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세팔렉신 함유 생체막점착성 마이크로캅셀의 생체이용율 평가
한건,김정환,정연복,지웅길,Han, Kun,Kim, Jung-Hwan,Chung, Youn-Bok,Jee, Ung-Kil 한국약제학회 1994 Journal of Pharmaceutical Investigation Vol.24 No.3
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 microcapsules 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 $Cephalexin-Eudragit^{\circledR}$ 마이크로캅셀의 생물약제학적 평가
한건,김광덕,정연복,지웅길,김신근,Han, Kun,Kim, Kwang-Dug,Chung, Youn-Bok,Jee, Ung-Kil,Kim, Shin-Keun 한국약제학회 1993 Journal of Pharmaceutical Investigation Vol.23 No.2
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. Controlledrelease 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 $K_r$, without change in $K_a$, showed that the rate-limiting step of absorption moved from absorption step to releasestep.
$Eudragit^{\circledR}$ 마이크로캅셀화에 의한 ${\beta}$-락탐계 항생물질의 방출제어제제 개발
한건,신도수,지웅길,정연복,Han, Kun,Shin, Do-Su,Jee, Ung-Kil,Chung, Youn-Bok 한국약제학회 1992 Journal of Pharmaceutical Investigation Vol.22 No.4
Microencapsulations of amoxicillin and cephalexin, using Eudragit RS, RL, E, S and L were investigated. The microcapsules were prepared by the solvent evaporation process in liquid paraffin phase, which is based on dispersion of acetone/isopropanol containing the drug in liquid paraffin. Aluminium tristearate was used as an additive for the preparation of microcapsules. The size distribution, dissolution test and observation by SEM were examined. Good reproducibility in microcapsule preparation was observed. The microcapsules obtained were spherical and free-flowing particles. The dissolution rates of amoxicillin and cephalexin from the microcapsules were considerably decreased as compared with those from amoxicillin and cephalexin powder, respectively. As the dispersing agents (aluminium tristearate) increased, the particle size of microcapsules decreased and the dissolution rate increased. In order to control the release rate of drugs, microcapsules were prepared by mixing Eudragit RS/RL or Eudragit S/L. As Eudragit RL ratio in microcapsule of Eudragit RS/RL increased, the dissolution rate increased. As Eudragit L ratio in microcapsule of Eudragit S/L increased, the dissolution rate increased. Furthermore, the release rates of drugs from Eudragit RS/L or RS/polyelthylene glycol 1540 (PEG 1540) were examined. The dissolution rate of drugs increased with increasing of Eudragit L or PEG 1540 ratio. In conclusion, the release rates of drugs from Eudragit RS/RL or RS/PEG 1540 microcapsule could be controlled, and these microcapsules will be convenient for reducing frequency of administration.
황체호르몬 유리호르몬의 경점막 수송: 수종의 흡수촉진제를 사용한 $[D-Ala^6]$ LHRH의 점막투과촉진 및 흰쥐에 있어서의 배란유도효과 향상
한건,정남주,박정숙,박희범,정연복,문동철,Han, Kun,Jeong, Nam-Joo,Park, Jeong-Sook,Park, Hee-Beom,Chung, Youn-Bok,Moon, Dong-Cheul 대한약학회 1994 약학회지 Vol.38 No.4
Due to the limited bioavailability of $[D-Ala^6]$LHRH from nonparenteral transmucosal sites of administration, enhancement of mucosal permeability by coadministration of several protease inhibitors and/or penetration enhancers were studied in rabbit mucosa. As a reliable bioassay method for $[D-Ala^6]$LHRH, ovulation-inducing effect were measured after vaginal administration in the rat. The permeation of $[D-Ala^6]$LHRH through the mucosal membrane of rabbit mounted on George-Grass diffusion cells were examined in the presence of polyoxyethylene 9-lauryl ether (POE), ${\beta}$-cyclodextrin$({\beta}-CyD)$ or ethylene diamine tetra acetate disodium salt(EDTA). The vaginal membrane showed higher permeability of $[D-Ala^6]$LHRH than the rectal and nasal membrane. POE and ${\beta}-CyD$ showed a small promoting effect on the membrane permeation of $[D-Ala^6]$LHRH, but EDTA showed significant enhancement. Ovaluation was enhanced by the coadministration of sodium laurate(0.5%), a protease inhibitor but was not enhanced by EDTA, a penetration enhancer. On the other hands, coadministration of sodium tauro 24,25 dihydrofusidate(1%) and EDTA(2%) enhanced the ovulation inducing-effect 2.8 times. These results suggest that the vaginal administration of $[D-Ala^6]$LHRH with STDHF or sodium laurate as a protease inhibitor, and EDTA as a penetration enhancer, may become an elective method for transmucosal delivery of $[D-Ala^6]$ LHRH.
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,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.
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.
푸로세미드의 안정성 및 생체내 이용율에 미치는 ${\beta}-$시클로덱스트린의 영향
한건,유병권,Han, Kun,Yu, Byeong-Kwun 한국약제학회 1988 Journal of Pharmaceutical Investigation Vol.18 No.3
Inclusion complex formation of furosemide with ${\beta}-cyclodextrin({\beta}-CyD)$ in solid state was confirmed by X-ray diffractometry, IR spectroscopy and differential scanning calorimetry (DSC). The solid complexes of ${\beta}-CyD$ with furosemide in molar ratio of 2 : 1 were prepared by solvent evaporation method. The photodegradation of furosemide in alkaline solution under the light and the hydrolysis of furosemide in acidic solution were not inhibited by complex formation with ${\beta}-CyD$. However, the bioavailability of furosemide was improved by complex formation with ${\beta}-CyD$ after oral administration to rats.
황체호르몬 유리호르몬의 경점막 수송: 가토 점막균질액 중에서 중쇄지방산염의 LHRH에 대한 안정화 효과
한건(Kun Han),박정숙(Jeong Sook Park) 대한약학회 1994 약학회지 Vol.38 No.1
In order to investigate the feasibility of transmucosal delivery of the model peptide, LHRH, metabolism of LHRH and inhibition effect of medium chain fatty acid salts were studied in rabbit mucosal homogenate. LHRH incubated in homogenates of rectal(RE), nasal(NA) and vaginal(VA) mucosa were assayed by HPLC. Five to six degradation products of LHRH were detected and the degradation of LHRH(500mcg/ml) followed the first order kinetics. The main degradation products were found as LHRH1-5(M-I), LHRH1-3(M-II) and LHRH1-6(M-III) by the method of amino acid analysis. The half-lives of LHRH in the mucosal homogenates were found to be less than 20 min at protein concentration of 2.5mg/ml with the order of VA>NA>RE mucosal homogenate. Medium chain fatty acid salts such as sodium caprylate (C8), sodium caprate (C10) and sodium laurate (C12) at the concentration of 0.5%-1.O% inhibit the proteolysis of LHRH significantly. The addition of sodium laurate(O.5%) into the NA and VA mucosal homogenates protected LHRH completely from the degradation.