Journal: Drug Invention Today

Article Id: JPRS-D(DD)-00002134
Title: Formulation and evaluation of non-effervescent floating tablets of linagliptin using low-density carriers
Category: Drug (Discovery/Development)
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  • Abstract

    Aim and Objective: The objective of the present work was to formulate floating tablets containing linagliptin to provide a prolonged effect and improve bioavailability in the treatment of type II diabetes. Materials and Methods: Linagliptin is a dipeptidyl peptidase-4 enzyme inhibitor used in the treatment of type-II diabetes. It is rapidly absorbed after oral intake and has 30% of bioavailability while remaining drug is excreted unchanged in urine and enterohepatic system. Due to its lower bioavailability and absorption is more at acidic pH conditions, it is selected as a suitable drug for the design of a gastroretentive floating drug delivery system with a view to improve its bioavailability. Linagliptin non-effervescent floating tablets can be prepared by direct compression method using hydroxypropyl methylcellulose (HPMC) K15, HPMC E15, and chitosan as polymers and Accurel, Gelucire as low-density carriers. Results and Discussion: The Fourier transform-infrared spectra revealed that there was no interaction between polymers an drug; hence, they are compatible. The formulations were evaluated for pharmacopoeial quality control tests and all the physical parameters evaluated were within the acceptable limits. Linagliptin non-effervescent floating tablets were remained buoyant for more than 20 h. The optimized formulation F1 gave 98% of drug release in 20 h with floating lag time of 22 s and total floating time more than 20 h. Conclusion: This study shows that optimum concentration of polymer and low-density carrier increases bioavailability. Stability studies were carried out on the optimized formulation F1 for 3 months at 40°C/75% RH. Finally, it was observed that there was no change in physiochemical and physical properties as well as in drug release profile even after storage at 45°C and 75% for 3 months.

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    Author(s) Name:

    S. Jeganath*, K. Mohammed Shafiq, P. G. Mahesh, S. Sathesh Kumar

    Affiliation(s) Name:

    Department of Pharmaceutics, School of Pharmaceutical Sciences, Vels Institute of Science, Technology and Advanced Studies, Pallavaram, Chennai, Tamil Nadu, India.

    *Corresponding author: Dr. S. Jeganath, Department of Pharmaceutics, School of Pharmaceutical Sciences, Vels Institute of Science, Technology and Advanced Studies Vels University, Pallavaram, Chennai - 600 117,

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    Author:

    S. Jeganath*, K. Mohammed Shafiq, P. G. Mahesh, S. Sathesh Kumar

    Title:Formulation and evaluation of non-effervescent floating tablets of linagliptin using low-density carriers
    Journal:Drug Invention Today
    Vol(issue):10 (March)
    Year:2018
    Page No: (322-329)
  • Experimental Methods Keywords

    Methodology:ormulation and evaluation,Stability study, Type-II diabetes
    Research Materials:Linagliptin

Keywords

Linagliptin Low-density carriers Stability study Type-II diabetes

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