• Journal of Pharmaceutical Investigation
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• 제34권2호
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• pp.131-138
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• 2004

This study was aimed to investigate the feasibility of nasal delivery of caffeine for the elimination of sleepiness. The effects of various vehicles, solubilizers, and enhancers on the permeation of caffeine through rabbit nasal mucosa was observed. The permeation study was carried out using a Franz-type permeation system at $37^{\circ}C$, and the amount of caffeine permeated though the rabbit nasal mucosa was determined by a validated HPLC. The apparent solubility and phys iochemical stability of caffeine in various nasal formulations were was determined. The effect of hydrotropes and modified cyclodextrins on the solubility of caffeine in water was determined by equilibrium solubility method. The solubility of caffeine in water was 29 mg/mL at $30^{\circ}C$. The addition of sodium benzoate and nicotinamide at 10% improved the solubility of caffeine (115 and 132 mg/mL, respectively) in aqueous solution. The flux of caffeine though the nasal mucosa from aqueous solution was $2.1{\pm}0.26\;mg/cm^2/hr$. The addition of sodium benzoate reduced its permeation $(1.4{\pm}0.01\;mg/cm^2/hr)$, but sodium benzoate with 5% $2HP{\beta}CD$ and 0.03% monoterpenes increased its permeation $(2.4{\pm}0.04\;mg/cm^2/hr)$ markedly. The addition of nicotinamide also increased also increased its permeation $(2.5{\pm}0.36\;mg/cm^2/hr)$. markedly. As the concentration of caffeine in nasal formulation increased, the permeation flux increased linearly. Caffeine was stable physicochemically and enzymatically in the nasal mucosa extract at $37^{\circ}C$. These results suggest that caffeine can be efficiently delivered nasally and the development of nasal formulation will be feasible.

• 대한화장품학회지
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• 제23권3호
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• pp.108-114
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• 1997

The skin permeation study has two meanings in cosmetics. One is how to promote the skin permeation of active meterials for improving their bioavailabilities and the other is how to decrease it of irritants for reducing their skin side effects. In this study, we selected methyl paraben, one of the preservatives, as a model irritant and tried to reduce the skin irritation by the decrease of skin permeation. Furthermore, the relationship between skin permeation and skin primary irritation was discussed. For in vitro skin permeation experiments, Franz type diffusion cells and the excised skin of female hairless mouse from 8 weeks old were used. The donor compartment was charged with oil only or O/W emulsion containing 0.3% MP. We selected 19 oils, including esters, triglycerides, plant oils, hydrocarbons, and alchols, which are broadly used in cosmetics. We evaluated with female guinea pig. The skin permeahility of MP from the oils showed following order: ester oils > triglycerides > plant oils > hydrocarbons > alcohols. We considered that this result was based on the different effect of each oil on the barrier function of stratum corneum. In O/W emulsion containing each oil, the skin permeability of MP decreased as the oil/water partition coefficient of MP increased. The skin primary irritation increased as the skin permeability of MP increased. In conclusion, we suggest that the skin irritation could be reduced by the decrease of skin permeability of MP, which may be obtained by the good selection of oils in cosmetic preparations.

• Journal of Pharmaceutical Investigation
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• 제29권2호
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• pp.137-143
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• 1999

Ketoprofen together with various permeation enhancers was incorporated into a novel soft hydrogel which is semi-solid in a container and to form a thin film within a few minutes after applying on the skin. The effect of various enhancers on the skin permeation of ketoprofen from a soft hydrogel was investigated using in vitro and in vivo method. In vitro rat skin permeation of ketoprofen from soft hydrogel was conducted using modified Keshary-Chien diffusion cells. In vivo ketoprofen absorption was also investigated in rats, and the results were compared with that of commercial products. Anti-inflammatory activities were determined using carrageenan-induced paw edema method and adjuvant-induced arthritis method in rats. The anti-inflammatory activity of ketoprofen soft hydrogel formulation with that of commercial products were compared. In vitro as well as in vivo studies showed that $HPE-101^{\circledR}$ was the most effective skin permeation enhancer among those used in this study. Addition of an adhesive (polyisobutylene) in the soft hydrogel decreased skin permeation of ketoprofen. Paw edema and anti-arthritis tests showed that soft hydrogel containing $HPE-101^{\circledR}$ was more effective than the commercial products, which was consistent with the in vivo absorption experiment results.

• 멤브레인
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• 제9권1호
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• pp.43-50
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• 1999

폴리설폰 중공사막에 대한 산소와 질소의 투과도에 미치는 수분의 영향에 대한 실험을 수행하였다. 상대습도가 증가할수록 수분을 함유한 산소와 질소의 투과도는 감소하였따. 공급압력 3 kgf/$cm^2$와 온도 3$0^{\circ}C$에서, 상대습도 100% 인 산소의 투과도는 건조산소의 투과도보다 20%만큼 감소하였으며, 질소는 14%만틈 감소하였다. 수분을 gkadmb한 산소의 투과도는 운전시간이 경과함에 따라 단조하게 감소하여 정상상태에 도달하였다. 그러나, 질소의 투과도는 일시적으로 증가하였다가 감소하여 정상상태에 도달하였다.

• Archives of Pharmacal Research
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• 제27권7호
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• pp.763-768
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• 2004

To investigate the feasibility of developing a new quercetin transdermal system, a preformulation study was carried out. Therefore, the effects of vehicles and pressure-sensitive adhesives (PSA) on the in vitro permeation of quercetin across dorsal hairless mouse skin were studied. Among vehicles used, propylene glycol monocaprylate (PGMC) and propylene glycol mono-laurate were found to have relatively high permeation flux from solution formulation (i.e., the permeation fluxes were 17.25$\pm$1.96 and 9.60$\pm$3.87 $\mu\textrm{g}$/$\textrm{cm}^2$/h, respectively). The release rate from PSA formulations followed a matrix-controlled diffusion model and was mainly affected by the amount of PSA and drug loaded. The overall permeation fluxes from PSA formulations were less than 0.30 $\mu\textrm{g}$/$\textrm{cm}^2$/h, which were significantly lower compared to those obtained from solution formulations. The lower permeation fluxes may be due to the decrease of solubility and diffusivity of quercetin in the PSA layer, considering the fact that the highest flux of 0.26 $\mu\textrm{g}$/$\textrm{cm}^2$/h was obtained with the addition of 0.2％ butylated hydroxyanisole in PGMC-diethyl-ene glycol monoethyl ether co-solvents (80-85 ： 15-20, v/v). Taken together, these observations indicate that improvement in the solubility and diffusivity of quercetin is necessary to realize fully the clinically applicable transdermal delivery system for the drug.

• Journal of Pharmaceutical Investigation
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• 제36권5호
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• pp.299-304
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• 2006

The aim of this study was to investigate the effect of deformable liposomes with sodium cholate on the skin permeation and skin deposition of arbutin, a hydrophilic skin-whitening agent. Various compositions of liposomes were prepared by the extrusion method. Particle size distribution and entrapment efficiency were determined by the laser light scattering and the gel permeation chromatography, respectively. The in vitro rat skin permeation and deposition of arbutin in various skin layers were investigated using the Keshary-Chien diffusion cells at $37^{\circ}C$. The average particle size of the deformable liposomes ranged from 217.4 to 117.4 nm, depending on the composition. The entrapment efficiency was dependent on surfactant concentration and loading dose of arbutin. The permeation rate of 5% arbutin in deformable liposomes was $8.91({\pm}1.33){\mu}g/cm^2/h$, and was not significantly different from 5% arbutin aqueous solution $[9.82({\m}0.86){\mu}g/cm^2/h]$. The deposition of arbutin was $43.34({\pm}12.13)$ and $16.99({\pm}7.83){\mu}g/cm^2$ in stratum corneum layer and epidermis/dermis layer, respectively, after 12 h of permeation study. These results are consistent with several earlier studies for the localization effect of liposomal formulations in stratum corneum, and demonstrated the feasibility of the deformable liposomes as a promising carrier for the skin deposition of hydrophilic skin-whitening compounds.

• 멤브레인
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• 제19권4호
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• pp.285-290
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• 2009

공칭 세공크기 $0.1\;{\mu}m$이고 내경이 5 mm인 정밀여과용 관형 분리막 내에 자체 설계한 배출봉을 삽입하여 막오염 감소효과에 따른 투과유속을 측정하였다. 원료용액으로는 에멀젼 상태의 dioctyl tinoxide (DOTO) 입자를 사용하였으며 0.5 wt%까지 농도를 변화시키면서 1.6 bar 이내에서 운전하였다. 배출봉의 효과는 매 실험마다 배출봉을 삽입한 경우와 사용하지 않은 경우의 투과유속을 비교하여 평가하였다. 배출봉을 사용할 경우 운전압력 1.6 bar에서 최대 20%의 투과유속이 향상되었다. 또한 DOTO 농도가 증가함에 따라서 배출봉에 의한 투과유속 향상효과는 크게 나타났으며 0.5 wt% 농도에서 43%까지 투과유속이 향상되었다.

• Journal of Pharmaceutical Investigation
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• 제27권1호
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• pp.65-69
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• 1997

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.

• 멤브레인
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• 제10권3호
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• pp.148-154
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• 2000

본 연구에서는 sulfur-succinic acid의 가교제를 이용한 가교된 폴리비닐알코올(poly(vinyl alcohol), PVA) 가교막을 이용하여 MTBE-methanol 혼합액에 대하여 조업온도, 가교제의 조성에 따른 증기투과 공정의 투과 특성을 조사 하였다. 팽윤 실험을 통해 PVA/SSA 가교막에 대하여 가교제 조성에 따른 막의 구조와 PVA의 하이드록실기(-OH), SSA의 설폰기(-$SO_3$H)와 용매와의 수소결합의 두 가지 인자가 상호 보완적으로 작용하고 있음을 알 수 있었다. 투과 특성에 있어 SSA의 설폰기가 중요한 인자로 작용하였다. 예를 들면 7% SSA 막에 대해서는 수소결합의 효과보다는 가교도의 효과가 투과 특성에 중요한 요인으로 작용하며 5% SSA에 대해서는 수소결합의 효과가 중요하게 작용하였다. 증기투과 공정에 있어 막과 직접 접촉하는 증기상이 액상에 비하여 methanol의 농도가 낮아 PVA의 하이드록실기와 methanol과의 수소결합 확률이 감소함에 따라 투과 특성에 영향을 미친다. 결과적으로 7% SSA 막에 대하여 MTBE/mthanol=80/20 혼합액에 대하여 공급액의 온도 3$0^{\circ}C$에서 선택도 2187, 투과도 4.84g/$m^2$hr를 보여 주었다.

• 열처리공학회지
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• 제13권3호
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• pp.151-157
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• 2000

This study aims to investigate the effect of carbon content on the surface nitrogen permeation of 13%Cr-1.8%Al alloyed stainless steels. The surface nitrogen permeation was performed at $1050^{\circ}C{\sim}1200^{\circ}C$ in the $1kg/cm^2$ nitrogen gas atmosphere. The nitrogen permeated surface layer of the specimen containing 0.03%C consists of AlN, martensite and retained austenite phases. while the surface layer of the specimen containing 0.14%C appears the $AlFe_3C_x$ phase including former three phases. The specimen containing 0.14%C shows lower total case depth than that containing 0.03%C at the nitrogen permeation temperatures of $1050^{\circ}C$ and $1100^{\circ}C$, while the total case depth of the specimen containing 0.14%C is remarkably increased at the temperature of $1150^{\circ}C$ and $1200^{\circ}C$ due to the increase in the retained austenite content. Martensitic phase, AlN and $AlFe_3C_x$ precipitate of the nitrogen permeated surface layer cause to increase the surface hardness of 550~600Hv.