Keratinized epithelial transport of beta-blocking agents. I. Relationship between physicochemical properties of drugs and the flux across rat skin and hamster cheek pouch.

The maximum fluxes (Jmax) of beta-blockers through keratinized membranes were determined in vitro and compared with their physiochemical parameters such as lipophilicity (log k'0) and melting point (mp). Rat abdominal skin and hamster cheek pouch mucosa were used as the model membranes. Propranolol, metoprolol, timolol, pindolol, nadolol and agenolol were used as beta-blockers with a variety of physicochemical characters. Linear relations of Jmax with either log k'0 or mp were observed both in intact rat skin and in intact hamster cheek pouch, suggesting that the lipophilicity and thermodynamic activity of a drug in the crystal state primarily affect the drug's permeation through these membranes. However, the slope, dJmax/d(log k'0), for cheek pouch mucosa was greater than that for rat skin, corresponding to the lack of appendigeal shunt pathways in cheek pouch. Penetration studies using the delipidized membranes and the isolated stratum corneum sheet of hamster cheek pouch mucosa clarified that the primary rate-limiting barrier function might exist in the lipid layer of the stratum corneum. Jmax values for the tape-stripped and delipidized skins correlated with both the solubilities of drugs in the vehicle and with the mp, suggesting the polar porous characteristics of both model membranes. However, a theoretical approach confirmed that the contribution of an intracellular or aqueous pore route in the intact membrane to the permeation of drugs with positive lipophilic indexes is negligible.     

Recyclization of 4-oxo-1,3-benzoxazinium perchlorates to 4-substituted 5-(o-hydroxyphenyl)-1,2,4-oxadiazolium salts

Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 2, pp. 280–281, February, 1992.     

Measurements of total and positronium-formation cross sections for the scattering of positrons by alkali atoms

We present a review of our recent measurements of total cross sections (Q _T's) for the scattering of positrons by Na, K, and Rb, and positronium-formation cross sections (Q _Ps's) for Na and K. For our total cross section measurements, a beam transmission technique has been used. For ourQ _Ps measurements, our approach involves setting upper and lower limits onQ _Ps using a combination of (1) measuring the transmission of the positron beam with the angular discrimination of the apparatus made as poor as possible, and (2) measuring the 511 keV annihilation gamma rays in coincidence produced by the decay of para-Ps formed in the scattering cell. Comparison with theoretical calculations shows that our measuredQ _T's andQ _Ps's for Na and K agree reasonably well with a close coupling approximation (CCA) calculation which takes into account the formation of Ps in then=1 andn=2 states. In the 3–10 eV energy range, this calculation predicts a peak in theQ _T's andQ _Ps's for K which also appears in our measurements. The absence of such a peak in our measuredQ _T's andQ _Ps's (preliminary) for Na in this energy range is also consistent with the same theory. Comparisons with five-state CCA calculations ofQ _T which do not take Ps-formation into account also show good agreement with our positron-Na, K, and RbQ _T measurements for energies above 20 eV, but show dramatic departures from our measurements below 10 eV for K and Rb.     

Specular reflectance of cold-rolled aluminum surfaces

The specular reflectance of cold-rolled aluminum surface is studied using a fiber optic system. An approximation for the determination of surface roughness is presented.     

Attractors of dynamical systems with control: topology of purposeful formation

The definitions of homogeneous and mosaic attractors of codimension one are given. A topological method for their purposeful formation by using the feedback control laws of controlled dynamical systems is suggested.Published in Ukrainskii Matematicheskii Zhurnal, Vol. 47, No. 1, pp. 129–132, January, 1995.     

Collective mechanism for nuclear stopping and transverse flow in heavy-ion collisions

The role of filamentation instability of quark-gluon plasma, in explaining collective phenomena in relativistic heavy-ion collisions, has been analyzed. Using equations of SU(2) two fluid color hydrodynamics it is shown that this instability can significantly enhance nuclear stopping and might contribute to collective sideward flows.     

Identification of metabolites of halofantrine, a new candidate anti-malarial drug, by gas chromatography-mass spectrometry.

Two previously unknown metabolites of halofantrine, a candidate anti-malarial drug, have been isolated by thin-layer chromatography from the plasma of dogs administered a single oral dose of 60 mg/kg. Their identifies were investigated after trimethylsilylation by gas chromatography-mass spectrometry under electron-impact and negative-ion chemical ionization conditions. The structural assignment was further confirmed by using a combination of elemental composition analysis of all the isotope peaks at low mass resolution and isotope pattern matching. These two metabolites were formed by modification of the dibutylaminopropyl side-chain of the parent compound involving deamination and oxidation or reduction.     

Time-resolved EPR studies on magnetic interactions between excited triplet (tetraphenylporphinato) zinc and doublet nitroxide radical

By time-resolved electron paramagnetic resonance (TREPR), four (tetraphenylporphinato) zinc (ZnTPP) complexes coordinated by an axial ligand containing a nitroxide radical (NRX; X=4, 5, 8, and 10, denotes the bond number from zinc to nitroxide nitrogen) have been studied in terms of magnetic interactions between the photoexcited triplet state of ZnTPP and NRX. The TREPR spectrum of ZnTPP coordinated by NR10 is almost the same as the one of ZnTPP coordinated by pyridine, indicating that the electron exchange interaction,J, between ZnTPP and the doublet nitroxide is negligibly small. On the other hand, TREPR spectra of the NR4 and NR5 complexes are assigned to the Q₁ state constituted by the ZnTPP and the nitroxide radical. In the case of the ZnTPP-NR8 complex, both T₁ and Q₁ TREPR signals are seen, which may originate from two conformations or degenerate T₁ states of ZnTPP. This EPR study is useful for understanding the photophysical and photochemical properties of chromophores.     

Enantiospecific synthesis of isomers of AES, a new environmentally friendly chelating agent

Three four-step enantiospecific syntheses of different diastereomers of AES, a new biodegradable chelating agent, are described. The stereocenters in each of the isomers are accessible from l- and d-malic and aspartic acids.