• Biomolecules & Therapeutics
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• v.17 no.3
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• pp.305-310
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• 2009

The aim of this study was to determine if a meloxicam hydrogel could be administered in vivo via phonophoretic transdermal delivery using pulsed ultrasound by examining its anti-hyperalgesic effects in a rat carrageenan inflammation model. Carrageenan (1%) was injected into the plantar surface of the right hindpaw, and meloxicam hydrogel was administered via phonophoretic transdermal delivery. Changes in the mechanical and thermal hyperalgesia, as well as swelling, showed that phonophoretic delivery of meloxicam exhibited significantly better anti-hyperalgesic and anti-inflammatory effects than pulsed ultrasound. Topical and systemic application of meloxicam hydrogel using phonophoresis showed similar anti-hyperalgesic effects. These findings suggest that the transdermal administration of a meloxicam hydrogel using phonophoresis by pulsed ultrasound might be useful for treating acute inflammation.

• Journal of Pharmaceutical Investigation
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• v.41 no.6
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• pp.347-354
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• 2011

Repeated oral administration of loxoprofen can induce many side effects such as gastric disturbances and acidosis. Therefore, we considered alternative routes of administration for loxoprofen to avoid such adverse effects. The aim of this study was to develop an ethylene-vinyl acetate (EVA) matrix system containing a permeation enhancer for enhanced transdermal delivery of loxoprofen. The EVA matrix containing loxoprofen was fabricated and the effects of drug concentration, temperature, enhancer and plasticizer on drug release were studied from the loxoprofen-EVA matrix. The solubility of loxoprofen was highest at 40% (v/v) PEG 400. The release rate of drug from drug-EVA matrix increased with increased loading dose and temperature. The release rate was proportional to the square root of loading dose. The activation energy (Ea), which was measured from the slope of log P versus 1000/T, was 5.67 kcal/mol for a 2.0% loaded drug dose from the EVA matrix. Among the plasticizer used, diethyl phthalate showed the highest release rate of loxoprofen. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the greatest enhancing effect. In conclusion, for the enhanced controlled transdermal delivery of loxoprofen, the application of the EVA matrix containing plasticizer and penetration enhancer could be useful in the development of a controlled drug delivery system.

• Journal of Pharmaceutical Investigation
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• v.39 no.6
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• pp.437-443
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• 2009

To develop a topical bioadhesive formulation of clotrimazole for enhanced transdermal delivery, hydroxypropyl methylcellulose gel containing permeation enhancer was formulated and permeation studies were carried out. The release characteristics of the drug from the gel formulation were examined according to the receptor medium, drug concentration, and temperature. The rate of drug release from the gel increased with increasing drug concentration and temperature. The activation energy (Ea) of drug permeation, which was calculated from the slope of log P versus 1/T plots, was 14.41kcal/mol for a 1%(w/w) loading dose. The enhancer, such as saturated, unsaturated fatty acids, pyrrolidones, propylene glycol derivatives, glycerides, and non-ionic surfactants, were incorporated onto the gels to increase the amount of drug permeation into the skin. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the highest level of enhancement. These results show that clotrimazole gels containing polyoxyethylene 2-oleyl ether could be used for the enhanced transdermal delivery of clotrimazole.

• Journal of Oriental Neuropsychiatry
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• v.24 no.2
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• pp.179-188
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• 2013

Objectives : The purpose of this study was to compare three therapies - auricular acupuncture, transdermal nicotine patch and therapy - in combination with auricular acupuncture and nicotine patch. Methods : The subjects of this study included 188 male smokers in their 20s, 30s, 40s and 50s, who visited Wonmi Public Health Center. They were evaluated with the Fagerstrom test for nicotine dependence, amounts of daily smoking and success rate of smoking cessation. The subjects decided on a therapy method strictly of their own choice. They were divided into three groups according to the therapy; auricular acupuncture group (62 persons), nicotine patch group (69 persons) and combination therapy group (57 persons). Results : All three groups resulted in statistically significant reducing effects of nicotine dependence and amounts of daily smoking. In the combination therapy group, nicotine dependence was significantly decreased by more than those of the other groups. There were no statistically significant differences in decrements of daily smoking and success rate of smoking cessation among the three groups. Conclusions : The above results suggest that auricular acupuncture and transdermal nicotine patch have significant effects of smoking cessation. If they are combined, it is expected that therapies for smoking cessation would be developed.

• 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.

• Archives of Pharmacal Research
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• v.25 no.4
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• pp.534-540
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• 2002

To develop novel transdermal formulation for aceclofenac, microemulsion was prepared for increasing its skin permeability. Based on solubiity and phase studies, oil and surfactant was selected and composition was determined. Microemulsion was spontaneously prepared by mixing ingredients and the physicochemical properties such was investigated. The mean diameters of microemulsion were approximately 90 nm and the system was physically stable at room temperature at least for 3 months. In addition, the in vitro and in vivo performance of microemulsion formulation was evaluated. Aceclofenac was released from microemulsion in acidic aqueous medium, and dissolved amounts of aceclofenac was approximately 30% after 240 min. Skin permeation of aceclofenac from microemulsion formulation was higher than that of cream. Following transdermal application of aceclofenac preparation to delayed onset muscle soreness, serum creatine phosphokinase and lactate dehydrogenase activity was significantly reduced by aceclofenac. Aceclofenac in microemulsion was more potent than cream in the alleviation of muscle pain. Therefore, the microemulsion formulation of aceclofenac appear to be a reasonable transdermal delivery system of the drug with enhanced skin permeability and efficacy for the treatment of muscle damage.

• Journal of Pharmaceutical Investigation
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• v.39 no.3
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• pp.177-183
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• 2009

A rapid and sensitive reversed-phase high performance liquid chromatography (HPLC) method was developed for the determination of piroxicam in the rabbit plasma. After a treatment of plasma sample by liquid-liquid extraction, the drug was analyzed on an HPLC system with ultraviolet detection at 330 nm. HPLC was carried out using reversed-phase isocratic elution with a C18 column, a mobile phase of a mixture of acetonitril, doubly deionized water and acetic acid 43.74:56.00:0.26 v/v%) at a flow rate of 1.1 mL/min. The chromatograms showed good resolution and sensitivity and no interference of plasma. The calibration curve for the drug in plasma sample was linear over the concentration range of 0.01-2.0 ${\mu}$g/mL. The intra- and inter-day assay accuracies of this method ranged from 86.82% to 108.33% of normal values and the precision did not exceed 13% of relative standard deviation. The plasma concentration of piroxicam decreased to below the quantifiable limit at 12 hr after the i.v. bolus administration to rabbits following dose of 0.375 mg/kg yielding a apparen t plasma half life of 1.38 hr. The transdermal route prolongs plasma levels of piroxicam. The bioavailability, calculated from the dose-adjusted ratio of the $AUC_{transdermal}$ to the $AUC_{i.v.}$, was 7.44%. The plasma concentration of piroxicam was detected by 48 hr after the transdermal administration of patch at a dose of 32 mg/kg. This method was suitable for cutaneous absorption studies of piroxicam in the rabbit after transdermal administration of different types of dosages of the drug.

• Korean Journal of Biological Psychiatry
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• v.2 no.1
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• pp.91-99
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• 1995

A on-off study was designed to evaluate the effects of addition of transdermal esrtradiol to tricyclic antidepressants on depression level, vasomotor symptom(hot flush), sexual functions and hormonal status, plasma 5-hydroxyindoleascetic acid(5-HIAA) level in postmenopausal women with depression. Plasma level of estradiol, progesterone, LH, FSH, prolactin and 5-HIAA was measured by Time-resolved fluoroimmunoassay and HPLC(High Performance Liquid Chromatography). To asses their symptoms, the BDI(Beck Depression Inventory) and modified symptom scale, extracted from women's health questionnaire were used. Depression score, sexual function score were decreased by the last 4-weeks of addition of transdermal estradiol to antidepressant treatment, not Significant, but vasomotor symptom (hot flushes) score was decreased significantly(p<0.05) by the last 4-weeks of the given treatment. Thus, during addition of transdermal estradiol to antidepressants treatment, only vasomotor symptom(hot flushes) was improved significantly, but depression level was not changed in postmenopausal women with depression. Plasma FSH, estradiol and prolactin level was not changed in postmenopausal women with depression. Plasma FSH, estradiol and prolactin levels were increased by the last 4-weeks of the treatment. There were not significant correlations between clinical symptoms and plasma hormonal status and 5-HIAA level in baseline. After the last 4-weeks of transdermal estradiol treatment, the change of depression score was correlated significantly with change of serum prolactin and 5-HIAA level and the change of vasomotor symptom score was correlated significantly with the change of plasma prolactin level.

• Journal of Pharmaceutical Investigation
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• v.40 no.3
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• pp.167-173
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• 2010

Repeated oral administration of hydrochlorothiazide, a loop diuretic, due to transient high blood levels, may cause adverse effects such as gastric disturbance, nausea, high blood sugar, and hyper lipidemia. Transdermal administration could avoid some of these systemic side effects and gastric disorders. We have developed a matrix using ethylene-vinyl acetate (EVA), a heat-processible and flexible material, for transdermal delivery of hydrochlorothiazide. Drug solubility was highest at 40% PEG-400 volume fraction. Drug release increased as concentration increased with a linear relationship between the release rate and the square root of loading dose. Increasing temperature increased drug release from the EVA matrix. The activation energy, measured from the slope of log P versus 1000/T, was 11.9 kcal/mol for a 2.5% loading dose from EVA matrix. Diethyl phthalate had the highest plasticizing effects on the release of hydrochlorothiazide. To increase the skin permeation of hydrochlorothiazide from the EVA matrix, enhancers such as the saturated fatty acids, the unsaturated fatty acids, and the non-ionic surfactants were added to the EVA matrix, and skin permeation was evaluated using a modified Keshary-Chien diffusion cell fitted with intact excised rat skin. Polyoxyethylene 23-lauryl ether showed the highest enhancing effects. In conclusion, transdermal delivery of hydrochlorothiazide could be improved from an EVA matrix containing plasticizer and permeation enhancer.

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