• Archives of Pharmacal Research
• /
• v.28 no.5
• /
• pp.612-618
• /
• 2005

A mucoadhesive microsphere was prepared by an interpolymer complexation and solvent evaporation method, using chitosan and poly(acrylic acid) (PAA), to prolong the gastric resid ence time of the delivery system. The Fourier transform infrared results showed that microspheres were formed by an electrostatic interaction between the carboxyl groups of the PAA and the amine groups of the chitosan. X-ray diffraction and differential scanning calorimetry analysis showed that the enrofloxacin in the chitosan-PAA microsphere was molecularly dispersed in an amorphous state. Scanning electron microscopy of the surface and the quantity of mucin attached to the microspheres indicated that chitosan-PAA microspheres had a higher affinity for mucin than those of chitosan alone. The swelling and dissolution of the chitosan-PAA microspheres were found to be dependent on the pH of the medium. The rate of enrofloxacin released from the chitosan-PAA microspheres was slower at higher pH; therefore, based on their mucoadhesive properties and morphology, the chitosan-PAA microspheres can be used as a mucoadhesive oral drug delivery system.

• Archives of Pharmacal Research
• /
• v.28 no.2
• /
• pp.129-141
• /
• 2005

(-)-Fumagillol (1), a hydrolysis product of fumagillin, has been synthesized by several group from commercially available 1,2:5,6-di-O-isopropylidene-${\alpha}$-D-allofuranose in a highly stereoselective manner. Chiral centers on C5 and C6 came from D-allofuranose and the asymmetric center on C4 was accomplished by 1,3-chirality transfer using the Claisen rearrangement on a chiral allyl alcohol. Chirality, which is necessary on an epoxide consisting of the spiro-ring system, was diastereoselectively constructed by the well-known reaction, intramolecular ester enolate alkylation (IEEA), which showed that this reaction can be applied to the alpha-alkoxy ester system. The epoxide on the side chain was regioselectively introduced by the difference between the number of substituents on the vinyl groups. This accomplishment proved that IEEA can be a useful tool for the synthesis of complex molecules.

• Archives of Pharmacal Research
• /
• v.29 no.1
• /
• pp.59-63
• /
• 2006

Secalonic acid D(SAD) was isolated as the major secondary metabolite of the marine lichen-derived fungus Gliocladium sp. T31. Its structure was established on the basic of physicochemical and spectroscopic data. This is the first report on the isolation of SAD from this fungus, as well as its inhibitory effect on K562 cell cycle and its cytotoxicity against several tumor cell lines in vitro.

• Archives of Pharmacal Research
• /
• v.14 no.4
• /
• pp.311-318
• /
• 1991

Corneal permeability of various n-alkyl p-hydroxybenzoates (parabens) was studied in vitro using excised rabbit corneas, and the effect of lipophilicity of parabens on the corneal permeability was also investigated. Permeability coefficients were obtained from the least-square linear regression after the steady state had been reached. Lipophilicity of parabens was calculated by distribution coefficients determined in octanol-S | $12{\phi}{\parallel}$) rensen's buffer solution (pH 5.0). The relationship between lipophilicity and corneal permeability of parabens was not linear, but the optimum lipophilicity for the maximum permeation was found. The influence of tween 80 on corneal permeability of methyl and butylparaben was not significant.

• Archives of Pharmacal Research
• /
• v.14 no.4
• /
• pp.364-369
• /
• 1991

The synthesis and regioselective reactions of a chiral allyl sulfide. (S)-(+)-(1-methylpyrrolidin-2-yl)methyl allyl sulfide (MAS, 1) are described. Remarkable ${\alpha}-regioselectivity$ was observed in the alkylation of the carbanion of MAS while 1:3 mixtures of ${\alpha}-and\;{\gamma}-adducts$ were produced in the addition of the MAS anion to aldehydes. However, a dramatic change of the regioselectivity was witnessed when Lewis acids such as $Et_3Al$, $Et_3B$, and $Ti(O^iPr)_4$ were used as additives in the addition reaction. In these cases, ${\alpha}-adducts$ were formed exclusively. A rationale for the change of regioselectivity is provided. And the stereochemical aspect of the addition reaction is also described.

• Archives of Pharmacal Research
• /
• v.22 no.6
• /
• pp.554-558
• /
• 1999

The effects of ethanolic extract (EEP) of propolis on chronic inflammation were evaluated using rat adjuvant arthritis. In the chronic inflammatory animal model, the arthritis index was suppressed by EEP treatments (50 mg/kg/day and 100 gm/kg/day, p.o.). Moreover, physical weakness, induced by the chronic disease state, was dose-dependently improved in the EEP-treated groups. It s analgesic effect, assessed using the tail-flick test, was comparable to prednisolone (2.5 mg/kg/day, p.o.) and acetyl salicylic acid (100 mg/kg/day, p.o.). In carrageenan rat hind paw edema, which was conducted to test the effects of subfractions of EEP, the petroleum ether sub-fraction (100 mg/kg, p.o.) showed an inhibitor effect on the paw edema whereas EEP (200 mg/kg, p.o.) showed a significant anti-inflammatory effect at 3 and 4 hrs after carrageenan injection. From these results, we conclude that the ethanolic extract of propolis had a profound anti-inflammatory effects on both chronic and acute inflammations.

• Journal of the Korea Furniture Society
• /
• v.17 no.4
• /
• pp.85-99
• /
• 2006

Fredrick Krause's chair in the Brooklyn Museum of Art (accession no. 87. 19) is a key to the understanding of factory-made, patent furniture, and the Modern Gothic style in the United States. However, research has rarely done for this chair as well as for the designer. Since this piece is incorporating the utility patent, it is a valuable example to understand the nineteenth-century patented furniture. Because of the popularity of Modern Gothic style, the similar style of chairs were often manufactured. This study explores how other examples are related and what the significance of the Brooklyn Museum chair is. The book of Sharon Darling provided especially helpful information about other Krause chairs in Fond du Lac and chair manufactures in Chicago. The interview with John Ebert at Galloway House in Fond du Lac, Wisconsin was especially helpful. Several primary sources proved helpful in researching the chair. The photo archives. of Kimbel and Cabus at the Cooper-Hewitt National Design Museum provides me a key to this research.

• Archives of Plastic Surgery
• /
• v.45 no.1
• /
• pp.74-79
• /
• 2018

The aim of this study was to present a case series of the orthognathic treatment of facial asymmetry due to temporomandibular joint (TMJ) ankylosis and to characterize the current treatment modalities through a literature review. Four patients who presented with facial asymmetry due to TMJ ankylosis between 2010 and 2014 were included in this study. TMJ ankylosis was surgically treated before bimaxillary surgery with advancement genioplasty in some of the cases. In 2 cases, 3-dimensional (3D) models were used for diagnosis and treatment planning, as 3D models are very important tools for planning surgical maneuvers. Aesthetically pleasant facial symmetry and a good facial profile were obtained in all the cases.

• Archives of Pharmacal Research
• /
• v.27 no.1
• /
• pp.1-12
• /
• 2004

Initial burst is one of the major challenges in protein-encapsulated microparticle systems. Since protein release during the initial stage depends mostly on the diffusional escape of the protein, major approaches to prevent the initial burst have focused on efficient encapsulation of the protein within the microparticles. For this reason, control of encapsulation efficiency and the extent of initial burst are based on common formulation parameters. The present article provides a literature review of the formulation parameters that are known to influence the two properties in the emulsion-solvent evaporation/extraction method. Physical and chemical properties of encapsulating polymers, solvent systems, polymer-drug interactions, and properties of the continuous phase are some of the influential variables. Most parameters affect encapsulation efficiency and initial burst by modifying solidification rate of the dispersed phase. In order to prevent many unfavorable events such as pore formation, drug loss, and drug migration that occur while the dispersed phase is in the semi-solid state, it is important to understand and optimize these variables.

• Archives of Pharmacal Research
• /
• v.29 no.7
• /
• pp.577-581
• /
• 2006

Oxidative mechanisms are thought to have a major role in cataract formation and diabetic complications. Antioxidant enzymes play an essential role in the antioxidant system of the cells that work to maintain low steady-state concentrations of the reactive oxygen species. When HLE-B3 cells, a human lens cell line were exposed to 50-100 mM glucose for 3 days, decrease of viability, inactivation of antioxidant enzymes, and modulation of cellular redox status were observed. Significant increase of cellular oxidative damage reflected by lipid peroxidation and DNA damage were also found. The glycation-mediated inactivation of antioxidant enzymes may result in the perturbation of cellular antioxidant defense mechanisms and subsequently lead to a pro-oxidant condition and may contribute to various pathologies associated with the long term complications of diabetes.