title: Transbuccal delivery of chlorpheniramine maleate from mucoadhesive buccal patches.
abstract: This article describes buccal permeation of chlorpheniramine maleate (CPM) and its transbuccal delivery using mucoadhesive buccal patches. Permeation of CPM was calculated in vitro using porcine buccal membrane and in vivo in healthy humans. Buccal formulations were developed with hydroxyethylcellulose (HEC) and evaluated for in vitro release, moisture absorption, mechanical properties, and bioadhesion, and optimized formulation was subjected for bioavailability studies in healthy human volunteers. In vitro flux of CPM was calculated to be 0.14 +/- 0.03 mg.h(-1).cm(-2) and buccal absorption also was demonstrated in vivo in human volunteers. In vitro drug release and moisture absorbed were governed by HEC content and formulations exhibited good tensile and mucoadhesive properties. Bioavailability from optimized buccal patch was 1.46 times higher than the oral dosage form and the results showed statistically significant difference.
authors: College of Pharmacy and Health Sciences, Mercer University, Atlanta, Georgia, USA.
authors: K Chandra
authors: KC
authors: Sekhar
authors: K V S
authors: KV
authors: Naidu
authors: Y Vamshi
authors: YV
authors: Vishnu
authors: Ramesh
authors: R
authors: Gannu
authors: V
authors: V
authors: Kishan
authors: Y Madhusudan
authors: YM
authors: Rao
mesh_terms: D000268:Adhesiveness; D000278:Administration, Buccal; D000284:Administration, Oral; D000328:Adult; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002462:Cell Membrane / Q000378:metabolism; D002463:Cell Membrane Permeability; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D002744:Chlorpheniramine / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D004337:Drug Carriers / Q000737:chemistry; D006801:Humans; D008297:Male; D009061:Mouth Mucosa / Q000166:cytology / Q000378:metabolism*; D011108:Polymers / Q000737:chemistry; D013552:Swine; D013678:Technology, Pharmaceutical / Q000379:methods; D013718:Tensile Strength
chemical_list: D004337:Drug Carriers; D011108:Polymers; D002744:Chlorpheniramine; D002482:Cellulose; C002283:hydroxyethylcellulose