title: HPMC as a potential enhancer of nimodipine biopharmaceutical properties via ball-milled solid dispersions.
abstract: The poor solubility of drugs remains one of the most challenging aspects of formulation development. Aiming at improving the biopharmaceutical limitations of the calcium channel blocker nimodipine, the development of solid dispersions is proposed herein. Three different proportions of nimodipine:HPMC were tested and all of them generated amorphous solid dispersions. Improvements of up 318% in the solubility and a 4-fold increase in the dissolution rate of nimodipine were achieved. Stability studies conducted over 90 days in a desiccator indicated that the initial characteristic of the formulations were maintained. However, at 40 °C/75% RH recrystallization was observed for solid dispersions with 70 and 80% of HPMC, whilst the formulation composed of 90% of the carrier remained amorphous. The increase in the stability observed when the HPMC concentration was increased from 70 to 90% in the solid dispersions was attributed to the dilution mechanism.
authors.affiliation: Programa de Pós-Graduação em Farmácia, Universidade Federal de Santa Catarina, Florianópolis 88040-970, Brazil. Electronic address: manoelakr@hotmail.com.
authors.forename: Manoela Klüppel
authors.initials: MK
authors.lastname: Riekes
authors.forename: Gislaine
authors.initials: G
authors.lastname: Kuminek
authors.forename: Gabriela Schneider
authors.initials: GS
authors.lastname: Rauber
authors.forename: Carlos Eduardo Maduro
authors.initials: CE
authors.lastname: de Campos
authors.forename: Adailton João
authors.initials: AJ
authors.lastname: Bortoluzzi
authors.forename: Hellen Karine
authors.initials: HK
authors.lastname: Stulzer
mesh_terms: D000959:Antihypertensive Agents / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D002851:Chromatography, High Pressure Liquid; D004355:Drug Stability; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D009553:Nimodipine / Q000737:chemistry*; D011208:Powders; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014867:Water
chemical_list: D000959:Antihypertensive Agents; D011208:Powders; D014867:Water; D065347:Hypromellose Derivatives; D009553:Nimodipine; D008747:Methylcellulose
keywords: Biopharmaceutical properties; HPMC; Nimodipine; Solid dispersion