A new biodegradable polydepsipeptide microsphere for application in drug delivery systems

A sequential polydepsipeptide containing a tripeptide sequence L-alanyl-Lalanyl-ethyl L-glutamyl and an-hydroxy acid L-lactic acid, poly(Ala-Ala-Glu(OEt)-Lac), was synthesized to prepare the microspherical particles by the solvent evaporation process. In this case, the solvents play the most important role for the preparation of polydepsipeptide microspheres and, as an example, when 200 mg of the polydepsipeptide dissolved in 10 ml of 98/2% chloroform/dichloroacetic acid mixture was stirred at 400 rpm and 30 C, the microspherical particles with mean diameter of 58m were formed after pouring into 200 ml of 1% (w/v) poly(vinyl alcohol) solution. 17-Estradiol was incorporated into the particles, and the resulting particles were found to contain 5 mg of drug per 25 mg of the particle. The in vivo release of drug from the microspherical formulation was evaluated by measuring the pharmacological influence on rat prostate. It was found that the sufficient amount of drug, keeping the effective pharmacological influence, is supplied during the first 12-week period, followed by an incomplete supplying of drug intil the implant is perfectly degraded in vivo in the 25th week from the start of implantation.     

Boron chelates with 5,5,5-trifluoro- and 5,5,5-trichloro-4-aminopent-3-en-2-ones

Boron chelates were obtained by the reaction of butoxy(butylthio)diphenylborane with 5,5,5-trifluoro(trichloro)-4-aminopent-3-en-2-one, and their reactions with primary amines were investigated. -Diiminate complexes of boron with trifluoro- and trichloromethyl groups were synthesized.N. D. Zelinskii Institute of Organic Chemistry, Russian Academy of Sciences, 117913 Moscow. Translated fromIzvestiya Akademii Nauk, Seriya Khimicheskaya, No. 11, pp. 2657–2661, November, 1992.     

Liquid chromatography of the s-triazines

Summary A series of thirty s-triazine compounds have been separated using reversed-phase high-pressure liquid chromatography. A relationship between substituent activity and retention time was developed to predict molecular structure.Work partially completed at the CIBA-GEIGY Corp., McIntosh, Ala., USA.     

Chiral recognition in aqueous solutions. Preferential configurations of α-aminoacids bearing substituted alkyl chains at 25°C

Calorimetric measurements were carried out at 25°C on binary and ternary aqueous solutions containing L and D forms fo the following -aminoacids: tryptophan, cysteine, methionine, phenylalanine, histidine, threonine, and citrulline, which contain both hydrophilic and hydrophobic domains. Differences were found between the values of the homochiral and heterochiral pairwise enthalpic interaction coefficients for tryptophan, cysteine, and methionine. To the contrary, chiral recognition was not detected for phenylalanine, histidine, citrulline, and threonine. The data were interpreted in terms of a preferential configuration model. Chiral recognition is detected only when the interactions of the side chains in the homo- and heterochiral configurations are different. Chiral recognition disappears when a competition exists between zwitterion-zwitterion interactions and side chain-side chain interactions. In some cases, such as for citrulline, compensation effects can occur due to thermal contributions from different domains which mask chiral recognition.     

Second Dissociation Constants of 4-[N-morpholino]butanesulfonic Acid and N-[2-hydroxyethyl]piperazine-N′-4-butanesulfonic Acid from 5 to 55°C

The values of the second dissociation constant, pK ₂, for the dissociation of the NH⁺ charge center of the zwitterionic buffer compounds 4-(N-morpholino)butanesulfonic acid (MOBS), and N-(2-hydroxyethyl)piperazine-N-4-butanesulfonic acid (HEPBS) have been determined from 5 to 55°C, including, 37°C at intervals of 5°C. The electromotive-force (emf) measurements have been made utilizing hydrogen electrodes and silver–silver chloride electrodes. The value of pK ₂ for MOBS was found to be 7.702 ± 0.0005, and 8.284 ± 0.0004 for HEPBS, at 25°C, respectively. The related thermodynamic quantities, G ^o, H ^o, S ^o, and C _p ^o for the dissociation processes of MOBS and HEPBS have been derived from the temperature coefficients of pK ₂. Both the MOBS and HEPBS buffer materials are useful as primary pH standards for the control of pH 7.3 to 8.6 in the region close to that of physiological fluids.     

A class of interaction-round-a-face models and its equivalence with an ice-type model

A new model (called the Temperley-Lieb interactions model) is introduced, in two-dimensional lattice statistics, on a square lattice . The Temperley-Lieb equivalence of this model to the six-vertex, self-dual Potts, critical hard-hexagons and critical nonintersecting string models is established. A graphical equivalence of this model to the six-vertex model generalizes this equivalence to noncritical cases of the above models. The order parameters of a specialization of this model are studied.     

A rigorous control of logarithmic corrections in four-dimensional ϕ4 spin systems

Using Gawedzki and Kupiainen's rigorous block spin transformation method, we study critical phenomena in ⁴ spin systems in four dimensions. In Part I of this work we investigate in detail the renormalization group trajectory of the system not exactly at the critical point.     

Equilibrium polymerization in a solvent: Solution on the Bethe lattice

The lattice model for equilibrium polymerization in a solvent proposed by Wheeler and Pfeuty is solved exactly on a Bethe lattice (core of a Caylay tree) with general coordination numberq. Earlier mean-field results are reobtained in the limitq, but the phase diagrams show deviations from them for finiteq. Whenq=2, our results turn into the solution of the one-dimensional problem. Although the model is solved directly, without the use of the correspondence between the equilibrium polymerization model and the diluten0 model, we verified that the latter model may also be solved on the Bethe lattice, its solution being identical to the direct solution in all parameter space. As observed in earlier studies of the puren0 vector model, the free energy is not always convex. We obtain the region of negative susceptibility for our solution and compare this result with mean field and renormalization group (-expansion) calculations.     

Fields as Kolmogzrov flows

It is widely recognized that for highly unstable dynamical systems there exists a fundamental limitation on predictability and determinism. An important class of such highly unstable systems is the class of K-flow, which is further characterized by the existence of time-asymmetric objects in the form of K-partition. Our recent approach to the problem of irreversibility has shown that when the implications of the limitation on determinism arising from strong form of instability and those of the existence of K-partition are consistently taken into account, one is naturally led from the physically unrealizable deterministic evolution of phase points to an entropy-increasing stochastic Markovian evolution. Furthermore, this transition is not the result of extraneously imposed coarse graining and/or approximation schemes, but can be brought about by an invertible transformation whose existence and construction are determined by the nature of the instability of the dynamical system itself. After a brief review of this theory which also contains some relatively new remarks, we prove that classical Klein-Gordon field (both massive and massless) possess the structure of K-flow. This seems to provide the first examples of relativistic systems that are K-flows. Some of the implications of this result are briefly discussed. From a mathematical point of view, this seems to be a first step toward an ergodic theory of partial differential equations. In the process, we also provide an independant group-theoretic proof of the existence of incoming and outgoing subspaces of the scattering theory of Lax and Phillips for the wave equation.     

Infrared asymptotic freedom of a hierarchical φ 3 6 lattice theory

For the weakly coupled lattice ₃ ⁶ theory in a hierarchical model approximation a nonperturbative renormalization group analysis in the spirit of Gawedzki and Kupiainen is performed to study the flow of the effective actions. We deduce a domain of attraction to the tricritical (Gaussian) fixed point. The two relevant coupling constants of the problem are controlled by analytic continuation to complex domains, tracing their images under the renormalization group iterations.