• Biomolecules & Therapeutics
• /
• 제19권1호
• /
• pp.109-117
• /
• 2011

In this work, we have investigated the effect of polyoxyethylene alkyl ester nonionic surfactants on percutaneous permeation enhancement of a model drug, ketoprofen. We also investigated the mechanism involved in the enhancement using impedance and solubility measurement. Three groups of nonionic surfactants with different ethylene oxide content were studied. The permeation results showed that all surfactants enhanced the percutaneous absorption, irrespective of the molecular weight. The permeation results from PEG-45 monostearate (PEGMS45) were rather unexpected. Impedance and solubility results indicate that the mechanism involved in the enhancement of permeation by PEG-10 monooleate (PEGMO10) and PEGMS45 is rather different. The results from PEGMS45 suggest that it could be a potential candidate as a skin penetration enhancer with high molecular weight, which may poses less skin irritation and systemic side effect than the smaller surfactant molecules. Overall, this work provided some useful information on percutaneous transport enhancement and the mechanistic insights involved in skin permeation for these nonionic surfactants.

• 한국응용과학기술학회지
• /
• 제26권2호
• /
• pp.103-109
• /
• 2009

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. Many other human attributes and absorption evaluation studies are underway in various areas. This study were used rats and carried out to find out the effects of commercial permanent wave products to skin which are composed with thioglycolic acid and bases. Results were as follows. Permanent wave penetrated to 3 hours later with steady state in skins and was not significant changeable after 20hr later. In case of neutralizer with thioglycolic acid lag time and permeability coefficient in healthy skin were 3.32hr and $0.101{\mu}g/cm^2/hr$, in old skin were 3.08hr and $0.117{\mu}g/cm^2/hr$, and in wounded skin were 3.02hr and $0.166{\mu}g/cm^2/hr$. In conclusion, lag time and permeability coefficient in old skin and wounded skin were faster than healthy skin. In vivo, We were studied to general time and method of permanent wave. We found out that fine wrinkle and rash of skin were changeable in the case of treating with permanent wave drugs than normal skin.

• 한국응용과학기술학회지
• /
• 제29권4호
• /
• pp.552-560
• /
• 2012

약물 전달 시스템은 약물의 방출 프로파일, 흡수, 분배 및 제품의 효율성과 안전성, 환자의 편의성과 협조를 향상시키기 위한 제거를 개선하는 명백하게 보호화된 공식화 기술이다. 가장 일반적으로 쓰이는 transdermal 시스템은 다양한 종류의 기술을 사용하는 skin patch다. 다른 투약 방법과 달리, transdermal 시스템은 장기간 사용이 가능하다. 또한, 부작용이 생길 경우, 약물 투약의 중단이 가능하다. karaya gum and locust bean gum(LBG)/water-soluble chitosan oligomer(WSCO)과 같은 Polysaccharide를 TDS의 기본 물질로 선택하였다. 또한, 이 polymers들은 tacrine 물질, 강화제로 규정되어진다. 이러한 polysaccharide 중에서, karaya gum matrix의 침투율은 lipophilic drug in vitro 와 같은 tacrine 내에서 가장 빠르다. 우리는 glycerin, PEG 400, and PEG 800를 강화제로 사용하였다. 그러므로, transdermal의 tacrine 흡수율은 vehicle 구성을 바꿈으로써, 혹은 침투 강화제를 사용함으로써 향상되었을 것이다. 특히, vehicle이 스스로의 효과를 강화하는 것과 더불어, vehicle에 강화제를 첨가함으로써 높은 침투 효율이 얻어질 것으로 기대된다.

• Archives of Pharmacal Research
• /
• 제11권3호
• /
• pp.185-196
• /
• 1988

The inflence of hydrophilic vehicles on percutaneous absorption rate of griseofulvin was studied using intact skin of full thickness of hairless rat. The in vitro absorption rates were used as the characteristics for deciding the optimum formula of ointment vehicles. The optimum formula of vehicle compositions for maximum absorption rate was obtained from the polynomial regression equation and the two graphical techniques, contour graph and partial derivative graph. It was composed of sodium lauryl sulfate (1.65 W /W%), white petrolatum (16.5 W /W%), propylene glycol (12.0 W /W%), and stearyl alcohol (19.6W /W%). The experimental value obtained from the optimum formula and the prediction value were 33.99 and 33.87 ${\mu}g/\sqrt{min}$, respectively. From these results, it was believed that optimum formula for semisolid dosage forms could be obtained from the application of the optimization technique used in this study.

• Journal of Pharmaceutical Investigation
• /
• 제31권3호
• /
• pp.181-184
• /
• 2001

The purpose of this study was to develop transdermal drug delivery system (TDDS) for the combination of physostigmine and procyclidine. The effects of various pressure sensitive adhesives (PSA) on the percutaneous absorption of procyclidine across hairless mouse skin were evaluated to select an appropriate PSA. In addition, the influences of various vehicles on the percutaneous absorption of procyclidine from PSA matrix across hairless mouse skin were evaluated using flow-through diffusion cell system at $37^{\circ}C$. Physostigmine did not have any influence on the permeation rate of procyclidine. The flux of procyclidine was the highest in silicone and PIB and was relatively lower in SIS, Acryl, and SBS adhesive matrices, however, their use was limited by the crystallization of the drug in the matrix. Among acrylic adhesives, the permeability of procyclidine was the highest from poly (ethylene oxide) grafted acrylic adhesive. Some enhancers show different enhancing effect depending on the drug, however, many of the tested enhancers showed enhancing effect for the permeation of both procyclidine and physostigmine to some extent. $Crovol^{\circledR}$ EP 40 showed the highest enhancing effect on the permeation of both compounds. The size of TDDS to provide required permeation rate was estimated to be $35\;cm^2$ based on available information.

• Archives of Pharmacal Research
• /
• 제24권6호
• /
• pp.578-583
• /
• 2001

To investigate the feasibility of developing a new tenoxicam plaster, the effects of vehicles and penetration enhancers on the in vitro permeation of tenoxicam from a pressure-sensititre adhesive (PSA) matrices across the dorsal hairless mouse skin were studied. Vehicles employed in this study were propylene glycol (PC)-oleyl alcohol (OAI), PG-oleic acid (OA), and diethylene glycol monoethyl ether (DCMI)-propylene glycol monolaurate (PCML) cosolvents with/without fatty acids. In this studys amines such as triethanolamine (TEA) and tromethamine (TM) were additionally used as a solubilized. Among PSAs used, $Duro-Tak^{\circledR}$87-2510 showed much higher release rate than either $Duro-Tak^{\circledR}$ 87-2100 or $Duro-Tak^{\circledR}$87-2196. The relatively high flux rate was obtained with the formulation of DCMI-PCML (40:60, v/v) with 3% OA and 5% TM, and the flux increased as a function of the dose;the initial flux up to 12 h was $4.98{\pm}1.38{\;}{\mu\textrm{g}}/{\textrm{cm}^2}/h$ at the tenoxicam dose of $50{\;} mg/70{\;}{\textrm{cm}^2}$. This flux was much higher than that of a commercial piroxicam patch ($Trast^{\circledR}$) ($1.24{\pm}0.73{\;}{\mu\textrm{g}}/$\textrm{cm}^2/hr$) with almost only one-third that of the commercial patch. Therefore, these observations indicated that these composition of tenoxicam plaster may be practically applicable.

• Journal of Pharmaceutical Investigation
• /
• 제18권1호
• /
• pp.31-41
• /
• 1988

Computer optimization technique was applied to obtain the optimum formula of o/w type ointment vehicle containing sodium lauryl sulfate and 1-methyl-2-pyrrolidinone (MP). In order to determine the feasibility of optimizing a vehicle composition with the aid of computer, the amounts of sodium lauryl sulfate $(X_1)$, salicylic acid $(X_2)$, and MP $(X_3)$ were selected as the independent variables for the solubility and the absorption rates of salicylic acid (dependent variables). The experimental values of absorption rates agreed well with the calculation values obtained from the polynomial regression analysis, and the contour charts drawn by computer were useful in optimization process.

• Journal of Pharmaceutical Investigation
• /
• 제21권2호
• /
• pp.97-101
• /
• 1991

Six different O/W cream bases containing 4% ascorbic acid dipalmitate and two different O/W cream bases containing 1% ascorbic acid were prepared. Percutanceous absorption of ascorbic acid as well as safety were determined using rabbits. The stability of the creams was also tested at room temperature. Ascorbic acid concentrations in urines varied depending on the characteristics of cream bases used. The absorption of ascorbic acid was increased and sustained with the cream bases containing branched chain esters of fatty acid instead of natural oils used currently. The excretion level of ascorbic acid in urine was high with the cream base including nonionic surfactants and a small quantity of natural oils. The creams containing nonionic surfactants showed excellent stability, while those containing anionic surfactants were not stable in terms of pH, odor and coloring test at room temperature during six months. But, the two creams containing ascorbic acid were unstable. All the cream bases tested showed good safety.

• Journal of Pharmaceutical Investigation
• /
• 제24권1호
• /
• pp.11-16
• /
• 1994

In order to reduce the systemic side effects and gastrointestinal irritation of ketoprofen after its oral administration, it was formulated as a 3% ketoprofen gel (ID-GEL) with Pluronic F-127. The pharmacokinetic characteristics of ID-GEL was evaluated following its transdermal application on the dorsal skin of rats at the dose of 9 mg/kg in reference to those of existing 3% ketoprofen gels. Even though the maximum concentration of 810 ng/ml was reached at 6 hrs postdose, the plasma concentration was kept almost constant until 24 hrs postdose, which suggested that ketoprofen was released continuously from the gel during this period. The bioavailability of ID-GEL was two times higher than those of existing 3% ketoprofen gels, based on the calculated area under the plasma concentration-time curves after the percutaneous administration.

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