Floating dosage forms to prolong gastro-retention--the characterisation of calcium alginate beads.
Floating calcium alginate beads, designed to improve drug bioavailability from oral preparations compared with that from many commercially available and modified release products, have been investigated as a possible gastro-retentive dosage form. A model drug, riboflavin, was also incorporated into the formula. The aims of the current work were (a) to obtain information regarding the structure, floating ability and changes that occurred when the dosage form was placed in aqueous media, (b) to investigate riboflavin release from the calcium alginate beads in physiologically relevant media prior to in vivo investigations. Physical properties of the calcium alginate beads were investigated. Using SEM and ESEM, externally the calcium alginate beads were spherical in shape, and internally, air filled cavities were present thereby enabling floatation of the beads. The calcium alginate beads remained buoyant for times in excess of 13h, and the density of the calcium alginate beads was <1.000gcm(-3). Riboflavin release from the calcium alginate beads showed that riboflavin release was slow in acidic media, whilst in more alkali media, riboflavin release was more rapid. The characterisation studies showed that the calcium alginate beads could be considered as a potential gastro-retentive dosage form.
Stops
Frances
F
GlaxoSmithKline Pharmaceuticals, Park Road, Ware SG12 0DP, UK. frances.x.stops@gsk.com
Fell
John T
JT
Collett
John H
JH
Martini
Luigi G
LG
D000464:Alginates / Q000008:administration & dosage* / Q000737:chemistry; D016503:Drug Delivery Systems; D005753:Gastric Mucosa / Q000378:metabolism*; D020723:Glucuronic Acid / Q000008:administration & dosage / Q000737:chemistry; D006603:Hexuronic Acids / Q000008:administration & dosage / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D008433:Mathematics; D018613:Microscopy, Confocal; D008855:Microscopy, Electron, Scanning; D010781:Photography; D012256:Riboflavin / Q000008:administration & dosage / Q000737:chemistry; D012995:Solubility
D000464:Alginates; D006603:Hexuronic Acids; D020723:Glucuronic Acid; D012256:Riboflavin