Journal: Drug Invention Today

Article Id: JPRS-D(DD)-00002133
Title: Design, formulation, and in vitro evaluation of sustained release tablets for losartan potassium
Category: Drug (Discovery/Development)
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    Objective: The purpose of the present research investigation was to formulate sustained release (SR) formulations for losartan potassium using 32 factorial designs. Methods: Losartan potassium is an antihypertensive agent, non-peptide angiotensin-II receptor (type AT1) blocker, and BCS class-III agent. SR tablet formulations of losartan potassium were formulated using variable quantities of hydroxymethyl propyl cellulose (HPMC) K100M and xanthan gum in combinations by direct compression technique. The amount of polymers, HPMC K100M, and xanthan gum required to achieve the drug release was selected as independent variables, X1 and X2 , respectively, whereas time required to release 10% (t 10%), 50% (t 50%), 75% (t 75%), and 90% (t 90%) of drug from formulation was selected as dependent variables. Nine formulations were prepared and evaluated for various pharmacopoeial tests. Results: The results reveal that all formulations were found to be with in the pharmacopoeial limits and in vitro drug release profiles of all formulations were subjected to kinetic modeling. The statistical parameters such as intercept, slope, and correlation coefficient were determined. Polynomial equations were developed for dependent variables. Validity of developed polynomial equations was checked by designing two checkpoint formulations (C1 and C2 ). According to SUPAC guidelines, formulation (F4 ) containing mixture of 15% HPMC K100M and 20% xanthan gum is the most identical formulation (similarity factor f2 = 86.747, dissimilarity factor f1 = 1.760, and no significant difference, t = 0.0477) to marketed product (LOSACAR). Conclusion: Best Formulation F4 follows the first-order, Higuchi kinetics, and the mechanism of drug release was found to be non-Fickian diffusion anomalous transport (n = 0.825).

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    Author(s) Name:

    Raghavendra Kumar Gunda, A. Vijayalakshmi*

    Affiliation(s) Name:

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

    *Corresponding author: A. Vijayalakshmi, Department of Pharmacognosy, School of Pharmaceutical Sciences, Vels Institute of Science, Technology and Advanced Studies, Pallavaram, Chennai - 600 117, Tamil Nadu, India.

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    Author:

    Raghavendra Kumar Gunda, A. Vijayalakshmi*

    Title:Design, formulation, and in vitro evaluation of sustained release tablets for losartan potassium
    Journal:Drug Invention Today
    Vol(issue):10(3)
    Year:2018
    Page No: (315-321)
  • Experimental Methods Keywords

    Methodology:Design, formulation, and in vitro evaluation
    Research Materials:losartan potassium

Keywords

32 factorial design First-order kinetics Hydroxymethyl propyl cellulose K100M Losartan potassium Non-fickian diffusion mechanism Sustained release tablet Xanthan gum

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