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The objective of this study is to achieve a fundamental understanding of polymorphic interconversion during the tableting process, including during compaction, dwell, decompression/unloading, and ejection using an in situ mechanical Raman spectroscopy. The fit-for-purpose in situ mechanical Raman spectroscopy developed herein can provide simultaneous measurement of Raman spectra and densification for the powder compacts. Chlorpropamide (CPA), an antidiabetic drug, was selected as a model pharmaceutical compound because of its mechanical shear-induced polymorphic conversions. The results confirm that CPA polymorph A (CPA-A) was transformed to CPA polymorph C (CPA-C) under different compaction stresses. We also observed that the converted polymorph CPA-C could be reverted to the CPA-A due to the elastic recovery of powder compacts as detected during dwelling and unloading. This study is the first depiction of the dynamics of CPA polymorphic interconversion during compression, dwell, unloading, and ejection. Mechanistically, this study illustrates a correlation between the change in the powder compact's relative density and polymorphic interconversion of the drug substance in different solid-state forms. The present research suggests that the process-induced polymorph conversion is a complicated dynamic process, which could be affected by the compaction pressure, the elasticity/plasticity of the material, the level of elastic recovery, and the dissipation of residual stress. In summary, this study demonstrates that the in situ mechanical Raman spectroscopy approach enables the simultaneous detection of mechanical and chemical information of the powder compact throughout the tableting process.

Wood-based materials are multifunctional green and environmentally friendly natural construction materials, and are widely used in decorative building materials. For this reason, a lot of research has been carried out to develop new and innovative wood surface improvements and make wood more appealing through features such as fire-retardancy, hydrophobicity, and antibacterial properties. To improve the performance of wood, more and more attention is being paid to the functioning of the surface. Understanding and mastering technology to improve the surface functionality of wood opens up new possibilities for developing multifunctional and high-performance materials. Examples of these techniques are ion crosslinking modification and coating modification. Researchers have been trying to make wooden surfaces more practical for the past century. This study has gradually gained popularity in the field of wood material science over the last 10 years. This paper provides an experimental reference for research on wood surface functionalization and summarizes the most current advancements in hydrophobic, antibacterial, and flame-retardant research on wood surfaces.

A novel design for thermally activated delayed fluorescence (TADF) emitters was developed by decorating dibenzofuran with four carbazole type electron donors and two CN electron withdrawing units. The four carbazole type donors were attached to one side of the dibenzofuran, and two CN units were introduced on the other side of the dibenzofuran for highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO) separation. The HOMO and LUMO were largely separated, and they were overlapped in the dibenzofuran due to aromatic nature of dibenzofuran. Two TADF emitters, DBFCzCN and DBFtCzCN, were built on the design platform decorating the dibenzofuran, and they showed high EQEs of 25.2% and 17.4% in the vacuum deposited TADF devices. Additionally, the DBFtCzCN emitter showed a high EQE of 13.9% in the solution processed TADF devices.

A newly designed ruthenium(II) complex (Ru-Se) bearing a selone moiety showed unexpected enhancement in low-oxidation-potential (LOP) electrochemiluminescence (ECL) observed at electrode potentials before the oxidation of Ru-Se in the presence of tri-n-propylamine (TPrA), which was primarily attributed to the heavy atom effect caused by the selone in Ru-Se.

We propose a novel airway segmentation method in volumetric chest computed tomography (CT) and evaluate its performance on multiple datasets. The segmentation is performed voxel-by-voxel by a 2.5D convolutional neural net (2.5D CNN) trained in a supervised manner. To enhance the accuracy of the segmented airway tree, we simultaneously took three adjacent slices in each of the orthogonal directions including axial, sagittal, and coronal and fine-tuned the parameters that influence the tree length and the number of leakage. The gold standard of airway segmentation was generated by a semi-automated method using AVIEW™. The 2.5D CNN was trained and evaluated on a subset of inspiratory thoracic CT scans taken from the Korean obstructive lung disease study, which includes normal subjects and chronic obstructive pulmonary disease patients. The reliability and further practicality of our proposed method was demonstrated in multiple datasets. In eight test datasets collected by the same imaging protocol, the percentage detected tree length, false positive rate, and Dice similarity coefficient of our method were 92.16%, 7.74%, and 0.8997 ± 0.0892, respectively. In 20 test datasets of the EXACT’09 challenge, the percentage detected tree length was 60.1% and the false positive rate was 4.56%. Our fully automated (end-to-end) segmentation method could be applied in radiologic practice.

Three novel green thermally activated delayed fluorescence (TADF) materials, (5,5′-bis(4-(9,9-dimethylacridin-10(9H)-yl)phenyl)-2,2′-bipyrimidine (22bpmAc), 10,10′-([2,5′-bipyrimidine]-2′,5-diylbis(4,1-phenylene))bis(9,9-dimethyl-9,10-dihydroacridine) (25bpmAc), and 2,2′-bis(4-(9,9-dimethylacridin-10(9H)-yl)phenyl)-5,5′-bipyrimidine (55bpmAc)) based on bipyrimidine cores as the new electron-accepting units and acridine as the electron-donating unit were designed, synthesized, and applied as green emitters in TADF devices. The TADF emitters were designed to have different nitrogen orientations in the bipyrimidine core. Two emitters, 25bpmAc and 55bpmAc, showed higher quantum efficiencies and narrower emission spectra relative to 22bpmAc. The former emitters have restricted geometry by hydrogen-bonding interactions on a central core, whereas the latter emitter does not have hydrogen bonding. The intramolecular hydrogen-bonding interaction suppressed a nonradiative mechanism in the 25bpmAc and 55bpmAc TADF e...

A high triplet energy material with the ability to suppress intermolecular interactions was synthesized as a host for a blue thermally activated delayed fluorescence (TADF) emitter for blue-shifted emission color and high quantum efficiency in solution-processed TADF organic light-emitting diodes. The host material, (5-(tert-butyl)-2-(4-(tert-butyl)phenoxy)phenyl)diphenylphosphine oxide (POBBPE), was designed to have a phenoxyphenyl core structure for high triplet energy, a diphenylphosphine oxide group for electron transport, and two tert-butyl units to prevent intermolecular interaction. Solution-processed blue TADF devices were developed using the POBBPE host and 2,3,4,5,6-penta(9H-carbazol-9-yl)benzonitrile (5CzCN) as the emitter, and a high quantum efficiency of 23.3% was achieved. In particular, the color coordinates of the solution-processed POBBPE:5CzCN devices were (0.16, 0.23), which were significantly blue-shifted compared to the color coordinates of (0.17, 0.31) from a previous 5CzCN device fabricated using a well-known bis[2-(diphenylphosphino)phenyl]ether oxide host.

The solubilities of cilostazol in aqueous solutions containing polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), polyvinylpyrrolidone K30 (PVP K30), and poly(1-vinylpyrrolidone-co-vinyl acetate) (PVP/VA) are measured at temperatures ranging from 298.15 to 318.15 K. It increased with the increase in the hydrophilic carrier concentration and temperature. PVP/VA was the most effective polymer to solubilize cilostazol. The transfer Gibbs free energy (Δ tr G °) and enthalpy (Δ tr H °) values were negative, indicating that the transfer of cilostazol from only water to an aqueous hydrophilic polymer solution is spontaneous and energetically favorable. Furthermore, the Δ tr G ° and Δ tr H ° values decreased with the increase in the hydrophilic polymer concentration, indicating that solubilization is more favorable with the increase in the hydrophilic polymer concentrations. In particular, the Δ tr G ° values considerably decreased for PVP/VA compared to PEG 4000, PEG 6000, and PVP K30. This result indicated that PVP/VA is an effective solubilizing additive for developing oral solid formulations of cilostazol.

New green thermally activated delayed fluorescence (TADF) materials built on a directly coupled dual emitting core based backbone structure were designed, synthesized, and applied as green dopants in TADF devices. An ortho-linkage between a carbazole or 3,6-di-tert-butylcarbazole donor and a triazine acceptor facilitated the TADF emission, and direct coupling of the two TADF emitting cores more than doubled the external quantum efficiency of the TADF devices. The TADF emitter based on the directly coupled dual emitting core design exhibited a green emission with a CIE coordinate of (0.23, 0.52) and a maximum external quantum efficiency of 20.8% compared with less than 10% efficiency of a conventional TADF emitter with the corresponding chemical structure.

We present a regenerative molecular sensor for biothiols where a non-fluorescent copper(II) coumarin complex (CuIIL) probe turns to a strongly fluorescent Cu(I) complex by thiol-containing amino acids (Cys, Hcy, GSH). During the recognition process, Cu(II) ion of CuIIL undergoes chemical reduction followed by substitution of the coordinating ligands with the biothiols. Interestingly, the strongly fluorescent Cu(I) complex, which quantifies the amount of the target biothiol, was oxidized back to its original CuIIL by chemical (or electrochemical) oxidation, and could be repeatedly reused as a thiol probe for several turn-overs. CuIIL was successfully applied in fluorescent imaging of the cellular GSH.

New and highly stable Eu(III) and Tb(III) complexes based on two triarylborane functionalized cyclen derivative ligands L1 and L2, have been achieved. The Eu(III) and Tb(III) lanthanide compounds have been found to display highly distinct and contrasting temperature-dependent dual emission and decay lifetimes, rendering them as potential sensitive temperature probes. The emission colors of the new lanthanide complexes can be tuned by controlling the ratio of the Eu(III) and Tb(III) complexes in a binary composite and the temperature. Bright white light emission based on the new binary Eu(III) and Tb(III) complexes has been achieved. Furthermore, the triarylborane functionality of the new complexes enables their use as effective probes for anions such as fluoride ions, allowing the further tuning of the lanthanide emission.

The aim of this study was to formulate probiotics-encapsulated pellets with hydroxypropyl methylcellulose acetate succinate (HPMCAS) using a dry powder coating technique to improve the storage stability, acid resistance, and intestinal adherence of viable bacteria (Lactobacillus acidophilus and Bifidobacteria animalis ssp. Lactis). Dry coated pellet (DCP) loaded with probiotics was optimized with respect to the quantity of the HPMCAS, an enteric coating polymer (108 mg), and the kinds and amounts of plasticizer (triethyl citrate, 15.7 mg; acetylated monoglyceride, 6.8 mg), by evaluating the survival rate of the bacteria during preparation process and in an acidic medium. Dry coating process allows the whole survivals of living bacteria during preparation process. The DCP formulation exhibited markedly higher acid tolerability and storage stability compared to uncoated viable bacteria. In an in vivo mucosal adherence study in rats, a profound colonization of viable bacteria in the small and large intestine was observed in rats receiving DCP system (p0.05) compared to rats receiving uncoated probiotics. Moreover, we found that the repeated DCP administration noticeably inhibited intestinal penetration of endotoxin, a potent inflammatory stimulant, from intestinal mucus. The novel DCP system may be an alternative approach for improving bacterial viability in the preparation process and in an acidic medium, and to promote mucosal colonization of probiotic bacteria in the human gut.

Three triarylboron- (Mes2BAr-) functionalized dipicolinic acids, namely, 4-(4-(dimesitylboranyl)-2,3,5,6-tetramethylphenyl)pyridine-2,6-dicarboxylic acid (H2L1), 4-(4-(4-dimesitylboranyl)-2,3,5,6-tetramethylphenyl)-1H-1,2,3-triazol-1-yl)pyridine-2,6-dicarboxylic acid (H2L2), and 4-(4-(4-dimesitylboranyl) phenyl)-1H-1,2,3-triazol-1-yl)pyridine-2,6-dicarboxylic acid (H2L3), have been designed and synthesized. Lanthanide(III) complexes with the general formula of [NBu4]3[LnL3] (Ln = Eu or Tb; L = L1, L2, or L3) were obtained. The new triarylboron-functionalized ligands were found to be effective in the selective sensitization of the emissions of Eu(III) and Tb(III) ions with a high quantum efficiency (e.g., 0.54 for [NBu4]3[TbL13] in the solid state) upon excitation at ∼330 nm. An intraligand charge-transfer (ILCT) transition from the mesityl or aryl group to the boron or boron-aryl unit was found to play a key role in the activation of the Eu(III) and Tb(III) emissions, based on TD-DFT computational data and luminescence titration experiments performed using fluoride and cyanide ions.

Four BMes2Ar (Mes = mesityl, Ar = phenyl or duryl) functionalized 1,3-diketonato ligands have been investigated for use in selective sensitization of Tb(III) and Eu(III) emission. These ligands have the general formula of [R1C(O)CR2C(O)R3](-) (R1 = Ph, R2 = H, R3 = p-Ph-BMes2, L1; R1 = R3 = p-Ph-BMes2, R2 = H, L2; R1 = R3 = Me, R2 = p-Ph-BMes2, L3; R1 = R3 = Me, R2 = p-duryl-BMes2, L4) and belong to class I (L1 and L2) and class II (L3 and L4), respectively. In class I, the boron unit is conjugated with the phenyl linker and the diketone backbone, while in class II, the boron unit, the linker unit, and the diketone unit are nonconjugated with a mutually orthogonal arrangement. To understand the impact of the location of the BMes2Ar unit on the electronic properties of the 1,3-diketone molecules and their ability in activating lanthanide emission, the difluoroboron chelate compounds (1-BF2 to 4-BF2) of ligands L1-L4 were synthesized and examined. The class I ligands were effective in activating Eu(III) emission, while the class II ligands were effective in activating Tb(III) emission. Four Ln(III) complexes, 1Eu, 2Eu, 3Tb, and 4Tb, based on the L1-L4 ligands, respectively, were prepared and examined. The emission quantum efficiency of 1Eu and 2Eu is low (Φ(Eu) ≤ 0.01 in THF, 0.07-0.13 in the solid state), but can be greatly enhanced by the addition of fluoride ions. In contrast, the complex 4Tb has a moderate emission efficiency (Φ(Tb) = 0.14 in THF, 0.47 in the solid state) and experiences a distinct emission quenching upon the addition of fluoride. The selective sensitization of Eu(III) and Tb(III) by L1-L4 and the distinct luminescent response of their Ln(III) complexes toward fluoride ions are caused by the distinct intraligand charge transfer transitions of the two different classes of ligands involving the BMes2 unit.

Mono complex [Cl(CO) 3 Re I ( IL-2 )](PF 6 ) and bimetallic complexes Cl(CO) 3 Re I ( IL-2 )–Ir I ( Ligand ) n Cl, where IL-2 = 1,3-dimethyl-2,3-dihydro-1H-imidazo[4,5- f ][1,10]phenanthroline-2-yl and Ligand = 1,5-cyclooctadiene ( n = 1) or carbon monoxide ( n = 2), were synthesized, characterized, and applied to react with carbon monoxide. Bis(chelating) ligand, IL-2 , has two coordinating sites, 1,10-phenanthroline and imidazolium moieties. These complexes display typical intraligand transition (π–π ∗ ) and metal-to-ligand charge-transfer (MLCT) bands in the ultraviolet and visible regions, respectively. It was demonstrated that complex Cl(CO) 3 Re I ( IL-2 )–Ir I (COD)Cl can be used as a carbon monoxide (CO) indicator because Cl(CO) 3 Re I ( IL-2 )–Ir I (CO) 2 Cl, a CO-substituted bimetallic complex, displays distinct optical behaviors compared to those of Cl(CO) 3 Re I ( IL-2 )–Ir I (COD)Cl.

Junsung Park,1,2,* Wonkyung Cho,1,2,* Hee Jun Park,1,2 Kwang-Ho Cha,1,2 Dae-Chul Ha,2,5 Youn-Woong Choi,5 Ha-Young Lee,3 Sun-Hang Cho,5 Sung-Joo Hwang1,41Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Incheon, Republic of Korea; 2College of Pharmacy, Chungnam National University, Daejeon, Republic of Korea; 3Biomaterials Laboratory, Korea Research Institutes of Chemical Technology, Daejeon, Republic of Korea; 4College of Pharmacy, Yonsei University, Incheon, Republic of Korea; 5Korea United Pharm Inc, Seoul, Republic of Korea *These authors contributed equally to this workObjectives: The purpose of this study was to observe the pharmacokinetic behavior of newly synthesized biocompatible polymers based on polyhydroxyethylaspartamide (PHEA) to be used to coat an iron oxide core to make superparamagnetic iron oxide nanoparticles (SPION).Materials and methods: The isotopes [14C] and [59Fe] were used to label the polymer backbone (CLS) and iron oxide core (FLS), respectively. In addition, unradiolabeled cold superparamagnetic iron oxide nanoparticles (SPION/ULS) were synthesized to characterize particle size by dynamic light scattering, morphology by transmission electron microscopy, and in vivo magnetic resonance imaging (MRI). CLS and FLS were used separately to investigate the behavior of both the synthesized polymer and [Fe] in Sprague Dawley (SD) rats, respectively. Because radioactivity of the isotopes was different by β for CLS and γ for FLS, synthesis of the samples had to be separately prepared.Results: The mean particle size of the ULS was 66.1 nm, and the biodistribution of CLS concentrations in various organs, in rank order of magnitude, was liver > kidney > small intestine > other. The biodistribution of FLS concentrations was liver > spleen > lung > other. These rank orders show that synthesized SPION mainly accumulates in the liver. The differences in the distribution were caused by the SPION metabolism. Radiolabeled polymer was metabolized by the kidney and excreted mainly in the urine; [59Fe] was recycled for erythrocyte production in the spleen and excreted mainly in the feces. The MR image of the liver after intravenous injection demonstrated that [Fe] effectively accumulated in the liver and exhibited high-contrast enhancement on T2-weighted images.Conclusion: This newly synthesized, polymer-coated SPION appears to be a promising candidate for use as a liver-targeted, biocompatible iron oxide MR imaging agent.Keywords: SPION, radiolabeled, polyhydroxyethylaspartamide, pharmacokinetic, liverCorrigendum for this paper has been published

Palpation techniques are widely used in medical procedures to detect the presence of lumps or tumors in the soft breast tissues. Since these procedures are very subjective and depend on the skills of the physician, it is imperative to perform detailed a scientific study in order to develop more efficient medical sensors to measure and generate palpation parameters. In this research, we propose an optical-based, artificial palpation sensor for lesion characterization. This has been developed using a multilayer polydimethylsiloxane optical waveguide. Light was generated at the critical angle to reflect totally within the flexible and transparent waveguide. When a waveguide was compressed by an external force, its contact area would deform and cause the light to scatter. The scattered light was captured by a high-resolution camera and saved as an image format. To test the performance of the proposed system, we used a realistic tissue phantom with embedded hard inclusions. The experimental results show that the proposed sensor can detect inclusions and provide the relative value of size, depth, and Young’s modulus of an inclusion.

Larch bark was liquefied in the presence of phenol and the obtained liquefied resultant was reacted with formaldehyde to prepare the liquefied bark-modified phenol formaldehyde resin (BPF) in an attempt to apply for preparing straw boards. The dynamic wettability of the BPF resin was evaluated on the surfaces of rice straw; either on the alkali solution treated or untreated rice straw surfaces. A new wetting model was employed to quantify the resins’ penetration performances using the spreading–penetration parameters (K value) as a constant to characterize penetration rate. The bigger the K value was, the stronger the penetration and spreading capacity was. Moreover, the curing kinetics of the BPF resin was also investigated with dynamic differential scanning calorimetry. The results showed that the K value of BPF resin was the highest, followed by those of BPF mixed with polymethylene diphenyl diisocyanate PMDI resin and conventional phenol formaldehyde (PF) resin, indicating that the BPF resin had the best wettability. The activation energy of BPF was close to that reported for wood/phenol/formaldehyde resins, but was higher than that of PF resin. The curing reaction was almost complete at 40 % conversion.

Ru(II) complexes 1–3 bearing various N-heterocyclic carbene (NHC) ligands were synthesized, and their photophysical, electrochemical, and electrogenerated chemiluminescence (ECL) properties were discussed to evaluate a potential of their use as multicolor ECL labels. Interestingly, they exhibited ECL emission ranging from greenish-yellow to red both in nonaqueous and mixed aqueous solutions, which might show the potential of the Ru(II) complexes as multicolor ECL labels.

A series of mono-Ru II and di-nuclear complexes, [ Ru II –M I (COD)Cl and Ru II –M I (CO) 2 Cl ] (M = Ir, Rh), have been prepared by using a bridging ligand, 1,3-dibutyl-2,3-dihydro-1H-imidazo[4,5- f ][1,10]phenanthroline-2-yl ( IL ). This bridging ligand consists of 1,10-phenanthroline and N-heterocyclic carbene (NHC) and has two coordinating sites which can bind two different metals. The complexes synthesized have been fully characterized by 1 H NMR, 13 C NMR, high resolution mass spectrometry (HRMS), elemental analysis, and X-ray crystallography in one case. These complexes exhibited typical π–π ∗ and metal-to-ligand charge transfer (MLCT) bands in the UV and visible regions, respectively. Compounds Ru II –Ir I (CO) 2 Cl and Ru II –Rh I (CO) 2 Cl have the stronger emission intensities and the longer luminescence lifetimes ( τ ) than those of Ru II –Ir I (COD)Cl and Ru II –Rh I (COD)Cl , respectively. Complex Ru II –Ir I (COD)Cl was applied to detect carbon monoxide.

Sulfuretin, a flavonoid isolated from heartwood of Rhus verniciflua, has been reported to have anti-cancer activities but the underlying molecular mechanism was not clear. In this study, sulfuretin induced apoptosis by activating caspases-8, -9, and -3 as well as cleavage of poly(ADP-ribose) polymerase. Furthermore, treatment with sulfuretin caused mitochondrial dysfunctions, including the loss of mitochondrial membrane potential (ΔΨ(m)), the release of cytochrome c to the cytosol, and the translocations of Bax and tBid. Sulfuretin also activated the extrinsic apoptosis pathway, that is, it increased the expressions of Fas and FasL, the activation of caspase-8, and the cleavage of Bid. Furthermore, blocking the FasL-Fas interaction with NOK-1 monoclonal antibody prevented the sulfuretin-induced apoptosis. The therapeutical effect of sulfuretin in leukemia is due to its potent apoptotic activity through the extrinsic pathway driven by a Fas-mediated caspase-8-dependent pathway.

Miscanthus sacchariflorus straw was used as a raw material for the manufacture of Miscanthus–wood particle composite board with Douglas-fir particles in ratios of 100/0, 80/20, 60/40, 40/60, 20/80, and 0/100. A commercial phenol–formaldehyde resin was used as a binder at 9 and 11 % for target densities of 0.50 and 0.65 g/cm3, respectively. The effects of the Miscanthus/wood particle ratio on the composite board properties were investigated. In addition, the density profile was also examined to improve the understanding of the composite board manufacturing process. Results indicate that the internal bonding value increased drastically in the board containing up to 50 % wood particles, providing a valuable parameter for subsequent research. The board properties were greatly improved with increasing density and binder addition level.

Microcrystals of megestrol acetate (MA), a poorly water-soluble drug, were successfully prepared using an antisolvent precipitation technique for improving the dissolution rate. The effective hydrophilic polymers and surfactants used were screened for their abilities to produce smaller particle sizes. Raw micronized MA and processed MA microcrystals were ranked by the Student-Newman-Keuls test in order of increasing particle size and SPAN values as follows: processed MA microcrystals in the presence of polymer and surfactant (mean diameter 1048nm)

The objective of the study was to prepare amorphous atorvastatin hemi-calcium using spray-drying and supercritical antisolvent (SAS) process and evaluate its physicochemical properties and oral bioavailability. Atorvastatin hemi-calcium trihydrate was transformed to anhydrous amorphous form by spray-drying and SAS process. With the SAS process, the mean particle size and the specific surface area of amorphous atorvastatin were drastically changed to 68.7+/-15.8nm, 120.35+/-1.40m2/g and 95.7+/-12.2nm, 79.78+/-0.93m2/g from an acetone solution and a tetrahydrofuran solution, respectively and appeared to be associated with better performance in apparent solubility, dissolution and pharmacokinetic studies, compared with unprocessed crystalline atorvastatin. Oral AUC0-8h values in SD rats for crystalline and amorphous atorvastatin were as follow: 1121.4+/-212.0ngh/mL for crystalline atorvastatin, 3249.5+/-406.4ngh/mL and 3016.1+/-200.3ngh/mL for amorphous atorvastatin from an acetone solution and a tetrahydrofuran solution with SAS process, 2227.8+/-274.5 and 2099.9+/-339.2ngh/mL for amorphous atorvastatin from acetone and tetrahydrofuran with spray-drying. The AUCs of all amorphous atorvastatin significantly increased (P

The Pd(PPh3)4-catalyzed decarboxylation of buta-2,3-dienyl 2'-alkynoates allows the rapid construction of 2-alkynyl buta-1,3-dienes. The carbon-carbon bond-forming reaction occurs at the central position of an allene moiety.

The purpose of this study was to develop and optimize oral controlled-release formulations for tamsulosin hydrochloride using a combination of two cellulose ester derivatives, hydroxypropyl methylcellulose (HPMC) and hydroxypropyl methylcellulose phthalate (HPMCP), with Surelease as a coating material. A three-factor, three-level Box-Behnken design was used to prepare systematic model formulations, which were composed of three formulation variables, the content of HPMC (X(1)) and HPMCP (X(2)) and the coating level (X(3)), as independent variables. The response surface methodology (RSM) and multiple response optimization utilizing the polynomial equation were used to search for the optimal coating formulation with a specific release rate at different time intervals. The drug release percentages at 2, 3 and 5h were the target responses and were restricted to 15-30% (Y(1)), 50-65% (Y(2)) and 80-95% (Y(3)), respectively. The optimal coating formulation was achieved with 10% HPMC and 20% HPMCP at a coating level of 25%, and the observed responses coincided well with the predicted values from the RSM optimization technique. The drug release from pellets coated with the optimized formulation showed a controlled-release pattern (zero-order), in comparison with a commercial product (Harunal capsule). In conclusion, a novel, oral, controlled-release delivery system for tamsulosin hydrochloride was successfully developed by incorporating HPMC and HPMCP as coating additives into Surelease aqueous ethylcellulose dispersion.

In the present study, the practically insoluble drug, simvastatin (SV), and its inclusion complex with hydroxypropyl beta-cyclodextrin (HP-beta-CD) prepared using supercritical antisolvent (SAS) process were investigated to improve the aqueous solubility and the dissolution rate of drug, thus enhancing its bioavailability. Inclusion complexation in aqueous solution and solid state was evaluated by the phase solubility diagram, differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD), Fourier-transform infrared spectroscopy (FT-IR) and scanning electron microscopy (SEM). The phase solubility diagram with HP-beta-CD was classified as A(L)-type at all temperatures investigated, indicating the formation of 1:1 stoichiometric inclusion complex. The apparent complexation constants (K(1:1)) calculated from phase solubility diagram were 774, 846 and 924 M(-1) at 25, 37 and 45+/-0.5 degrees C, respectively. No endothermic and characteristic diffraction peaks corresponding to SV was observed for the inclusion complex in DSC and PXRD. FT-IR study demonstrated the presence of intermolecular hydrogen bonds between SV and HP-beta-CD in inclusion complex, resulting in the formation of amorphous form. Aqueous solubility and dissolution studies indicated that the dissolution rates were remarkably increased in inclusion complex, compared with the physical mixture and drug alone. Moreover, SV/HP-beta-CD inclusion complex performed better than SV in reducing total cholesterol and triglyceride levels. This could be primarily attributed to the improved solubility and dissolution associated with inclusion complex between drug and HP-beta-CD. In conclusion, SAS process could be a useful method for the preparation of the inclusion complex of drug with HP-beta-CD and its solubility, dissolution rate and hypolipidemic activity were significantly increased by complexation between SV and HP-beta-CD.

The effect of compatibilizing agents on mechanical properties and morphology of a lignocellulosic material-thermoplastic polymer composite was examined. Using rice-husk flour as the reinforcing filler and polypropylene as the thermoplastic matrix polymer, a particle-reinforced composite was prepared, and its mechanical and morphological properties examined as a function of the amount of compatibilizing agent used. In the sample preparation, four levels of filler loading (10, 20, 30 and 40 wt%) and three levels of compatibilizing agent content (1, 3 and 5 wt%) were used, and in the tensile test, six test temperatures (−30, 0, 20, 50, 80 and 110 °C) and five crosshead speeds (2, 10, 100, 500 and 1500 mm/min) were used. The tensile strengths of the composites decreased as the filler loading increased, but the tensile properties were significantly improved with the addition of the compatibilizing agent. Both the notched and unnotched Izod impact strengths were almost the same with the addition of compatibilizing agent. A morphological study revealed that the positive effect of compatibilizing agent on interfacial bonding.

The supercritical antisolvent (SAS) process was used to modify solid state characteristics of fluconazole. Fluconazole was recrystallized at various temperatures (60-80 degrees C) and pressures (8-16MPa) using dichloromethane (DCM) as a solvent. Acetone and ethanol were also employed as solvents. The fluconazole polymorphs prepared by the SAS process were characterized by differential scanning calorimetry (DSC), thermogravimetry analysis (TGA), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FT-IR) and scanning electron microscopy (SEM). Furthermore, the equilibrium solubility of the samples in aqueous solution was determined. Fluconazole anhydrate form I was obtained at low temperature (40 degrees C) and anhydrate form II was obtained at high temperature (80 degrees C). The variation of pressure during the SAS process may influence the preferred orientation. Anhydrate forms I and II were also obtained using various solvents. Therefore, it was shown that solid state characteristics of fluconazole, including the polymorphic form and preferred orientation, can be controlled by changing operating conditions of the SAS process such as temperature, pressure, and solvent.

To determine certain physical properties, viz. the thickness swelling and water absorption, and mechanical properties, viz. the tensile strength and Izod impact strength, of lignocellulosic filler reinforced polyolefin bio-composites, polyolefin was used as the matrix polymer and rice-husk flour as the reinforcing filler. Wood flour was also used as a reinforcing filler, and commercial particleboard, medium-density fiberboard and solid woods (red pine and birch) were also included in this study, in order to obtain comparative water absorption behavior measurements. Test samples were prepared, in order to determine the physical and mechanical properties of the bio-composites as a function of filler loading and according to filler type as well as with respect to the thermoplastic polymer itself. The thickness swelling and water absorption of the bio-composites slightly increased as the filler loading increased, but to a negligible extent as compared with the wood-based composites (particleboard and fiberboard) and the solid woods (red pine and birch). The mechanical properties of the composites decreased as the filler loading increased, but the composites had an acceptable strength level. It was concluded that these bio-composites are suitable to be used for the interior of bathrooms, wood decks, food packaging, etc.

Hepatoprotective effects of momordin Ic and oleanolic acid obtained from Kochiae Fructus (KF), the fruit of a traditional Oriental medicinal plant, were evaluated against carbon tetrachloride (CCl4)-induced liver damage in rats. Male Sprague-Dawley rats were divided into four groups: control, CCl4-treated, CCl4 plus momordin Ic-treated (MMDIc-CCl4), and CCl4 plus oleanolic acid-treated (OAA-CCl4). Momordin Ic (30 mg/kg of body weight) and oleanolic acid (30 mg/kg of body weight) were orally administered once a day for 14 days. A mixture of 0.2 mL/100 g of body weight of CCl4 in olive oil (1:1, vol/vol) was injected 30 minutes after the final administration of momordin Ic and oleanolic acid. The momordin Ic and oleanolic acid pretreatments resulted in significantly lower serum transaminase, lactic dehydrogenase, and gamma-glutamyltransferase levels in the CCl4-treated rats. The CCl4-treated rats had significantly lower activities of glutathione, glutathione reductase, glutathione S-transferase, superoxide dismutase, catalase, and glutathione peroxidase. However, pretreatment with momordin Ic and oleanolic acid reduced the effect of CCl4 and helped maintain levels of the enzymes. Pretreatment with momordin Ic and oleanolic acid resulted in significantly lower production of aminopyrine N-demethylase and aniline hydroxylase in the CCl4-treated rats. Pretreatment with momordin Ic resulted in lower catalase and aminopyrine N-demethylase activity induction by CCl4, towards normalization. Momordin Ic and oleanolic acid obtained from KF appear to contribute to alleviating the adverse effects of CCl4 treatment by enhancing the hepatic antioxidant defense system.

We develop an optimal task allocation and scheduling algorithm which minimizes the computing period for multiprocessor systems with general network structures considering task execution time and communication contentions and routing delays explicitly. We presented new ideas of scheduling: (i) individual start allowing overlapping two different iterations, (ii) the scheduling space and the scheduling graph representing feasible schedules, and (iii) the check-and-diffusion algorithm utilizing property of the start-time difference vs. the computing period. With concrete examples of scheduling spaces, segments, and schedules for various multiprocessor network architectures, we showed that individual start reduces the computing period, and our algorithm can find the optimal computing period without exhaustive search.

To determine the possibility of using lignocellulosic materials as reinforcing fillers in the thermoplastic polymer composite, polypropylene as the matrix and rice-husk flour as the reinforcing filler were used to prepare a particle-reinforced composite in order to determine testing data for the physical, mechanical and morphological properties of the composite according to the filler loading in respect to thermoplastic polymer. In the sample preparation, four levels of filler loading (10, 20, 30 and 40 wt.%) were designed. In the tensile test, six levels of test temperature (−30, 0, 20, 50, 80 and 110 °C) and five levels of crosshead speed (2, 10, 100, 500 and 1500 mm/min) were designed. Tensile strengths of the composites slightly decreased as the filler loading increased. Tensile modulus improved with increasing filler loading. Notched and unnotched Izod impact strengths were lowered by the addition of rice-husk flour. The composite became brittle at higher crosshead speed, and showed plastic deformation with increasing test temperature.

We present a practical and systematic strategy for measuring machine intelligence quotient (MIQ) of human-machine cooperative systems. So far, much research related to intelligent control has been established, but the issues about definition and measurement of machine intelligence are not yet clearly formulated. We propose the intelligence task graph (ITG) as a modeling and analysis tool. By using the ITG, the machine contribution of human-machine cooperative systems can be explicitly separated from the human contribution and directly formulated by equations. Thus, the ITG is a very useful modeling tool for estimating the MIQ that was introduced as the index of machine intelligence. We propose a new human-oriented method for estimating the MIQ. This research will help engineers assess intelligent machines that are designed to perform human-like qualities with a high degree of autonomy.

The objectives of this study were to investigate the effects of hydrophilic polymer on the supersaturation and oral absorption of amorphous atorvastatin calcium. Solid dispersions of atorvastatin calcium were prepared by a supercritical antisolvent (SAS) process. The solid dispersion with polyvinylpyrrolidone vinyl acetate (PVP VA64) achieved a higher degree and extent of supersaturation than the dispersions prepared with water-soluble polymers such as hydroxypropylmethyl cellulose (HPMC) and polyvinylpyrrolidone (PVP K30). The absorption of atorvastatin in rats was markedly increased when atorvastatin was orally administered in a PVP VA64 solid dispersion due to enhanced supersaturation and dissolution properties. Therefore, the oral absorption of atorvastatin calcium increased with the degree of supersaturation of solid dispersions prepared using an SAS process.

The aim of this study was to investigate the effects of micronization and amorphorization of cefdinir on solubility and dissolution rate. The amorphous samples were prepared by spray-drying (SD) and supercritical anti-solvent (SAS) process, respectively and their amorphous natures were confirmed by DSC, PXRD and FT-IR. Thermal gravimetric analysis was performed by TGA. SEM was used to investigate the morphology of particles and the processed particle had a spherical shape, while the unprocessed crystalline particle had a needle-like shape. The mean particle size and specific surface area were measured by dynamic light scattering (DLS) and BET, respectively. The DLS result showed that the SAS-processed particle was the smallest, followed by SD and the unprocessed cefdinir. The BET result was the same as DLS result in that the SAS-processed particle had the largest surface area. Therefore, the processed cefdinir, especially the SAS-processed particle, appeared to have enhanced apparent solubility, improved intrinsic dissolution rate and better drug release when compared with SD-processed and unprocessed crystalline cefdinir due not only to its amorphous nature, but also its reduced particle size. Conclusions were that the solubility and dissolution rate of crystalline cefdinir could be improved by physically modifying the particles using SD and SAS-process. Furthermore, SAS-process was a powerful methodology for improving the solubility and dissolution rate of cefdinir.