title: A critical evaluation of fasted state simulating gastric fluid (FaSSGF) that contains sodium lauryl sulfate and proposal of a modified recipe.
abstract: The aim of this work is to evaluate one of the most commonly used fasted state simulating gastric fluids (FaSSGFs), which contains sodium lauryl sulfate (SLS) (FaSSGF(SLS)), and propose a more appropriate surfactant concentration. Surface tension studies clearly show that the critical micelle concentration (CMC) of SLS in the relevant media (a media whose pH and sodium chloride concentration are representative of physiological conditions) is significantly lower (p<0.05) than 8.67 mM, which is the SLS concentration in FaSSGF(SLS). The CMC of SLS in the relevant media was determined to be 1.75 mM. Based on this a modified recipe is proposed in which the concentration of SLS is sufficient to achieve a surface tension similar to that in vivo without causing artificial micellar solubilization. Solubility, intrinsic dissolution, and GastroPlus modeling studies are presented to support and give rationale for the modified recipe. In addition, a comparison between the modified recipe and other FaSSGFs reported in the literature is made.
authors.affiliation: Eli Lilly and Company, Pharmaceutical Sciences R&D, Lilly Research Laboratories, Indianapolis, IN 46285, USA. aburub_aktham@lilly.com
authors.forename: Aktham
authors.initials: A
authors.lastname: Aburub
authors.forename: Donald S
authors.initials: DS
authors.lastname: Risley
authors.forename: Dinesh
authors.initials: D
authors.lastname: Mishra
mesh_terms: D003198:Computer Simulation; D004987:Ethers / Q000737:chemistry / Q000493:pharmacokinetics; D005215:Fasting / Q000378:metabolism*; D005750:Gastric Juice / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D006845:Hydrocarbons, Fluorinated / Q000737:chemistry / Q000493:pharmacokinetics; D006851:Hydrochloric Acid / Q000737:chemistry; D007052:Ibuprofen / Q000737:chemistry; D008823:Micelles; D009994:Osmolar Concentration; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D011374:Progesterone / Q000737:chemistry; D012965:Sodium Chloride / Q000737:chemistry; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry*; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D013500:Surface Tension; D014867:Water / Q000737:chemistry
chemical_list: C118183:CH3OCF2CH(CF3)OCH2F; D004987:Ethers; D006845:Hydrocarbons, Fluorinated; D008823:Micelles; D004364:Pharmaceutical Preparations; D014867:Water; D012967:Sodium Dodecyl Sulfate; D012965:Sodium Chloride; D011374:Progesterone; D006851:Hydrochloric Acid; D007052:Ibuprofen