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Studies on Synthesis, Hydrolysis and Oral Absorption of Piperacillin Phthalidyl Ester
박기배,최승호,최영욱,김종갑,Park, Gee-Bae,Choi, Seung-Ho,Choi, Young-Wook,Kim, Johng-Kap 한국약제학회 1988 Journal of Pharmaceutical Investigation Vol.18 No.3
Piperacillin phthalidyl ester was synthesized by reacting piperacillin with triethylamine and bromophthalide in acetone and its chemical structure was determined by UV, IR, and PMR. The partition coefficient of the ester was increased and the ester was more lipophilic and less water soluble than piperacillin. The ester did not show the antimicrobial activity against Bacillus subtilis ATCC 6633 in vitro, but when hydrolyzed, the parent drug of ester, piperacillin, revealed antimicrobial activity in vivo. After a single oral dose of both piperacillin and the ester to rabbits, the serum piperacillin concentration was measured by bioassay. The ester exhibited improved pharmatokinetic characteristics: $T_{max}\;of\;2hr,\;C_{max}\;of\;4.26{\mu}g{\cdot}ml^{-1},K_{el}\;of\;0.057hr^{-1},\;and\;total\;AUC\;of\;85.42{\mu}g{\cdot}hr{\cdot}ml^{-1}$. Piperacillin on the other hand, did not exhibit any gastro-intestinal absorption.
토끼에서 아세트아미노펜 연질캅셀제의 생체이용율에 미치는 제제처방들의 영향
박기배(Gee Bae Park),이용석(Yong Suk Lee),최명호(Myung Ho Choi),이도익(Do Ik Lee),이광표(Kwang Pyo Lee) 대한약학회 1992 약학회지 Vol.36 No.6
The purpose of this study was to assess the effect of three formulations; product A (polyethylene glycol was used as a main dispersing agent), product B (wax mixture was used as a main dispersing agent) and product C((silicon dioxide was used as a main dispersing agent) on bioavailability of acetaminophen soft gelatin capsules(softgels) and to develop an effective acetaminophen softgel which exhibits an excellent bioavailability. Acetaminophen softgels of various formulations were prepared as 4 minim round type by rotary die method. Four softgels of the three formulation (A, B, C), each of which contained 50 mg acetaminophen, were administered orally to 12 normal healthy rabbits using a three-way cross over design. Plasma acetaminophen concentrations were measured by HPLC. The results obtained in this study were as follows: 1. The Tmax rank order of acetaminophen softgel was C(63.75 +/- 10.62 min) > A(36.25 +/- 5.37 min) > B(35 +/- 6.74 min). 2. The decreasing Cmax order of softgel product was A(93,51 +/- 0.55 mcg/ml) > B(3.16 +/- 0.37 mcg/ml) > C(2.6 +/- 0.55 mcg/ml). 3.The [AUC]0infinite rank order for three acetaminophen softgel formulations was A (14.89 +/- 1.56mcg/ml.min) > B(14.39 +/- 1.43 mcg/ml.min) > C(11.45 +/- 1.49mcg/ml.min). 4. Pharmacokinetic parameters such as Tmax, Cmax and [AUC]0infinite of product A and B did not differ significantly(p>0.05). On the other hand, those of product C were significantly different(p>0.05).
박기배(Gee Bae Park),노현구(Hyun Goo Roh),이광표(Kwang Pyo Lee) 대한약학회 1994 약학회지 Vol.38 No.2
A study on the absorption mechanism of cefixime(CF), an oral alpha-amino group deficient cephalosporin antibiotic, has been undertaken through the rat jejunum and nasal cavity using an in situ simultaneous perfusion technique developed in our laboratory. CF was well absorbed in the jejunum and nasal cavity of rats at pH 5.0, but not at pH 7.0. CF absorption was studied over four orders of magnitude in concentration to determine saturability. Disappearance of CF in the perfusate followed first-order kinetics at all tested concentrations. The apparent first-order absorption rate constant was found to be dependent on the concentration over the range of 0.1mM-3mM in the jejunum and nasal cavity of rats. Inhibitors were added to determine the competitive inhibition of CF absorption. The presence of L-tyrosine, L-phenylalanine, alanine-alanine, glycine-glycine and cefadroxil produced the significant inhibition of CF absorption in the nasal cavity and jejunum. However, there was no evidence of the inhibition in the presence of cefazolin. In addition, The CF absorption in the nasal cavity and jejunum was inhibited significantly by ouabain and 2,4-dinitrophenol(DNP). This study suggested that CF is absorbed across the rat nasal cavity and jejunum by carrier-mediated transport mechanism and energy consuming system.
시메티딘 및 제산제가 미노싸이클린의 약물동태에 미치는 영향
정의차,박기배,신화우,최영욱,이광표,Jung, Eui-Cha,Park, Gee-Bae,Shin, Hwa-Woo,Choi, Young-Wook,Lee, Kwang-Pyo 한국약제학회 1991 Journal of Pharmaceutical Investigation Vol.21 No.4
Effects of aluminum magnesium hydroxide (A) and cimetidine (C) on the pharmacokinetics of minocycline (M) were investigated in female rats. Blood samples were collected at various time intervals until 36 hrs following oral dosing of drugs. Plasma minocycline concentrations were determined by HPLC. Control group (M), $T_1$ group (M+A), $T_2$ group (A+M after 2 hrs), $T_3$ group (M+A after 2 hrs), $T_4$ group (M+C) and $T_5$ group (C+M after 2 hrs) were divided to examine interaction of the drugs with minocycline. Plasma minocyline level-time curves were well described by two-compartment open model with first-order absorption in rats. Antacid treatment was associated with reduced of 71.0, 45.9, 35.7% in minocycline absorption rate $constant(K_{\alpha})$, maximum plasma $concentration(C_{max})$, and relative $bioavailability(F_{rel})$, respectively. Cimetidine treatment group exhibited no significant changes in plasma level-time curve when compared with control group and did not affect minocycline absorption as by any of these three parameters.
랫트에 있어서 시프로플록사신의 흡수와 생체이용율에 미치는 돔페리돈, 스코폴라민부틸브로마이드 및 시메티딘의 영향
임혜숙,박기배,이도익,이광표,Yim, Hye-Suk,Park, Gee-Bae,Lee, Do-Ike,Lee, Kwang-Pyo 한국약제학회 1992 Journal of Pharmaceutical Investigation Vol.22 No.2
The effects of domperidone, scopolamine butylbromide and cimetidine on the absorption and bioavailability of ciprofloxacin were studied in female rats. Ciprofloxacin was given in a single oral dose of 30 mg/kg to control group. Ciprofloxacin was concurrently administered with domperidone $(T_1\;group)$, scopolamine butylbromide $(T_2\;group)$, and cimetidine $(T_3\;group)$ to rats, respectively. Significantly changed pharmacokinetic parameters observed in $T_2$group when compared with control group were first-order absorption rate constant, $Ka(4.43{\pm}0.85$\;versus\;2.86{\pm}0.41\;hr^{-1},\;p<0.05)$, time needed to reach peak concentration, $T_{max}\;(32.27{\pm}2.46\;versus\;51.75{\pm}5.51\;min,\;p<0.05)$, area under the plasma concentration-time curve, AUC $(332{\pm}19\;versus\;477{\pm}27\;{\mu}g{\cdot}min/ml,\;p<0.05)$ and absolute bioavailability, Fabs $(60.6{\pm}3.6\;versus\;87.0{\pm}5.0%,\;p<0.05)$. On the other hand, domperidone and cimetidine did not significantly affect the absorption of ciprofloxacin. It is suggested that when scopolamine butylbromide is selected for clinical use, there is need for awareness of the reduction in absorption rate and the enhancement in absorption extent of ciprofloxacin.
Oral Absorption of Cefoperazone Pivaloyloxymethyl Ester
최영욱,박기배,최승호,김종갑,Choi, Young-Wook,Park, Gee-Bae,Choi, Seung-Ho,Kim, Johng-Kap 한국약제학회 1988 Journal of Pharmaceutical Investigation Vol.18 No.4
Pivaloyloxymethyl ester of cefoperazone was synthesized by treating sodium cefoperazone with chloromethyl pivalate and its chemical structure was determined by spectroscopic trials. The pharmaceutical properties of the ester were investigated to assess its potential as a prodrug of cefo perazone. Cefoperazone pivaloyloxymethyl ester was microbiologically inactive itself in vitro, but hydrolyzed into the parent drug in vivo. After a single oral dose of each drug to rabbits, serum concentrations of cefoperazone were determined by high performance liquid chromatographic assay. The ester showed higher and more sustained blood level than cefoperazone. Therefore, the total area under the serum concentration-time curve of the derivative was 16.8 times larger than that of the parent drug.
Absorption of Itraconazole from Rat Small Intestine
김영화,이용석,박기배,이광표,Kim, Young-Hwa,Lee, Yong-Suk,Park, Gee-Bae,Lee, Kwang-Pyo 한국약제학회 1991 Journal of Pharmaceutical Investigation Vol.21 No.4
The absorption characteristics of itraconazole, which is an antifungal agent, from intestinal segments in the anesthetized rat i1l situ were investigated in order to design an effective oral drug delivery system. The pH-solubility profile of itraconazole, the rate and extent of absorption of itraconazole, the optimal absorption site(s) of itraconazole and the absorption enhancing effect of sodium cholate on itraconazole were examined in the present study. In situ single-pass perfusion method and recirculating perfusion technique using duodenum(D), jejunum(J) and ileum(I) were employed for the calculation of apparent permeability(Pe) and apparent first-order rate constant(Kobs). respectively. The results of this study were as follows; (1) Itraconazole showed appreciable aqueous solubility only at pH values of below 2.0. (2) pe(cm/sec) decreased in the following order: $D(10.24{\pm}1.78{\times}10^{-4})>J(8.86{\pm}0.79{\times}10^{-4})>I(3.78{\pm}0.13 X 10^{-4})$. (3) $Kobs(min^{-1})$ decreased in the following order: $J(17.12{\pm}3.19{\times}10^{-3})>D(13.37{\pm}0.6{\times}10^{-3})>I(11.05{\pm}0.91{\times}10^{-3})$. (4) The solubility of itraconazole markedly increased with the increase of the concentration of sodium cholate. (5) The addition of 10 mM sodium cholate significantly increased the apparent first-order rate constant of itraconazole in the ileum by a factor of 6.8.