Controlled release effervescent buccal discs of buspirone hydrochloride: in vitro and in vivo evaluation studies

Drug Deliv. 2016;23(2):452-8. doi: 10.3109/10717544.2014.917388. Epub 2015 Sep 10.

Abstract

In the present study controlled release effervescent buccal discs of buspirone hydrochloride (BS) were designed using HPMC as rate controlling and bioadhesive polymer by direct compression method. Sodium bicarbonate and citric acid were used in varying amounts as effervescence forming agents. Carbon dioxide evolved due to reaction of sodium bicarbonate and citric acid was explored for its potential as buccal permeation enhancer. The designed buccal discs were evaluated for physical characteristics and in vitro drug release studies. Bioadhesive behavior of designed buccal discs was assessed using texture analyzer. In vivo animal studies were performed in rabbits to study bioavailability of BS in the designed buccal discs and to establish permeation enhancement ability of carbon dioxide. It was observed that effervescent buccal discs have faster drug release compared to non-effervescent buccal discs in vitro and effervescent buccal discs demonstrated significant increase in bioavailability of drug when compared to non-effervescent formulation. Hence, effervescent buccal discs can be used as an alternative to improve the drug permeation resulting in better bioavailability. However, the amount of acid and base used for generation of carbon dioxide should be selected with care as this may damage the integrity of bioadhesive dosage form.

Keywords: Buccal discs; buspirone hydrochloride; drug delivery; effervescent; pharmacokinetics.

Publication types

  • Comparative Study

MeSH terms

  • Adhesiveness
  • Administration, Buccal
  • Animals
  • Biological Availability
  • Buspirone / administration & dosage*
  • Buspirone / chemistry
  • Buspirone / pharmacokinetics*
  • Carbon Dioxide / chemistry
  • Citric Acid / chemistry
  • Delayed-Action Preparations
  • Dopamine D2 Receptor Antagonists / administration & dosage*
  • Dopamine D2 Receptor Antagonists / chemistry
  • Dopamine D2 Receptor Antagonists / pharmacokinetics*
  • Dosage Forms
  • Drug Carriers*
  • Drug Compounding
  • Gases
  • Hypromellose Derivatives / chemistry*
  • Male
  • Mouth Mucosa / metabolism
  • Oral Mucosal Absorption
  • Permeability
  • Rabbits
  • Serotonin Receptor Agonists / administration & dosage*
  • Serotonin Receptor Agonists / chemistry
  • Serotonin Receptor Agonists / pharmacokinetics*
  • Sodium Bicarbonate / chemistry
  • Solubility
  • Technology, Pharmaceutical / methods

Substances

  • Delayed-Action Preparations
  • Dopamine D2 Receptor Antagonists
  • Dosage Forms
  • Drug Carriers
  • Gases
  • Serotonin Receptor Agonists
  • Carbon Dioxide
  • Citric Acid
  • Hypromellose Derivatives
  • Sodium Bicarbonate
  • Buspirone