In vitro/in vivo studies on a buccal bioadhesive tablet formulation of carbamazepine

Pharmazie. 2000 Oct;55(10):762-5.

Abstract

A buccoadhesive controlled-release system for delivery of carbamazepine (CBZ) was prepared by compression of hydroxypropyl methylcellulose (HPMC) and carbomer, incorporating a penetration enhancer, sodium glycodeoxycholate (GDC). The release behaviour of systems containing CBZ and various amounts of the two polymers with and without GDC was found to be non-Fickian. Formation of an interpolymer complex between HPMC and carbomer was confirmed in acidic medium by turbidity, viscosity and FT-IR measurements. Addition of the drug to the buccoadhesive formulation reduced the adhesion force significantly (p < 0.1). GDC did not have any effect on bioadhesion. Permeability of bovine buccal mucosa to CBZ was determined using Ussing diffusion chambers [1]. In vivo interaction between the tablet and tissue was examined histologically as well as by scoring mucosal irritation. Histological changes observed in the buccal epithelium after 4 h contact with the tablets containing GDC recovered completely within 24 h after removal. No measurable plasma level of CBZ was obtained either in the absence or presence of GDC.

Publication types

  • Clinical Trial

MeSH terms

  • Absorption
  • Adhesives
  • Adult
  • Animals
  • Anticonvulsants / administration & dosage*
  • Anticonvulsants / adverse effects
  • Anticonvulsants / pharmacokinetics
  • Carbamazepine / administration & dosage*
  • Carbamazepine / adverse effects
  • Carbamazepine / pharmacokinetics
  • Cattle
  • Female
  • Humans
  • In Vitro Techniques
  • Irritants
  • Kinetics
  • Lactose / analogs & derivatives
  • Male
  • Methylcellulose / analogs & derivatives
  • Mouth Mucosa / metabolism*
  • Oxazines
  • Solubility
  • Tablets

Substances

  • Adhesives
  • Anticonvulsants
  • Irritants
  • Oxazines
  • Tablets
  • Carbamazepine
  • Methylcellulose
  • MK 458
  • Lactose