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한건,M. A. Jalil Miah,Srinivasan Shanmugam,용철순,최한곤,김정애,유봉규 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.10
Mixed micellar nanoparticle consisting of amphotericin B (AmB) and poly styrene-block-poly ethylene oxide (PS-block-PEO) was prepared by high pressure homogenizer. Nephrotoxicity of the nanoparticle was investigated along with antifungal activity and self-aggregation status of the drug in the nanoparticle. Nephrotoxicity was markedly reduced when AmB was intravenously administered to rats as mixed micellar nanoparticle with PS-block-PEO in terms of transmission electron microscopy of tubular cells and creatinine clearance. Antifungal activity of AmB was not altered when the drug was in the form of mixed micellar nanoparticle compared to both conventional formulation and AmB micelle treated by same procedure without PS-block-PEO. Self-aggregation status of AmB molecules revealed monomeric in the mixed micellar nanoparticle with PS-block-PEO up to the therapeutic level of the drug (1-3 mM). The reduced nephrotoxicity of AmB in mixed micellar nanoparticle may be associated with the existence of the drug as monomeric form in the nanoparticle. Based on our result, formulation of AmB as mixed micellar nanoparticle with PS-block-PEO may be a promising alternative for the treatment of fungal diseases in patients who are at risk of renal dysfunction.
서방성 Cephalexin-Eudragit^� 마이크로캅셀의 생물약제학적 평가
한건,김광덕,정연복,지웅길,김신근 충남대학교 약학대학 의약품개발연구소 1993 藥學論文集 Vol.9 No.-
Microcapsules(Mc) of cephalexin (CEPH), using Eudragit RS, RL, L, S and polyethylene glycol 1540, were evaluated biopharmaceutically. The area under the curve of CEPH-Eudragit RS/RL Mc administered orally once was larger than that of cephalexin powder twice every 6 hrs. Controlled-release effectiveness and the absorption rate effectiveness, two important parameters of Vallner's method, of CEPH-Eudragit RS/RL Mc indicate that these Mc can be good sustained-release preparations. And a simple pharmacokinetic model is introduced which allows the gastric emptying and intestinal-transit rates of a drug itself and a solid-state drug contained in Mc. Decreasing k, without change in k_α showed that the rate-limiting step of absorption moved from absorption step to release-step.
한건,이민화,김신근,Han, Kun,Lee, Min-Hwa,Kim, Shin-Keun 한국약제학회 1983 Journal of Pharmaceutical Investigation Vol.13 No.1
The interactions of ${\alpha}-cyclodextrin({\alpha}-CyD)$ and ${\beta}-cyclodextrin({\beta}-CyD)$ with several non-steroidal antiinflammatory drugs were studied on the effects of ${\alpha}-$ and ${\beta}-CyD$ on the solubility of the drugs in aqueous medium. Indoprofen, niflumic acid, alclofenac, and naproxen were chosen as representatives of antiinflammatory drugs. The solubility of all drugs studied increased with the addition of ${\beta}-CyD$, while not with glucose or ${\alpha}-CyD$. The increase of the solubility with ${\beta}-CyD$ was considered due mainly to the formation of inclusion complexes between ${\beta}-CyD$ and drugs. From the solubility data, the apparent stability constants K of the complex could be calculated. Ultraviolet absorption and circular dichroism confirmed the inclusion of indoprofen, niflumic acid and naproxen with ${\beta}-CyD$ in the molar ratio of 1 : 1. Inclusion complexes in solid powder form were obtained by the freeze-drying method and the inclusion formation was confirmed again by infrared, diffential thermal analysis, and X-ray diffraction measurements.
한건,이민화,김신근,Han, Kun,Lee, Min-Hwa,Kim, Shin-Keun 한국약제학회 1984 Journal of Pharmaceutical Investigation Vol.14 No.1
The pharmaceutical characteristics of solid indoprofen inclusion complex such as dissolution, permeation through a cellophane membrane, model analysis of interfacial tranesfer, absorption behaviors in rat intestine, and the plasma concentration of indoprofen after oral administrations to rabbits were examined in comparison with those indoprofen alone. The inclusion complex obtained by freeze-drying method showed the higher dissolution rate and membrane permeability among the test powders, and increased significantly the amont of indoprofen absorbed in rat intestine and the levels of plasma concentration of indoprofen after oral adminstrations to rabbits. The increase of bioavailability of $indoprofen-{\beta}-cyclodextrin$ complex was considered due to the increased solubility and dissolution rate of solid powder form.
한건,Han, Kun,Lin, Emil T. 한국약제학회 1987 Journal of Pharmaceutical Investigation Vol.17 No.2
WR 2721 (S-2-(3-aminopropylaminoethylphosphorothioate) is a radioprotective drug that is now undergoing clinical trials in the United States and Japan. a liquid chromatographic electrochemical method for the determination of WR 2721 an WR 3689 [S-2-(3-methylaminopropylamino)ethylphorothioate] in human plasma was developed in this study. This method includes the use of a Hg/Au electrochemical detector and a cyano column for the direct measurement of WR 2721 and WR 3689 in plasma. An analog of WR 2721, WR 149846 was used as an internal standard. WR 2721 and WR 3689 could be well separated from the solvent front, with a mobile phase of acetonitrile-water (20:80), 0.1M acetic acid and 1.2 mM sodium octane sulfonate. This method was shown to be precise. Both intra-day and inter-day results were within 10% CV. Also, sample preparation was fairly simple. Since WR 2721 and WR 3689 were unstable at room temperature, it was essential to use an automatic sample processor with a refrigerator, especially for carrying out routine analyses.