Abstract

Objective: The aim of this current research was to formulate and analyze the characteristics of atenolol-β-cyclodextrin which using co-process crospovidone-sodium starch glycolate as the disintegrants. Evaluation which has been conducted on orally disintegrating tablets consist of wetting time, water absorption ratio, in vitro dispersion time, and dissolution.Methods: Inclusion complex of atenolol-β-cyclodextrin which were prepared using solvent evaporation method, then formulated using co-processed crospovidone-sodium starch glycolate 1:1 (formula 1) and 1:2 (formula 2) into orally disintegrating tablets by direct compression technique. Orally disintegrating tablets of atenolol-β-cyclodextrin using a physical mixture of crospovidone-sodium starch glycolate 1:1 (formula 3), 1:2 (formula 4) was also prepared as a control. The prepared formulations (F1-F4) were evaluated by several parameters such as wetting time, water absorption ratio, in vitro dispersion time, and dissolution.Results: Orally disintegrating tablets of atenolol-β-cyclodextrin using co-processed crospovidone-sodium starch glycolate 1:1 (formula 1) showed shorter wetting time (53.53±2.26 seconds) and in vitro dispersion time (47.44±2.49 seconds) compare to the other formulas. Formula 1 also exhibited the highest dissolution efficiency compare to the formula which was used in the physical mixture. The results of this study also revealed that there was a high correlation between in vitro dispersion time and dissolution efficiency of atenolol-β-cyclodextrin orally disintegrating tablets.Conclusion: Orally disintegrating tablets of atenolol-β-cyclodextrin showed enhanced dissolution efficiency due to the presence of inclusion complex and co-processed crospovidone-sodium starch glycolate. Formula 1 was found to be the best formula in this study. This formula effectively reduces in vitro dispersion time, hence the dissolution efficiency became higher.

Highlights

  • Peroral drug delivery route was the most commonly used and convenient to deliver the drug because it is the most natural, not harmful, easy to use, and safe in terms of drug delivery [1]

  • Formula 3 and formula 4 were prepared as a control, using a physical mixture of crospovidone-sodium starch glycolate in the same ratio compare to the co-processed superdisintegrants

  • The compressed tablets were evaluated for physical properties such as organoleptic, dimension, uniformity of weight, wetting time, water absorption ratio, in vitro dispersion time, and disintegration time

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Summary

Introduction

Peroral drug delivery route was the most commonly used and convenient to deliver the drug because it is the most natural, not harmful, easy to use, and safe in terms of drug delivery [1]. The use of conventional tablets has caused trouble, such as the elderly who are experiencing difficulties in using conventional dosage forms because of hand tremors and dysphagia [1, 2] This condition produces non-compliance in a specified group of patients, especially geriatric. The outcomes from previous work revealed that the cost of treatment, discomfort with treatment, and long-term therapy were common reasons for non-compliance [4]. To overcome these problems, an effective drug delivery system is needed to provide a solution to the noncompliance issues. The orally disintegrating tablet is one of the peroral delivery systems which can exhibit improvement in compliance, especially in geriatric patients who take long-term therapy

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