• Journal of Pharmaceutical Investigation
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• v.18 no.3
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• pp.139-144
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• 1988

Piperacillin phthalidyl ester was synthesized by reacting piperacillin with triethylamine and bromophthalide in acetone and its chemical structure was determined by UV, IR, and PMR. The partition coefficient of the ester was increased and the ester was more lipophilic and less water soluble than piperacillin. The ester did not show the antimicrobial activity against Bacillus subtilis ATCC 6633 in vitro, but when hydrolyzed, the parent drug of ester, piperacillin, revealed antimicrobial activity in vivo. After a single oral dose of both piperacillin and the ester to rabbits, the serum piperacillin concentration was measured by bioassay. The ester exhibited improved pharmatokinetic characteristics: $T_{max}\;of\;2hr,\;C_{max}\;of\;4.26{\mu}g{\cdot}ml^{-1},K_{el}\;of\;0.057hr^{-1},\;and\;total\;AUC\;of\;85.42{\mu}g{\cdot}hr{\cdot}ml^{-1}$. Piperacillin on the other hand, did not exhibit any gastro-intestinal absorption.

• Korean Chemical Engineering Research
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• v.49 no.3
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• pp.306-313
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• 2011

Lactic acid is widely used in the food, chemical and pharmaceutical industries, and there is an increasing demand for lactic acid as the raw material of polylactic acid, which is a biodegradable polymer. The presence of high boilers and non volatility of lactic acid makes the separation of lactic acid very difficult job. Esterification of lactic acid with methanol followed by hydrolysis of the separated methyl lactate was employed for the recovery of lactic acid. Reactive dividing wall column was proposed for the simultaneous reaction and separation. The intensified process poses a challenging control problem. Dynamic characteristics of the proposed process were examined and control systems were proposed to get a stable control performance for a disturbance in feed. Control performances of the proposed control systems were compared.

• Bulletin of the Korean Chemical Society
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• v.34 no.8
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• pp.2387-2393
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• 2013

Benzotriazole is an important synthetic auxiliary for potential clinical applications. A series of benzotriazoles as potential antiproliferative agents by inhibiting histone deacetylase (HDAC) were recently reported. Three-dimensional quantitative structure-activity relationship (3D-QSAR), including comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA), were performed to elucidate the 3D structural features required for the antiproliferative activity. The results of both ligand-based CoMFA model ($q^2=0.647$, $r^2=0.968$, ${r^2}_{pred}=0.687$) and CoMSIA model ($q^2=0.685$, $r^2=0.928$, ${r^2}_{pred}=0.555$) demonstrated the highly statistical significance and good predictive ability. The results generated from CoMFA and CoMSIA provided important information about the structural characteristics influence inhibitory potency. In addition, docking analysis was applied to clarify the binding modes between the ligands and the receptor HDAC. The information obtained from this study could provide some instructions for the further development of potent antiproliferative agents and HDAC inhibitors.

• Journal of Pharmaceutical Investigation
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• v.34 no.3
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• pp.177-183
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• 2004

Recently, studies on intranasal mucosa delivery of influenza vaccine have been actively developed because of lack of pain and ease of administration. We studied on preparation of nanoparticle delivery system using biodegradable polymer as a poly(DL-lactide-co-glycolide) (PLGA) and their binding characteristics with vaccine. Three kinds of PLGA nanoparticles were prepared by spontaneous emulsification solvent diffusion (SESD) method using sodium dodecyl sulfate and sodium laurate as an anionic surfactant and Lutrol F68 (polyethylene glycol-block-polypropylene glycol copolymer) as a nonionic surfactant. The 5-aminofluorescein labeled vaccine was coated on the surface of nanoparticles by ionic complex. The complexes between vaccine and nanoparticles were confirmed by change of the size. After vaccine coating on the surface of anionic nanoparticles, particle size was increased from 174 to 1,040 nm. However the size of nonionic nanoparticles was not more increased than size of anionic nanoparticles. The amount of coated vaccine on the surface of PLGA nanoparticles was $14.32\;{\mu}g/mg$ with sodium dodecyl sulfate, $12.41\;{\mu}g/mg$ with sodium laurate, and $9.47{\mu}g/mg$ with Lutrol F68, respectively. In conclusion, prepared nanoparticles in this study is possible to use as a virus-like nanoparticles and it could be accept in the field of influenza vaccine delivery system.

• The Korean Journal of Physiology and Pharmacology
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• v.22 no.6
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• pp.637-647
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• 2018

Extra-hypothalamic growth hormone-releasing hormone (GHRH) plays an important role in reproduction. To study the treatment effect of Grin (a novel hGHRH homodimer), the infertility models of 85 male Chinese hamsters were established by intraperitoneally injecting 20 mg/kg of cyclophosphamide once in a week for 5 weeks and the treatment with Grin or human menopausal gonadotropin (hMG) as positive control was evaluated by performing a 3-week mating experiment. 2-8 mg/kg of Grin and 200 U/kg of hMG showed similar effect and different pathological characteristics. Compared to the single cyclophosphamide group (0%), the pregnancy rates (H-, M-, L-Grin 26.7, 30.8, 31.3%, and hMG 31.3%) showed significant difference, but there was no difference between the hMG and Grin groups. The single cyclophosphamide group presented loose tubules with pathologic vacuoles and significant TUNEL positive cells. Grin induced less weight of body or testis, compactly aligned tubules with little intra-lumens, whereas hMG caused more weight of body or testis, enlarging tubules with annular clearance. Grin presented a dose-dependent manner or cell differentiation-dependentincrease in testicular GHRH receptor, and did not impact the levels of blood and testicular GH, testosterone. Grin promotes fertility by proliferating and differentiating primitive cells through up-regulating testicular GHRH receptor without triggering GH secretion, which might solve the etiology of oligoasthenozoospermia.

• Journal of Environmental Health Sciences
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• v.39 no.4
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• pp.360-368
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• 2013

Objectives: Phthalates are used in a large variety of products including as coatings of pharmaceutical tablets, film formers, stabilizers, dispersants, emulsifying agents, and suspending agents. They have been the subject of great public concern in recent years. The extensive uses of this material have attracted attention and issues regarding its safety have been raised. Methods: In this study, three types of phthalate skin permeation were studied using matrixes such as ointments, creams and lotions in vitro. The absorption of phthalate diesters [Dimethyl phthalate (DMP), Di-n-propyl phthalate (DPP) and Di-n-pentyl phthalate (DNPP)] using film former has been measured in vitro through rat skin. Epidermal membranes were set up in Franz diffusion cells and their permeability to PBS measured in order to establish the integrity of the skin before the phthalates were applied to the epidermal surface. Results: Absorption rates for each phthalate ester were determined and permeability assessment made to quantify any irreversible alterations in barrier function due to contact with the esters. Types of phthalate in vitro experimental results quickly appeared in the following order DMP > DPP ${\geq}$ DNPP. Conclusions: In the experimental results, lotion> cream> ointment, and the permeation rate of lotion with a great amount of moisture was the fastest. Skin permeation rate is generally influenced by the chemical characteristics of a given chemical, such as molecular weight and lipophilicity. As the esters became more lipophilic and less hydrophilic, the rate of absorption decreased.

• Archives of Pharmacal Research
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• v.18 no.5
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• pp.346-350
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• 1995

To assess the behavior of the various chemicals, such as ethylcholine axiridinium (AF54A), scopolamine and morphine, the chemicals were administered into eitheer rat or mice. And water maze tests were performed before and during drug administration. In AF64A-treated groups (3 nmol/each ventricle), the latencies to escape was significantly increased in both of the pretraining-and posttraining groups. In scopolamine-treatment (2mg/kg, sc) to the pretrained group, the latency to escape was significantly shortened after the acute administration of scopolamine. However in subscute treatment group with scopolamine, the latency to escape was significantly increased. In morphine-treated groups (10 mg/kg, ip), the subacute treatmment with morphine, the latency to escape was not ahcnged. The results indicate that each chemical induces the learning impariment. However the chrmical-induced learning impairment may have different characteristics upon the exposed chemical. Also the results suggest that both the motivation and the retrieval of memory might be impaired by AF64A.

• YAKHAK HOEJI
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• v.54 no.4
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• pp.240-243
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• 2010

High-performance liquid chromatography (HPLC) screening method revealed that a propolis product marketed as a functional food contained an undeclared substance similar to tadalafil, the active ingredient of the prescription drug Cialis$^{(R)}$ approved for the treatment of male erectile dysfunction. In order to identify the illegal additive, the propolis product was extracted with methylene chloride, and the extract was purified further using semipreparative HPLC. The chemical structure of the isolated substance was elucidated based on IR, LC/MS-ESI, and $^1H$- and $^{13}C$-NMR spectroscopy, which showed the characteristics similar to tadalafil. The only difference was the substitution of the methyl group at the piperazinedione ring of tadalafil to the amino group of the identified illegal additive.

• Archives of Pharmacal Research
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• v.18 no.2
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• pp.84-89
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• 1995

The complexation and physical characteristics of egg phosphatidylcholine (PC) liposome containing amphotericin B(AmB) were investigated through circular dichrosim(CD) spectra, the size distribution, the turbidity change, and the calcein release. CD spectra of AmB-containing egg PC mxture exhibited a positive peak around 330 nm indicative of complexation of AmB and four negative peaks. The positive peak increased up to $2.2{\;}millidegree/{\mu}g$ AmB as AmB contents increased up to 12% (w/w), suggesting that AmB-phospholipid complexation was promoted by the antibiotics. The effective diameter of liposomesa by dynamic light scattering decreased from 450 nm to 220 nm as the amount of AmB in liposomes increased from o to 30% (w/w). The complexation may be responsible for the reduction in size. On the other hand, at around 1 mN deoxycholate (DOC), the reltive turbidities of 5 and 10% (w/w) AmB-containing liposome suspension were less than 1 probably due to the soblubilization of the complex, while those of pure PC liposome suspension were larger than 1 at the same concentration. Deoxycholate-induced release of liposomes, indicating the intercalation of the drug into the bilayers. Therefore, it is concluded that in AmB/eggPC/water system, AmB-phospholipid complexcoexists with AmB-containing liposomes.

• Archives of Pharmacal Research
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• v.9 no.3
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• pp.145-152
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• 1986

Magnetically reponsive gelatin microspheres for the targeting of drugs have been prepared using a water-in-oil emulsion technique with chemical cross-linking of the protein. The manufacturing variables affecting microsphere size, size distribution and surface characteristics have been examined as well as the magnetic responsiveness in vitro. Sesame oil was utilized for non-aqueous phase and magentic gelatin microspheres of different size from 1. 89 to 14.88 $\mu\textrm{m}$ in mean diameter could be obtained with variation of HLB values of non-ionic surfactants. The content of magnetite which uniformly distributed throughout the microspheres was 26.7% (w/w). It was possible to control the localization of magnetic gelatin microspheres at specific sites within capilary models by using external magnetic field of under 5K gauss.