• 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.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.234.1-234.1
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• 2003

The effects of vehicles and penetration enhancers on the in vitro permeation of ketorolac tromethamine (KT) across excised hairless mouse skins were investigated. Among pure vehicles examined, propylene glycol monolaurate (PGML) showed the highest permeation flux, which was 94.3${\pm}$17.3 mg/cm$^2$/hr. Even though propylene glycol monocaprylate (PGMC) alone did not show high permeation rate, the skin permeability of DT was markedly increased by the addition of diethylene glycol monoethyl ether (DGME); the enhancement factors were 19.0 and 17.1 at 20 and 40% of DGME, respectively. (omitted)

• Journal of Pharmaceutical Investigation
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• 제41권1호
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• pp.1-7
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• 2011

The effects of different formulation variables including pressure sensitive adhesive (PSA), permeation enhancer, thickness of the matrix and loading amount of drug on the transdermal absorption of galantamine were investigated across the hairless mouse skin. The permeation profile of galantamine was different depending on the types of PSA, loading amount of drug, thickness of the matrix and type of enhancer used. Highest flux of galantamine was obtained from acrylic PSA but crystals were formed in the patch within 72 h. Among the PSAs screened, crystal formation was not observed only in the patches formulated in Styrene Butadiene Styrene (SBS) matrix. Permeation rate increased linearly as the concentration of galantamine in SBS matrix increased from 2.5 to 15% w/w. Among the enhancers screened, Brij$^{(R)}$ 30 provided highest flux of galantamine. Matrix thickness of 80 ${\mu}m$ was optimum for maintaining adhesiveness as well as consistently delivering galantamine for longer period of time.

• Biomolecules & Therapeutics
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• 제5권4호
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• pp.357-363
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• 1997

The effects of formulation variables of topical lotion on the skin permeation of ketoprofen were evaluated using excised rat skins. The formulation variables were the amounts of poloxamer 407, drug and ethanol, and penetration enhancers. The Keshary-Chien diffusion cells were used for the diffusion study. The flux of ketoprofen linearly decreased as the concentration of poloxamer increased from 5% to 15% in the preparation, and linearly increased as the amount of drug increased. Penetration enhancers such as fatty acids and fatty alcohols showed markedly enhancing effects at the level of 5%. Among them, the highest flux was shown in linolenic acid. From these results, optimum formula containing 3% ketoprofen, 5% poloxamer 407, 40% ethanol and 5% linolenic acid having the flux of 537.6 $\mu$g/$\textrm{cm}^2$/hr were noted.

• 멤브레인
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• 제15권1호
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• pp.44-51
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• 2005

유기증기에 대한 PDMS의 단점을 보완하기 위해 4,4'-diphenylmethane diisocyanate (MDI)와 1,4-butanediol(BD)를 이용하여 poly(dimethylsiloxane)를 기초로 한 polyurethane-polysiloxanes (PU/PDMS)를 합성하였다. 그리고 poly(tetrafluoroethylene) (PTFE)를 다공성 지지체로 이용하여 복합막을 제조하여 SEM 분석으로 코팅층의 존재와 두께를 확인하였다. 증기투과실험에서 투과온도와 feed의 농도가 증가할수록 flux는 점차 증가하였고, separation factor는 이와 반대로 점차 감소하는 'trade-off'현상을 보였다. 본 연구에서의 PU/PDMS는 soft segment의 함량보다는 비교적 hard segment의 함량이 높기 때문에 투과온도의 증가에 따른 영향이 크지 않았던 것으로 사료된다. PU/PDMS막은 VOCs와 상대적으로 높은 친화도를 가지고 있기 때문에 PU/PDMS 균질막과 비교하여 복합막의 형태에서도 향상된 flux와 높은 separation factor를 나타내었다.

• 산업기술연구
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• 제20권A호
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• pp.179-184
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• 2000

The surface of porous alumina membrane was modified with silane coupling agent in order to enhance hydrophobicity. The contact angle of water to the surface-modified alumina membrane was greater than $90^{\circ}$. The surface-modified membrane was tested in vapor permeation for the concentration of aqueous ethanol. With the increase of ethanol concentration in the feed, permeation flux increased due to the greater affinity of ethanol with surface-modified alumina membrane than that of water. The experimental results showed that the permeation rate of surface-modified alumina membrane was 15~1000 times greater than that of polymer membranes.

• 멤브레인
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• 제16권1호
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• pp.68-76
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• 2006

본 연구는 투과증발법을 이용하여 수용액 중 미량의 감귤 향 성분을 농축하는 방법으로, 4종류의 실록산계 고분자 복합막을 이용하여 막 종류와 구조에 따른 투과 특성을 살펴보았다. 또한 최적의 막을 선정하여 공급액의 온도와 농도, 순환 유속에 따른 투과 특성을 살펴보고, 이를 resistance-in series model을 이용하여 해석하였다. 4종류의 실록산계 고분자 복합막을 통한 감귤 essence aroma 모델액의 투과 실험에서 지지층이 polyvinylidene fluoride (PVDF)이고 활성층이 polyoctylmethyl siloxane (POMS)인 막이 가장 높은 향 성분 플럭스와 농축계수 값을 나타내었으며, 공급액의 온도와 농도, 순환유속을 변화시키며 투과 실험을 하였다. 그 결과 공급액의 온도와 농도가 증가됨에 따라 향성분의 플럭스는 증가하고 농축계수 값은 감소하였으며 순환유속이 증가됨에 따라 향성분의 플럭스와 농축계수 값 모두 증가하였다.

• Biomolecules & Therapeutics
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• 제10권2호
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• pp.104-113
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• 2002

The effects of enzyme inhibitors and penetration enhancers on the permeation of leucine enkephalin (Leu-Enk) and its synthetic analog, [${D-ala}^2$]-leucine enkephalinamide (YAGFL) across the nasal, rectal and vaginal mucosae were evaluated. Enzyme inhibitors and penetration enhancers employed for Leu-Enk permeation study were amastatin(AM), thimerosal(TM) and ethylenediaminetetraacetic acid disodium salt(EDTA), and sodium taurodihydrofusidate (STDHF). Those for YAGFL permeation study were TM, benzalkonium chloride(BC) and EDTA, and STDHF, sodium deoxycholate(SDC), sodium glycholate(SGC), glycyrrhizic acid ammonium salt (GAA), L-$\alpha$-Iysophosphatidylcholine(LPC) and mixed micelle (MM, STDHF: linoleic acid = 15 mM : 5 mM). The addition of TM alone on the donor and receptor solutions for Leu-Enk permeation study across all the three kinds of mucosae failed to inhibit the degradation; it completely degraded in 6 hrs, and no permeation occurred. However, with addition of three kinds of inhibitors together, the fluxes across nasal, rectal and vaginal mucosae were $\20.7{pm}2.5$>/TEX>,$\0.3{pm}0.05$>/TEX> and $\1.4{pm}0.5$ $\mu$\mid$textrm{m}$/$\textrm{cm}^2$/hr, respectively. Moreover, the addition of STDHF in the presence of the above three inhibitors enhanced permeation across nasal, rectal and vaginal mucosae 1.3, 15 and 1.3 times, respectively. YhGFL also degraded in the donor and receptor solutions rapidly as time went. With mixed inhibitors of TM and EDTA, the percents of YAGFL remaining in the donor solutions facing nasal, rectal and vaginal mucosae were 69.7, 69.8 and 79.8%, respectively; the percent permeated increased to 10, 2.1 and 5.7%, respectively. The addition of STDHF in the presence of either BC/EDTA or TW/EDTA increased the permeation 2.2, 11.0 and 2.9 times, and 2.21, 14.0 and 2.7 times for nasal, rectal and vaginal mucosae, respectively. With SDC, SGC, GAA, LPC ud MM in the presence of TM/EDTA increased permeation; especially, they increased permeation across vaginal mucosae effectively, and the enhancement factors were 12.5, 7.6, 8.7, 5.7 and 5.5, respectively. The degradation extent of YAGFL was correlated with protein concentrations in the epidermal and serosal extracts. The flux of YAGFL across nasal mucosa increased dose-dependently.

• 한국막학회:학술대회논문집
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• 한국막학회 2000년도 춘계 총회 및 학술발표회
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• pp.79-81
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• 2000

• Journal of Pharmaceutical Investigation
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• 제31권2호
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• pp.95-100
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• 2001

Various alkyl ester prodrugs of diclofenac were synthesized in order to investigate the relationship between their skin permeation characteristics and physicochemical properties. Solubility in various vehicles was measured at room temperature. 1-Octanol/water partition coefficients (Log P) and capacity factors (k') were measured to determine the lipophilicity of the prodrugs. Stability of prodrugs in the skin extract and homogenate was also investigated before conducting the skin permeation studies. Increases in the Log P and capacity factor values were observed when alkyl esters of diclofenac were prepared. Since the aqueous solubility of the prodrugs was not high enough, they were saturated in propylene glycol (PG) for skin permeation studies. Prodrugs were rapidly metabolized to diclofenac, both in skin homogenate and in dermal extract of skin. The skin permeation rate of alkyl ester prodrugs was significantly higher than diclofenac with shorter lag time. Moreover, a parabolic relationship was observed between the permeation rate and the log P values of prodrugs, and the maximum flux was achieved at a log P value of around 4.0.