Development and in vivo floating behavior of verapamil HCl intragastric floating tablets.
A novel gastro retentive controlled release drug delivery system of verapamil HCl was formulated in an effort to increase the gastric retention time of the dosage form and to control drug release. Hydroxypropylmethylcellulose (HPMC), carbopol, and xanthan gum were incorporated for gel-forming properties. Buoyancy was achieved by adding an effervescent mixture of sodium bicarbonate and anhydrous citric acid. In vitro drug release studies were performed, and drug release kinetics was evaluated using the linear regression method. The optimized intragastric floating tablet composed of 3:2 of HPMC K4M to xanthan gum exhibited 95.39% drug release in 24 h in vitro, while the buoyancy lag time was 36.2 s, and the intragastric floating tablet remained buoyant for >24 h. Zero-order and non-Fickian release transport was confirmed as the drug release mechanism from the optimized formulation (F7). X-ray studies showed that total buoyancy time was able to delay the gastric emptying of verapamil HCl intragastric floating tablet in mongrel dogs for more than 4 h. Optimized intragastric floating tablet showed no significant change in physical appearance, drug content, total buoyancy time, or in vitro dissolution pattern after storage at 40 degrees C/75% relative humidity for 3 months.
Patel
Anand
A
Department of Pharmaceutics, APMC College of Pharmaceutical Education and Research, Himatnagar, Gujarat, India. anandpatel208@yahoo.com
Modasiya
Moin
M
Shah
Dushyant
D
Patel
Vishnu
V
D000179:Acrylates / Q000737:chemistry; D000180:Acrylic Resins / Q000737:chemistry; D000284:Administration, Oral; D000818:Animals; D002121:Calcium Channel Blockers / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical; D019343:Citric Acid / Q000737:chemistry; D003692:Delayed-Action Preparations; D004285:Dogs; D004339:Drug Compounding; D004355:Drug Stability; D005753:Gastric Mucosa / Q000378:metabolism*; D005782:Gels; D006813:Humidity; D065347:Hypromellose Derivatives; D016014:Linear Models; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D008956:Models, Chemical; D011135:Polysaccharides, Bacterial / Q000737:chemistry; D011859:Radiography; D017693:Sodium Bicarbonate / Q000737:chemistry; D012995:Solubility; D013270:Stomach / Q000000981:diagnostic imaging; D013607:Tablets; D013696:Temperature; D014700:Verapamil / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics
D000179:Acrylates; D000180:Acrylic Resins; D002121:Calcium Channel Blockers; D003692:Delayed-Action Preparations; D005782:Gels; D011135:Polysaccharides, Bacterial; D013607:Tablets; D019343:Citric Acid; D065347:Hypromellose Derivatives; C006903:carbopol 940; D017693:Sodium Bicarbonate; D008747:Methylcellulose; D014700:Verapamil; C453622:carbopol 934P; C002563:xanthan gum