Comparative studies on Effervescent and Non-Effervescent Floating sustained release Matrix Tablets of Febuxostat

Nithya, T (2018) Comparative studies on Effervescent and Non-Effervescent Floating sustained release Matrix Tablets of Febuxostat. Masters thesis, College of Pharmacy, Madurai Medical College, Madurai.


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Floating drug delivery system offers a simple and practical approach to achieve increased Gastric Residence Time(GRT) and to modify drug release profiles essential for sustained, site specific and localized drug action. An attempt was made to formulate and evaluate floating drug delivery system containing Febuxostat as model drug by both Effervescent technique and non-effervescent techniques. The present work has aimed towards developing a floating drug delivery system of Febuxostat based on Novel approaches. It was hypothesized that a system that combines advantages of both floating and sustained release technology can be successful in the field of novel drug delivery system. The solubility of Febuxostat was enhanced by the melting method using PEG 6000 as a carrier. The λmax of Febuxostat was found to be 317nm in 0.1N HCl. The Febuxostat obeys the Beer’s law within the concentration of 2 to 20μg/ml. DSC and FT-IR studies indicated that there was no interaction between drug and excipients. The formulations (F1 to F9) were prepared by Effervescent technique and formulations (G1 to G9) were prepared by non- effervescent techniques using hydrophilic and hydrophobic polymers. The formulated tablets were analysed for Pre-compression and Postcompression parameters, In vitro release studies, release kinetics, In vivo x-ray studies, stability studies. The Pre-compression parameters of all the formulations were within the required limit that was suitable for formulation of the tablet. The Post-compression parameters, such as Hardness, Friability, Uniformity in weight and Drug content of all the formulated tablets were within the acceptable limits. The floating lag time and duration of buoyancy were found to be satisfied, for all the formulations. Among all, formulation (F5) was selected as best formulation based on in-vitro release studies, Swelling index and in-vitro buoyancy studies. The extent of drug release was found to be 68.34 in 12 hrs. The drug release model of all the formulations complies with the Zeroorder kinetics followed by Non-Fickian diffusion mechanism. The in-vivo X-Ray study was performed for the best formulation.It shows the gastric residence time of more than 12 hrs. Selected formulation of Febuxostat was compared with marketed formulation. CONCLUSION: The results of the present study clearly indicate the feasibility to develop Febuxostat in the form of floating drug delivery system with prolongation of gastric retention time and controlled release. In my present study, the Effervescent formulations had better drug release, Floating Lag time, Swelling Index as compared to Non-Effervescent formulations. Increment in the concentration of swelling agent, decrement in the drug release. This may be due to increase in diffusion length of drug from dosage form to the dissolution studies. Increment in the concentration, of swelling agent, increment in Floating lag time, this may be due to gas generated by the gas generating agent was entangled between matrix formed by the swelling agent. Polymer swelling was crucial in determining the drug release rate and also important for floatation. The viscosity of the polymer had a major influence on swelling process and matrix integrity. Hydrophilic polymers induce the formation of strong viscous gel layer when they come in contact with the aqueous media that slowed down the rate of diffusion of medium into the tablet, which may result in the retardation or decrease in the drug release. The combination of hydrophilic and hydrophobic polymers, which restricts the penetration of dissolution medium inside the matrix, also restricts the formation of gel, layer around the matrix. So, that the drug release from the hydrophobic matrix tablets gets decreased.

Item Type: Thesis (Masters)
Additional Information: Reg.No: 261611305
Uncontrolled Keywords: Effervescent ; Non-Effervescent Floating sustained release Matrix Tablets ; Febuxostat ; Comparative study.
Subjects: PHARMACY > Pharmaceutics
Depositing User: Subramani R
Date Deposited: 01 May 2019 11:39
Last Modified: 01 May 2019 11:39

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