatric patients who have difficulty in handling and swallowing solid oral dosage forms. The prepared gels were characterized for solution viscosity, floating lag time, physical appearance, water uptake study, in vitro drug release studies. It was observed that both the concentration of sodium alginate and the concentration of calcium carbonate have significant influence on the prepared in situ gelling system characteristics of viscosity, drug content, 50 % and 80 % drug release and similarity factor. In vitro drug release study indicated that the release of the drug from the gel matrix followed non-Fickian diffusion. Pharmacodynamic studies carried out in albino rats revealed significantly increased analgesic/anti-inflammatory response from IGS compared to conventional suspension. Rat pylorus ligation method was employed for in vivo study of the optimized formulation and the results show the formation of gel in gastric juice of the stomach. Studies of the short term stability indicated little or no significant changes. This investigation demonstrates the feasibility of preparing a liquid; stomach specific IGS of MLX for better patient compliance.