Formulation study for lansoprazole fast-disintegrating tablet. III. Design of rapidly disintegrating tablets

Lansoprazole fast-disintegrating tablets (LFDT) are a patient-friendly formulation that rapidly disintegrates in the mouth. LFDT consist of enteric-coated microgranules (mean particle size, approximately 300 microm) and inactive granules. In the design of the inactive granules, mannitol was used as a basic excipient. Microcrystalline cellulose, low-substituted hydroxypropyl cellulose (L-HPC), and crospovidone were used as binders and disintegrants. A new grade of L-HPC (L-HPC-33), with a hydroxypropoxy group content of 5.0-6.9%, was developed and it has no rough texture due to a decrease in water absorption. It was clarified that L-HPC-33 could be useful as a binder and disintegrant in rapidly disintegrating tablets. LFDT contain enteric-coated microgranules in tablet form. The enteric-coated microgranule content in LFDT affect qualities such as tensile strength, disintegration time in the mouth, and dissolution behavior in the acid stage and in the buffer stage of LFDT. The 47.4% content of the enteric-coated microgranules was selected to give sufficient tensile strength (not less than 30 N/cm(2)), rapid disintegration time in the mouth (not more than 30 s), and dissolution behavior in the acid stage and buffer stage similar to current lansoprazole capsules. Compression force affected the tensile strength and the disintegration time in the mouth, but did not affect the dissolution behavior in the acid and buffer stages.     

Towards identification of traditional European and indigenous Australian paint binders using pyrolysis gas chromatography mass spectrometry

We report a pyrolysis GC–MS method capable of analysing Indigenous Australian and European binders typically used in the manufacture of culturally important painted works. Eleven different traditional European binders and ten different Indigenous Australian binders were examined. The method allows discrimination between highly complex and impure lipid, resin, polysaccharide, wax, and protein-based binders. Each was found to have characteristic pyrolysis products that were unique to the binder material, demonstrating the potential for differentiation of these binders on Australian Aboriginal artworks towards identification and conservation of cultural heritage.     

GC-MS characterization of proteinaceous and lipid binders in UV aged polychrome artifacts

This paper presents the most significant results obtained from the characterization of protein and lipid binders in a broad range of reference paint materials prepared and stored at Opificio delle Pietre Dure in Florence (Italian Ministry of the Cultural Heritage, Italy). The amino acid distribution for protein binders and the fatty acid distribution for lipid binders were determined by gas chromatography-mass spectrometry before and after being artificially aged through exposure to UV light at 254 nm or 366 nm for different time periods in a climatic chamber (20°C and 80% RH). The results were compared with those relevant to old paintings of different ages, and showed that UV light aging does not significantly affect the amino acid profile of protein binders. Consequently, protein binders in old paintings can be reliably identified by comparing the amino acid composition with that of reference paint materials which have not been aged. However, the composition of lipid binders is substantially affected by UV irradiation, leading to a lowering of oleic acid and the formation of azelaic acid and other dicarboxylic acids including oxalic acid. An oleic to stearic acid ratio of less than 0.5 was observed in all the samples of works of art, and this parameter can be used to evaluate the extent of the artificial aging process. The formation of oxalic acid was also observed starting with pure unsaturated fatty acids, thus supporting the chemical origin of oxalate patina.     

The organization of the surface of multicomponent plasma-electrolytic anode layers on aluminum

The elemental composition of characteristic formations on the surface of anodic films containing transition metal compounds (Ni, Cu, Co, Mn, and W) and formed on an aluminum alloy in aqueous electrolytes under the conditions of the action of electric spark and arc discharges (plasma-electrolytic or plasmaelectrochemical oxidation) was studied. The main formations on the surface were fritted structures, pores, caverns covered by “lids” on top, and disperse particles (microgranules). Electrolyte transition metals largely concentrated in caverns, pores, and microgranules. The composition of microgranules was different from that of caverns, pores, and fritted structures. The main elements that formed microgranules were nickel and carbon. Cobalt and manganese were differently built into surface formations. Cobalt replaced nickel in micro-granules, and manganese replaced aluminum in fritted surface structures.     

Facile synthesis of benzobisimidazole and bibenzimidazole-based bisnitriles as potential precursors for DNA minor groove binders

The synthesis of bisnitrile derivatives of benzobisimidazole and bibenzimidazole in a good yield is described in detail for the first time. Nucleophilic substitution of 1,5-difluoro-2,4-dinitrobenzene using different amines produced the intermediate diamines that were reduced using sodium borohydride/Pd(C) to produce the tetramines. These tetramines were allowed to couple with different aldehydes to produce the final benzimidazoles. In a different investigation, these bisnitrile derivatives will be used to make benzimidazole diamidines that could be used as potential mixed sequence minor groove binders.     

Formulation study for lansoprazole fast-disintegrating tablet. II. Effect of triethyl citrate on the quality of the products

The purpose of this study was to develop enteric-coated microgranules for the lansoprazole fast-disintegrating tablet (LFDT), which is a rapidly disintegrating tablet containing enteric-coated microgranules. In our previous study, it was clarified that sufficient flexibility of the enteric layer was achieved by the optimized combined ratio of methacrylic acid copolymer dispersion to ethyl acrylate-methyl methacrylate copolymer dispersion and adding the optimized concentration of triethyl citrate to reduce the damage during the compression process. However, since triethyl citrate has an unpleasant bitter taste and is especially incompatible with lansoprazole, it adversely affects the taste and stability of lansoprazole in the enteric-coated microgranules. The enteric layer containing macrogol 6000 was proven useful to improve the unpleasant bitter taste and stability of lansoprazole, because macrogol 6000 does not have an unpleasant bitter taste and is more compatible than triethyl citerate. By covering the inner (first enteric layer) and outer side (third enteric layer) of the enteric layer containing triethyl citrate (second enteric layer) with the enteric layer containing macrogol 6000, we resolved the stability problem of lansoprazole and the unpleasant bitter taste. Finally, we developed enteric-coated microgranules comprising seven layers: 1) core, 2) active compound layer, 3) intermediate layer, 4) first enteric layer, 5) second enteric layer, 6) third enteric layer, and 7) over coating layer. The enteric-coated microgranules have the multiple functions of reducing the damage to the enteric layer during the compression process, improving the stability of lansoprazole, and masking the unpleasant bitter taste.     

Physico-chemical characterization of protein-pigment interactions in tempera paint reconstructions: casein/cinnabar and albumin/cinnabar

In this work, we characterized paint reconstructions using ovalbumin and casein as binders, and cinnabar (HgS) as a pigment, before and after artificial ageing. Egg and casein are common paint binders that were used historically in the technique of tempera painting. Despite extensive research on the identification of proteinaceous binders in paintings, there is a substantial lack of knowledge regarding the ageing pathway of their protein content, and their chemical interaction with inorganic pigments. Thermogravimetric analysis, infrared spectroscopy and size-exclusion chromatography (SEC) were used to reveal the physico-chemical processes involved in the ageing of proteins in paintings. Taken together, the three techniques highlighted that proteins are subject to both cross-linking and hydrolysis upon ageing, and to a lesser extent, to oxidation of the side chains. Mercury–protein interactions were also revealed using a cold vapour generation atomic fluorescence spectrometer mercury-specific detector coupled to SEC. The study clearly showed that HgS forms stable complexes with proteins and acts as a sensitizer in cross-linking, hydrolysis and oxidation.     

Influence of catalyst binder on the acidity and activity/selectivity of Ga/H-ZSM-5 zeolite in propane aromatization

The acidity and initial and time-on-stream activity in propane aromatization (at 550°C, space velocity of 3100 cm³g⁻¹ _(zeolite)h⁻¹) of Ga-impregnated H-ZSM-5 zeolite without or with binders (50 wt%), such as silica, alumina and kaolin, have been investigated. Both the acidity and catalytic activity of the zeolite are influenced by the presence of binder in the catalyst, depending upon the binder. The influence is found to be lowest for alumina and highest for kaolin. Among the binders, alumina is the most preferred binder for the zeolite catalyst.     

Gas chromatography/mass spectrometry of oils and oil binders in paintings

A GC/MS procedure has been developed, optimized, and applied to characterization of oil binders in paintings. The procedure involves hydrolysis of lipids to fatty acids (FAs) and derivatization of FAs to fatty acid methyl esters (FAMEs) by a solution of sodium methanolate in methanol at an elevated temperature. FAMEs are analyzed by temperature-programed GC followed by full-scan MS. Old and dried samples are subjected to extraction of nonpolymerized FAMEs into dichloromethane prior to hydrolysis. The method provides a good repeatability of results and has been applied to the characterization of common plant oils used in paintings, to commercial oil and tempera paints, to model painting samples, and to samples taken from real paintings. The fresh oils and binders can readily be identified and characterized. The ratio of the methyl esters of palmitic and stearic acids can be used to characterize oil binders in old works of art.     

Rheology of polyacrylate binders produced via catalytic chain transfer polymerization as an alternative to bitumen in road pavement materials

Catalytic chain transfer polymerization has been successfully used to produce a range of methyl acrylate (MA) and butyl acrylate (BA) synthetic polymers of specific, targeted molecular weights, with polydispersity index values in the range of 2–4.5. The rheological properties of a subgroup of these synthetic binders consisting of four MA homo-polymers and one MA–BA co-polymer were then determined by means of oscillatory testing using a dynamic shear rheometer (DSR). The rheological tests consisted of a combination of stress/strain amplitude and frequency sweeps using a standard 8 mm diameter parallel plate testing geometry. The rheological parameters of phase angle and complex, storage and loss moduli were then shifted to form master curves at a reference temperature of 25 °C and isochronal plots at 0.1, 1 and 10 Hz. The rheological properties of the synthetic polymers were also compared to those of standard road pavement bitumens. The results show that it is possible to produce a range of synthetic polyacrylates with different rheological responses by altering the reactant type, reactant concentration and polymerization conditions to match the rheological properties of road bitumens. All the polyacrylate binders showed a similar rheological profile with a unique viscoelastic response as represented by the phase angle master curves together with an upper limiting stiffness and intermediate temperature/frequency ‘plateau’ region as shown in the complex modulus master curves. The results of the rheological examination of the binders showed that the key material property that influenced the performance of the polyacrylates in these specific application tests was glass transition temperature rather than molecular weight. Over this range of investigated molecular weights, it is the ratio between the two polymers which determines the glass transition and as such determines the material properties. These findings suggest that such sustainably sourced polyacrylate binders may allow for a move from petrochemical feed stocks to be made and allow for targeted road pavement design based on local climates, offering improved mechanical robustness.     

HIV-1 protease inhibitors from inverse design in the substrate envelope exhibit subnanomolar binding to drug-resistant variants

The acquisition of drug-resistant mutations by infectious pathogens remains a pressing health concern, and the development of strategies to combat this threat is a priority. Here we have applied a general strategy, inverse design using the substrate envelope, to develop inhibitors of HIV-1 protease. Structure-based computation was used to design inhibitors predicted to stay within a consensus substrate volume in the binding site. Two rounds of design, synthesis, experimental testing, and structural analysis were carried out, resulting in a total of 51 compounds. Improvements in design methodology led to a roughly 1000-fold affinity enhancement to a wild-type protease for the best binders, from a Ki of 30-50 nM in round one to below 100 pM in round two. Crystal structures of a subset of complexes revealed a binding mode similar to each design that respected the substrate envelope in nearly all cases. All four best binders from round one exhibited broad specificity against a clinically relevant panel of drug-resistant HIV-1 protease variants, losing no more than 6-13-fold affinity relative to wild type. Testing a subset of second-round compounds against the panel of resistant variants revealed three classes of inhibitors: robust binders (maximum affinity loss of 14-16-fold), moderate binders (35-80-fold), and susceptible binders (greater than 100-fold). Although for especially high-affinity inhibitors additional factors may also be important, overall, these results suggest that designing inhibitors using the substrate envelope may be a useful strategy in the development of therapeutics with low susceptibility to resistance.     

Fingerprinting of egg and oil binders in painted artworks by matrix-assisted laser desorption ionization time-of-flight mass spectrometry analysis of lipid oxidation by-products

A matrix-assisted laser desorption ionization time-of-flight mass spectrometry-based approach was applied for the detection of various lipid classes, such as triacylglycerols (TAGs) and phospholipids (PLs), and their oxidation by-products in extracts of small (50–100 μg) samples obtained from painted artworks. Ageing of test specimens under various conditions, including the presence of different pigments, was preliminarily investigated. During ageing, the TAGs and PLs content decreased, whereas the amount of diglycerides, short-chain oxidative products arising from TAGs and PLs, and oxidized TAGs and PLs components increased. The examination of a series of model paint samples gave a clear indication that specific ions produced by oxidative cleavage of PLs and/or TAGs may be used as markers for egg and drying oil-based binders. Their elemental composition and hypothetical structure are also tentatively proposed. Moreover, the simultaneous presence of egg and oil binders can be easily and unambiguously ascertained through the simultaneous occurrence of the relevant specific markers. The potential of the proposed approach was demonstrated for the first time by the analysis of real samples from a polyptych of Bartolomeo Vivarini (fifteenth century) and a “French school” canvas painting (seventeenth century).     

Identification of lysophosphatidylcholine (LPC) and platelet activating factor (PAF) from PC12 cells and mouse cortex using liquid chromatography/multi-stage mass spectrometry (LC/MS3)

Lipids play essential roles in cellular structural support, energy storage and signal transduction. Recently, mass spectrometry (MS) has been used to produce three-dimensional maps that elucidate the lipid composition of complex cellular lysates. The identification of individual lipids within these maps is slow and requires the synthesis and spiking of each candidate lipid. We present a novel MS-based technique that rapidly elucidates the atomic connectivity of the fatty acid/alcohol substituent on the sn-1 position of several different families of glycerophosphocholine-containing lipids within the confines of a chromatographic separation. Sodiated lipid species were fragmented to produce radical cations which lost successive methylene groups upon further collisional activation to reveal the identity of the parent molecule. This approach was demonstrated to be effective on isobaric members of the lysophosphatidylcholine (LPC) and platelet activating factor (PAF) families of glycerophospholipids. We demonstrate the application of this technique to unambiguously identify these species within complex cellular lysates and tissue extracts.     

EFFECTS OF BINDERS ON THE PRODUCTION OF LIGHT ALKENES FROM SYNGAS OVER K-Fe-MnO/SILICALITE-2 CATALYST I. EFFECT OF VARIOUS BINDERS ON CO HYDROGENATION

The performance of the K-Fe-MnO/Si-2 catalyst for the production of light olefins via Co hydrogenation changes obviously with the addition of binders. The results of CO hydrogenation. TPR, Mossbauer spectra CI0TPF, CO/H2-TPSR and C2H4/H2-TPSR are employed to investigate the effects of various binders on the physical-chemical states and catalytic behaviors of K-Fe-MnO/Si-2 catalyst to produce light olefins via syngas, TiO2 can promote the reduction of Fe and strengthen the adsorption of CO resulting in raising olefin selectivity. Other binders such as Al2O3, SiO2, MgO, once added into the catalyst, may cause formation of inorganic salts between FeO and Binders leading to a decrease of Fe reduction and a loss of olefin selectivity for CO hydrogenation. Especially, For K-Fe-MnO/Si-2 catalyst with Al2O3 binder directly, the strong secondary reactions of ethylene during CO hydrogenation cause a very poor light olefin selectivity, which will be improved greatly by modifying Al2O3.     

Morphology and photoelectrochemical properties of TiO2 electrodes prepared using functionalized plant oil binders

Chemically functionalized plant oils, viz. acrylated epoxidized soybean oil (AESO) and maleinized acrylated epoxidized soybean oil (MAESO), were used as bio-based binders for the TiO₂ electrodes of dye-sensitized solar cells (DSSC). The surface roughness and number of appropriate pores were increased in the TiO₂ films prepared using the plant oil binders in comparison with the film prepared using polyethylene glycol (PEG), due to the larger number of functionalities. The short circuit photocurrent (I_SC) and open circuit photovoltage (V_OC) were increased, and the conversion efficiency was significantly improved, in the cell using the plant oil binders.     

Kinetics of the sorption of metal ions from sea water on clinoptilolite

Based on a study of the sorption kinetics of metal ions from sea water onto granular clinoptilolite and powdered clinoptilolite incorporated into a grain of a highly permeable inert support it has been shown that the rate of the sorption processes is limited principally by diffusion in the microgranules of zeolite. For the Tedzami clinoptilolite studied the characteristic dimensions of the microgranules are 15–20 m and are commensurate with the dimensions of microcrystals determined independently.Translated from Izvestiya Akademii Nauk SSSR, Seriya Khimicheskaya, No. 2, pp. 263–267, February, 1990.We thank E. V. Venetsianov, L. S. Kamenetskii and M. V. Veksler for assistance in the investigation.     

Diminishing hazardous air pollutant emissions from pyrolysis of furan no-bake binders using methanesulfonic acid as the binder catalyst

The formation of hazardous air pollutants (HAPs) in thermal decomposition of furan no-bake foundry binders was investigated using analytical pyrolysis techniques. Two furan binders cured with p-xylenesulfonic acid (conventional acid catalyst used in foundries) and methanesulfonic acid (alternative catalyst proposed for diminishing HAPs) were flash pyrolyzed in a Curie-point pyrolyzer at 920 °C and slowly pyrolyzed in a thermogravimetric analyzer from 50 to 800 °C with a heating rate of 20 °C min^?1. Similar HAPs (mainly benzene, toluene, and xylenes) were identified in the emissions of the two binders. However, the HAP yields were much higher for the binder cured with p-xylenesulfonic acid than for the binder cured with methanesulfonic acid (3.74 and 1.24 mg HAPs/g binder pyrolyzed, respectively). By analyzing the HAP formation pathways, it was concluded that for the binder cured with p-xylenesulfonic acid, the aromatic HAPs were originated mainly from the acid catalyst. In addition, some HAPs (predominantly benzene) could be formed from the recombination of furan-derived fragments (e.g., C₂–C₄ radicals generated from ring-opening of furans). The results suggest that by replacing the conventionally used catalysts (arylsulfonic acids) with methanesulfonic acid, the HAP emissions from furan no-bake molds can be decreased significantly in metal casting processes.     

Control release effects of binders used in pills of traditional Chinese medicine herbs

This research investigated the effects of control release of binders that are used in the pills of Chinese herbal medicine, namely, as processed honey, starch paste, beeswax, or mixtures thereof. Aspirin and baicalin were used as the active pharmaceutical ingredients (API). The processed honey was heated to 110 degrees C, 120 degrees C, or 130 degrees C. In these pills, the binders were the only excipients. The pills were prepared by the stir method using a mixer at 80 degrees C without pressure. The differential thermal analysis (DTA) showed that the melting points of aspirin and baicalin were changed by the binders. The Fourier Transform infrared spectra (FT-IR) of aspirin and baicalin suggest that there are different non-covalent molecular interactions between the API and the binders, such as C-H-pi and hydrogen bond interaction. The dissolution profiles indicate that changing the ratio of the binders altered the patterns of dissolution of the API; thus, this ration may be used to control the release of API from the pills.     

Synergic effect of catalyst/binder in passivation side-products of Li-oxygen cells

Journal of Solid State Electrochemistry - While used in minor proportion respect to other components in cathode formulations, binders play a crucial role in lithium batteries cathode. This is...     

水性黏结剂海藻酸钠和果胶酸钠对锂离子电池石墨负极电化学性能的影响

利用循环伏安和恒电流充放电测试,结合扫描电镜观测,研究了水性黏结剂海藻酸钠和果胶酸钠对石墨负极电化学性能的影响.结果表明,石墨负极在这两种黏结剂中均可以进行有效的嵌锂脱锂循环,且电化学循环性能较好,50次循环后可逆比容量损失不超过5%.两种水性黏结剂在改善石墨电极的嵌脱锂循环性能方面具有较好的发展前景.