Suigen, South Korea
Suigen, South Korea

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Provided are a novel streptomyces filamentosus strain with improved daptomycin productivity, and a method for producing daptomycin using the same.


Jung Y.-S.,Catholic University of Korea | Park W.,Catholic University of Korea | Park H.,Catholic University of Korea | Lee D.-K.,Dongkook Pharm. Co. | Na K.,Catholic University of Korea
Carbohydrate Polymers | Year: 2017

The aim of this research is the development of a new type of intra-articularly injectable thermo-sensitive hydrogels for the long-term delivery of Piroxicam (PX). The thermo-sensitive hydrogel was prepared by the simple physical mixing of HA and Pluronic F-127 (HP) in aqueous solution. The addition of high-molecular-weight HA not only enhanced the mechanical strength of the hydrogel but also elicited a sustained drug release. This result could be attributed to the high-molecular-weight HA-assisted inter-micellar packing in the hydrogel inner structure. The critical gelation temperature value of HP hydrogel was considerably lower than native Pluronic F-127. To evaluate the bioavailability, pharmacokinetic parameters were analyzed after articular-cavity injection of the HP hydrogel in beagle dogs. The HP hydrogel exhibits both sustained drug release behavior and superior bioavailability in physiological conditions. Thus, we believe that the NSAID PX-loaded HP hydrogel could be a promising hydrogel-based drug delivery platform for the treatment of arthritis. © 2016 Elsevier Ltd


Ha E.-S.,Pusan National University | Lee Y.-R.,Pusan National University | Lee Y.-R.,Dongkook Pharm. Co. | Kim M.-S.,Pusan National University
Journal of Molecular Liquids | Year: 2016

The aim of this study was to measure the mole fraction solubility of dronedarone hydrochloride in six pure solvents across a temperature range of 298.15-323.15 K. The experimental solubility of dronedarone hydrochloride correlated with the Apelblat equation. The maximum mole fraction solubility of dronedarone hydrochloride was observed to be 0.119 in methanol at 323.15 K followed by ethanol (3.62 × 10- 2 at 323.15 K), 1-propanol (1.59 × 10- 2 at 323.15 K), 1-butanol (8.05 × 10- 3 at 323.15 K), 2-propanol (2.93 × 10- 3 at 323.15 K), and water (6.11 × 10- 5 at 323.15 K). Based on these results, dronedarone hydrochloride can be considered freely soluble in methanol, soluble in ethanol, and slightly soluble in 1-propanol, 2-propanol, 1-butanol, and water. These data could be important for the recrystallization and formulation development of dronedarone hydrochloride. © 2016 Elsevier B.V. All rights reserved.


Oh N.M.,Catholic University of Korea | Oh K.T.,Chung - Ang University | Youn Y.S.,Sungkyunkwan University | Lee D.-K.,Dongkook Pharm. Co. | And 3 more authors.
Colloids and Surfaces B: Biointerfaces | Year: 2013

Advanced materials that have controllable pH-responsive properties when submerged in the lysosome have a great potential in intracellular drug delivery. We developed novel poly(l-amino acid) nanogels that were prepared by a facile cross-linking of poly[. l-aspartic acid-g-(3-diethylaminopropyl)]-b-poly(ethylene glycol)-maleimide [poly(l-Asp-g-DEAP)-b-PEG-Mal] and poly(l-aspartic acid-g-ethyl thiol)-b-PEG [poly(l-Asp-SH)-b-PEG] in an oil/water emulsion condition. Interestingly, these nanogels (~125. nm in diameter) modulated volume expansion (~375. nm in diameter) in a lysosomal pH (~pH 5.0) due to an extensive proton absorption of DEAP at a low pH, which mediated lysosome swelling and the subsequent lysosome destabilization. In the in vitro tumor cell cytotoxicity test, they encouraged tumor cell death, probably owing to the leakage of lysosomal enzymes. Furthermore, encapsulating antitumor drug (e.g., doxorubicin, DOX) into these nanogels enhanced tumor cell cytotoxicity. We conclude that this nanogel system will have great potential for tumor therapy. © 2012 Elsevier B.V.


Yoo N.Y.,Catholic University of Korea | Youn Y.S.,Pusan National University | Oh N.M.,Catholic University of Korea | Oh K.T.,Chung - Ang University | And 4 more authors.
Colloids and Surfaces B: Biointerfaces | Year: 2011

The purpose of this study was to fabricate porous poly(lactide-co-glycolide) (PLGA) microparticles for efficient pulmonary deposition and increased therapeutic duration of the antioxidant anthocyanin (ATH). These microparticles were prepared by a water-in-oil-in-water (W 1/O/W 2) multi-emulsion method with vaporizing ammonium bicarbonate (AB) as a porogen and starch as a viscous additive. High porosity achieved by the decomposition reaction of AB to the base of ammonia, carbon dioxide, and water vapor at 50°C enabled efficient deposition of ATH throughout the entire lung in BALB/c mice. In addition, the porous microparticles incorporating starch showed sustained ATH release characteristics (up to 5 days) and protracted antioxidant activity (up to 5 days) for 2,2-diphenyl-1-pikryl-hydrazyl (DPPH) radicals, which was comparable to that of the porous microparticles without starch which completely released ATH in 2h. Furthermore, these porous microparticles incorporating starch led to longer ATH residence (up to 20 days) in in vivo lung epithelium. We believe that this system has great pharmaceutical potential as a long-acting antioxidant for continuously relieving oxidative stress in pulmonary diseases like chronic obstructive pulmonary disease (COPD). © 2011 Elsevier B.V.


Provided are a novel streptomyces filamentosus strain with improved daptomycin productivity, and a method for producing daptomycin using the same.


Disclosed are a novel montelukast 4-halobenzylamine salt, and a method for preparing a montelukast sodium salt by using the same. In the disclosed method, a montelukast 4-halobenzylamine salt represented by Formula 2 or a montelukast sodium salt represented by Formula 1 is prepared by obtaining a compound represented by Formula 3 from a compound represented by Formula 5, in the same reactor, without an additional obtaining process. In Formula 2, X represents F, Cl, Br or I.


PubMed | Catholic University of Korea and Dongkook Pharm. Co.
Type: | Journal: Carbohydrate polymers | Year: 2016

The aim of this research is the development of a new type of intra-articularly injectable thermo-sensitive hydrogels for the long-term delivery of Piroxicam (PX). The thermo-sensitive hydrogel was prepared by the simple physical mixing of HA and Pluronic F-127 (HP) in aqueous solution. The addition of high-molecular-weight HA not only enhanced the mechanical strength of the hydrogel but also elicited a sustained drug release. This result could be attributed to the high-molecular-weight HA-assisted inter-micellar packing in the hydrogel inner structure. The critical gelation temperature value of HP hydrogel was considerably lower than native Pluronic F-127. To evaluate the bioavailability, pharmacokinetic parameters were analyzed after articular-cavity injection of the HP hydrogel in beagle dogs. The HP hydrogel exhibits both sustained drug release behavior and superior bioavailability in physiological conditions. Thus, we believe that the NSAID PX-loaded HP hydrogel could be a promising hydrogel-based drug delivery platform for the treatment of arthritis.


The present invention relates to entecavir microspheres and a pharmaceutical composition for parenteral administration containing the same. The entecavir microspheres are manufactured by a method comprising the steps of: dissolving entecavir and a biodegradable biocompatible polymer in at least one solvent; putting the solution of the entecavir and biodegradable biocompatible polymer in a hydrophilic polymer solution, followed by stirring, to form microspheres; and removing the solvent. The entecavir is sufficiently sealed in the entecavir microsphere at approximately 80% or more based on the input amount, and the elution of the entecavir is maintained for 30 days or more, and thus the entecavir microspheres can continuously exhibit efficacy, thereby improving medication compliance of patients.


PubMed | Korea Institute of Oriental Medicine, Konkuk University and Dongkook Pharm. Co.
Type: | Journal: Evidence-based complementary and alternative medicine : eCAM | Year: 2015

We previously reported that Fructus mume (F. mume) extract shows protective effects on memory impairments and anti-inflammatory effects induced by chronic cerebral hypoperfusion. Neurodegeneration of basal cholinergic neurons is also observed in the brain with chronic cerebral hypoperfusion. Therefore, the present study was conducted to examine whether F. mume extracts enhance cognitive function via the action of cholinergic neuron using a scopolamine-induced animal model of memory impairments. F. mume (50, 100, or 200mg/kg) was administered to C57BL/6 mice for 14 days (days 1-14) and memory impairment was induced by scopolamine (1mg/kg), a muscarinic receptor antagonist for 7 days (days 8-14). Spatial memory was assessed using Morris water maze and hippocampal level of acetylcholinesterase (AChE) and choline acetyltransferase (ChAT) was examined by ELISA and immunoblotting. Mice that received scopolamine alone showed impairments in acquisition and retention in Morris water maze task and increased activity of AChE in the hippocampus. Mice that received F. mume and scopolamine showed no scopolamine-induced memory impairment and increased activity of AChE. In addition, treatments of F. mume increased ChAT expression in the hippocampus. These results indicated that F. mume might enhance cognitive function via action of cholinergic neurons.

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