Formulation and in Vitro Evaluation of Combined Floating-Bioadhesive Tablets of Imatinib Mesylate

Abstract

Objective: Gastro retentive drug delivery system (GRDDS) pertaining to its attributes like gastric retention time and the extended drug release profile has significantly improved patient compliance. The objective of the present study was to formulate and evaluate a stomach-specific floating-bioadhesive tablets (FBTs) of imatinib mesylate (IM) for prolonged residence in the stomach in the treatment of gastrointestinal stromal tumours (GIST). Methods:All the FBTs were prepared with hydroxypropyl methyl cellulose (HPMC) K 15M, guar gum, sodium alginate, and carbopol 971P using direct compression technique. Physical characterization, in vitro dissolution, swelling characteristics, the mucoadhesive force along with data analysis was done for each FBT. Results:The pre-compression characteristics of powder mixtures found to be satisfactory for all formulation batches. The results of physical evaluation for all batches were complying with pharmacopoeia specification. The swelling index for all formulation batches was approximately 100% after 8 h. The bioadhesive force (mean±SD) reported in a range of 0.05±0.09 to 0.18±0.06 N/m 2 Conclusion: Formulation batch IB9 reported a considerable swelling index, floating behaviour, more bioadhesive strength with uniform drug release pattern. Therefore formulation batch IB9 was selected as optimized batch and kept for further evaluation studies.. It was observed that the release rate of FBTs was decreased with an increment of viscosity and concentration of the polymer. Formulation batches IB1, IB2, IB4, IB5, IB6, IB9, IB10, IB11, and IB13 follows Higuchi Matrix model kinetics; whereas IB3, IB7, IB8, and IB12 follows Korsmeyer-Peppas model kinetics.

Synthesis and Characterization of Novel Sa-Pa-Lsa/C-30b/Ag Nanocomposites for Swelling, Antibacterial, Drug Delivery, and Anticancer Applications

“…The above values of n and k are indicating swift from Quasi-fickian diffusion type mechanism to non-fickian diffusion (Anamouls) type of mechanism [66]. And the best linearity has been achieved in all models except zero-order kinetic model and samples of SA-PA at pH 2 in Korsmeyer-Peppas method (R 2 = 0.956-0.984) and the diffusion exponent "n" was between 0.412-0.727at pH2 and 0.41-0.457 which seems to indicate the diffusion mechanism is non-fickian diffusion.…”

An Outline of Variables in Pelletization by Extrusion and Spheronization

“…Presence and absence of drug is important, which influences mean diameter of pellets. Formulations containing a lower proportion of drugs and water-insoluble drugs are easy to spheronize [33][34][35]. Various researchers have reported the formulation of pellets for different purposes using various excipients to overcome the issues of solubility, stability and drug release properties etc.…”

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“…The FBT containing 5FU were prepared by direct compression technique 6 . The ingredients along with their quantities used for the preparation of the tablet have been illustrated in Table 1.…”

“…A constant weight (10 g) was placed in the upper vial and applied for 2 min, after which it was removed, and the upper vial was then connected to the balance. Weights were added at a constant rate to the pan on the other side of the modified balance of the device until the two vials were separated 6 .…”

“…Subsequently, the glass slide was moved up and down position such that the tablet was completely dipped in the buffer solution at the lowest point and was out at the highest point. The time taken for complete displacement of the tablet from the mucosal surface was noted 6,17 .…”