Development and in vitro evaluation of buccoadhesive carvedilol tablets

Acta Pharm. 2007 Jun;57(2):185-97. doi: 10.2478/v10007-007-0015-7.

Abstract

Buccoadhesive tablets of carvedilol were prepared using HPMC K4M, HPMC K15M and Carbopol 934 as mucoadhesive polymers. Fifteen formulations were developed with varying concentrations of polymers. Formulations of the BC or BD series were composed of HPMC K4M or HPMC K15M in ratios of 1:1 to 1:5 whereas in the BE series Carbopol 934 was used (1:0.25 to 1:1.50). The formulations were tested for in vitro drug release, in vitro bioadhesion, moisture absorption and in vitro drug permeation through porcine buccal mucosa. Formulation BC3 showed maximum release of the drug (88.7 +/- 0.4%) with the Higuchi model release profile and permeated 21.5 +/- 2.9% of the drug (flux 8.35 +/- 0.291 microg h(-1)cm(-2)) permeation coefficient 1.34 +/- 0.05 cm h(-1)) through porcine buccal membrane. BC3 formulation showed 1.62 +/- 0.15 N of peak detachment force and 0.24 +/- 0.11 mJ of work of adhesion. FTIR results showed no evidence of interaction between the drug and polymers. XRD study revealed that the drug is in crystalline form in the polymer matrix. The results indicate that suitable bioadhesive buccal tablets with desired permeability could be prepared.

MeSH terms

  • Absorption
  • Acrylates / chemistry
  • Adhesiveness
  • Administration, Buccal
  • Adrenergic beta-Antagonists / chemistry
  • Adrenergic beta-Antagonists / pharmacokinetics
  • Animals
  • Carbazoles / chemistry
  • Carbazoles / pharmacokinetics*
  • Carvedilol
  • Delayed-Action Preparations / chemistry
  • Delayed-Action Preparations / pharmacokinetics*
  • Drug Evaluation, Preclinical / methods
  • Hypromellose Derivatives
  • In Vitro Techniques
  • Mannitol / chemistry
  • Methylcellulose / analogs & derivatives
  • Methylcellulose / chemistry
  • Mouth Mucosa / metabolism*
  • Permeability
  • Powder Diffraction
  • Propanolamines / chemistry
  • Propanolamines / pharmacokinetics*
  • Spectrophotometry, Infrared
  • Swine
  • Tablets
  • Technology, Pharmaceutical
  • X-Ray Diffraction

Substances

  • Acrylates
  • Adrenergic beta-Antagonists
  • Carbazoles
  • Delayed-Action Preparations
  • Propanolamines
  • Tablets
  • Carvedilol
  • Hypromellose Derivatives
  • Mannitol
  • Methylcellulose
  • carbopol 934P