Home About us Contact
|
Home About us Contact | ||
|
|
||
Permeation Coefficient (permeation + coefficient)
Selected AbstractsPlasma-induced grafting of hydroxyethyl methacrylate (HEMA) onto chitosan membranes by a swelling methodPOLYMER INTERNATIONAL, Issue 2 2003Yeping Li Abstract Hydroxyethyl methacrylate (HEMA) was grafted onto chitosan membranes by plasma-graft polymerization. Effects of monomer concentration, plasma power and plasma time on the amount of grafting were investigated. The results showed that there were two processes: grafting polymerization and etching of the membrane. The surface of the grafted membrane was evaluated by FTIR. Scanning electron microscopy indicated that the surface morphology of the grafted membrane could be adjusted through plasma power. Water contact angles of the chitosan surface decreased from 78.2° to 45.4° while the amount of grafting increased from 0 to 12.2%, indicating improved hydrophilicity of the membrane surface. Permeation coefficients through the original membrane, the membrane treated at 55,W for 15,min, and the membrane treated at 55,W for 30,min for creatinine were 9.12,×,10,7, 10.6,×,10,7 and 8.57,×,10,7,cm2,s,1, respectively. Thermogravimetry and mechanical testing showed that there were no significant changes on the bulk property of chitosan membrane after modification. © 2003 Society of Chemical Industry [source] Nonlinear quantitative structure-property relationship modeling of skin permeation coefficientJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 11 2009Brian J. Neely Abstract The permeation coefficient characterizes the ability of a chemical to penetrate the dermis, and the current study describes our efforts to develop structure-based models for the permeation coefficient. Specifically, we have integrated nonlinear, quantitative structure-property relationship (QSPR) models, genetic algorithms (GAs), and neural networks to develop a reliable model. Case studies were conducted to investigate the effects of structural attributes on permeation using a carefully characterized database. Upon careful evaluation, a permeation coefficient data set consisting of 333 data points for 258 molecules was identified, and these data were added to our extensive thermophysical database. Of these data, permeation values for 160 molecular structures were deemed suitable for our modeling efforts. We employed established descriptors and constructed new descriptors to aid the development of a reliable QSPR model for the permeation coefficient. Overall, our new nonlinear QSPR model had an absolute-average percentage deviation, root-mean-square error, and correlation coefficient of 8.0%, 0.34, and 0.93, respectively. Cause-and-effect analysis of the structural descriptors obtained in this study indicates that that three size/shape and two polarity descriptors accounted for ,70% of the permeation information conveyed by the descriptors. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:4069,4084, 2009 [source] Preparation and characterization of a customized cellulose acetate butyrate dispersion for controlled drug deliveryJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 6 2002Siva Vaithiyalingam Abstract The purpose of the present experiment was to prepare and characterize the aqueous-based pseudolatex system of cellulose acetate butyrate (CAB) for controlled drug delivery. Aqueous pseudolatex systems are advantageous over organic-based coating systems because these systems are devoid of criteria pollutants such as carbon monoxide, nitrogen oxides, nonmethane volatile organic compounds, and sulfur dioxide. Pseudolatex was prepared with CAB and polyvinyl alcohol (stabilizer) by a polymer emulsification technique. The stability of pseudolatex was evaluated. Particle size was measured and rheological experiments were conducted. The glass transition temperature, microscopic free volume, permeation coefficient, and mechanical properties of plasticized pseudolatex films were estimated. Surface roughness of coating on inert Nu-Pareil® beads (Ingredient Technology Corp., Mahwah, NJ) was measured as a function of coating weight gain. The CAB Pseudolatex was found to be stabilized by steric forces. From intrinsic viscosity, the thickness of the stabilization layer was estimated. An increase in polymeric particles proportionately decreased the thickness of the stabilization layer. All the essential properties of a coating membrane such as microscopic free-volume fraction, permeability coefficient, mechanical properties, and glass transition temperature were fairly controllable as a function of plasticizer concentration. The pseudolatex dispersion of CAB was stable with negligible sedimentation volume and a particle size of 300 nm. Because CAB is water insoluble and non-ionizable, this pseudolatex can be used for pH-independent coating. The films obtained were strong and flexible for controlled drug delivery applications. Coating with the CAB dispersion reduced the surface roughness of beads but it remained stable as a function of increase in coating weight gain. © 2002 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 91:1512,1522, 2002 [source] Permeation of tetracyclines through membranes of liposomes and Escherichia coliFEBS JOURNAL, Issue 2 2000Albrecht Sigler Uptake of tetracycline (tc), 2-tetracyclinonitrile (CN-tc), and 9-(N,N -dimethylglycylamido)-6-demethyl-6-deoxytetracycline (DMG-DMDOT) by liposomes containing Tet repressor (TetR) and by Escherichia coli cells overexpressing TetR was examined. TetR specifically binds to tetracyclines, enhances their fluorescence and thereby allows selective detection of tetracyclines that have crossed the membranes. Analysis of the diffusion of tc and DMG-DMDOT into liposomes yielded permeation coefficients of (2.4 ± 0.6) × 10,9 cm·s,1 and (3.3 ± 0.8) × 10,9 cm·s,1, respectively. Similar coefficients were obtained for uptake of these tetracyclines by E. coli, indicating that diffusion through the cytoplasmic membrane is the rate-limiting step. The permeation coefficients translate into half-equilibration times of approximately 35 ± 15 min and explain how efflux pumps can mediate resistance against tetracyclines. Furthermore, diffusion of CN-tc into liposomes was at least 400-fold slower than that of tc, indicating that the carboxamide group at position C2 is required for efficient permeation of tc through lipid membranes and thereby explaining the lack of antibiotic activity of CN-tc. [source] Combined 4D-fingerprint and clustering based membrane-interaction QSAR analyses for constructing consensus Caco-2 cell permeation virtual screensJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 1 2008Osvaldo A. Santos-Filho Abstract A set of 30 structurally diverse molecules, for which Caco-2 cell permeation coefficients were determined, formed the training set for construction of Caco-2 cell permeation models based upon membrane-interaction (MI) QSAR analysis and a new QSAR method called 4D-fingerprint QSAR analysis. The descriptor terms of the 4D-fingerprints equation are molecular similarity eigenvalues, and this set of descriptors is being evaluated as a potential "universal" QSAR descriptor set. The 4D-fingerprint model suggests that Caco-2 cell permeation is governed by the spatial distribution of hydrogen bonding and nonpolar groups over the molecular shape of a molecule. Moreover, a complementary resampling of the original Caco-2 cell permeation training set, followed by the construction of several "clustered" MI-QSAR models, led to a consensus model consistent in interpretation with the 4D-fingerprint model. © 2007 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:566,583, 2008 [source] | ||||||||||