• Title/Summary/Keyword: diabetic osteoporosis

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Pharmacokinetic Characterization of KR-67500, a Novel 11β-HSD1 Inhibitor (새로운 11β-HSD1 저해제인 KR-67500의 약물동태)

  • Im, So Hee;Ahn, Jin Hee;Kim, Ki Young;Bae, Myung Ae;Kim, Sang Kyum;Ahn, Sung-Hoon
    • YAKHAK HOEJI
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    • v.59 no.2
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    • pp.59-65
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    • 2015
  • KR-67500, trans-4-(2-(4-methyl-1,1-dioxido-6-(2,4,6-trichlorophenyl)-1,2,6-thiadiazinan-2-yl)acetamido)adamantane-1-carboxamide, is a novel $11{\beta}$-HSD1 inhibitor with its therapeutic effects of its anti-diabetic, anti-adipogenic and anti-osteoporotic activity. This study was performed to evaluate in vitro and in vivo pharmacokinetic properties of KR-67500 as a new drug candidate. KR-67500 was stable and highly bound to proteins in rat plasma. The microsomal stabilities of KR-67500 in human and rat liver were high. The inhibitory effect of KR-67500 for five cytochrome P450 enzymes was low. Preclinical pharmacokinetic studies have been carried out with intravenous or oral administrations of KR-67500 (10 mg/kg) to male rats and monkey. KR-67500 showed low clearance (0.68 l/h/kg) and high oral bioavailability (102%) in male rats. These results suggest that KR-67500 has good drug-like pharmacokinetic properties with a low first-pass effect and high bioavailability for an oral therapeutic agent of diabetes and osteoporosis.

The Comparative Effects of Yugmijihwangtang in Donguibogam and Experiment Research Results -Focusing on the Korean Medicine and Traditional Chinese Medicine- (육미지황탕 효능의 동의보감과 실험연구결과의 비교고찰 -한의학과 중의학을 중심으로-)

  • Han, Yoochang;Kim, Myung Dong;Lee, Sundong
    • Herbal Formula Science
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    • v.25 no.2
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    • pp.223-251
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    • 2017
  • Objectives : A lot of experiment results of Yugmijihwangtang(YM) are reported in various kinds of journals. Many of them report on the new effects that are not recorded in the traditional medical texts. So it is necessary to take it into consideration that newly reported effects could be of help to clinical practice, because this process of comparison of Donguibogam and scientific experiment results will have basis to lead into the evidence based medicine. Methods : We compared the effects of in Donguibogam and the experiment results of YM. Results : The effects of YM in Donguibogam are to replenish essence and marrow, and to treat red wen, fatigue, treat hypouresis, urinary sediment, urinary urgency, hematuria, hydrocephalus, speech and movement retardation, yin-deficiency, diabetes mellitus, nonalcoholic fatty liver, melanoma, disability to see near and far sight, tinnitus, hearing loss, alopecia, angiogenesis, cough, cough at night, trachyphonia, and, infantile convulsion. The experiment results of YM since 2000 in both Korea and China are to inhibit atopic dermatitis, renal interstitial fibrosis, anti-oxidant, emphysema, stress, glomerulosclerosis, diabetic nephropathy, chronic glomerulonephritis, hemorrhage, plantar sweating, dermal aging, kidney aging, bone loss, breast cancer, pathological myocardial cell, primary liver cancer, thrombosis, osteoporosis, intrauterine growth retardation, chronic renal failure, IgA nepropathy, slow cerebral development, and hippocampal tissue lesions on the one hand, and to help bone formation, renin-angiotensin- aldosterone system, cerebral recovery, cognitive function and expression, osteoblast proliferation and differentiation, learning and memory, cold-tolerance and oxygen deficit-tolerance and anti-fatigue, endometrial formation, humoral and cell-mediated immunity, immune regulation effect, Hypothalamus-Pituitary-Ovary Axis, and spermatogenesis, on the other hand. Conclusion : When we compared the effects of YM with the experiment results of YM, there existed a considerable gap between them. So, from now on, it is expected that a great effort and consideration are needed to solve these gaps from an academic and clinical point of view.

Relationship between bone mineral density and the remaining teeth in Korean adults (성인의 골밀도와 잔존치아수와의 관련성)

  • Song, Hye-Jeong;Lee, Duk-Hee
    • Journal of Korean society of Dental Hygiene
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    • v.15 no.1
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    • pp.63-71
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    • 2015
  • Objectives: The purpose of the study is to investigate the relationship between bone mineral density and remaining teeth in Korean adults. Methods: Using National Health and Nutrition Examination Survey(KNHANES) 5th Year 1(2010), 1,985 adults over 50 years old having bone mineral density test were selected. Male adults were 883, and female adults were 1,102. The raw data consisted of general characteristics of the subjects, bone density data, and oral examination data. The questionnaire consisted of general health survey, laboratory examination study, and nutrition study. Data were analyzed using SPSS 18.0 program for multiple regression analysis, ANOVA, t-test. The variables included general characteristics of the subjects, health behavior, diet habit, and oral health behavior. General characteristics consisted of gender, age, residence area, education level, marital status, monthly income, and vocation. Health behavior consisted of smoking, alcohol drinking, body mass index(BMI), physical activity, and mental health. Diet habit consisted of frequency of meal, milk, coffee, and calcium ingestion. Oral health behavior consisted of frequency of tooth brushing, use of oral health care devices, and oral examination. Systemic diseases were measured by the questionnaire for hypertension, diabetes mellitus, and hyperlipidemia. Bone density was measured in T-score of femoral bone, neck of femur, and lumbar vertebrae. Bone density was classified into normal($T-score{\geq}-1.0$), osteopenia(-2.5 < T-score < -1.0), and osteoporosis ($T-score{\leq}-2.5$). The remaining teeth were measured by the differences between normal teeth and missing teeth. Results: Smoking and age are the most influencing factors on the number of remaining teeth and bone density(p<0.01)(p<0.05). Those who had higher bone density, younger age, and nonsmoker significantly had more remaining teeth. Those who were men, diabetic, lowly educated women, and low birth weighted persons tended to have less number of teeth(p<0.01). Conclusions: The study suggested that there were significant differences between men and women according to the oral health management behavior and systemic disease control. Proper management of the oral health and good quality of bone mineral density can reserve the remaining teeth through the whole life.