scholarly journals Permeation characteristics of tetracyclines in parallel artificial membrane permeation assay

ADMET & DMPK ◽  
2019 ◽  
Vol 7 (3) ◽  
pp. 151-160
Author(s):  
Sachika Yamauchi ◽  
Kiyohiko Sugano
Keyword(s):  
Ionic Strength ◽  
Phosphatidic Acid ◽  
Lipid Composition ◽  
Soybean Lecithin ◽  
Distribution Coefficients ◽  
Ion Pair ◽  
Membrane Permeation ◽  
Artificial Membrane ◽  
Weak Correlation ◽  
Transport Inhibitors

The purpose of the present study was to characterize the passive permeation of tetracyclines in the parallel artificial membrane permeation assay (PAMPA). Tetracyclines exist as zwitterion at physiological pH. The PAMPA membrane was prepared by impregnating a phospholipid/decane solution to a filter support. The permeation coefficient (Pe) of tetracycline (TC) was markedly affected by the lipid composition of the PAMPA membrane. No permeation was observed when phospholipid was not added (pure decane membrane, Pe < 0.05 × 10-6 cm/sec). With the addition of 2 % PC, little or no increase in Pe was observed. The addition of 1 % PE increased the Pe value more than tenfold. The addition of 2 % soybean lecithin containing phosphatidylinositol (PI) and phosphatidic acid (PA) increased the Pe value to above 4 × 10-6 cm/sec. The Pe value was further increased to 15 × 10-6 cm/sec by increasing the concentration of soybean lecithin from 2 to 10 %. The Pe value showed pH and temperature dependence, whereas it was not affected by the ionic strength, TC concentration, and ion-pair transport inhibitors. A weak correlation was observed between the Pe values and octanol-buffer distribution coefficients of tetracyclines. These results suggest that inter-molecular interactions between TC and PE, PI and/or PA facilitate the passive diffusion of TC across the PAMPA membrane.

scholarly journals Permeation characteristics of tetracyclines in parallel artificial membrane permeation assay II: Effect of divalent metal ions and mucin

ADMET & DMPK ◽  
2020 ◽  
Author(s):  
Sachika Yamauchi ◽  
Daisuke Inoue ◽  
Kiyohiko Sugano
Keyword(s):  
Soybean Lecithin ◽  
Speciation Analysis ◽  
Divalent Metal ◽  
Membrane Permeation ◽  
Divalent Metal Ions ◽  
Artificial Membrane ◽  
Chelate Formation ◽  
Molecular Speciation ◽  
Mucosal Side ◽  
Intestinal Permeation

<p class="ADMETabstracttext">The bioavailability of tetracyclines is markedly decreased when co-administered with antacids, milk, or food containing Ca<sup>2+</sup>. Previously, it was suggested that the effective intestinal permeation of tetracycline (TC) was decreased due to Ca<sup>2+</sup> linked mucin binding in the mucosal side. In the present study, we investigated the effect of Ca<sup>2+</sup>, Mg<sup>2+</sup>, and mucin on the membrane permeation of six tetracyclines (TC, oxytetracycline (OTC), minocycline (MINO), doxycycline (DOXY), demeclocycline (DMCTC), and chlortetracycline (CTC)). The membrane permeability values (P<sub>e</sub>) of tetracyclines were measured by the parallel artificial membrane permeation assay (PAMPA) using soybean lecithin – decane (SL–PAMPA) and octanol (OCT–PAMPA) membranes. In SL–PAMPA, Ca<sup>2+</sup> markedly decreased the P<sub>e</sub> values of all tetracyclines. In OCT–PAMPA, Ca<sup>2+</sup> increased the P<sub>e</sub> values of TC, CTC, and DMCTC, but not DOXY, OTC, and MINO. Mg<sup>2+</sup> decreased the P<sub>e</sub> values of all tetracyclines in both SL–PAMPA and OCT–PAMPA (except for CTC in OCT–PAMPA). The addition of mucin had little or no effect in all cases. In contrast to the previously suggested mechanism, the results of the present study suggested that Ca<sup>2+</sup> chelate formation decreased the membrane permeation of tetracyclines, irrespective of Ca<sup>2+</sup> linked mucin binding. Molecular speciation analysis suggested that the permeation of TC – metal chelates was negligibly small in SL-PAMPA.</p>

scholarly journals High salt compatible oxyanion receptors by dual ion imprinting

2020 ◽  
Vol 11 (16) ◽  
pp. 4246-4250 ◽  
Author(s):  
Sudhirkumar Shinde ◽  
Mona Mansour ◽  
Anil Incel ◽  
Liliia Mavliutova ◽  
Celina Wierzbicka ◽  
...  
Keyword(s):  
Ionic Strength ◽  
Ion Pair ◽  
High Ionic Strength ◽  
High Salt ◽  
Ion Uptake ◽  
Ion Imprinting

Imprinting of an ion-pair in presence of mutually compatible anion and cation host monomers leads to polymers showing enhanced ion uptake in competitive high ionic strength buffers.

The chemical buffer system in raw and digested animal slurry

1995 ◽  
Vol 124 (1) ◽  
pp. 45-53 ◽  
Author(s):  
S. G. Sommer ◽  
S. Husted
Keyword(s):  
Ionic Strength ◽  
Ammonia Volatilization ◽  
Ion Pair ◽  
Pair Formation ◽  
Chemical Components ◽  
Buffer System ◽  
Ionic Balance ◽  
Strongly Correlated ◽  
Electrical Conductivities ◽  
Inorganic Phosphates

SUMMARYSlurry pH is of great importance for the regulation of ammonia volatilization from livestock slurry, and therefore more knowledge of the buffer system controlling pH is urgently needed for modelling ammonia losses from stored and surface-applied slurry. The composition of 17 different Danish cattle, pig and biogas plant-digested slurries was studied. The results were used to describe the main buffer components in the slurries, and to discover the most important chemical components necessary for modelling slurry pH. The results showed that the pH of slurry was mainly controlled by the species NH4+/NH3, CO2/HCO3-/CO32- and CH3COOH/CH3COO-, and that ion pair formation did not change the ionic balance significantly. There were only trace amounts of Ca2+, Mg2+ and inorganic phosphates in solution due to precipitation of CaCO3 (calcite) and MgNH4PO4.6H2O (struvite). Measured electrical conductivities were found to be strongly correlated with the calculated ionic strength.

In Situ Artificial Membrane Permeation Assay under Hydrodynamic Control: Permeability-pH Profiles of Warfarin and Verapamil

2010 ◽  
Vol 27 (8) ◽  
pp. 1644-1658 ◽  
Author(s):  
Matěj Velický ◽  
Dan F. Bradley ◽  
Kin Y. Tam ◽  
Robert A. W. Dryfe
Keyword(s):  
Membrane Permeation ◽  
Artificial Membrane ◽  
Ph Profiles

scholarly journals Ion-pair chromatographic monitoring of photographic effluents

2007 ◽  
Vol 5 (2) ◽  
pp. 455-465
Author(s):  
Giedrė Kesiũnaitė ◽  
Birutė Pranaitytė ◽  
Audrius Padarauskas ◽  
Arvydas Dikčius ◽  
Romas Ragauskas
Keyword(s):  
Ionic Strength ◽  
Mobile Phase ◽  
Ion Pair ◽  
Chromatographic Technique ◽  
Two Samples ◽  
Neutral Compounds ◽  
Before And After ◽  
Rapid Monitoring ◽  
Chromatographic Monitoring

AbstractIon-pair chromatographic technique was developed for the rapid and simple determination of the main contaminants (bromide, iodide, sulphite, thiosulphate, thiocyanate, iron(III)-EDTA chelate, free EDTA, hydroquinone and phenidone) in spent photographic solutions. Free EDTA was converted into stable Ni(II)-EDTA chelate prior to analysis. The optimal mobile phase conditions were established by varying the concentrations of tetrabutylammonium (TBA) phosphate and acetonitrile, pH and ionic strength. Separation of five inorganic anions, two metal chelates and two neutral compounds was accomplished in about 30 min using a mobile phase containing 7.5 mmol/L TBA-phosphate, 10 mmol/L NaCl (pH 6.5) and 20% (v/v) acetonitrile. The detection limits (UV detection at 210 nm) ranged from 0.4 µmol/L for phenidone to 8 µmol/L for sulphite with a linearity of 2–2.5 orders of magnitude. The method was applied to the rapid monitoring of spent photographic solutions before and after decomposition. The recovery tests established for two samples were within the range 95–103%.

scholarly journals High Throughput Prediction of Oral Absorption: Improvement of the Composition of the Lipid Solution Used in Parallel Artificial Membrane Permeation Assay

2001 ◽  
Vol 6 (3) ◽  
pp. 189-196 ◽  
Author(s):  
Kiyohiko Sugano ◽  
Hirokazu Hamada ◽  
Minoru Machida ◽  
Hidetoshi Ushio
Keyword(s):  
Stearic Acid ◽  
Chain Length ◽  
Lipid Membrane ◽  
Negative Charge ◽  
Oral Absorption ◽  
Membrane Permeation ◽  
Artificial Membrane ◽  
Intestinal Membrane ◽  
Charged Membrane ◽  
Precise Prediction

The purpose of the present study was to improve the composition of the lipid solution used in parallel artificial membrane permeation assay for the precise prediction of oral absorption. We modified the composition of lipid solution, which was used to make a lipid membrane on the filter support. First, we changed the chain length of organic solvent (PC/alkyldienes [C7-C10]). A negative charge was then added to the membrane to mimic the intestinal membrane (PC/stearic acid/1,7-octadiene and PC/PE/PS/PI/cholesterol/1,7-octadiene). Finally, we examined the predictability of the PC/PE/PS/PI/CHO/1,7-octadiene membrane using structurally diverse compounds. Permeability coefficients of tested compounds were increased as the chain length of alkyldiene became shorter. The addition of a negative charge to the membrane increased the permeability of the basic compounds. However, the negatively charged membrane with stearic acid showed different permeability profiles from PC/PE/PSIPI/CHO. The predictability of the PC/PE/PS/PI/CHO/1,7-octadiene membrane was adequate (r = 0.858, n = 31) for use during the early stages of the drug discovery/development process.

Prediction of Distribution Coefficients from Structure. The Influence of Ion Pair Formation as Reflected in Experimental and Calculated Values

1997 ◽  
Vol 16 (4) ◽  
pp. 315-316 ◽  
Author(s):  
Anna Tsantili-Kakoulidou ◽  
Stavroula Piperaki ◽  
Irene Panderi ◽  
Ferenc Csizmadia ◽  
Ferenc Darvas
Keyword(s):  
Distribution Coefficients ◽  
Ion Pair ◽  
Pair Formation ◽  
Ion Pair Formation

scholarly journals A comparison of the in vitro permeation of niacinamide in mammalian skin and in the Parallel Artificial Membrane Permeation Assay (PAMPA) model

2019 ◽  
Vol 556 ◽  
pp. 142-149 ◽  
Author(s):  
Yanling Zhang ◽  
Majella E. Lane ◽  
Jonathan Hadgraft ◽  
Michael Heinrich ◽  
Tao Chen ◽  
...  
Keyword(s):  
Membrane Permeation ◽  
Artificial Membrane ◽  
In Vitro Permeation ◽  
Mammalian Skin

scholarly journals Reversed phase parallel artificial membrane permeation assay for log P measurement

ADMET & DMPK ◽  
2016 ◽  
Vol 4 (1) ◽  
pp. 54 ◽  
Author(s):  
Zihao Song ◽  
Katsuhide Terada ◽  
Kiyohiko Sugano
Keyword(s):  
Linear Correlation ◽  
Physical Stability ◽  
Reversed Phase ◽  
Water Phase ◽  
Log P ◽  
Membrane Permeation ◽  
Artificial Membrane ◽  
Apparent Permeability ◽  
Oil Water

<p class="ADMETabstracttext">A reversed phase parallel artificial membrane permeation assay (RP-PAMPA) was newly invented for log P measurement. An oil/water/oil sandwich was constructed using a conventional PAMPA instrument. 1 % agarose was used to improve the physical stability of the water phase. A linear correlation between log P and the apparent permeability was observed in the -0.24 &lt; log P &lt; 2.85 region (R<sup>2</sup> = 0.98). RP-PAMPA was also applied to pKa measurement.</p>

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