• Title/Summary/Keyword: topical

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Structure-Activity Relationship of 2-Substituted Hydroquinones as Tyrosinase Inhibitors for Topical Delivery

  • Lee, Yeon-Jung;Yoon, Sung-Il;Kim, Dae-Duk;Kim, Jung-Sun
    • Journal of Pharmaceutical Investigation
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    • v.36 no.2
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    • pp.103-107
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    • 2006
  • In order to develop hydroquinone analogues for topical delivery, a structure-activity relationship study has been performed. A series of 2-substituted hydroquinones were tested for their ability to inhibit mushroom tyrosinase, alter melanin release and exert cytotoxicity in B6-F10 melanocytes. The electronic property of the 2-substituents did not affect the tyrosinase inhibition nor melanocyte toxicity. However, lipophilicity did affect to some degree the tyrosinase inhibition. The discrepancy in the structure-activity relationship may be due to the poor aqueous solubility of select analogues. Compounds with steric bulk at the 2-position seems to be less soluble, not enabling the analogue to interact effectively with the tyrosinase enzyme. Among the analogues tested, 2-isopropyl hydroquinone seems to be the most promising candidate for topical delivery, being the least toxic analogue with moderate melanin release inhibition.

Effect of Toluene Application to the Rat Skin on the Oxygen Free Radical Metabolizing System (흰쥐에 있어서 피부조직의 Oxygen Free Radical 대사계에 미치는 Toluene의 영향)

  • 채순님;윤종국;박원학
    • Toxicological Research
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    • v.17 no.1
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    • pp.33-39
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    • 2001
  • To evaluate the skin toxicity oj topical toluene application, toluene (35 mg/$cm^2$) was sequentially applied to the portion rat skin for five days. The topical toluene application resulted in increased xanthine oxidase activity and CYP content, and significantly decreased superoxide dismutase and glutathione peroxidase activities at five days in rat skin. Especially catalase activity was remarkably decreased in toluene-applied rat skin. And benzylalcohol dehydrogenase activity showed also a significant decrease in toluene-applied skin. On the other hand, histopathological ultrastructural examination revealed disrupted epidermal basement membrane, rared intercellular adhensions and degenerated keratin layer due to topical toluene application. Increased deposit of cerrous perhydroxide resulted from reaction with $H_2O_2$was abserved in toluene-treated animals. These results indicate that oxygen free radical may be responsible for ultrastructural changes in skin tissue by toluene application to rat skin.

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Drug Screening for the Formulation of Topical Antiblister Preparations (수포독성 처치용 외용제 제제설계를 위한 약물의 검색)

  • 김동욱;박은석;지상철
    • Biomolecules & Therapeutics
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    • v.7 no.2
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    • pp.191-197
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    • 1999
  • The effects of various drugs on the alleviation of the symptoms of chemical bums were evaluated in mice to formulate topical antiblister preparations. After a chemical bum was induced on the mouse dorsal skin with 2-chloroethylethyl sulfide, the drug was applied on the disease site. The effectiveness of the drug was evaluated by determining blister size, necrosis score of skin and appearance of the chemical burns induced. It showed that steroids and aminoglycoside antibiotics had a tendency to protect skin cell, and antihistamines decreased the size of chemical bums. While oleaginous base resulted in deleterious effect, hydrophilic base didn't show a significant difference on the alleviation of the chemical burn symptoms compared to the control.

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Antibacterial Activity of Topical Agent Extracted from Phellodendri cortex, Forsythia fructus and Glycyrrhizae radix Against Staphylococcus intermedius in Dogs (황백, 연교 및 감초 추출물을 이용한 국소제제의 Staphylococcus intermedius에 대한 항균효과)

  • Jeong Hyo-Hoon;Oh Tae-Ho
    • Journal of Veterinary Clinics
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    • v.22 no.4
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    • pp.353-356
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    • 2005
  • This study was performed to examine the antibacterial efecacy of topical agent extracted from Phellodendri cortex, Forsythia fructus and Glycyrrhizae radix as an alternative dermatological agent. Also, the most efficacious concentration of this agent and the skin-contact time inhibiting the vegetation of bacterial cells in various dilutions were determined. Five strains of Staphylococcus intermedius were exposed to various dilutions of this agent. The efficacy was assessed after exposure for time periods varying between 0 and 30 min. The antibacterial efficacy was shown to be the strongest at dilution of 1: 2. The number of viable organisms decreased significantly after 8 minutes of exposure time and was the smallest after 30 minutes of exposure time. This alternative dermatological agent is considered to be effective against Staphylococcus intermedius and has a potential to be a new topical agents far the treatment of pyoderma in dogs.

Two Cases of Alopecia Totalis treated with Diphenylcyclopropenone (DPCP) Immunotherapy (Diphenylcyclopropenone (DPCP) 면역요법으로 호전된 전두 탈모증 2 예)

  • Moon, Seok-Ki;Shin, Young-Min;Kim, Chan-Woo;Shin, Dong-Hoon;Choi, Jong-Soo;Kim, Ki-Hong
    • Journal of Yeungnam Medical Science
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    • v.23 no.2
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    • pp.232-239
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    • 2006
  • Treatments for alopecia areata include topical corticosteroid treatment, corticosteroid intralesional injection, systemic corticosteroid treatment, PUVA(psoralen-UVA) and topical immunotherapy. The therapeutic effects are variable. Alopecia totalis is hard to treat completely. Topical immunotherapy with dinitrochlorobenzene (DNCB), squaric acid dibutyl ester (SADBE) or diphenylcyclopropenone (diphencyprone, DPCP) represents the most accepted therapeutic modality for the treatment of extensive alopecia areata. We report two cases of alopecia totalis treated with DPCP. After DPCP treatment, total scalp hair was completely recovered.

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Acute Subcutaneous Toxicity Study of Syndella Gel, Topical Drug Containing Deproteinised Dialysate of Calf′s Blood and Micronomicin Sulfate in Rats (랫트에 있어서 신델라 겔 (송아지의 제단백혈액추출물: 황산 미크로노마이신=20:1 혼합물)의 피하급성독성시험)

  • 남석우;서동완;안성훈;장만식;최완수;김규봉;우태욱;한정환;홍성렬
    • Biomolecules & Therapeutics
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    • v.4 no.4
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    • pp.411-414
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    • 1996
  • Single subcutaneous administration to S.D rats of both sexes was performed to investigate the acute toxicity of Syndella gel, a new topical drug containing deproteinised dialysate of calf's blood and micronomicin sulfate. $LD_{50}$ values for S. D rats were 23,047 mg/kg for male and 23,725 mg/kg for female. The death occurred within 24 hours after administration at doses over 19,200 mg/kg. The main cause of death seemed to be respiratory disturbance by acute shock. Major general symptoms induced by injection subcutaneously with Syndella gel were underactivity, decreased respiratory rate, salivation, tremor and loss of consciousness. No significant body weight changes and gross findings of internal organs in treatment groups in comparison with those of control groups was observed at any dose levels in Syndella gel.

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Alternative Therapies with Tacrolimus and Low-Dose Doxycycline for Oral Chronic Graft-versus-Host Disease That Is Resistant to Topical Corticosteroid Medication: Case Report

  • Ju, Hye-Min;Ahn, Yong-Woo;Ok, Soo-Min;Jeong, Sung-Hee
    • Journal of Oral Medicine and Pain
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    • v.43 no.1
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    • pp.16-20
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    • 2018
  • Graft-versus-host disease (GVHD) is frequent complications of hematopoietic stem cell transplantation. In the chronic GVHD (cGVHD), the oral cavity is the most commonly affected region. The clinical manifestations include erythema, ulceration, lichenoid-hyperkeratotic change in oral mucosa, dry mouth, and limitation of mouth opening. The initial treatment strategy of oral cGVHD patients is topical corticosteroid therapy in various formulation. However, corticosteroid resistance appears in some patients. We report a case of a 25-year-old male patient with oral cGVHD, who has resistance to topical corticosteroid medication, treated with 0.03% tacrolimus ointment and low-dose doxycycline. The patient showed subjective and objective improvement without side effect.

Traditional topical herbal therapies in psoriasis

  • Keseroglu, Havva Ozge;Gonul, Muzeyyen
    • CELLMED
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    • v.4 no.4
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    • pp.23.1-23.8
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    • 2014
  • Psoriasis is a common, chronic, recurrent, immune-mediated inflammatory disorder of skin. Although conventional topical and systemic therapies yield remission for a while, they carry a risk of many side effects that limit the long term use of these agents and the disease recurs generally in a short period of time after cessation of therapy. An increasing number of psoriatic patients are using herbal products as a treatment to control their disease with less side effects. Clinicians should be aware of plants used in psoriasis and side effects related with them. The aim of this article is to review the different herbs used in psoriasis treatment.

Inhibitory Effect of Shimotsu-to, a Traditional Chinese Herbal Prescription, on Acute Inflammation in Rats and Guinea Pigs

  • Sakuma, Katsuya;Izumi-Kaji;Masahiko-Ogihara;Katsumi-Yamamoto
    • Archives of Pharmacal Research
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    • v.19 no.2
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    • pp.122-125
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    • 1996
  • We examined the effect of topical application of Shimotsu-to, a traditional Chinese herbal prescription, on carrageenin-induced edema in rats and ultraviolet radiation-induced erythema in guinea pigs. Shimotsu-to (5% in water) markedly suppressed an acute edema of rat hindpaw induced by 1% carrageenin, and was more effective than any other single crude drug componcent of Shimotsu-to, Topical treatment with this prescription also inhibited ultraviolet erythema on the back skin of guinea pigs (a human sunbrun model). These results suggest the therapeutic effect on acute inflammation by topical application of Shimotsu-to.

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Anesthesia for Office Based Vocal Fold Injection (외래 시행 성대주입술을 위한 마취 방법)

  • Kim, Han Su
    • Journal of the Korean Society of Laryngology, Phoniatrics and Logopedics
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    • v.31 no.2
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    • pp.56-60
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    • 2020
  • Vocal fold injections are usually performed with a patient wake in an office under local anesthesia. For comfortable and safe office-based procedures, thorough anesthesia and premedication should be provided to the following three regions; nasal cavity, oropharynx, and larynx. Topical lidocaine is most widely used anesthetics on office based procedure. Lidocaine has a low to intermediate potency, 45 minutes to 60 minutes' duration of action, and onset of sufficient anesthesia within 90 seconds of topical administration. Tetracaine, prilocaine, ropivacaine, and bupivacaine also have been used in the office-based procedures. Nasal decongestant, oxymetazoline, is also used for widening nasal cavity by constriction of nasal mucosa. The amount of topical and local anesthetics used in vocal fold injection rarely exceeds toxic doses. The physician should know proper anesthesia techniques and must be familiar with the safe dose and complication of all anesthetics used.