Modeling of flux through silicone membranes from water
| Autor: | Karen Ulmer, Kenneth B. Sloan, Surjit Singh, Hema Devarajan, Donna Nickels, Scott Wasdo, Juha Juntunen, Thomas L. Murray, Thea Shanks |
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| Rok vydání: | 2008 |
| Předmět: |
Octanol
Octanols Analytical chemistry Pharmaceutical Science Permeability 2-Propanol Diffusion chemistry.chemical_compound Flux (metallurgy) Polymer chemistry Animals Humans Dimethylpolysiloxanes Isopropyl myristate Skin Aqueous solution Molecular Structure Polydimethylsiloxane Water Membranes Artificial Lipids Silicone membrane Molecular Weight Membrane Models Chemical Pharmaceutical Preparations Solubility chemistry Lipophilicity Solvents |
| Zdroj: | European Journal of Pharmaceutical Sciences. 34:321-332 |
| ISSN: | 0928-0987 |
| DOI: | 10.1016/j.ejps.2008.05.008 |
| Popis: | Do the Roberts–Sloan (RS) or modified Kasting–Smith–Cooper (KSC) equations that provide good fit to data for maximum flux, from water through mouse or human skin also provide a good fit to data for maximum fluxes through silicone membranes (polydimethylsiloxane, PDMS). The maximum fluxes through silicone membranes from water (JMPAQ), molecular weights (MW), solubilities in isopropyl myristate (SIPM) and water (SAQ) of 31 prodrugs and one parent drug have been fitted to the RS equation, which includes a parameter for dependence on SAQ, and the KSC equation, which does not, to determine which equation gave the better fit. In addition, the JMPAQ, MW, SAQ and solubilities in octanol (SOCT) of 26 diverse molecules from other laboratories were collected and fitted to the RS and KSC equations to determine if the choice of lipid parameter (SIPM or SOCT) had an effect on which equation gave the better fit. RS gave the better fit to the present prodrug database where: log JMPAQ = −2.454 + 0.716 log SIPM + 0.284 log SAQ + 0.00208 MW, r2 = 0.77. RS also gave the better fit to the database from other laboratories where: log JMPAQ = −2.046 + 0.667 log SOCT + 0.333 log SAQ − 0.00374 MW, r2 = 0.878 after four obvious outliers were removed to give n = 22. Thus, data for JMPAQ can be fitted to the RS equation, which also provides the best fit to maximum flux from water through mouse or human skin and includes a dependence on SAQ. |
| Databáze: | OpenAIRE |
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