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Extending the residence time of a dosage form at a particular site and controlling the release of drug from the dosage form are useful especially for achieving controlled plasma level of the drug as well as improving bioavailability. The objective of this study was to extend the GI residence time of the dosage form and control the release of Tramad...
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... 2002, Baumgartner S et.al., 2000). Results are summarized in (Table 3 Fig. 1 Adhesive strength of formulation F1 -F16. Fig. 2 Swelling index of formulation F1 -F16. ...
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Extending the residence time of a dosage form at a particular site and controlling the release of drug from
the dosage form are useful especially for achieving controlled plasma level of the drug as well as improving bioavailability. The objective of this study was to extend the GI residence time of the dosage form and control the release of Tramad...
Citations
... The slide-containing tablet was immersed in the USP paddle type dissolution apparatus containing 900 mL of 0.1 N HCl and the temperature was maintained at 37 ± 0.5 o C. A distance of 2.5cm was adjusted for the paddle of the dissolution apparatus from the tablet, which was rotated at 50 rpm. The time taken by tablet to detach from the membrane was recorded in minutes (Ranga Rao et al., 1989 andSingh et al., 2010). ...
The present research work was focused to develop a mucoadhesive tablet dosage form for dipyridamole, which shows pH dependent solubility, it is highly soluble in acidic pH and as the pH increases the solubility of the drug decreases. Hence it was selected as the drug candidate for the present research. Mucoadhesive tablets of Dipyridamole were successfully prepared by using polymers like HPMC K 4 M, Chitosan and Isabgul husk by wet granulation method. FT-IR studies showed that there is no incompatibility between drug, polymer and various excipients used in the formulations. Formulated tablets have shown satisfactory results for physical parameters and complied with the pharmacopeial limits. The ex-vivo mucoadhesive strength and mucoadhesive force was found to be in the range of 16.15-21.20 g and 1.56-2.06 N. Total ex-vivo mucoadhesive time was observed in between 10 to 12 hours. The in-vitro drug release was found to be more than 90% for the formulations FMD2, FMD3 and FMD8, up to 12 hours. Based on in-vitro drug release and mucoadhesive properties, formulation FMD2 was selected as optimized formulation. The dissolution data were further characterized by fitting the data into various kinetic models. The drug release from the matrices followed zero order with non-fickian release (diffusion + erosion controlled) for the optimized formulation. The optimized formulation was further subjected to swelling studies, which showed a swelling index of 286% up to 24 hours. The results indicated that the selected polymers were of swellable type. The stability studies were carried for 6 months as per ICH and WHO guidelines and the results of the stability study revealed that the optimized formulation is stable during the storage period. The in-vivo radiographic studies in fed condition, for the Mucoadhesive tablets (FMD2) showed a gastric residence time of more than 6 hours. When the radiographic images were taken at different time intervals and it was found to be in a particular location, which suggested that the retention of the dosage form might be due to the adhesion of dosage form to the gastric mucosa.
This study was planned to formulate, characterize, and evaluate to establish the bioavailability of gastroretentive mucoadhesive dosage of atenolol in human subjects with possible in-vitro-in-vivo correlation. In this investigation gastroretentive mucoadhesive dosage of Atenolol was formulated using HPMCK 4 M, chitosan and Isabgul husk by wet granulation technique. The prepared tablets were subjected to physical evaluation, in-vitro drug release, and in-vivo X-ray studies, followed by the pharmacokinetic study in human volunteers. All the prepared tablets showed physicochemical properties within the limits and good in-vitro mucoadhesion. Formulation F2 was selected based on the in-vitro characteristics and in-vivo radiographic studies by replacing part of the drug by adding barium sulphate. From the radiographic studies it was found that the F2 could be successfully retained in stomach for more than 6 hours. Pharmacokinetic studies showed a significant improvement in AUC 0-14 ; 6414.93 ± 58.221 ng.h/mL (p < 0.05) when compared to reference AUC 0-14 ; 4752.18 ± 76.759 ng.h/mL in healthy human volunteers with good in vitro-in vivo correlation. Based on in-vitro characteristics and in-vivo radiographic studies, F2 was selected as optimized gastroretentive mucoadhesive dosage form with improved bioavailability for better patient compliance and disease management.
The present study deals with drug release enhancement of Metformin HCl using mucoadhesive technology by optimization of mucoadhesive agent to improve the mucoadhesion time. Metformin HCl is an oral antihyperglycemic agent of biguanide class used in treatment of type 2 Diabetes. It is hydrophilic drug which absorbed slowly and not completely from the gastrointestinal tract. The absolute bioavailability is reported to be 50-60%. The sustained release trilayered mucoadhesive tablets of Metformin HCl were formulated by direct triple compression method using various mucoadhesive polymers. First and third layer (mucoadhesive layers) was comprises a blend of polymers such as Carbopol 940 and HPMC K100M. The second layer which is sandwiched between first and third layer contained 250 mg Metformin HCl along with release retardant Ethyl Cellulose. Batches F1, F2 and F3 were formulated. The formulated tablets were evaluated for weight variation, hardness, thickness and friability. Tablets were also evaluated for swelling index, mucoadhesive force, mucoadhesion time and in vitro drug release study. All the tablets were hydrated rapidly, mucoadhesive time were found highest in batch F2 which comprises of 1:2 ratio of Carbopol 940 and HPMC K100M in both first and third layer. The 83.80% drug released was observed in batch F2 within 8 hrs.
