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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,Emil T Lin 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.
중쇄지방산염 함유 Eudispert hv 하이드로겔의 인슐린 직장 흡수증대효과
한건,정연복,김준식,유정희 한국약제학회 1997 Journal of Pharmaceutical Investigation Vol.27 No.3
The purpose of the present study was to investigate the effect of medium chain fatty acid salts, reported as enhancers in insulin nasal absorption, on the rectal absorption of insulin in rats. The serum glucose and remained insulin level in perfusate were measured after rectal recirculation of insulin with or without sod. laurate, sod. caprate and sod. caprylate in situ. The addition of sod. laurate or sod. caprate reduced serum glucose concentration considerably. Sod. caprate (1.0%) showed the greatest promoting effect on the decrement of serum glucose. Eudispert hv hydrogels containing insulin with medium chain fatty acid salts were, thereby, prepared and evaluated. The release rate of insulin from Eudispert hv hydrogels was reduced with an increase in the content of Eudispert hv, and was raised with increasing NaOH concentration. Ten percent Eudispert hv hydrogels were offered for the rectal administration of insulin. The addition of 1.0% sod. caprate reduced serum glucose concentration remarkably after rectal administration of 10% Eudispert hv hydrogels containing insulin. The level of glucose decrement was greater by 30% compared to subcutaneous administration of insulin solution. From the above findings. Eudispert hv hydrogels would be used as useful rectal delivery systems of insulin.
생체막점착성 하이드로겔을 이용한 황체형성호르몬 유리호르몬의 질점막 수송
한건,박희범,박정숙,정연복 ( Kun Han,Hee Beom Park,Jeong Sook Park,Youn Bok Chung ) 한국약제학회 1997 Journal of Pharmaceutical Investigation Vol.27 No.1
N/A The mucosal route of administration(nasal, buccal, conjunctival and vaginal) has recently been considered as an alternative to parenteral delivery for many peptide drugs because enzymatic degradation of these agents may be partly avoided. The objective of these study was to establish the optimal mucosal administration dosage form of LHRH/[D-Ala^6]LHRH, based on presystemic metabolism. We reported previously the peptidase inhibition effect of medium chain fatty acid salts(sodium caprylate, soadium caprate and sodium laurate). EDTA and STDHF on the proteolysis of LHRH/[D-Ala^6]LHRH in rabbit mucosal homgenates. We also reported that EDTA. STDHF and sodium laurate markedly increased the potency of LHRH/[D-Ala^6]LHRH solution applied vaginally. In the present study, by administration of polycarbophil hydrogel containing LHRH the ovulation inducing activity was 3.3 times greater than solution. These results indicate not only peptidase inhibitor but also polycarbophil hydrogel significantly improved the absorption of this drug. The results of this study would provide the feasibility as a rational dosage form for improving bioavailability and self administration of this hydrogel by the vaginal application.
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.
세팔렉신 함유 생체막점착성 마이크로캅셀의 생체이용율 평가
한건,김정환,정연복,지웅길 충남대학교 약학대학 의약품개발연구소 1994 藥學論文集 Vol.10 No.-
Bioadhesive microcapsules of cephalexin, using Eudragit RS/RL coated with polycarbophil or carbopol, were evaluated biopharmaceutically. The GI transit of microcapsules in rats was studied. Bioadhesive microcapules coated with polycarbophil or carbopol were shown to have substantially longer GI transit time than Eudragit RS/RL microcapsule. The delay in transit time was due to bioadhesion of the polymer to the mucin-epithelial cell surface which was clearly observable on animal autopsy. Plasma drug levels in rabbits showed that bioadhesive microcapsules resulted in a longer duration of action and greater bioavailability than other microcapsule or drug powder. Thus, the principle of bioadhesion can significantly improve therapy, due to a reduced rate of gastric emptying, an increase in contact time, and the intimacy of contact of the drug with the absorbing membrane.
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.