• Archives of Pharmacal Research
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• v.26 no.8
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• pp.644-648
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• 2003

To investigate the feasibility of developing a new ondansetron transdermal system, the effects of vehicles and penetration enhancers on the in vitro permeation of ondansetron hydrochloride (OS) from a pressure-sensitive adhesive (PSA) matrices across dorsal hairless mouse skin were studied. Vehicles employed in this study consisted of various ratios of propylene glycol monocaprylate (PGMC)-diethylene glycol monoethyl ether (DGME) co-solvents and PGMC-propylene glycol (PG) co-solvents with 3% oleic acid. $Duro-Tak^\circledR$ 87-2100 and $Duro-Tak^\circledR$ 87-2196 were used as PSAs. The concentration of DGME in PGMC-DGME co-solvent system affected the release rate; as the concentration of DGME increased, the release rate decreased. The cumulative release amount of OS increased as the ratio of PSA to drug solution decreased. The permeation flux was also primarily affected by the amount of PSAs; as the amount decreased, the permeation flux increased. The overall fluxes from matrix formulations were significantly lower when compared to those obtained from solution formulations. The ratio of PG to PGMC did not affect permeation flux, while the lag time decreased significantly from $5.14\pm3.31 to 0.31\pm0.12$ h as the PG increased from 40% to 60%.

• Archives of Pharmacal Research
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• v.24 no.6
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• pp.578-583
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• 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
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• v.33 no.2
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• pp.79-84
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• 2003

The effects of various pressure sensitive adhesives (PSA) and enhancers on the percutaneous absorption of tulobuterol were investigated. The permeation rate of tulobuterol through hairless mouse skin from various adhesives was evaluated using a flow-through diffusion cell system at $37^{\circ}C$. The permeability of tulobuterol was variable depending on the physicochemical property of the PSA. The permeation rate of tulobuterol from polyethylene oxide grafted acrylic adhesive matrix was higher than that from other PSA matrices. The flux of tulobuterol was $4.37{\pm}0.34\;{\mu}g/hr/cm^2$ from polyethylene oxide grafted acrylic adhesive matrix. When the effects of various enhancers on the percutaneous absorption of tulobuterol from grafted acrylic adhesive were evaluated, Plurol $oleique^{\circledR}$ showed higher flux than all other enhancers tested.

• Journal of Pharmaceutical Investigation
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• v.32 no.2
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• pp.107-112
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• 2002

To investigate the feasibility of developing a novel melatonin plaster, the effects of vehicles and drug loading dose on the in vitro permeation of melatonin across dorsal hairless mouse skin from pressure-sensitive adhesive (PSA) matrices were examined. Vehicles employed were propylene glycol laurate (PGL), propylene glycol monocaprylate (PGMC) and diethylene glycol monoethyl ether (DGME). Among PSAs used, only $Duro-Tak^{\circledR}$ 87-2196 showed a good peeling property. The release from $Duro-Tak^{circledR}$ 87-2196 was proportional to the square root of time, and dose-dependent. The fluxes increased as the loading dose increased over the doses under solubility. The relatively high permeation flux $(3.03{\pm}1.37\;{\mu}g/cm^2/hr)$ was obtained when using PGMC at the melatonin loading dose of $45\;mg/140\;cm^2$. Lag time was not affected by the vehicles used but by the thickness spread. The melatonin plasters prepared using PGMC showed a good adhesive property onto skin, and showed no crystal formation.

• Journal of Pharmaceutical Investigation
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• v.37 no.3
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• pp.173-177
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• 2007

The purpose of this study was to investigate the effect of salt formation on the percutaneous absorption of meloxicam through hairless mouse skin from a pressure sensitive adhesive (PSA) matrix. In addition, the influences of enhancers on the permeation of meloxicam or meloxicam-ethanolamine (MX-EA) salts across the hairless mouse skin were evaluated using a flow-through diffusion cell system. The salt formation of meloxicam resulted in lower permeation rate than the parent drug. $Span^{(R)}$ 80 provided the highest enhancing effect for meloxicam and meloxicam monoethanolamine salt. The maximum amount of the drug that can be loaded without retarding permeation rate was different depending on the compound. No relationship was found between the fluxes of meloxicam or MX-EA salts from saturated solutions and those from PSA matrices containing the same enhancer.

• Journal of Pharmaceutical Investigation
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• v.31 no.3
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• pp.181-184
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• 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.