• YAKHAK HOEJI
• /
• v.38 no.5
• /
• pp.525-529
• /
• 1994

Antiinflammatory activity of an 1% flurbiprofen transdermal gel was evaluated using the carrageenan-Induced rat paw edema method. The application of 50 mg of the gel on the rat hind paw, at various time intervals from 0 to 24 hrs before the carrageenan injection, significantly inhibited edema formation in all groups of dosed rats, indicating that the antiinflammatory activitv was maintained up to 24 hrs after the transdermal application of the 1% flurbiprofen gel. The topical $ED_{50}$ of flurbiprofen in the gel was 1.0 mg/kg, whereas the oral $ED_{50}$ of the drug in a suspension was 1.7 mg/kg.

• Journal of Korean Physical Therapy Science
• /
• v.10 no.1
• /
• pp.170-179
• /
• 2003

This study was performed that how phonophoresis using ultrasound for piroxicam affects transdermal permeation and anti-inflammative effects. Transdermal permeation study conducted by using hairless mouse had two categories: control group and ultrasound group. Transdermal permeation was observed according to duty cycle and intensity. Anti-inflammatory effects were determined using in Sprague-Dawley rat. The subjects were divided into three groups of six SD rat each 24 hour, 48 hour, 72 hour. The results of this study were as follows: 1. Transdermal permeation of piroxicam was measured according to ultrasound duty cycle. This research demonstrates that ultrasound group retains more transdermal permeation than control group, and that pulsed ultrasound group holds a little more transdermal permeation than continuous ultrasound group. 2. The transdermal permeation of piroxicam is closely related with ultrasound intensity. Effect of each group of transdermal permeation was significant rises in proportion to ultrasound intensity. 3. By observing inflammation of the tissue caused by trauma, phonophoresis group showed more significant of anti-inflammatory effect. The conclusion of phonophoresis was found to improve significantly the transdermal permeation and the anti-inflammatory effect.

• YAKHAK HOEJI
• /
• v.41 no.2
• /
• pp.203-211
• /
• 1997

This study was conducted to investigate the subacute transdermal toxicity of Syndella gel, a new topical drug containing deproteinized dialysate of calf's blood and micronomicin sulfate in Sprague-Dawley rats. Three doses (1.97, 3.94, 7.88 g/kg) of Syndella gel was daily treated transdermally to male and female rats for 30 days. No death was occurred in either control or treated rats. No significant toxic clinical signs and body weight change were not observed at any doses in the male or female rats treated. There were no significant alterations in hematologic and biochemical parameters in both sexes, however slight increase of potassium concentration was observed in 3.94g/kg and 7.88 g/kg female groups. No significant necrotic changes were not observed in examined organs. This study showed that up to 7.88g/kg Syndella gel did not induce subacute transdermal toxicity.

• Archives of Pharmacal Research
• /
• v.29 no.5
• /
• pp.412-417
• /
• 2006

Triamcinolone acetonide (TA) is a corticosteroid that is used in the systemic and topical treatment of many inflammatory diseases. In this study, a phonophoretic drug delivery system was designed to enhance the TA permeability and the influence of ultrasound was examined. In order to establish the transdermal delivery system for TA, a hydrophilic carbopol gel containing TA was prepared after adopting phonophoresis. A permeation study through mouse skin was performed at $37^{\circ}C$ using a Franz diffusion cell, and the ultrasound treatment was carried out for 10 h. The level of TA permeation through the skin was evaluated under various ultrasound conditions including the frequency (1.0, 3.0 MHz), intensity (1.0, $2.5W/cm^2 $), and duty cycle (continuous, pulse mode) using a 0.5% TA gel. The highest permeation was observed under the ultrasound treatment conditions of low frequency, high intensity, and in continuous mode.

• Korean Chemical Engineering Research
• /
• v.46 no.2
• /
• pp.217-221
• /
• 2008

To investigate the enhancing effects in transdermal permeation of drug using newly designed ultrasound apparatus of 500 kHz, the transdermal permeation studies through the hairless mouse skin were conducted with lidocaine. The ultrasound apparatus of 500 kHz frequency and transducer were newly developed. The drug permeation studies were performed according to the ultrasound frequencies such as 1 MHz and 500 kHz at $1W/cm^2$ in intensity in continuous mode or pulsed mode, respectively. The results on transdermal permeation of lidocaine according to ultrasound intensity showed that the drug permeation increased as the intensity was higher.

• YAKHAK HOEJI
• /
• v.38 no.5
• /
• pp.483-487
• /
• 1994

The pharmacokinetic characteristics of an 1% flurbiprofen gel were evaluated using rats in reference to IV bolus and oral administration of the drug using rats. Following the transdermal application of the gel at the dose of 2 mg/kg as flurbiprofen, the $C_{max}$ and $T_{max}$ of the drug were $2.14\;{\mu}g/ml$ and 2 hr, respectively, whereas those after the oral administration of the drug as a suspension were $9.90\;{\mu}g/ml$ and 0.25 hr, respectively. These results indicate that, by the transdermal administration fo flubiprofen as the gel, the absorption of the drug was much slowed down and the lower $C_{max}$ compared to the oral administration may reduce the systemic side effects of the drug. The relative bioavailability of the flurbiprofen gel in reference to the oral dose was 48.5%. Tissue levels of flurbiprofen following the application of 50 mg of the 1% flurbiprofen gel onto ventral skin of rats showed that the maximum drug concentrations in the skin $(8.52\;{\mu}g/g)$ and the muscle $(2.06\;{\mu}g/g)$ occurred at 2 hrs postdose. The drug concentration in the both tissues remained relatively constant over the next 6 hrs following the peak concentration.

• Journal of the Korean Applied Science and Technology
• /
• v.27 no.4
• /
• pp.407-414
• /
• 2010

New biological treatments were being developed at a record place, but their potential could be compromised by a significant obstacle: the delivery of these drugs into a body. Pharmaceutical delivery is now nearly as important as product. New systems are being developed, and Drug Delivery Markets Series cover these new systems. Transdermal Delivery System(TDS) is often used as a method of drug dosage into the epidermic skin. An approach used to delivery drugs through the skin for therapeutic use as an alternative to oral, intravascular, subcutaneous and transmucosal routes. Various transdermal drug delivery technologies are described including the use of suitable formulations, carriers and penetration enhancers. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other methods of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stopped if the drug dosage lead to side effect. Polysaccharides, such as karaya gum and glucomannan, were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers, drug contents. Among these polysaccharide, the permeation rate of karaya gum matrix was fastest in fibric acid(ciprofibrate) such as lipophilic drug in vitro. We used glycerin, PEG400 and PEG800 as enhancers. Since dermis has more water content(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when PEG400 was more effective for lipophilic drug. Proper selection of the polymeric materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate. Especially, this result suggests a possible use of polysaccharide gel ointment matrix as a transdermal delivery system of anti-hyperlipoproteinemic agent.

• Journal of Pharmaceutical Investigation
• /
• v.33 no.3
• /
• pp.163-169
• /
• 2003

In order to develop a film-forming transdermal drug delivery system, polyurethane (PU) based on poly(ethylene glycol) and poly(tetramethylene oxide) was synthesized and characterized. The synthesized PU was blended with Gantrez ES 225 (GT) to improve the adhesion property of film-forming agent to the skin. When film-forming gel formulation containing 3% ketoprofen (KP) was applied, transparent thin film was obtained within 5 minutes and adhered to the skin for 8 hours. In vitro percutaneous absortion studies were performed to determine the rate of ketoprofen absorption through guinea pig skin. A prominent effect of limonene on the skin permeability of ketoprofen was observed among the various skin permeation enhancers investigated. Considering mechanica properties of film and skin permeability of ketoprofen, 2% of limonene was optimal content in the film forming transdermal formulation.

• Journal of Pharmaceutical Investigation
• /
• v.33 no.1
• /
• pp.21-28
• /
• 2003

Ketorolac tromethamine(KT) is a nonsteroidal agent with potent analgesic and moderate anti-inflammatory activity. The lipid-water partition coefficient of KT was evaluated and KT gel was formulated as a gel containing different pH, different concentrations of polymer (poloxamer 407, carbopol 941), propylene glycol, ethanol and various enhancers. The resulting KT gels were evaluated with respect to their viscosity, in vitro drug permeation rate through hairless mouse skin and stability. In n-octanol and chloroform, the lipid-water partition coefficient of KT was the highest at pH 4 phosphate buffer. The apparent viscosity of KT gel increased with an increase in gel pH, polymer and enhancer concentration. But the apparent viscosity of KT gel decreased with an increase in ethanol concentration. The permeation rate of KT through hairless mouse skin from gels different pH was maximum at pH 4 which is close to KT $pK_{a}$ 3.54. The permeation rate decreased with an increase in polymer, propylene glycol concentration. But the permeation rate increased with an increase in ethanol. The increase of drug concentration from 1 to 3% induced linear increase in permeation rate. The best enhancer was the combination of $Labrasol^{\circledR},\;Transcutol^{\circledR}$, oleic acid and l-menthol. In the accelerated stability test(25, 40 and $50{\circ}C$), pH 5 gel was most stable and pH 4 gel was most unstable for 90 days.

• Archives of Pharmacal Research
• /
• v.17 no.4
• /
• pp.240-243
• /
• 1994

Release rates of flurbiprofen from transdermal gels made of poloxamer 407 were evaluated using a membraneless diffusion cell in order to study the effects of formulation variables on flurbiprofen release such as poloxamer 407 (17.5-25%) drug (0.1-1.0%), ethanol (10-20%), PG or PEF 300 (5-15%) concentrations and gel pH(3-7). Isopropyl myristate was employed as a receptor medium for the drug released from the gel. The diffusion coefficient of flurbiprofen decreased linearly as the amount of poloxamer 407 and the drug in the gel increased. The release rate of flurbiprofen was gel increased. The The addition of more ethanol in the gel increased the drug release, resulting from the increase of the thermodynamic activity of the drug in the aqueous phase of the gel. However, the concentration effects of PG and PEG 300 on the release rate of flurbiprofen were negligible over the concentration range used.