PubMed · 3178693
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C Franzelius, K Besserer. 1988. [Oxazepam glucuronide].. https://pubmed.ncbi.nlm.nih.gov/3178693/
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The aim of this study was to find an effective carrier for recombinant human tumor necrosis factor-alpha (rHuTNF-alpha). The influence of solvent systems containing poly(methoxy-polyethyleneglycol cyanoacrylate-co-n-hexadecyl cyanoacrylate) (PEGylated PHDCA) on the biological activity of rHuTNF-alpha was investigated. The PEGylated PHDCA nanoparticles loading rHuTNF-alpha were prepared with the double emulsion method. The influence of main experimental factors on the entrapment efficiency was evaluated by the Uniform Design. The physicochemical characteristics and in vitro release of rHuTNF-alpha from the nanoparticles were determined. The results showed that serum albumin such as human serum albumin (HSA) or bovine serum albumin (BSA) could play a protective action on rHuTNF-alpha in the preparation process. At > or =2.0% (w/v) HSA concentration, more than 85% of rHuTNF-alpha activity remained and the role of HSA was not affected by copolymer concentrations from 0.5 to 3.0% (w/v). The entrapment efficiency of the nanoparticles was about 60% and the nanoparticle size was about 150 nm. The nanoparticles were spherical in shape and uniform with the value of the zeta potential about -9 mV. The rHuTNF-alpha release from the nanoparticle showed an initial burst and then continued in a sustained fashion. The results showed that the PEGylated PHDCA nanoparticles could be an effective carrier for rHuTNF-alpha.
The dehydration of nedocromil magnesium (NM) pentahydrate proceeds in two steps, corresponding to the loss of four water molecules in the first step and one water molecule in the second step. The effects of temperature, particle size, sample weight, water vapor pressure and dehydration-rehydration cycle on both the kinetics and activation energy of the dehydration of NM pentahydrate were studied using isothermal TGA and temperature-ramp DSC analyzed by Kissinger's method. The dehydration kinetics for both steps are best described by the Avrami-Erofeev equations, suggesting a nucleation-controlled mechanism. The high activation energy for the second dehydration step indicates that the last water molecule, which is bonded both to a magnesium ion and to a carboxylate oxygen atom, is more 'tightly bound'. The activation energy decreased with increasing sample weight and decreasing particle size. The dehydration rate increased with decreasing water vapor pressure and with repetition of the dehydration-hydration cycle. Dynamic and isothermal PXRD, and 13C solid-state NMR were employed to provide an insight into the dehydration mechanism and the nature of solid-state phase transformation during the dehydration. Molecular modeling with Cerius(2) was used to visualize the crystal structure and to construct the molecular packing diagram. A correlation was noted between the dehydration behavior and the bonding environment of the water molecules in the crystal structure.
Effects of 5-R substitution (R = NO2, F, Cl, Br, I, CH3) and N-deprotonation on the 4000-400 cm(-1) region of the low temperature FT IR spectrum and the molecular structure of solid isatin are investigated. Harmonic IR spectra and molecular geometries of the 5-R isatins (except for Br and I analogues) are calculated at the HF/6-31G(d, p) level and compared with the experimental solid-state data. In general, substitution has small effect on the molecular structure and the IR spectrum of isatin. The v(CO) triplet in the IR spectra of isatin and its 5-substituted analogues is resulted by vibrational splitting of the out-of-phase CO stretching, v(op)[(CO)2]. While the frequency of the v(op)[(CO)2] mode is relatively less affected by 5-substitution and mainly depends on the substituent mass, the frequency of the in-phase stretching, v(ip)[(CO)2], is strongly sensitive to both mass and electronic properties of the substituent. Substitution at C5 has relatively greater influence on the electron density and the force constant of the amide than on the ketone carbonyl group. Strong electron-donors shorten and stabilize the unusually long alpha-dicarbonyl CC bond, while electron-accepting groups tend to stretch this bond further. N-Deprotonation brings to elongation of the five membered-ring along the N-C(CO(ketone)) vector and expansion of the bonds within the alpha-dicarbonyl part. Theoretical v(CO) frequency of isatin is lowered for about 180 cm(-1) upon conversion into isatinato ion. Harmonic vibrational analysis reveals that only the highest-frequency v(CO) mode of the isolated isatinato anion can be considered good group vibration for empirical assignments in spectra of solid isatinates. Owing to the solid-state influences on the v[(CO)2] modes, no reliable spectra structure correlations could be established from the present experimental spectroscopic data.