• Korean Journal of Clinical Pharmacy
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• v.13 no.2
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• pp.97-105
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• 2003

아스코마이신(ascomycin)의 macrolactam 유도체인 피메크로리무스(pimecrolimus; 엘리델 [Elidel], SDZ ASM 981; Novartis Pharma AG, 바젤, 스위스)는 세포선택성을 지닌 염증성 사이토카인(cytokines) 억제제로서 아토피피부염, 알레르기성 접촉피부염, 자극성 접촉피부염 및 판형 건선 등 염증성 피부질환의 치료제로 개발되었다. T세포와 비만세포의 염증성 사이토카인 생산 분비를 억제하고 사전 형성된 염증성 매개물질의 비만 세포 분비를 저해한다. 국소 투여된 피메크로리무스는 알레르기성 접촉피부염(allergic contact dermatitis [ACD]) 돼지 모델에서 고역가 코르티코스테로이드 클로베타졸-17-propionate(corticosteroid clobetasol-17-propionate)와 동등한 효과를 나타낸다. 하지만 피메크로리무스는 클로베타졸과는 달리 피부 위축을 일으키지 않는다. 경구 투여시 피메크로리무스는 마우스와 랫트 ACD 치료에 있어서 타크로림무스(tacrolimus [FK 506])와 동등한 혹은 더 우수한 효과를 나타낸다. 또한 피메크로리무스는 아토피피부염 급성 징후 유사 모델인 저마그네슘 혈증 탈모 랫트(hypomagnesemic hairless rat)의 피부 염증과 소양증을 효과적으로 감소시킨다. 피메크로리무스는 랫트에서 다음과 같은 측면의 전신 면역반응 손상 효과가 타크로리무스 와 비교하여 낮게 평가된다: (1)국소 이식편대 숙주 반응, (2)양(sheep) 적혈구에 대한 항체 형성, (3)신장이식. 시험관내 평가시 돼지 피부를 통한 피메크로리무스 투과 속도가 타크로리무스보다 10배 낮게 측정되므로 생체에서 경피 흡수가 더 적게 될 것으로 판단된다. 상기 자료로 판단컨대 피메크로 리무스는 피부에 대한 항염증 활성이 높을 뿐 아니라 전신 면역반응 손상 부작용이 낮은것으로 사료된다.

• Journal of Pharmaceutical Investigation
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• v.33 no.1
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• pp.29-36
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• 2003

Clenbuterol, a selective ${\beta}_2-adrenergic$ receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic obstructive bronchial disease, chronic bronchitis and pulmonary emphysema. The percutaneous permeation of clenbuterol was investigated in hairless mouse skin after application of 50/50 buffer(pH 10)/propylene glycol solvent mixture. The enhancing effects of various penetration enhancers such as terpenes, non-ionic surfactants, pyrrolidones, fatty acids and some other enhancers on the permeation of clenbuterol were evaluated using Franz diffusion cell. Among terpenes studied, 1,8-cineole was the most effective enhancer, which increased the permeability of clenbuterol approximately 39.33-fold compared with the control without penetration enhancer, followed by menthone with enhancement ratio of 23.57. Nonionic surfactants did not have significant enhancing effects. N-Lauryl-2-pyrrolidone increased the permeability of clenbuterol approximately 4.51-fold compared with the control. Lauric acid increased the permeability of clenbuterol approximately 35.57-fold with decreasing the lag time from 2.64 to 0.52 hr. Oleic acid, linoleic acid, linolenic acid and capric acid showed enhancement ratio of 22.62, 19.60, 17.45 and 16.51, respectively. $Labrafil^{\circledR}$ enhanced the permeability of clenbuterol 9.24-fold compared with that without enhancer.

• Journal of Pharmaceutical Investigation
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• v.32 no.4
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• pp.259-265
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• 2002

Piroxicam is one of the NSAID, which is used in the systemic and topical treatment of a variety of inflammatory conditions. Conventionally, for topical use, the drug is formulated in gel. We designed an phonophoretic drug delivery system to investigate the piroxicam permeability and the influence of ultrasound application (continuous mode, pulsed mode), frequency (1.0 MHz, 3.0 MHz) and intensity $(1.0\;w/cm^2,\;1.5\;w/cm^2,\;2.0\;w/cm^2)$ with 0.5% piroxicam gel. Per cutaneous absorption studies were performed in vitro models to determine the rate of drug absorption via the skin. Permeation study using hairless mouse skin was performed at $37^{\circ}C$ using buffered saline (pH 7.4, 10% propylene glycol solution) as the receptor solution. Anti-inflammatory activity was determined using carrageenan-induced foot edema model in rat. A pronounced effect of ultrasound on the skin absorption of the piroxicam was observed at all ultrasound energy level studied. Ultrasound was carried out for 10 hr. The highest permeation was observed at intensity of $2.0\;w/cm^2$, frequency of 1.0 MHz and continuous output. The inclusion of phonophoresis was found to improve significantly the skin permeation in vitro and the anti-inflammatory activity in vivo.

• Journal of Pharmaceutical Investigation
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• v.39 no.2
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• pp.121-125
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• 2009

The objective of this study was to investigate the feasibility of applying the Intense Pulsed Light (IPL) as a tool to enhance the skin absorption of arbutin, a well-known skin-whitening agent. Arbutin solution or skin formulation was applied on the back of hairless mouse skin in vivo after IPL treatment, and then the skin deposition of arbutin was determined by HPLC. IPL treatment significantly increased the amount of arbutin in the skin after 6 hours when arbutin solution was applied 20 times. IPL also enhanced the skin deposition of arbutin when arbutin formulation was applied, although it was not significantly different. Significant increase of surface skin temperature was observed by IPL treatment, which might be a mechanism of the enhanced skin absorption of arbutin. These results suggest the feasibility of using IPL as a tool to increase the skin absorption of whitening agents, although further research needs to be conducted to understand its exact mechanism.

• YAKHAK HOEJI
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• v.44 no.6
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• pp.595-600
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• 2000

Transdermal delivery of ketorolac tromethamine, a potent non-narcotic analgesic, through human cadaver skin was investigated in vitro. A mixture of ethanol/water (40/60) containing 0, 1, 3, 5, and 8 (w/v)% L-menthol were used as a vehicle and penetration enhancer respectively. The permeation of ketorolac through human cadaver skin from saturated drug solution was evaluated at $37^{\circ}C$ with modified Franz diffusion cell. The in vitro skin flux and lag time were $1.23\;{\pm}\;0.11\;{\mu}g/cm^2{\cdot}hr$ and $5.56\;{\pm}\;0.34\;hr$, respectively. The cumulative amount of penetrated ketorolac containing L-menthol in ethanol/water (40/60) binary system was increased by the following order; 3%, 5%, 8%, 1%, 0%, and the lag time was decresed by the following order; 3%, 5%, 8%, 0%, 1%. The results suggested that a potential use of 3% L-methol is an effective penetration enhancer of ketorolac tromethamine through the human cadaver skin.

• YAKHAK HOEJI
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• v.34 no.3
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• pp.161-165
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• 1990

An automated, simple, and reliable method was developed for determining in vitro drug release rate from transdermal delivery dosage forms. The patch is held in position in the heating block by sandwiching it between the middle plate and the bottom plate of diffusion cell. The dissolution profile of the commercially available transdermal scopolamine patch was determined over a 72-h period, and the results were compared with those obtained with other methods; paddle-over-disk method, reciprocating method, and diffusion cell method. It was demonstrated that the flow-through method is equivalent in terms of release rate profile and accumulated released drug amount over the lifetime of the dosage form tested. Also this method is simple, reliable and reproducible. Therefore, this technique can be used in a quality control for assuring product uniformity.

• Journal of Pharmaceutical Investigation
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• v.29 no.4
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• pp.337-341
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• 1999

We have studied the stability and transdennal flux of prostaglandin $E_1\;(PGE_1)$ from various donor solutions through hairless mouse skin. Stability in HEPES buffer or in propylene glycol (PG) solution where enhancer (oleic acid (OA), propylene glycol monolaurate (PGML), transcutol (TC), ethanol (EtOH))s dissolved was investigated. $$PGE_1 was not stable in HEPES buffer. The concentration of $$PGE_1 decreased continuously for 7 days, and the degradation rate constant was $0.0028\;h^{-1}$, assuming first order reaction. The effect of current or penetration enhancer on the degradation was minimal. Percutaneous transport from HEPES buffer by passive or iontophoretic delivery without enhancer was close to nil. When OA or PGML was used together with PG, both passive and iontophoretic flux increased. PGML showed better enhancing effect than OA. Flux by cathodal delivery was about 2 times larger than that by passive delivery. Flux by anodal delivery was lower than that by passive delivery. TC and EtOH also increased the transdermal flux, but the effect was not as good as that observed when OA or PGML was used. These stability and flux data provide important information on how to formulate the patch, which will be the next step of this work, and on the polarity of current to use during iontophoresis.

• Journal of Pharmaceutical Investigation
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• v.30 no.4
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• pp.283-288
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• 2000

The purpose of the present study was to investigate the topical bioavailability of retinol (vitamin A) after its transdermal administration. For this purpose, we developed the convenient HPLC method to measure the retinol concentration in the biological fluids such as plasma and skin tissues. The low detection limit was $0.1\;{\mu}g/ml$ using a gradient HPLC system of UV detection. The initial plasma concentration of retinol was about $20\;{\mu}g/ml$ after its i.v. bolus administration (4.32 mg/kg). The half life $(t_{1/2{\alpha}})$ in the distributive phase was 1.3 min, while retinol was slowly disappeared in the post-distributive phase. On the other hand, the maximum plasma concentration $(C_{max})$ was about 776 ng/ml after appling to rat skin at a dose of 43.2 mg/kg. Furthermore, the concentration of retinol in the skin tissues was about 600 ng/g tissue at 12 hr after its transdermal administration. In conclusion, the initial plasma concentration of retinol was comparable with the skin concentration after its cutaneous absorption, followed by being decreased with the passage of the time.

• Journal of the Korean Applied Science and Technology
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• v.25 no.2
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• pp.137-143
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• 2008

Chemicals for cosmetics, including skin, the skin absorbs some of the research in the field of science or pharmacy recently, about the environment and the health of the heightened interest in skin absorption, and many other human attributes and absorption evaluation studies are underway in various areas. In this study, The effects of commercial permanent wave products to skin which are composed with cysteine and bases using rat. Results are as follows; the content of penetration 4 hours later with steady state and no significant changeable after 20 hours later. In cysteine groups lag time and permeability coefficient of young skin is 3.32hr and $0.102{\mu}g/cm^2{\cdot}hr$, lag time and permeability coefficient of old skin is 4.04hr and $0.106{\mu}g/cm^2{\cdot}hr$. In conclusion of study lag time and permeability coefficient in old skin and wounded skin are faster than healthy skin. We notified that fine rinkle and rash of skin were changeable in the case of treating with permanent wave drugs than normal skin.

• Polymer(Korea)
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• v.37 no.3
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• pp.347-355
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• 2013

In this study, the porous cellulose hydrogel as a carrier to enhance the skin delivery of quercetin and its glycoside, rutin known as flavonoid antioxidants was prepared and its properties were investigated. The optimum cellulose hydrogel for quercetin and rutin was made by the reaction of 2 wt% cellulose with 12% ECH. In the release test of the hydrogel containing the flavonoids, the release of quercetin was diffusion-controlled at $10{\sim}500{\mu}M$, but rutin was released by the erosion of hydrogel system at $10{\sim}50{\mu}M$. Both the encapsulation efficiency and release amount of rutin in hydrogel were higher than quercetin. However, in skin permeation experiment using Franz diffusion cell, quercetin showed higher skin permeation capacity than rutin. The hydrogel containing flavonoids showed remarkable transdermal permeation than the control group. These results suggest that porous cellulose hydrogel is potential drug delivery system to enhance transdermal permeation of water-insoluble flavonoid antioxidants.