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신규 Capsaicin 유도체 DA - 5018 을 함유한 외용진통제의 제제설계 Ⅰ: 평가법 확립 및 외용크림제의 설계
차봉진,이응두,김원배,이민화 ( Bong Jin Cha,Eung Doo Lee,Won Bae Kim,Min Hwa Lee ) 한국약제학회 1997 Journal of Pharmaceutical Investigation Vol.27 No.1
N/A To formulate the topical analgesic preparation of a new capsaicin derivative. DA-5018, a skin penetration evaluation system was established and the effect of composition of formulation on skin penetration using this system was evaluated. The effect of massage on hairless mouse skin penetration and inter-day variation of this effect were investigated using test formulations (cream). In massage group, compared with non-massage group, absolute penetration amount of DA-5018 increased and this experimental system was found to be reproducible. The effects of pH of water phase, ratio of oil/water and the concentration of active ingredient in cream on skin penetration were investigated. The permeation of DA-5018 from the cream increased with increasing pH of water phase to 9. But at pH 10, the permeation of DA-5018 decreased, because of the physical instability of the cream. The permeation of DA-5018 from the cream increased with increasing the ratio of oil/water of the cream. The increase of the content of DA-5018 to 0.3% increased the permeation of DA-5018. but at high concentration(1.0%), the permeation of DA-5018 decreased, due to the instability of the cream.
신규 Capsaicin 유도체 DA-5018을 함유한 외용진통제의 제제설계 I : 평가법 확립 및 외용크림제의 설계
차봉진,이응두,김원배,이민화,Cha, Bong-Jin,Lee, Eung-Doo,Kim, Won-Bae,Lee, Min-Hwa 한국약제학회 1997 Journal of Pharmaceutical Investigation Vol.27 No.1
To formulate the topical analgesic preparation of a new capsaicin derivative, DA-5018, a skin penetration evaluation system was established and the effect of composition of formulation on skin penetration using this system was evaluated, The effect of massage on hairless mouse skin penetration and inter-day variation of this effect were investigated using test formulations(cream). In massage group, compared with non-massage group, absolute penetration amount of DA-5018 increased and this experimental system was found to be reproducible, The effects of pH of water phase, ratio of oil/water and the concentration of active ingredient in cream on skin penetration were investigated. The permeation of DA-5018 from the cream increased with increasing pH of water phase to 9. But at pH 10, the permeation of DA-5018 decreased, because of the physical instability of the cream. The permeation of DA-5018 from the cream increased with increasing the ratio of oil/water of the cream. The increase of the content of DA-5018 to 0.3% increased the permeation of DA-5018, but at high concentration(1.0%), the permeation of DA5018 decreased, due to the instability of the cream.
새로운 Capsaicin 유도체 DA - 5018 의 구조 및 물리화학적 성질 연구
김흥재,이종진,이응두,심현주,이상득,옥광대,김원배,박노상 ( Heung Jae Kim,Jong Jin Lee,Eung Doo Lee,Hyun Joo Shim,Sang Deuk Lee,Kwang Dae Ok,Won Bae Kim ) 한국약제학회 1997 Journal of Pharmaceutical Investigation Vol.27 No.2
N/A The physicochemical and structural properties of new capsaicin derivative. DA-5018, were examined. The reference standard of this compound was obtained by the recrystallization. A method for the determination of the dissociation constant of the compound is described. pH-solubility and distribution coefficient were determined by chromatographic method. Fundamental properties on thermal behaviors were investigated by TG, DTA and DSC. Structural analysis based on spectroscopic method coincided with the chemical structure of DA-5018. Approximate dissociation constant of the compound determined by UV spectral method was 9.35. Solubilities and partition coefficients in various pH buffer solution appeared pH-dependency. No crystal transition or further transition was found in the thermal analysis. This compound showed good stability, but pH 13 buffer and acetone made some degradative products.
Recombinant Human Erythropoietin (DA-3285) 의 실험동물에서의 약동력학 및 조직분포
심현주(Hyun Joo Shim),이응두(Eung Doo Lee),이종진(Jong Jin Lee),김흥재(Heung Jae Kim),이상득(Sang Deuk Lee),이성희(Sung Hee Lee),김원배(Won Bae Kim),양중익(Junn Ick Yang) 한국응용약물학회 1996 Biomolecules & Therapeutics(구 응용약물학회지) Vol.4 No.1
The pharmacokinetics and tissue distribution of DA-3285 (recombinant human erythropoietin, recently manufactured by Research Laboratories of Dong-A Pharmaceutical Company) were studied in the laboratory animals. The plasma, urine, and tissue concentration of DA-3285 were measured by a double-antibody sandwich enzyme immunoassay. After intravenous administration of DA-3285, 20, 100, 500 and 2500 units/㎏ to rats, the plasma concentrations declined polyexponentially with the terminal half-lives of 2.15, 2.10, 2.31, and 2.35 hr, respectively. Total body clearance (20.7∼26.6 ㎖/hr/㎏) and apparent volume of distribution at steady state (57.2∼70.1 ㎖/㎏) were independent of the dose and AUC increased proportionally with the dose. The renal clearance was much lower than total body clearance, suggesting that extrarenal clearance, presumably metabolism , plays a significant role in elimination of DA-3285. In all rat tissues, the tissue to plasma ratios were smaller than unity, indicating less affinity of DA-3285 to rat tissues and was proved by considerably less value of Vdss. After 3 times a week for consecutive 3 weeks i.v. administration of DA-3285, 100 units/kg to rats, the plasma concentrations and pharmacokinetic parameters of DA-3285 were not significantly different from those in a single administration. After s.c. administration to the rat, plasma concentrations of DA-3285 peaked at 6 hr and the extent of bioavailability was 26.7%. In mice, rabbits and dogs, at DA-3285 dose of 100 units/kg, the mean terminal half-lives were 2.78, 3.05, and 4.01 hr, respectively. Compared with reported data in the literatures, DA-3285 has similar properties to rh-EPO manufactured by other companies in view of pharmacokinetics.
[3H]-메토트렉세이트-락토오스아미노화한 소 혈청 알부민 공유결합체의 간표적성 및 체내동태
김종국(Chong Kook Kim),이응두(Woong Doo Lee),박호군(Ho Koon Park) 대한약학회 1992 약학회지 Vol.36 No.6
The organ distribution of [3H]-methotrexate-lactosaminated bovine serum albumin conjugates ([3H]-MTX-LBSA) was investigated to examine their role as a liver-specific anticancer drug. Synthesis of lactosaminated bovine serum albumin(LBSA) with BSA, lactose and sodium cyanoborohydride through reductive animation was followed by its conjugation with methotrexate (MTX) and 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC), thereby synthesizing [3H]-MTX-LBSA conjugates. Organ distribution and plasma elimination profiles were studied in male Wistar rats after intravenous injection of [3H]-MTX-LBSA conjugates. The fates of [3H]-MTX and the [3H]-MTX-BSA conjugates fates were also investigated for comparison. The results showed that the plasma level of [3H]-MTX-LBSA conjugates declined more rapidly than those of [3H]-MTX-BSA and their liver concentration was significantly higher than those of other treatment (p<0.01). In addition, their uptake compared to the amount taken up by the liver (1 : 33.1 at 10min, 1 : 24.1 at 120min). All these suggested that MTX-LBSA conjugate is one of the drug delivery system (DDS) that is advanced in concentrating MTX in the liver and minimizing the renal toxicity of MTX.
피하주사 및 국소도포시 [14C]DA-5018 의 약동력학
김원배(Won Bae Kim),양중익(Junn Ick Yang),이상득(Sang Deuk Lee),이응두(Eung Doo Lee),심현주(Hyun Joo Shim),이종진(Jong Jin Lee),이명걸(Myung Gull Lee) 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.1
Pharmacokinetics of a new capsaicin analog, DA-5018 were evaluated after a subcutaneous injection or topical application of ^(14)C-labelled or unlabelled DA-5018 to rats and rabbits. After subcutaneous injection of ^(14)C-labelled or unlabelled DA-5018, 0.5 mg/kg (equivalent to DA-5018) to rats, the plasma total activity peaked at 2 hr with the terminal half life of 5.34 hr, however, unlabelled-DA-5018 peaked at 1 hr with the terminal half life of 1.26 hr. Moreover, the AUC (0.726 versus 0.233 ㎍ hr/ml) and MRT (7.82 versus 3.55 hr) increased significantly based on total radioactivity compared with intact DA-5018. Above data indicated that DA-5018 is extensively metabolized in rats and the terminal half- life of the metabolites) had a longer half-life than that of DA-5018. The cumulative percentages of biliary excretion of dose after subcutaneous injection of [^(14)C]DA-5018 was 40.2%, however, the value was only 2.14% when unlabelled DA-5018 was injected. After topical application of 0.1% or 0.3% ^(14)C-labelled or unlabelled DA-5018 cream, 500 mg/kg to rats, the plasma and tissue concentrations except applied skin were under the detection limit. After consecutive 7 days topical application of unlabelled DA-5018, 0.1% and 0.3% cream to rats, the plasma concentrations were also under the detection limit. But the urinary excretion of DA-5018 was significantly increased by repeated topical administration. After topical application of unlabelled DA-5018, 0.1% and 0.3% cream to rabbits, the plasma and urine concentrations were under the detection limit. Above data indicated that the skin permeation of DA5018 was lower and the metabolism of DA-5018 was higher in rabbits than that in rats.
김원배(Won Bae Kim),양중익(Jung Ick Yang),이상득(Sang Deuk Lee),강수형(Soo Hyung Kang),이응두(Eung Doo Lee),심현주(Hyun Joo Shim),이종진(Jong Jin Lee) 한국응용약물학회 1994 Biomolecules & Therapeutics(구 응용약물학회지) Vol.2 No.4
The pharmacokinetics and tissue distribution of DA-3030 (recombinant human granulocyte colony-stimulating factor, rhG-CSF, recently manufactured by Dong-A research laboratory of Dong-A Pharmaceutical Company) were compared with reported data in the literature. After intravenous(i.v.) administration of DA-3030, at dose of 5, 10 and 100 ㎍/㎏ to rats, some pharmacokinetic parameters, such as terminal half-lives(1.05, 1.19 and 1.83 hr, respectively) and clearance (84.0, 54.8 and 45.5 ㎖/hr/㎏, repectively), were dose-dependent. This could be due to the saturable metabolism of DA-3030 in rats. Similar results were also reported. After subcutaneous(s.c.) and intramuscular(i.m.) administrations of DA-3030, 10 ㎍/㎏ to rats, the extent of bioavailability(absolute bioavailability) were incomplete; the values were 23.3 and 18.2% after s.c. and i.m. injections, respectively, due to the degradation of DA-3030 by protease. After 7-consecutive day i.v. administrations of DA-3030, 10 ㎍/㎏/day, to rats, the plasma concentrations and pharmacokinetic parameters of DA-3030 were not significantly different from those in single administration. In mice and dogs at DA-3030 dose of 10 ㎍/㎏, the plasma concentrations of DA-3030 were also declined rapidly with terminal half-lives of 1.31 and 1.15 hr, respectively. DA-3030 was highly concentrated in the kidney after i.v. administration of DA-3030, 10 ㎍/㎏, to rats, and the results were similar to those obtained using radiolabelled rhG-CSF in the literature. Above data indicate that DA-3030 has similar properties to rhG-CSF manufactured by other companies in view of pharmacokinetics.