• Journal of Pharmaceutical Investigation
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• 제32권4호
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• pp.313-319
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• 2002

Rat skin permeation of various nonsteroidal antiinflammatory drugs (NSAIDs) was investigated in vitro using Franz diffusion cell at $37^{\circ}C$. The effect of various skin permeation enhancers was also observed as a preliminary study of developing transdermal delivery systems of NSAIDs. Lipophilicity of NSAIDs was determined from thε partition coefficient (log P) in 1-octanol/water and 1-octanol/IPB mutual-saturated solutions. The solubility was determined in water, isotonic phosphate buffer (IPB), and propylene glycol (PG) at $37^{\circ}C$. The rat skin permeation rate of acetaminophen, piroxicam, and aceclofenac was almost negligible, although they were saturated in PG. Addition of 1 % permeation enhancer increased the permeation rate of ketoprofen, ketorolac, and diclofenac. However, the skin permeation rate of ibuprofen did not increase with the addition of various enhancers. Among the permeation enhancers testεd, oleic acid was the most effective for various NSAIDs. Based on the daily dose, lipophilicity, and the skin permeation ratε achieved in this study, ketoprofen and ketorolac seem to be the most promising drug candidates for transdermal delivery systems, especially when formulated with unsaturated fatty acids, such as oleic acid.

• Korean Membrane Journal
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• 제7권1호
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• pp.19-27
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• 2005

PP hollow fiber membrane was hydrophilized by EVOH dip coating followed by low temperature plasma treatment and UV irradiation. EVOH coating attained high water flux without any prewetting but its stability did not guaranteed at high water permeation rate. At high water permeation rate, water flux declined gradually due to swelling and delamination of the EVOH coating layer causing pore blocking effect. However, plasma treatment reduces the swelling, which suppress delamination of the EVOH coating layer from PP support result in relieving the flux decline. Also, UV irradiation helped the crosslinking of the EVOH coating layer to enhance the performance at low water permeation rate. FT-IR and ESCA analyses reveal that EVOH dip coating performed homogeneously through not only membrane surface but also matrix. Thermogram of EVOH film modified plasma treatment and W irradiation show that crosslinking density of EVOH layer increased. Chemical modification by plasma treatment and UV irradiation stabilized the hydrophilic coating layer to increase the critical flux of the submerged membrane.

• Korean Membrane Journal
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• 제1권1호
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• pp.73-80
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• 1999

The removal of trace chlorinated and aromatic hydrocarbons from water by a pervaporation technique has been carried out through poly (dimethylsiloxane) membrane which had been fabricated by the addition crosslinking reaction. This study dealt with the swelling and permeation behaviors of the PDMS membranes with dichloroethane trichloroethane and toluene aqueous solutions. The swelling ratio in the toluene aqueous solution was much higher than those in the chloroethane solutions at all of the operating temperatures and concentrations. The solubility parameter theory was introduced to interpret the affinity between permeates and a membrane material and in all cases this approach seemed to be proper. It was suggested that the existence of water clusters in the membrane due to the hydrophobic characteristics of the membrane made the size of the permeating water larger resulting in suppressing water permeation and increasing enrichment of the organic components. The permeation behaviors at different membrane thicknesses were indirectly interpreted in terms of the effect of concentration polarization.

• 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.

• Journal of Pharmaceutical Investigation
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• 제26권2호
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• pp.99-103
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• 1996

Effects of glycerin and PEG 400 in donor and receptor solutions upon skin permeation of drug were investigated. Deoxycortisone was used as a model compound. In vitro skin permeation study with freshly excised hairless mouse skin was performed and the steady-state skin permeation rates of the drug were determined in different fractions of glycerin or PEG 400 in donor and receptor solutions. Glycerin in donor solution didn't show any effect on the skin permeation rate of deoxycortisone. However glycerin in receptor solution showed significant effect on the skin permeation rate of the drug. In glycerin, there's a critical concentration for balancing hydration and dehydration of skin. At low concentration, less than 20 %, glycerin showed the enhancement of the flux due to the hydration effect of skin. At high concentration, more than 30 %, glycerin retard the permeation rate which might be due to the dehydration effect on the dermis layer. Since dermis has more water content than the stratum corneum, the steady state skin permeation rates were more influenced when glycerin was in receptor solution than that of in donor solution. PEG 400 aqueous solutions doesn't affect the steady state permeation rate of deoxycortisone significantly.

• 멤브레인
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• 제6권4호
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• pp.227-235
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• 1996

PVA의 수산화기와 PAA의 카르복실산기 사이의 반응에 의해 가교구조를 갖는 PAA-PVA 막을 제조하였으며 팽윤실험을 통해 순수물, 순수초산 그리고 이들의 혼합물하에서의 가교막들의 팽윤거동을 각각 살펴보았다. 90wt% 초산 수용액하에서의 팽윤실험에서 막에 PAA함량이 높을때 물의 팽윤거동이 초산보다 더 촉진됨이 관찰되었는데 이는 팽윤과정에서의 각 구성 성분간의 짝짓기(coupling) 결과로 사료되며 또한 막의 팽윤비와 가교밀도는 경쟁적으로 투과물의 투과거동에 서로 상반되게 영향을 끼침이 관찰이 되었다. 온도에 따른 투과속도의 Arrhenius 관계에서 구한 투과활성화에너지를 통해 투과성분의 투과거동을 분석하였다.

• 산업기술연구
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• 제23권A호
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• pp.187-191
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• 2003

A hollow-fiber type polysulfone UF membrane was surface-coated with hydroxyethylmethacrylate (HEMA). The effect of various coating parameters on permeation flux, such as concentration ratio of AIBN/HEMA, solvent(water or methanol), and UV irradiation time, was investigated. The water permeation flux of oil-emulsion increased with concentration ratio of AIBN/HEMA, and increased with UV irradiation time. The flux of the membrane coated in solution using methanol as a solvent was greater than that of the membrane coated in solution using water as a solvent. The flux of both the coated and the uncoated membrane declined with the operation. The flux decline means that the membrane fouling by oil-emulsion occurs. However, the fouling of the coated membrane was much less than that of the uncoated membrane.

• 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.

• Bulletin of the Korean Chemical Society
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• 제25권5호
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• pp.687-693
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• 2004

Composite membranes with a titania layer were prepared by soaking-rolling method with the titania sol of nanoparticles formed in the sol-gel process and investigated regarding the vapor permeation of various organic mixtures. The support modification was conducted by pressing $SiO_2$ xerogel of 500 nm in particle size under 10 MPa on the surface of a porous stainless steel (SUS) substrate and designed the multi-layered structure by coating the intermediate layer of ${\gamma}-Al_2O_3$. Microstructure of titania membrane was affected by heat-treatment and synthesis conditions of precursor sol, and titania formed at calcination temperature of 300$^{\circ}C$ with sol of [$H^+$]/[TIP]=0.3 possessed surface area of 210 $m^2$/g, average pore size of 1.25 nm. The titania composite membrane showed high $H_2/N_2$ selectivity and water/ethanol selectivity as 25-30 and 50-100, respectively. As a result of vapor permeation for water-alcohol and alcohol-alcohol mixture, titania composite membrane showed water-permselective and molecular-sieve permeation behavior. However, water/methanol selectivity of the membrane was very low because of chemical affinity of permeants for the membrane by similar physicochemical properties of water and methanol.

• Archives of Pharmacal Research
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• 제27권11호
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• pp.1177-1182
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• 2004

The effect of poly[2-methacryloyloxyethyl phosphorylcholine] (pMPC) on the skin permeation property was investigated by performing in vitro skin permeation study of a model drug, nicotinic acid (NA). Effect of pMPC polymer in donor solution on skin permeation rates was evaluated using side-by-side diffusion cells. Also, the structural alterations in the stratum corneum (SC), inter-lamellar bilayer (ILB) and dermis layers in pMPC-treated and -untreated skin sections were investigated with transmission electron microscopy (TEM). The permeation profile of NA without pMPC in donor solution showed biphasic mode: initial $1^{st} phase and 2^{nd}$ hydration phase. The sudden, more than 10-fold increase in flux from the initial steady state (43.5 $\mu g/cm^2$/hr) to the $2^{nd}$ hydration phase (457.3 $\mu g/cm^2$/hr) suggests the disruption of skin barrier function due to extensive hydration. The permeation profile of NA with 3% pMPC in the donor solution showed monophasic pattern: the steady state flux (10.9 $\mu g/cm^2$/hr) without abrupt increase of the flux. The degree of NA permeation rate decreased in a concentration-dependent manner of pMPC. TEM of skin equilibrated with water or 2% pMPC for 12 h showed that corneocytes are still cohesive and epidermis is tightly bound to dermis in 2% pMPC-treated skin, while wider separation between corneocytes and focal dilations in inter-cellular spaces were observed in water-treated skin. This result suggests that pMPC could protect the barrier property of the stratum corneum by preventing the disruption of ILB structure caused by extensive skin hydration during skin permeation study.