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901.
In this study, we aimed to design orally disintegrating tablets by employing a formulation design approach that enables the production of such tablets in the same facilities used for the production of solid dosage forms on an industrial scale. First, we examined the relationships between the types of binders used in the tablets and the properties of orally disintegrating tablets prepared by the wet granulation method. Results revealed that partly pregelatinized starch is a relatively suitable binder for orally disintegrating tablets as it also serves as a disintegrant. Next, we employed a central composite design for 2 factors, namely, corn starch and partly pregelatinized starch, in order to design granules suited for orally disintegrating tablets composed of D-mannitol, corn starch or partly pregelatinized starch. The effects of these 2 factors on 3 types of responses, namely, 50% granule size, compressing index and disintegrating index, were analyzed with a software package, and responses to changes in the factors were predicted. This study investigated the effects of binder type and binder content in orally disintegrating tablets, and provided evidence that the binder exerts a strong influence on tablet properties, and is therefore an important component of orally disintegrating tablets. 相似文献
902.
Ogino M Fukui S Nakada Y Tokunoh R Itokawa S Kakoi Y Nishimura S Sanada T Fuse H Kubo K Wada T Marui S 《Chemical & pharmaceutical bulletin》2011,59(10):1268-1273
Acyl-CoA: cholesterol acyltransferase (ACAT) is an intracellular enzyme that catalyzes cholesterol esterification. ACAT inhibitors are expected to be potent therapeutic agents for the treatment of atherosclerosis. A series of potent ACAT inhibitors based on an (4-phenylcoumarin)acetanilide scaffold was identified. Evaluation of the structure-activity relationships of a substituent on this scaffold, with an emphasis on improving the pharmacokinetic profile led to the discovery of 2-[7-chloro-4-(3-chlorophenyl)-6-methyl-2-oxo-2H-chromen-3-yl]-N-[4-chloro-2-(trifluoromethyl)phenyl]acetamide (23), which exhibited potent ACAT inhibitory activity (IC50=12 nM) and good pharmacokinetic profile in mice. Compound 23 also showed regressive effects on atherosclerotic plaques in apolipoprotein (apo)E knock out (KO) mice at a dose of 0.3 mg/kg per os (p.o.). 相似文献
903.
Masaki Shimizu Ikuhiro NagaoYosuke Tomioka Tsugumi KadowakiTamejiro Hiyama 《Tetrahedron》2011,67(41):8014-8026
This study demonstrates that the double cross-coupling reaction of 1,2-bis(pinacolatoboryl)alkenes and -arenes with 2,2′-dibromobiaryls proceeds smoothly with the aid of a catalytic amount of Pd(PPh3)4 in the presence of excess base to give a variety of polycyclic aromatic hydrocarbons, such as phenanthrenes, [5]helicene, dithienobenzenes, triphenylenes, dibenzo[g,p]chrysenes, and triphenyleno[1,2-b:4,3-b′]dithiophenes in good to high yields. It is noteworthy that the annulations using 2,2′-dibromooctafluorobiphenyl as an electrophile furnish the otherwise difficult to synthesize octafluorophenanthrenes and semi-fluorinated dibenzo[g,p]chrysenes in high yields. 相似文献
904.
Atsuki OdaniKaoru Ishihara Masaki OhtawaHiroshi Tomoda Satoshi Omura Tohru Nagamitsu 《Tetrahedron》2011,67(42):8195-8203
The total synthesis of pyripyropene A, a potent ACAT2 inhibitor with high isozyme selectivity, was completed. Key features of the synthetic strategy include Ti(III)-mediated radical cyclization and Peterson olefination for the construction of the AB ring segment and stereoselective dihydro-γ-pyrone formation (C-ring). The total synthesis provided pyripyropene A in 5.3% overall yield over 17 steps. 相似文献
905.
Masaki Shimizu 《Tetrahedron letters》2011,52(32):4084-4089
A new molecular design of organic emitters exhibiting efficient solid-state fluorescence, which involves planarity breaking of N,N-diorganoquinacridones, is presented. The new design principle led to the development of dimethyl 2,5-diaminoterephthalates and 2,5-diamino-1,4-diaroylbenzenes, which emitted green to yellow and yellow to red light with high-to-excellent quantum yields, respectively. In addition, the photoluminescence properties of the diaroylbenzenes were dependent on the morphology and reversibly variable by thermal and solvent vapor stimuli. 相似文献
906.
907.
Takahashi M Ohno S Fujita N Sengoku T Yoda H 《Journal of colloid and interface science》2011,356(2):536-542
Detailed exploratory and mechanistic investigations on spontaneous formation of dye-functionalized gold nanoparticles (GNPs) using dye-based reverse micellar systems are described in this publication. The accumulated results from spectroscopic and microscopic investigations demonstrated that water molecules confined within nanoscopic enclosure of the self-assembled reverse micelles played critical role in the redox processes of aurate ions to produce GNPs, which are assumed to have approximately constant size distributions. The resulting dye-functionalized GNPs were found to offer their absorption and fluorescence emission tunability by changing the medium polarity as well as to exhibit excellent film-forming properties to give optically homogeneous polystyrene thin films. These key findings in addition to broad applicability of the self-assembling process with a variety of dye analogues have led to a conclusion that the protocol presented here serves as a versatile synthetic method to provide a potential convenience for future development of new organic-inorganic hybrid nanomaterials. 相似文献
908.
A theory accounting for the dynamical aspects of the superfluid response of one dimensional (1D) quantum fluids is reported. In long 1D systems, the onset of superfluidity is related to the dynamical suppression of quantum phase slips at low temperatures. The effect of this suppression as a function of frequency and temperature is discussed within the framework of the experimentally relevant momentum response function. Applications of these results to the understanding of the superfluid properties of helium confined in 1D pores with nanometer diameter, dislocations in solid 4He, and ultracold atomic gases are also briefly discussed. 相似文献
909.
12 W Q-switched Er:ZBLAN fiber laser at 2.8 μm 总被引:1,自引:0,他引:1
A diode-pumped, actively Q-switched 2.8 μm fiber laser oscillator with an average output power of more than 12 W has been realized through the use of a 35 μm core erbium-doped ZBLAN fiber and an acousto-optic modulator; to our knowledge, this is the first 3 μm pulsed fiber laser in the 10 W class. Pulse energy up to 100 μJ and pulse duration down to 90 ns, corresponding to a peak power of 0.9 kW, were achieved at a repetition rate of 120 kHz. 相似文献
910.
Positive contrast imaging methods produce enhanced signal at large magnetic field gradient in magnetic resonance imaging. Several postprocessing algorithms, such as susceptibility gradient mapping and phase gradient mapping methods, have been applied for positive contrast generation to detect the cells targeted by superparamagnetic iron oxide nanoparticles. In the phase gradient mapping methods, smoothness condition has to be satisfied to keep the phase gradient unwrapped. Moreover, there has been no discussion about the truncation artifact associated with the algorithm of differentiation that is performed in k-space by the multiplication with frequency value. In this work, phase gradient methods are discussed by considering the wrapping problem when the smoothness condition is not satisfied. A region-growing unwrapping algorithm is used in the phase gradient image to solve the problem. In order to reduce the truncation artifact, a cosine function is multiplied in the k-space to eliminate the abrupt change at the boundaries. Simulation, phantom and in vivo experimental results demonstrate that the modified phase gradient mapping methods may produce improved positive contrast effects by reducing truncation or wrapping artifacts. 相似文献