Gastroretentive mucoadhesive tablet of lafutidine for controlled release and enhanced bioavailability.
Lafutidine a newly developed histamine H2-receptor antagonist having biological half-life of 1.92 ± 0.94 h due to its selective absorption from upper part of gastrointestinal tract the development of mucoadhesive sustained release drug delivery system is recommended in order to enhance the bioavailability. A mucoadhesive tablets was developed using the natural polymer, sodium alginate, xanthan gum and karaya gum. Mucoadhesion is a complex phenomenon which involves wetting, adsorption and interpenetration of polymer chains. The prepared tablets of various formulations were evaluated for a total mucoadhesion time, buoyancy lag time and percentage drug released. The formulation with xanthan gum showed better results. Thus, it may be useful for prolonged drug release in stomach to improve the bioavailability and reduced dosing frequency. Non-fickians release transport was confirmed as the drug release mechanism from the optimized formulation by Korsmeyer-Peppas. The optimized formulation (B3) showed a mucoadhesive strength >35 g. In vivo study was performed using rabbits by X-ray imaging technique. Radiological evidences suggest that, a formulated tablet was well adhered for >10 h in rabbit's stomach. Optimized lafutidine mucoadhesive tablets showed no significant change in physical appearance, drug content, mucoadhesive properties and in vitro dissolution pattern after storage at 40 °C temperature 75 ± 5% relative humidity for 3 months.
Alkem Research Centre , Mumbai, Maharashtra , India and.
Satish
S
Patil
Gokul S
GS
Talele
D000081:Acetamides / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D000268:Adhesiveness; D000464:Alginates / Q000737:chemistry; D000818:Animals; D001682:Biological Availability; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D065546:Drug Liberation; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism*; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D006635:Histamine H2 Antagonists / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D066298:In Vitro Techniques; D007618:Karaya Gum / Q000737:chemistry; D010880:Piperidines / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D011135:Polysaccharides, Bacterial / Q000737:chemistry; D011725:Pyridines / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D011817:Rabbits; D017550:Spectroscopy, Fourier Transform Infrared; D013552:Swine; D013607:Tablets; D014014:Tissue Adhesives / Q000737:chemistry*
D000081:Acetamides; D000464:Alginates; D003692:Delayed-Action Preparations; D006603:Hexuronic Acids; D006635:Histamine H2 Antagonists; D010880:Piperidines; D011135:Polysaccharides, Bacterial; D011725:Pyridines; D013607:Tablets; D014014:Tissue Adhesives; C076948:lafutidine; D020723:Glucuronic Acid; D007618:Karaya Gum; C002563:xanthan gum
In vitro and in vivo study; lafutidine; mucoadhesive; sustained release