title: Properties of gastroretentive sustained release tablets prepared by combination of melt/sublimation actions of L-menthol and penetration of molten polymers into tablets.
abstract: A novel floating sustained release tablet having a cavity in the center was developed by utilizing the physicochemical properties of L-menthol and the penetration of molten hydrophobic polymer into tablets. A dry-coated tablet containing famotidine as a model drug in outer layer was prepared with a L-menthol core by direct compression. The tablet was placed in an oven at 80°C to remove the L-menthol core from tablet. The resulting tablet was then immersed in the molten hydrophobic polymers at 90°C. The buoyancy and drug release properties of tablets were investigated using United States Pharmacopeia (USP) 32 Apparatus 2 (paddle 100 rpm) and 900 ml of 0.01 N HCl. The L-menthol core in tablets disappeared completely through pathways in the outer layer with no drug outflows when placed in an oven for 90 min, resulting in a formation of a hollow tablet. The hollow tablets floated on the dissolution media for a short time and the drug release was rapid due to the disintegration of tablet. When the hollow tablets were immersed in molten hydrophobic polymers for 1 min, the rapid drug release was drastically retarded due to a formation of wax matrices within the shell of tablets and the tablets floated on the media for at least 6 h. When Lubri wax® was used as a polymer, the tablets showed the slowest sustained release. On the other hand, faster sustained release properties were obtained by using glyceryl monostearate (GMS) due to its low hydrophobic nature. The results obtained in this study suggested that the drug release rate from floating tablets could be controlled by both the choice of hydrophobic polymer and the combined use of hydrophobic polymers.
authors.affiliation: Development Research Laboratories, Kyorin Pharmaceutical Co., Ltd., Tochigi, Japan. mamoru.fukuda@mb.kyorin-pharm.co.jp
authors.forename: Mamoru
authors.initials: M
authors.lastname: Fukuda
authors.forename: Akinori
authors.initials: A
authors.lastname: Goto
mesh_terms: D055598:Chemical Phenomena; D019245:Compressive Strength; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000378:metabolism; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005079:Excipients; D015738:Famotidine / Q000737:chemistry* / Q000378:metabolism; D041981:Gastrointestinal Tract / Q000378:metabolism; D006635:Histamine H2 Antagonists / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D008610:Menthol / Q000737:chemistry*; D008956:Models, Chemical; D011108:Polymers / Q000737:chemistry*; D012995:Solubility; D000074706:Sublimation, Chemical; D013607:Tablets / Q000008:administration & dosage / Q000737:chemistry*; D013997:Time Factors; D014885:Waxes
chemical_list: D003692:Delayed-Action Preparations; D005079:Excipients; D006635:Histamine H2 Antagonists; D011108:Polymers; D013607:Tablets; D014885:Waxes; D008610:Menthol; D015738:Famotidine