Coefficient permeability

The permeability coefficient, P, combines the effects of the diffusion and solubility coefficients. The barrier characteristics of a polymer are commonly associated with its permeability coefficient values. The well-known relationship P = DS holds when D is concentration independent and S follows Henry s law. Standard methods for measuring the permeability of organic compounds are not yet available. ASTM E96 describes a method for measuring the water vapor transmission rate. ASTM D1434 describes a method for the determination of oxygen permeability. 

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Permeability coefficient Permeation Permenorm 5000 H2 Permenorm 3601 K2 Permenorm Z PermeOx Permethrin... 

The effect of the substituents on chain mobility and chain packing has been related to the gas transport properties [209]. Role of symmetry of methyl group placement on bisphenol rings in PES shows the permeability coefficients in the following order ... 

The gas sorption and transport properties also depend on the bisphenol connector groups [210]. The permeability coefficients for all gases rank in the order ... 

It should be recognized that all plastic materials over a time period allow a certain amount of water vapor, organic gas, or liquid to permeate the thickness of the material. It is only a matter of degree of permeation between various materials used as barriers against vapors and gases. It has been found that the permeability coefficient is a function of the solubility coefficient and diffusion coefficient. The process of permeation is explained as the solution of the vapor into the incoming surface of the barrier, followed by diffusion through the barrier thickness, and evaporation on the exit side. 

Nodes, E.E., Mazur, P., Watson, P.F., Kleinhans, F.W., Critser, J.K. (1993). Determination of water permeability coefficient for human spermatozoa and its activation energy. Biol, of Reprod. 48,... 

Mathai and Singh have estimated the permeability coefficient P, using the formula P = kD where k is the partition coefficient and D is the diffusivity. They have used both parallel and series models to calculate P. The experimental values are always greater than measured values. The poor agreement between the experimental and calculated values is attributed to the polar-polar interaction between the epoxy group and nitrile group. 

The release of steroids such as progesterone from films of PCL and its copolymers with lactic acid has been shown to be rapid (Fig. 10) and to exhibit the expected (time)l/2 kinetics when corrected for the contribution of an aqueous boundary layer (68). The kinetics were consistent with phase separation of the steroid in the polymer and a Fickian diffusion process. The release rates, reflecting the permeability coefficient, depended on the method of film preparation and were greater with compression molded films than solution cast films. In vivo release rates from films implanted in rabbits was very rapid, being essentially identical to the rate of excretion of a bolus injection of progesterone, i. e., the rate of excretion rather than the rate of release from the polymer was rate determining. 

FIG. 13 Reduction of the relative permeability coefficient is dependent on the clay platelet aspect ratio in the system of polyimide-clay hybrid with water vapor as the permeate. Each hybrid contains 2 wt% clay. The aspect ratios for hectorite, saponite, montmorillonite, and synthetic mica are 46, 165, 218, and 1230, respectively. (From Ref. 71.)... 

Artursson P and Karlsson J. Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells. Biochem Biophys Res Commun 1991 175 880-5. 

Figure 41-6. Permeability coefficients of water, some ions, and other small molecules in lipid bilayer membranes. Molecules that move rapidly through a given membrane are said to have a high permeability coefficient. (Slightly modified and reproduced, with permission, from Stryer L Biochemistry, 2nd ed. Freeman, 1981.)...

As described above, some solutes such as gases can enter the cell by diffusing down an electrochemical gradient across the membrane and do not require metabolic energy. The simple passive diffusion of a solute across the membrane is limited by the thermal agitation of that specific molecule, by the concentration gradient across the membrane, and by the solubility of that solute (the permeability coefficient. Figure 41—6) in the hydrophobic core of the membrane bilayer. Solubility is... 

The following factors affect net diffusion of a substance (1) Its concentration gradient across the membrane. Solutes move from high to low concentration. (2) The electrical potential across the membrane. Solutes move toward the solution that has the opposite charge. The inside of the cell usually has a negative charge. (3) The permeability coefficient of the substance for the membrane. (4) The hydrostatic pressure gradient across the membrane. Increased pressure will increase the rate and force of the collision between the molecules and the membrane. (5) Temperature. Increased temperature will increase particle motion and thus increase the frequency of collisions between external particles and the membrane. In addition, a multitude of channels exist in membranes that route the entry of ions into cells. 

Another relatively new lipophilicity scale proposed for use in ADME studies is based on MEKC [106]. A further variant is called BMC and uses mobile phases of Brij35 [polyoxyethylene(23)lauryl ether] [129]. Similarly, the retention factors of 16 P-blockers obtained with micellar chromatography with sodium dodecyl sulfate as micelle-forming agent correlates well with permeability coefficients in Caco-2 monolayers and apparent permeability coefficients in rat intestinal segments [130]. 

In PAMPA, the effective permeability coefficient, Pe, is related to the membrane and ABL permeability coefficients, P and Pabl. respectively, as... 

Permeability is a kinetic property expressed by the permeability coefficient (centimeters per second), a number indicating the rate at which molecules pass from aqueous solution across a membrane to another solution on the other side. Permeability is a molecular property used to screen for more complex absorption processes (i.e. in vitro permeabihty is measured to estimate in vivo absorption). 

Thus, the rate of change for the cumulative mass of diffusant passing through a membrane per unit area, or the flux of diffusant, j, may be evaluated from the steady-state portion of the permeation profile of a drug, as shown in Eq. (3). If the donor concentration and the steady-state flux of diffusant are known, the permeability coefficient may be determined. 

The solubility-diffusion theory assumes that solute partitioning from water into and diffusion through the membrane lipid region resembles that which would occur within a homogeneous bulk solvent. Thus, the permeability coefficient, P, can be expressed as... 

The rate-limiting step in the absorption of those compounds that readily penetrate the intestinal membrane (i.e., have a large permeability coefficient) may be the rate at which blood perfuses the intestine. However, absorption will be independent of blood flow for those compounds that are poorly permeable. Extensive studies have illustrated this concept in rats [106,107]. The absorption rate of tritiated water, which is rapidly absorbed from the intestine, is dependent on intestinal blood flow, but a poorly absorbed compound, such as ribitol, penetrates the intestine at a rate independent of blood flow. In between these two extremes are a variety of intermediate compounds whose absorption rate is dependent on blood flow at low flow rates but independent of blood flow at higher flow rates. By altering blood flow to the intestine of the dog, as blood flow decreased the rate of sulfaethidole absorption also decreased [108]. These relationships are illustrated in Fig. 16. 

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