Design and in vivo evaluation of carvedilol buccal mucoadhesive patches.
The buccal region offers an attractive route of administration for systemic drug delivery. Carvedilol (dose, 3.125-25 mg) is beta-adrenergic antagonist. Its oral bioavailability is 25-35% because of first pass metabolism. Buccal absorption studies of a carvedilol solution in human volunteers showed 32.86% drug absorption. FTIR and UV spectroscopic methods revealed that there was no interaction between carvedilol and polymers. Carvedilol patches were prepared using HPMC, carbopol 934, eudragit RS 100, and ethylcellulose. The patches were evaluated for their thickness uniformity, folding endurance, weight uniformity, content uniformity, swelling behaviour, tensile strength, and surface pH. In vitro release studies were conducted for carvedilol-loaded patches in phosphate buffer (pH, 6.6) solution. Patches exhibited drug release in the range of 86.26 to 98.32% in 90 min. Data of in vitro release from patches were fit to different equations and kinetic models to explain release profiles. Kinetic models used were zero and first-order equations, Hixon-Crowell, Higuchi, and Korsmeyer-Peppas models. In vivo drug release studies in rabbits showed 90.85% of drug release from HPMC-carbopol patch while it was 74.63 to 88.02% within 90 min in human volunteers. Good correlation among in vitro release and in vivo release of carvedilol was observed.
Thimmasetty
J
J
Bapuji Pharmacy College, Davangere, Karnataka, India. thimmasetty@yahoo.com
Pandey
G  S
G
Babu
P  R Sathesh
P
D000179:Acrylates / Q000737:chemistry; D000180:Acrylic Resins; D000278:Administration, Buccal; D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D000328:Adult; D000818:Animals; D002227:Carbazoles / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D000077261:Carvedilol; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D004304:Dosage Forms; D004337:Drug Carriers; D004339:Drug Compounding; D004355:Drug Stability; D004356:Drug Storage; D006801:Humans; D006863:Hydrogen-Ion Concentration; D065347:Hypromellose Derivatives; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D009061:Mouth Mucosa / Q000378:metabolism*; D011412:Propanolamines / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D011817:Rabbits; D012995:Solubility; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods; D013718:Tensile Strength; D014783:Viscosity
D000179:Acrylates; D000180:Acrylic Resins; D000319:Adrenergic beta-Antagonists; D002227:Carbazoles; D004304:Dosage Forms; D004337:Drug Carriers; D011412:Propanolamines; D000077261:Carvedilol; C050528:Eudragit RS; D065347:Hypromellose Derivatives; C013517:ethyl cellulose; D002482:Cellulose; D008747:Methylcellulose; C453622:carbopol 934P