Powdered formulation of liquid oil terpenoid included in cyclodextrins for chemical stabilization and improved handling

Teprenone (Tp) is a widely used pharmaceutically active ingredient in terpene anti-ulcer agents. We investigated Tp and cyclodextrin (CD) complexes for the objective of forming stable Tp powders. Tp was combined with each CD at a molar ratio of 1:2, kneaded together while adding an appropriate amount of water, then dried under reduced pressure and lightly milled into a powder to produce a kneaded mixture (KM). Powder X-ray diffraction of KM containing Tp and β- and γ-CD revealed new diffraction peaks. On infrared spectroscopy, the peak near 1718 cm^?1 corresponding to the carbonyl group of Tp had shifted to around 1701 cm^?1. Solid-state NMR spectroscopy showed signs of inhibited molecular mobility of Tp, which is liquid at room temperature, confirming that Tp had formed complexes with β- and γ-CD. Photostability analysis of Tp showed improved stability in the order of γ-CD > β-CD ? α-CD.     

Combined study with FDG PET and Tl SPECT in patients with idiopathic dilated cardiomyopathy

This study aimed to determine whether combined examinations of myocardial 2-[18F]fluoro-2-deoxy-D-glucose positron emission tomography (FDG PET) and stress-redistribution 201Tl single-photon emission computed tomography (Tl SPECT) were useful in clarifying myocardial ischaemia and evaluating the prognosis in patients with idiopathic dilated cardiomyopathy (IDCM). Twenty-two patients with IDCM underwent echocardiography, cardiac catheterization, FDG PET, and Tl SPECT. In scintigraphic analysis, the total defect score (TDS) was semiquantitatively determined as the sum of scores of the 17 left ventricular (LV) segments with a 5-point scale (0 as normal to 4 as absent). Patients were classified according to the scintigraphic findings as follows: eight patients with small defects on Tl and FDG (TDS < or = 20) (group I), eight patients with small defects on FDG (TDS < or = 20) with FDG uptake increased relative to Tl or 'mismatch' (group II), and six patients with large defects on FDG and Tl (TDS >20) (group III). Eleven patients (50%) showed reversible defects on Tl and all showed preserved FDG uptake. The patients in group III had significantly lower LV ejection fraction (LVEF) (P<0.05, respectively) and a poorer prognosis as shown by the Kaplan-Meier event-free curve compared with those in groups I and II (P<0.01, respectively). Although patients in group II had significantly greater TDS on Tl compared with those in group I (P<0.01), no significant differences in LVEF and prognosis were found between patients in groups I and II. In multivariate analysis, a TDS on FDG revealed an independent predictor of subsequent cardiac events. In conclusion, such mismatched areas can be assumed to consist of impaired but viable myocardium, and may be associated with ischaemia of the microvasculature. Impaired myocardial glucose metabolism is a more powerful predictor of future cardiac events than perfusion abnormality in patients with IDCM.     

Epitopes for thyroid stimulating and blocking autoantibodies on the extracellular domain of the human thyrotropin receptor

The majority (97%) of functional epitopes for stimulating thyrotropin receptor (TSHR) antibodies (stimulating TSHRAbs) in a large cohort (n = 59) of Japanese Graves' patients exists on the N-terminal region of the extracellular domain of TSHR, between residues 25 and 165 numbering from the methionine start site. This was determined by measuring the loss of stimulating activity in the Cos-7 cells transfected with TSHR/lutropin-choriogonadotropin receptor (LH-CGR) chimeras wherein TSHR residues 89-165 (Mc2) or 8-165 (Mc1 + 2) are replaced by comparable LH-CGR residues. There is no comparable loss when stimulating TSHRAb activity is measured in an Mc4 chimera, wherein TSHR residues 261 to 370 are replaced. In contrast, immunoglobulin (IgG) preparations from 35 patients with Hashimoto's disease or idiopathic myxedema, who have blocking TSHRAbs causing hypothyroidism, loose blocking TSHRAb activity in the Mc4 chimera, but not the Mc2 or Mc1 + 2 chimeras. Thus, in a large population of Japanese patients with autoimmune thyroid disease caused by TSHR autoantibodies, the major functional epitope for stimulating TSHRAbs is on the N-terminal portion of the TSHR extracellular domain, whereas that for blocking TSHRAbs is on the C-terminal portion of the extracellular domain. To further evaluate the nature of the critical functional epitope between residues 90 to 165, we divided this region approximately in half, creating chimeras Mc2a and Mc2b with, respectively, residues 90-124 or 125-165 replaced by comparable LH-CGR residues. IgGs from all patients tested lost significant stimulating activity using the Mc2a and Mc2b chimeras; however, when present, residual stimulating TSHRAb activity was evident on one or the other half of the region or on both halves, indicating that both segments are required for expression of the stimulating TSHRAb epitope within residues 90-165. Finally, we have identified a complex epitope involving both the N- and C-terminal portion of the extracellular domain that appears to account for the small fraction of stimulating TSHRAbs whose activity is not solely dependent on residues 25 to 165. Thus, using chimeras Mc1 + 2 + 4, with TSHR residues 8-165 and 261-370 substituted, or chimera Mc1 + 2 + 3 + 4, with residues 8-370 substituted, as well as Mc2, Mc1 + 2, and Mc4, we show that the Graves' IgGs which maintain stimulating TSHRAb activity when residues 8-165 of the TSHR are replaced by LH-CGR residues have an epitope involving residues 90-165 and the immunogenic 15mer peptide (YYVFFEEQEDEIIGF), residues, 352-366. Because that peptide can decrease the stimulating TSHRAb activity of these Graves IgGs in assays with the Mc2 chimera alone, we speculate that this complex epitope may be important in an epitope spreading process involved in the formation of stimulating TSHRAbs.     

Roll forming of SMC and TMC, considering the resin-fibre interface

The principal purpose of this study is to develop a design procedure for a new roll forming process. With SMC, the advantages are reduced forming force and power consumption caused by a spherical stress tensor during compression moulding. Basic information on the deformation behaviour is obtained from a T-shaped profile using carrier type roll forming.

As the SMC is a laminate with heterogeneous properties, consideration must be given to the macroscopic and microscopic interfaces caused by resin-rich surfaces and different stiffnesses of fibre and resin. The effect of feed rate on the flow pattern is also an important problem for the fabrication of different shape products. The fabrication behaviour is investigated with relation to the interfaces in the sequent process to target areas for future development.     

THERMOELECTRICAL PROPERTIES OF Si-Ti-B IN SITU COMPOSITE PLATES PREPARED BY CHEMICAL VAPOR DEPOSITION

Highly pure, dense SiB₄ and SiB₆ plates were prepared by chemical vapor deposition (CVD) at deposition temperatures (T_DEP) from 1323 to 1773 K, total gas pressures (P_tottot) from 4 to 40 kPa and B/Si source gas ratios (m_B/SI =2B₂H₆/SiCl₄) from 0.2 to 2.6 and their thermoelectrical properties were measured. The Seebeck coefficient (S) of CVD-SiB₆ (0.7 mm in thickness), which is known to be a high temperature thermoelectric material, was 320 μVK^-1, while its electrical conductivity (s) was 7 Ω ^-1cm^-1, SiB₆ + TiB₂ and SiB₆ + SiB₄ in situ composite plates were also prepared to improve the thermoelectric property of CVD-SiB₆, The a value of the CVD-SiB₆ + 12 wt% TiB₂ in situ composite plate (0.7 mm in thickness) was one order of magnitude larger than that of CVD-SiB₆ at room temperature, while the figure of merit for the thermoelectric materials (Z) was smaller because of the smaller value of S. However, the Z value of SiBe + 40 wt% SiB₄ in situ composite plate (0.5 mm in thickness) was 10^-5, larger than that of CVD-SiB₆     

Tyrosine phosphorylation of Crk-associated substrates by focal adhesion kinase. A putative mechanism for the integrin-mediated tyrosine phosphorylation of Crk-associated substrates

Integrin-ligand binding induces the tyrosine phosphorylation of various proteins including focal adhesion kinase (pp125(FAK)) and Crk-associated substrate (Cas). FAK is activated and autophosphorylated by the ligation of integrins, although the substrate of FAK has not been revealed. We show here that p130(Cas) and Cas-L are FAK substrates. FAK directly phosphorylates Cas proteins primarily at the YDYVHL sequence that is conserved among all Cas proteins. Furthermore, the phosphorylated YDYVHL sequence is a binding site for Src family protein-tyrosine kinases, and the recruited Src family kinase phosphorylates the other tyrosine residues within Cas. The Cas-L YDYVHL sequence is phosphorylated upon integrin-ligand binding, and this integrin-mediated tyrosine phosphorylation is inhibited by the cotransfection of the FAK COOH-terminal domain that does not contain a kinase domain. These findings strongly suggest that FAK initiates integrin-mediated tyrosine phosphorylation of Cas proteins; then, Src family tyrosine kinases, which are recruited to phosphorylated Cas and FAK, further phosphorylate Cas proteins.     

A mathematical model for a continuous esterification process with recycle between terephthalic acid and ethylene glycol

A new mathematical model for a continuous recycle esterification process has been derived by basically the same procedure as the continuous process of a cascade type, reported earlier, which includes material and heat balances. Such a model can give extensive information about the optimum design of a new plant through the predictions of oligomer characteristics (concentrations of carboxyl and hydroxyl end groups, number average molecular weight, number average degree of polymerization, esterification and saponification degree, DEG content, melting point of oligomer, etc.), distillate properties (concentrations of EG and water in the vapor phase), heat transfer area, mass flow rate of heating medium, amount of heat supplied by heating medium, enthalpy moving with recycle, and amount of heat removed from each reactor. © 1992 John Wiley & Sons, Inc.     

Plasma polymerized membranes and gas permeability. II

Thin films were deposited onto porous substrates by plasma polymerization using three kinds of organosilicic compounds, tetramethylsilane (TMS), hexamethyldisiloxane (M₂), and octamethylcyclotetrasiloxane (D₄). Those composite membranes showed different characteristics of gas permeability. When D₄ was plasma-deposited onto a porous substrate, the composites membrane showed the highest oxygen permeability and the lowest oxygen-to-nitrogen permeability ratio. The composite membrane prepared from TMS showed the permeability characteristics opposite to the membrane obtained from D₄. Infrared spectrum of the polymer from D₄ resembles that of dimethylpolysiloxane. The plasma polymers from TMS and M₂ showed different profiles in Si? O absorption bands in the range 1100–1000 cm^-1 or in absorption bands of SiCH₃ groups in the range 850–750 cm^-1 from respective monomers. X-ray photoelectron spectroscopic observation indicated that all the plasma polymers contained more than two species of Si atom with different oxidation states. The greater part of Si atoms in plasma polymers took the same oxidation states in corresponding monomer. The gas permeability characteristics were closely related to the oxidation states of Si atom in the plasma polymers.     

Periodate oxidation of cellulose by homogeneous reaction

Homogeneous periodate oxidation of cellulose was achieved through methylol cellulose. The dissolution of methylol cellulose into aqueous periodate solution was followed by the gradual decomposition of methylol groups at random sites along the methylol cellulose chain. The recovery of glycol hydroxyl groups at the C₂ and C₃ positions on the glucopyranose ring during the above decomposition process caused uniform cleavage of C₂? C₃ bonds by the periodate ion. The oxidation level reached nearly 100% in 10 h. The reduced product of the resulting dialdehyde cellulose, i.e., dialcohol cellulose, resulted in mechanical properties quite different from those of conventional dialcohol cellulose. Examination of the thermal deformation and tensile properties revealed that no notable cellulose degradation occurred during the reaction. Our dialcohol cellulose gave a clear and transparent film with a flexible nature.