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오승열 한국약제학회 1996 Journal of Pharmaceutical Investigation Vol.26 No.3
The kinetic change of electrical resistance of hairless mouse skin as a function of ionic strength of the bathing medium was determined from impedance measurements. After increasing (decreasing) the ionic strength of the bathing medium, resistance decreased (increased) continuously with time, finally reaching an equilibrium value. We have modelled this process, using nonsteady-state diffusion kinetics. The results show semi-quantitative correlation between theoretically derived and experimentally obtained values. Overall, this work provides further mechanistic insight into ion-conduction through the skin.
오승열 한국약제학회 2004 Journal of Pharmaceutical Investigation Vol.34 No.6
We investigated some important factors which affect the transdennal flux of ketoprofen. a nonsteroidal anti-inflammatory agent, as a first step to provide some basic knowledge for the development of a iontophoretic transdermal patch system. Factors such as current density. polarity. buffer (HEPES) and electrolyte concentration and pH were studied using hairless mouse skin. The effect of polv(L-lvsin). which is known to affect the electro-osmotic flow through skin, on flux was also studied. Passive flux was about 20 μg/cm²hr at pH 4.0. but was negligible at pH 7.4 where all ketoprofen molecules dissolved are ionized (ketoprofen pKa°5.94). At pH 4.0. application of anodal current increased the flux further above the passive level. however anodal flux at pH 7.4 was much smaller than passive flux at pH 4.0. The application of cathodal current at pH 4.0 increased the average flux to 30 - 40 μg/cm²hr. depending on the current density applied. At pH 7.4. cathodal flux was only about 5 μg/cm²hr. Decrease in butler and electrolyte concentration increased this cathodal flux about 10 fold. However decrease in HEPES buffer concentration 100 fold did not affect the flux. Anodal flux of acetaminophen was much larger than cathodal flux. indicating that electroosmotic flow can be playing an important role in the flux. Poly(L-lvsin) increased the cathodal flux at pH 7.4. These results provide some important insights into the mechanism of trans-dermal flux of ketoprofen and the role of electroosmotic flow.
김정애,오승열 한국약제학회 2004 Journal of Pharmaceutical Investigation Vol.34 No.4
We have studied the effect of polarity, current density, current duration, crosslinking density, swelling ratio, and permeation enhancers on the transdermal flux of ketoprofen from acrylamide hydrogel. Hydrogel was prepared by free radical crosslinking polymerization of acrylamide. Drug loading was made just before transport experiment by soaking the hydrogel in solution containing drug. In vitro flux study using hairless mouse skin was performed at 36.5℃ using side-byside diffusion cell, and the drug was analysed using HPLC/UV system. The result showed that, compared to passive flux, the total amount of drug transported increased about 18 folds by the application of 0.4 mA/㎠ cathodal current. Anodal delivery with same current density also increased the total amount of drug transported about 13 folds. It seemed that the increase in flux was due to the electrorepulsion and the increase in passive permeability of the skin by the current application. Flux increased as current density, the duration of current application and loading amount (swelling duration) increased. As the crosslinking density of the hydrogel increased, flux clearly decreased. The effect of hydrophilic enhancers (urea, N-methyl pyrrolidone, Tween 20) and some hydrophobic enhancers (propylene glycol monolaurate and isopropyl myristate) was minimal. However, about 3 folds increase in flux was observed when 5% oleic acid was used. Overall, these results provide some useful information on the design of an optimized iontophoretic delivery system of ketoprofen.
최보경,오승열 한국약제학회 2001 Journal of Pharmaceutical Investigation Vol.31 No.4
The purpose of this study is to characterize the iontophoretic transport of growth hormone releasing peptides (GHRP-6) through hairless mouse skin from aqueous solution. The effect of various factors, such as pH, poloarity, current profile, current density, current duration, ionic strength, drug concentration, and enhancer application was studied to obtain basic knowledge on the transport. We have also studied the stability of GHRP-6 in solution with/without current. The donor chamber was filled with phosphate buffer solution containing GHRP-6 and the receptor chamber was filled with phosphate buffer solution (pH 7.4). Ag/AgCl electrode was used for their stability and reversibility. At a predetermined time interval, sampling was made and the concentration of drug was analysed using HPLC system. The results showed that, compared to passive flux, the total amount of drug transported increased markedly by the application of anodal current. Cathodal flux was similar to passive flux. Flux increased with the current density, the duration of current application and drug concentration. The effect of enhancers on the flux was studied using hydrophilic (5% N-methyl pyrrolidone) and hydrophobic (5% propylene glycol monolaurate, 5% oleic acid) enhancers. Application of enhancer also increased the flux.
Iontophoresis 를 이용한 NADPH 의 피부투과 및피부자극
이승연,오승열 숙명여자대학교 약학연구소 2004 약학논문집-숙명여자대학교 Vol.20 No.-
Nicotinamide Adenine Dinucleotide Phosphate (NADPH) has antioxidant effect in the body and thus decreases the symptoms of senility. The delivery of NADPH through skin is a formidable challenge due to its physical and chemical properties (such as rapid decomposition by oxidation, low partition coefficient in stratum corneum, high molecular weight and charge). The purpose of this work is to prepare a hydrogel patch system containing NADPH, and to study its in-vitro iontophoretic transport through hairless mouse skin. We have investigated two factors (concentration of NADPH and current density) that can affect the iontophoretic flux. The stability of NADPH in aqueous solution and the possible skin irritation by iontophoretic delivery of NADPH was also investigated. The results showed that, compared to passive flux, the total amount of NADPH transported increased by the application of cathodal current. Anodal flux was similar to passive flux. Flux increase was proportional to the concentration of NADPH in the donor solution and to the current density. Nearly 50 % of NADPH degraded during the experimental period in aqueous solution. The results of primary irritatation test showed no erythema or edema after iontophorsis. These results suggest that therapeutic amount of NADPH can be delivered through skin using iontophoresis, without any development of erythema or edema.
이정화,오승열 한국약제학회 2005 Journal of Pharmaceutical Investigation Vol.35 No.2
We have prepared karaya gum patches containing ketoprofen and investigated the effect of short-time cur-rent pretreatment of skin on the permeability. Hairless mouse skin was treated with current before the patch was mounted on the skin. The effect of current density and current duration on the flux of ketoprofen was studied. The possibility of additive effect with penetration enhancer (PGML) was also investigated. lontophoretic pretreatment of skin increased the passive flux up to 3 folds at 0.4 mA/cm² current density, when the matrix contained no PGML. As the duration of current-pretreatment and current density increased, flux increased. PGML increased the average passive flux markedly, about 6 to 12 folds, depending on the concentration in the patch. Current pretreatment further increased the flux from this PGML containing patch, exhibiting additive effect. These results indicate that short-duration current pretreatment of skin can be an useful method for the enhancement of ketoprofen permeability through skin.
수용성 및 지용성 피부투과증진제의 피부의 전기적 성질에 미치는 영향
손미현,오승열 숙명여자대학교 약학연구소 2005 약학논문집-숙명여자대학교 Vol.22 No.-
무모생쥐 피부의 전기적 임피던스를 교류 주파수의 함수로 측정 한 후 Nyquist plot을 이용하여 전기적 저항 및 축전력을 계산하였으며 이 방법에 의해 수용성 (프로필렌 글리콜 및 에탄올) 및 지용성 (propylene glycol monolaurate, isopropyl mirystate) 투과증진제가 피부의 전기적 성질에 미치는 영향을 연구하였다. 피부에 각투과증진제를 적용하여 1시간동안 neat 처리를 한후시간에 따른 전기저항 및축전력의 변화를 8시간 동안조사하였다.수용성 투과증진제의 경우 neat 처리 후 바로측정하였을때 전기저항이 감소하였으나시간에 따라 점차 회복하였으며 축전력도 점차 증가하였다. 이 같은 전기저항의 증가는 피부 내로 투과되었던 수용성 투과증진제들이 용액으로 다시 용출되어 나오는 것에 기인된다고 사료된다.지용성 투과증진제의 경우전기저항은크게 감소하였고 축전력은 크게 증가하였다. 그러나 수용성 투과증진제의 경우에서와 같은 시간에 따른 큰 변화는 관찰되지 않았는데 이는 이틀 지용성 투과증진제의 경우 일단 피부 각질층 내로 투과된 후 시간에 따라 각질층 밖으로 역확산되어 나오지 않기 때문이라고 생각된다. 축전력의 증가는 각질층 내의 지질의 질서도감소에 의한유전상수의 증가때문으로사료되며 이상의 결과는 각질층이 피부의 전기적 성절에 미치는 역할에 대한 기초적인 자료를 제공하고 있다.
케토프로펜-폴리에틸렌글리콜 전구약물의 합성 및 가수분해
이세희,김희두,오승열 한국약제학회 2003 Journal of Pharmaceutical Investigation Vol.33 No.1
The objective of this study is to prepare ketoprofen (KP) - poly(ethylene glycol) (PEG) conjugates and to investigate their degradation kinetics. KP-PEG conjugates were synthesized from KP and PEG methylester by esterification in the presence of DCC. The KP-PEG conjugates (KPEG) were characterized by IR and ^1H-NMR spectroscopy. The hydrolysis of KPEG with time was studied using HPLC by simultaneous quantification of KP and KPEG. The hydrolysis rate constant was high at low and high pHs, and showed minimum at pH 4 and 5. As the size of KPEG increase, hydrolysis rate increased. The slope of degradation rate profile suggests that catalytic reaction seems to occur by specific acid/base catalysis. These results suggest that KPEG could be used as a prodrug for KP, which releases KP slowly in the body.
새로운 Celecoxib 전구체 약물의 가수분해와 체내동태 연구
민혜란,김희두,오승열 숙명여자대학교 약학연구소 2006 약학논문집-숙명여자대학교 Vol.23 No.-
난용성 약물인 세례콕시보의 용해도를 개선하고 서방성을 중진하기 위해 세레콕시브의 benzenesulfonamide ring을 수식한 전구체 약물(PCX)을 합성하여 그 가능성을 알아보고자 하였다. 우선 이들의 용해도를 알아보기 위하여 PEG 400을 보조 용매로 하여,생리 식염수와 인공 위액,인공장액에서의 용해도를 확인하였다. 또 한 쥐의 혈장,간 그리고 장에서의 in vitro 가수분해 실험을 통하여 각 약물이 모약물인 세레콕시보로 분해되는 것을 확인할 수 있었다. 용해도와 가수분해 결과를 바탕으로 하여 세례콕시브와 PCX의 약동학 실험을 실시하였다. 세례콕시브와 PCX(세레콕시브로서 50 ㎎/㎏ 용량)를 쥐의 경구와 정맥으로 투여하여 혈중 농도변화를 알아보았다. 경구투여 결과, PCX은 세례콕시브보다 혈중 농도는 낮으나 소실속도가 현저히 저하되었다. 세례콕시브의 경우, C_(max)는 1.89 ± 0.79 ㎍/㎖였으며,이에 비하여 PCX은 0.41 ± 0.14 ㎍/㎖을 나타내었다. k_(el)의 경우, PCX은 0.05 ± 0.01 hr^(-1)로 세례콕시브 (0.15 ± 0.06 hr^(-1))보다 약물소실속도가 저하되었다. 이상의 실험결과는 향후 세레콕시브 전구체 약물의 체내동태 연구와 개발에 도움이 될 것으로 기대된다.
NADPH의 안정화 및 이온토포레시스를 이용한 피부투과
신현택,이승연,오승열 숙명여자대학교 약학연구소 2005 약학논문집-숙명여자대학교 Vol.22 No.-
Nicotinamide Adenine Dinucleotide Phosphate (NADPH) has antioxidant effect in the body and thus decreases the symptoms of senility. The development of a transdermal delivery formulation for NADPH is a very difficult task, due to its rapid decomposition by oxidation, low partition coefficient into stratum corneum, high molecular weight and electrical charge at neutral pH in aqueous solution. The purpose of this work is to test several anti-oxidants as the stabilizing agent for NADPH in the aqueous formulation, and to study the effect of these agents on the in-vitro iontophoretic transport through hairless mouse skin. The stability of NADPH in aqueous solution with/without various antioxidants such as butylated hydroxy toluene (BHT), resveratrol, a-tocopherol and Vitamine C was studied. BHT an a-tocopherol (0.01 % w/w) exhibited minimal stabilizing effect, however resveratrol and vitamine C showed significant stabilizing effect. Stabilizing effect of vitamine C was proportional to the concentration in aqueous solution. Although vitamine C increased the stability ofNADPH significantly, it decreased flux of NADPH in a concentration dependent fashion, therapeutic amount ofNADPH can be delivered through skin using iontophoresis and These results suggest that, in order to develope a efficient iontophoresis formulation, it is important to choose a stabilizing agents which are not only potent in stabilizing effect but also not competitive for the delivery of NADPH.