Abstract

Objective: The aim of the study was to prepare and evaluate buccal-adhesive tablets of buspirone hydrochloric acid (HCl) that avoids gastric degradation and first-pass metabolism, thereby increasing the drug bioavailability and onset of action. Buspirone HCl belongs to a class anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds.
 Methods: In the present work, different ratios of Gantrez MS 955 along with Carbopol 934 were studied to give bioadhesive strength. A 32 full factorial design was applied to investigate the combined effect of Gantrez MS 955 concentration (X1) and Carbopol 934 concentration (X2).
 Results: Results of the multiple regression analysis revealed that the independent variables significantly affected the dependent variables (bioadhesive strength [Y1], Q2 [Y2], Q3 [Y3], Q4 [Y4]). On the basis of multiple linear regression analysis and contour plot evaluation, it was found that the combination of two polymers possessed excellent mucoadhesive properties allowing ease of application and removal of the tablets from the buccal mucosa.
 Conclusion: The formulation batch A9 fulfilled all the criteria set from the desirability search. From the in vitro diffusion study, flux was calculated for the optimized batch. A study of the effect of tablet diameter and the environmental factors on the bioadhesion of the tablet was done. To study the environmental factor on bioadhesion, prehydration time and contact time were considered. Results found that increase in prehydration time decrease in bioadhesive strength and increase in contact time increased bioadhesive strength. Thus, a stable buccoadhesive formulation optimized for formulation ingredients and process parameters was prepared successfully.

Highlights

  • Buccal mucosa is an attractive route for systemic delivery of drugs as it is relatively permeable with a rich blood supply

  • Buccal delivery for the transmucosal absorption of drugs into the systemic circulation offers a number of advantages over oral delivery, especially for those drugs that have poor oral bioavailability and/or those drugs that suffer from extensive first-pass metabolism in the liver

  • Buspirone hydrochloric acid (HCl) is an anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds

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Summary

Introduction

Buccal mucosa is an attractive route for systemic delivery of drugs as it is relatively permeable with a rich blood supply. Buspirone hydrochloric acid (HCl) is an anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. It is used in the treatment of generalized anxiety, where it has advantages over other anti-anxiety drugs because it does not cause sedation (drowsiness) and does not cause tolerance or physical dependence. Carbopol 934 (carbomers) is polyacrylic acid and Gantrez MS 955 is polyacrylic acid derivative, having both anion and cation [9,10]

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