title: Compressed collagen sponges as gastroretentive dosage forms: in vitro and in vivo studies.
abstract: The objective of the present investigations was to develop oblong tablets which expand after contact with gastrointestinal fluids within a few minutes to a length of 4-6 cm and which should remain in the stomach for a prolonged period of time due to their size. The tablets were prepared from riboflavin-containing collagen sponges using a computer controlled single punch tablet machine. The collagen material was compressed to oblong tablets with dimensions of 3.5 mm x 9 mm x 18 mm. In vitro investigations were carried out to characterise drug release. The model drug riboflavin was released from the collagen tablets over 12h. The gastrointestinal retention time of the new dosage form was indirectly estimated by determining the duration of riboflavin excretion after oral intake of the tablet. A crossover in vivo study with 12 healthy male and female subjects was performed. The renal excretion of riboflavin was measured after oral administration of collagen tablets and small sustained release hydrocolloid tablets as reference preparation. The amount of riboflavin excreted into the urine was enhanced after administration of the expanding collagen tablets in comparison with the hydrocolloid tablets. The differences were statistically significant after 5, 6, 8, 9, 10 and 12 h.
authors.affiliation: Institute of Pharmaceutical Technology and Biopharmaceutics, Westphalien Wilhelms-University, Corrensstr. 1, D-48149 Münster, Germany. groenin@uni-muenster.de
authors.forename: Rüdiger
authors.initials: R
authors.lastname: Gröning
authors.forename: Christina
authors.initials: C
authors.lastname: Cloer
authors.forename: Manolis
authors.initials: M
authors.lastname: Georgarakis
authors.forename: Rotraut S
authors.initials: RS
authors.lastname: Müller
mesh_terms: D001672:Biocompatible Materials / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D003102:Colloids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations / Q000008:administration & dosage* / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D004339:Drug Compounding; D005260:Female; D005612:Freeze Drying; D005753:Gastric Mucosa / Q000378:metabolism*; D006801:Humans; D008297:Male; D008855:Microscopy, Electron, Scanning; D013607:Tablets
chemical_list: D001672:Biocompatible Materials; D003102:Colloids; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D013607:Tablets