In vitro/in vivo studies on a buccal bioadhesive tablet formulation of carbamazepine.
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.
Ikinci
G
G
Department of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.
Capan
Y
Y
Senel
S
S
Alaaddinoğlu
E
E
Dalkara
T
T
Hincal
A A
AA
D000042:Absorption; D000269:Adhesives; D000328:Adult; D000818:Animals; D000927:Anticonvulsants / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D002220:Carbamazepine / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D002417:Cattle; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D007509:Irritants; D007700:Kinetics; D007785:Lactose / Q000031:analogs & derivatives; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives; D009061:Mouth Mucosa / Q000378:metabolism*; D010078:Oxazines; D012995:Solubility; D013607:Tablets
D000269:Adhesives; D000927:Anticonvulsants; D007509:Irritants; D010078:Oxazines; D013607:Tablets; D002220:Carbamazepine; D008747:Methylcellulose; C071191:MK 458; D007785:Lactose