title: Intercalation compounds of hydrotalcite-like anionic clays with anti-inflammatory agents, II: Uptake of diclofenac for a controlled release formulation.
abstract: The purpose of this study was to investigate whether hydrotalcite is able to intercalate diclofenac, a nonsteroidal anti-inflammatory drug, and release it in a controlled manner. Layered Mg-Al hydrotalcite in the chloride form was used as a host, and the intercalation compound was prepared by Cl-/diclofenac anionic exchange. Drug release from the intercalation compound was performed in vitro in simulated intestinal fluid at pH 7.5 according to USP 24 and in a pH 7.0 solution designed to mimic the ionic conditions of the small intestine. Results from the intercalation process show that hydrotalcite is able to intercalate diclofenac with a simple procedure and with a good drug loading (55% wt/wt). The in vitro drug release was remarkably lower than that from the corresponding physical mixture at both pH 7.5 and pH 7.0. In the latter case, the release was not complete at 24 hours. The kinetic analysis shows the importance of the diffusion through the particle in controlling the drug release rate. The obtained results show that hydrotalcite may be used to prepare modified release formulations.
authors.affiliation: Dipartimento di Chimica e Tecnologia del Farmaco, University of Perugia, Perugia, Italy.
authors.forename: Valeria
authors.initials: V
authors.lastname: Ambrogi
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Fardella
authors.forename: Giuliano
authors.initials: G
authors.lastname: Grandolini
authors.forename: Luana
authors.initials: L
authors.lastname: Perioli
authors.forename: Maria Cristina
authors.initials: MC
authors.lastname: Tiralti
mesh_terms: D000536:Aluminum Hydroxide / Q000737:chemistry*; D000538:Aluminum Silicates / Q000737:chemistry*; D000838:Anions; D000893:Anti-Inflammatory Agents / Q000737:chemistry*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000378:metabolism; D001826:Body Fluids / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D000077215:Clay; D003692:Delayed-Action Preparations / Q000737:chemistry; D004008:Diclofenac / Q000737:chemistry / Q000378:metabolism*; D006863:Hydrogen-Ion Concentration; D007364:Intercalating Agents / Q000737:chemistry*; D007422:Intestines / Q000737:chemistry; D007474:Ion Exchange; D008276:Magnesium Hydroxide / Q000737:chemistry*; D011208:Powders / Q000737:chemistry; D013056:Spectrophotometry, Ultraviolet; D014961:X-Ray Diffraction
chemical_list: D000538:Aluminum Silicates; D000838:Anions; D000893:Anti-Inflammatory Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D007364:Intercalating Agents; D011208:Powders; D004008:Diclofenac; C010467:hydrotalcite; D000536:Aluminum Hydroxide; D008276:Magnesium Hydroxide; D000077215:Clay