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호명진,이대로,정혁준,송우헌,박준상,강명주 대한화학회 2017 Bulletin of the Korean Chemical Society Vol.38 No.5
The objective of this study was to formulate hyaluronate (HA) combined with magnesium sulfate (MS) for intra-articular (IA) injection, to provide rapid and profound analgesia in the treatment of osteoarthritis (OA). The injectable HA/MS combination was optimized with respect to the kinds and amounts of buffering agent (10 mM histidine, pH 7.0) and stabilizer (10 mM sodium citrate), by evaluating changes in the appearance, pH, and intrinsic viscosity at 60°C. Increasing concentrations of sodium citrate significantly inhibited the decline in intrinsic viscosity, denoting the depolymerization of HA, preserving over 91% of initial value. In an efficacy study in iodoacetate-induced OA rats, treatment with the HA/MS combination (1/2% w/v) significantly reduced joint swelling and pain, compared to the vehicle- and HA-treated groups (p < 0.05) at 7 days postdosing. Thus, IA administration of the combination of HA, a slow-acting symptom-modifying agent, with the inorganic analgesic is a potentially effective therapeutic approach for rapid pain relief in the OA knee.
김성래,호명진,최영욱,강명주 대한화학회 2019 Bulletin of the Korean Chemical Society Vol.40 No.4
The purpose of this study was to construct a poly(lactic-co-glycolic acid) microparticle (PLGA MP) of entecavir (ETV), an anti-viral agent for hepatitis B, for parenteral sustained delivery. To improve entrapment efficiency of the hydrophilic small compound in MPs, different fabrication methods such as double emulsion solvent evaporation and spray-drying method were investigated. The prepared MPs were highly spherical, and the surface was smooth, irrespective of fabrication methods. On the other hand, the drug loading efficiency and in vitro release profile of ETV from the MPs were largely depending on fabrication methods. When the MPs were prepared by double emulsion method, the drug loading efficiency was extremely low (< 16.2%), with rapid drug release within two hours. On the other hand, the MPs prepared by spray-drying process after dissolving the hydrophilic drug and PLGA polymer in acetic acid exhibited high loading efficiency more than 95%, with prolonged release profile more than 25 days. The drug release profile from the MPs prepared by spray-drying technique was effectively adjusted by varying the lactide/glycolide ratio (75/25 or 50/50) or terminal group (carboxylic acid or ester terminated) of the biodegradable polymers. Therefore, the novel SR system fabricated by spray drying technique is expected to be an advantageous tool for the management of chronic hepatitis B with less frequent drug administration and improved patient's adherence.
정민영,호명진,최민구,한영택,최용석,강명주 대한화학회 2023 Bulletin of the Korean Chemical Society Vol.44 No.7
Entecavir (EV) is a first-line antiretroviral agent to treat chronic hepatitis B. However, its oral administration is challenging, due to food effect on intestinal absorption. Therefore, in order to afford improved patient’s compliance, a novel long-acting injectable oil depot (OD) system of entecavir-3-palmiate (EVP), a lipidic ester prodrug of EV, was formulated. The OD consisted of oleic acid and benzyl alcohol as oily vehicles, with a suitable viscosity (38.6 centipoise with shear rate of 1 s1). The prodrug was gradually released from the OD under sink conditions, providing delayed liberation than that by the hydrophilic parent compound. Following the intramuscular injection in rats, EV-P OD provided a markedly protracted EV profile compared to oral EV; the EV levels in plasma were expanded over 2 weeks, with elimination half-life of about 7 days. Therefore, we concluded that EV-P OD can be a promising approach for a prolonged delivery of EV.
이대로,김영한,박근원,호명진,정혁준,조하라,박준서,최용석,염동우,최영욱,강명주 한국약제학회 2015 Journal of Pharmaceutical Investigation Vol.45 No.7
The aim of the study was to formulate the solid dosage form of the supersaturable self-emulsifying drug delivery system (S-SEDDS) for tacrolimus, a poorly watersoluble immunosuppressant, to enhance the dissolution rate and oral absorption. A solid formulation was prepared by adsorbing the liquid S-SEDDS onto porous carriers including FujicalinⓇ (dibasic calcium phosphate). Macroscopic observation using scanning electron microscopy and drug crystallinity determination using X-ray powder diffraction revealed that the calcineurin inhibitor was effectively held within the intact porous carriers in a solubilized form. In an in vitro dissolution test in simulated gastric fluid (pH 1.2), there were no remarkable differences in the release rate and extent of dissolution between liquid and Fujicalin-based solid S-SEDDS, achieving over 90 % drug release after 15 min. Moreover, the pharmacokinetic parameters for tacrolimus in the liquid and FujicalinⓇ- based solid S-SEDDS after oral administration at a dose of 5 mg/kg were statistically equivalent in rats (p>0.05). This study suggests that solidification of liquid S-SEDDS using FujicalinⓇ, a soluble adsorbent in acidic medium, can be a promising approach to obtain the free-flowing powder form of liquid S-SEDDS while preserving the high and fast dissolution rate of the liquid self-emulsifying system.