• Title/Summary/Keyword: Transdermal administration

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Enhanced Iontophoretic Delivery of Risedronate Sodium Across Hairless Mice Skin (무모생쥐 피부에 리제드로네이트 소디움의 이온토포레시스 경피전달)

  • Hwang, In-Young;Lee, Mi-Jung;Jung, Suk-Hyun;Jeong, Seo-Young;Cho, Sun-Hang;Gil, Young-Sig;Jeong, Sang-Young;Shin, Byung-Cheol
    • Journal of Pharmaceutical Investigation
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    • v.40 no.2
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    • pp.79-84
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    • 2010
  • Osteoporosis was traditionally defined by the occurrence of nontraumatic fractures, especially of the spine, in the setting of low bone mass. Bisphosphonates are an important group of therapeutic agents for the management of osteoporosis, as they inhibit bone resorption and increase bone density, thereby potentially decreasing fracture risk. Risedronate sodium is a bisphosphonate class used by oral formulation. In this study, risedronate was transdermally delivered by iontophoresis. Effects of polarity, pH, current density, and drug concentration were studied using a side-by-side diffusion cell including the hairless mice skin. In addition we studied effect of enhancers. The flux was evaluated by HPLC/UV system. The amount of transported drug under iontophoretic delivery was approximately 186 fold higher than that under passive delivery. Flux was proportional to the increase of drug concentration and current density. The flux was observed about 0.68mg/$cm^2$ when the amout of Propyleneglycol monolaurate (PGML) used 1% as enhancer. Results indicated that iontophoresis is an effective method for transdermal administration of risedronate sodium

Clinical Efficacy of Transdermal Clonidine (St 155 BS) for Anesthetic Management in Hypertensive Patients (고혈압 환자 마취시 Transdermal Clonidine (St 155 BS)의 임상적 유용성)

  • Lee, Hyun-Hwa;Kim, Dong-Ok;Kim, Keon-Sik;Choi, Young-Kyoo;Shin, Ok-Young;Kwon, Moo-Il;Lee, Doo-Ik
    • The Korean Journal of Pain
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    • v.6 no.2
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    • pp.231-236
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    • 1993
  • Clonidine, a centrally-acting antihypertensive agent known to reduce central sympathetic outflow and modulate presynaptic transmitter's release, has shown to suppress central noradrenergic hyperactivity induced by immobilization stress in animals, by decreasing the MAC of halothane and the dose of narcotics required to prevent reflex cardiovascular response to noxious stimuli, and to have potent analgesic properties in humans. These characteristics suggest that clonidine might be a useful adjunct to the anesthetic management of patients with preexisting hypertension. Accordingly, we determined the clinical efficacy and safety on analgesia, sedation and hemodynamic stability in the perioperative period. Thirty patients(ASA physical status II-III) with a history of arterial hypertension, scheduled for elective orthopedic surgery were randomly assigned to two groups. We applied CPA-clonidine patch($6.9\;mg/cm^2$, 0.2 mg delivered daily) or placebo patch to each groups, 48 hours prior to induction of anesthesia. Antihypertensive medication was continued until the morning of the scheduled surgery. All patients received premedication of atropine and lorazepam, and induced anesthesia with thiopental and succinylcholine, and maintained with enflurane and 50% nitrous oxide, while sustaining the BP and pulse rate at acceptable range. For the relief of pain postoperatively, diclofenac and fentanyl were administered intramuscularly on demand. The results were as follows: 1) The change of hemodynamic responses in clonidine group was less compared to the placebo group. 2) Intraoperative anesthetic requirement for enflurane in clonidine group were significantly lower than placebo group. 3) Postoperative analgetic requirement in clonidine group were significantly lower than placebo group. In clonidine group, 5 cases out of 15 cases were required no analgetics, and the incidence of administration of additional fentanyl was decreased to 5 cases, comparing with 10 cases in placebo group.

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Inhibitory Effects of Camellia sinensis Extract on the Development of Atopic Dermatitis-like Lesions in NC/Nga Mice

  • Kim, Tae Hong;Ha, Si Young;Yang, Jae-Kyung
    • Journal of the Korean Wood Science and Technology
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    • v.42 no.5
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    • pp.579-589
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    • 2014
  • Atopic dermatitis (AD) syndrome is one of the most common and severe skin diseases in Korea; a large population has this disease. We examined the effects of the extract from the leaf and sprig of Camellia sinensis on the development of AD by using NC mice as a model of atopic dermatitis. Oral administration of the extract to NC/Nga mice treated with 2,4?dinitrochlorobenzene (DNCB) inhibited the development of AD-like skin lesions as shown by a significant decrease in the skin symptoms of the disease and a decrease in ear thickness and levels of immunoglobulin E (IgE) and thymus-and activation-regulated chemokine (TARC) level in the skin. Administration of the extract markedly suppressed the DNCB-induced mRNA expression of interleukin 4 (IL-4) and tumor necrosis factor ${\alpha}$ (TNF-${\alpha}$). The findings suggest that transdermal application of the extract may modulate in the skin of NC/Nga mice. The extract was effective for the prevention and treatment of AD.

Skin Irritation of Natural Dyes Extracted from Onion (Allium cepa) (양파로부터 추출한 천연염료의 피부자극성 시험)

  • 배순이;오태광;박승춘
    • Toxicological Research
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    • v.13 no.1_2
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    • pp.161-165
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    • 1997
  • This study was conducted to investigate the skin irritation by transdermal administration of the three dyes. These dyes were originated from onion by using extraction method. By the order of extraction from onion, A-dye was obtained from onion by using water at 90-100$\circ$C. B-dye was extracted from A-dye with ethylacetate. After ethylacetate extraction from A-dye, the lower layer named as C-dye. Twenty-four New Zealand white rabbits were divided into three groups. The each groups was consisted of two subgroups according to high dose (extracted dyes) and low dose (the 100-fold dilutions of A-, Band C-dye). In primary skin irritation test of male New Zealand White rabbits, body temperature and weights were not significantly changed and blood cells were positioned in normal blood cell ranges of health rabbits. Primary irritation index was "0" in the test and control sites of all animals used in this study. By the results obtained in the present test, all dyes were evaluated as a non-irritant on the basis of the criteria of Draize.of Draize.

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Skin Permeation of Flurbiprofen through Excised Rat Skin from Poloxamer 407 Gel

  • Gil, Hyung-Jun;Lee, Woo-Young;Chi, Sang-Cheol
    • Journal of Pharmaceutical Investigation
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    • v.24 no.3
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    • pp.27-32
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    • 1994
  • In order to reduce systemic side effects following oral administration, flurbiprofen was formulated as transdermal gels consisting of the drug, poloxamer 407 and ethanol in buffer solutions. The effect of formulation variables in the preparation of flurbiprofen gels on skin permeation of the drug was evaluated using Keshary-Chien diffusion cells fitted with excised rat skins. The permeation rate of flurbiprofen through rat skin was directly proportional to initial drug concentration (between 0.1% and 1.0%) in the gel while it was inversely proportional to poloxamer 407 concentration (between 17.5% and 25%). The skin permeation of flurbiprofen was substantially influenced by the gel pH between 3 and 7, exhibiting a maximum at pH 4. The concentration effect of ethanol on the permeation of the drug was negligible in the concentration range of $10{\sim}20%$.

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Current status of opioid prescription in South Korea using narcotics information management system

  • Soo-Hyuk Yoon;Jeongsoo Kim;Susie Yoon;Ho-Jin Lee
    • The Korean Journal of Pain
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    • v.37 no.1
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    • pp.41-50
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    • 2024
  • Background: Recognizing the seriousness of the misuse and abuse of medical narcotics, the South Korean government introduced the world's first narcotic management system, the Narcotics Information Management System (NIMS). This study aimed to explore the recent one-year opioid prescribing patterns in South Korea using the NIMS database. Methods: This study analyzed opioid prescription records in South Korea for the year 2022, utilizing the dispensing/administration dataset provided by NIMS. Public data from the Korean Statistical Information Service were also utilized to explore prescription trends over the past four years. The examination covered 16 different opioid analgesics, assessed by the total number of units prescribed based on routes of administration, type of institutions, and patients' sex and age group. Additionally, the disposal rate for each ingredient was computed. Results: In total, 206,941 records of 87,792,968 opioid analgesic units were analyzed. Recently, the overall quantity of prescribed opioid analgesic units has remained relatively stable. The most prescribed ingredient was oral oxycodone, followed by tapentadol and sublingual fentanyl. Tertiary hospitals had the highest number of dispensed units (49.4%), followed by community pharmacies (40.2%). The highest number of prescribed units was attributed to male patients in their 60s. The disposal rates of the oral and transdermal formulations were less than 0.1%. Conclusions: Opioid prescription in South Korea features a high proportion of oral formulations, tertiary hospital administration, pharmacy dispensing, and elderly patients. Sustained education and surveillance of patients and healthcare providers is required.

Use of the Stratum Corneum Reservoir for the Prediction of Skin Penetration

  • Cholee, Ae-Ri;Tojo, Kakuji
    • Journal of Pharmaceutical Investigation
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    • v.23 no.3
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    • pp.1-8
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    • 1993
  • A simple and quick method based on the transient diffusion theory for predicting the steady state rate of penetration of a drug after transdermal drug administration was proposed. The amount of drug entering the stratum corneum was determined by 20 strippings with an adhesive tape. From the profile of the amount of drug as a function of the number of strippings, the quantity of drug on the surface of stratum corneum was extrapolated. Based on the amounts of drug entering the stratum corneum during two time intervals $(t_1\;and\;t_2)$ within 1 hour after the application, the diffusion and partition coefficient were determined. Once the diffusion coefficient of the drug in the stratum corneum and the partition coefficient (stratum corneum/vehicle) were determined from the present approach, the steady-state flux of penetration across the stratum corneum was calculated. The steady-state rates of penetration of ascorbic acid and estradiol across hairless mouse skin were evaluated from this approach and compared with those obtained from ill vitro penetration experiment using excised hairless mouse skin. The data confirmed that the proposed method can predict the steady-state rate of penetration of these drugs across the stratum corneum.

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Evaluation or various vehicles and O/W Microemulsions of Flurbiprofen as Transdermal Delivery System (경피제제로서 수종의 플루비프로펜 Vehicle과 O/W 마이크로에멀젼의 평가)

  • Lee, Gye-Won;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.28 no.3
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    • pp.141-149
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    • 1998
  • In order to reduce systemic side effects following administration, flurbiprofen was formulated as O/W microemulsion consisting of the surfactant, oil phase and aqueous phase. Particle size distribution, apparent viscosity, solubility and skin permeation of flurbiprofen in various vehicles and microemulsion were evaluated. The domain of O/W microemulsion s phase diagram had difference between oil types and the area of O/W microemulsion was wide distributed by adding to PG and cosurfactant than that of water alone. As increasing 10, 15 and 20% of Brij 97 content and 1, 2.5, 5% of oil content, the solubility of flurbiprofen in O/W microemulsions and various vehicles was $400{\sim}1,000$ and $10{\sim}500$ times higher than that of control. Also, apparent viscosity of soybean oil microemulsions was higher than that of IPM microemulsions and that of vehicle were increased as increasing vehicle content. Since skin permeation of flurbiprofen decreased as increasing viscosity, in each vehicle, it was not affected 2% ${\beta}-CD$ and decreased as increasing PG content and to 2, 5 and 10% of $HP-{\beta}-CD$. In O/W microemulsion, 5% soybean oil. 20% Brij 97 and 75% water(A-1) with high viscosity showed low skin penetration.

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Skin Permeation of Indomethacin from Gels (겔제제로부터 인도메타신의 피부투과)

  • Kam, Sung-Hoon;Park, Eun-Seok;Chi, Sang-Cheol
    • Journal of Pharmaceutical Investigation
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    • v.25 no.2
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    • pp.129-136
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    • 1995
  • In order to reduce the systemic side effects and the gastrointestinal irritation of indomethacin following its oral administration, the drug was formulated as a transdermal gel using poloxamer 407. In vitro diffusion cells fitted with excised rat skins were used to evaluate the effects of formulation variables on skin permeation of indomethacin from poloxamer gels. The formulation variables were the concentrations of indomethacin, poloxamer 407 and ethanol, and the gel pH. The increase of the drug amount in the gel from 0.5% to 2.0% induced a direct but nonlinear increase in the skin permeation rate of indomethacin. The increase of poloxamer concentration from 17.5% to 25% in the gel resulted in a decrease of skin permeation rate of indomethacin, which was due to a reduction in the amount of free drug molecules available for permeation through skin by entrapping more drug molecules within the micelles formed by poloxamer. The increase of ethanol concentration from 10% to 20% in the gel resulted in a linear increase of permeation rate of indomethacin through skin, possibly due to the penetration enhancing effect of ethanol. The skin permeation of indomethacin was substantially influenced by the gel pH, exhibiting a maximum at pH 4.

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