• Title/Summary/Keyword: oral N-89

Search Result 38, Processing Time 0.025 seconds

Evaluating the activity of N-89 as an oral antimalarial drug

  • Nagwa S. M. Aly;Hiroaki Matsumori;Thi Quyen Dinh;Akira Sato;Shin-ichi Miyoshi;Kyung-Soo Chang;Hak Sun Yu;Takaaki Kubota;Yuji Kurosaki;Duc Tuan Cao;Gehan A. Rashed;Hye-Sook Kim
    • Parasites, Hosts and Diseases
    • /
    • v.61 no.3
    • /
    • pp.282-291
    • /
    • 2023
  • Despite the recent progress in public health measures, malaria remains a troublesome disease that needs to be eradicated. It is essential to develop new antimalarial medications that are reliable and secure. This report evaluated the pharmacokinetics and antimalarial activity of 1,2,6,7-tetraoxaspiro[7.11]nonadecane (N-89) using the rodent malaria parasite Plasmodium berghei in vivo. After a single oral dose (75 mg /kg) of N-89, its pharmacokinetic parameters were measured, and t1/2 was 0.97 h, Tmax was 0.75 h, and bioavailability was 7.01%. A plasma concentration of 8.1 ng/ml of N-89 was maintained for 8 h but could not be detected at 10 h. The dose inhibiting 50% of parasite growth (ED50) and ED90 values of oral N-89 obtained following a 4-day suppressive test were 20 and 40 mg/kg, respectively. Based on the plasma concentration of N-89, we evaluated the antimalarial activity and cure effects of oral N-89 at a dose of 75 mg/kg 3 times daily for 3 consecutive days in mice harboring more than 0.5% parasitemia. In all the N-89-treated groups, the parasites were eliminated on day 5 post-treatment, and all mice recovered without a parasite recurrence for 30 days. Additionally, administering oral N-89 at a low dose of 50 mg/kg was sufficient to cure mice from day 6 without parasite recurrence. This work was the first to investigate the pharmacokinetic characteristics and antimalarial activity of N-89 as an oral drug. In the future, the following steps should be focused on developing N-89 for malaria treatments; its administration schedule and metabolic pathways should be investigated.

Evaluation of customized oral health promotion program for North Korean defector (북한이탈주민 맞춤형 구강건강증진 프로그램의 효과)

  • Jeon, Kiha;Lee, Suyoung
    • Journal of Korean Academy of Oral Health
    • /
    • v.42 no.4
    • /
    • pp.109-117
    • /
    • 2018
  • Objectives: The purpose of this study was to evaluate the customized oral health promotion program for North Korean defectors (NKDs). Methods: Using a pre-survey comprising phases 1-5 of the PRECEDE-PROCEED model, a customized oral health promotion program was created. The participants, a total of 129 NKDs, were allocated to the experimental group (n=64; 43 females and 21 males) or the control group (n=65; 46 females and 19 males). After the interventions, phases 7 to 9 of the PRECEDE-PROCEED model were executed to determine the effect of the program. Results: The results for phase 7 revealed high satisfaction with the program, with an average of 2.89 out of 3 points. In phase 8, concerning the impact evaluation, it was found that oral health beliefs and oral health knowledge were improved, with statistically significance differences before and after the experiment. Phase 9, concerning the outcome evaluation, showed that there were statistically significant differences in the average within groups before and after education in oral health beliefs (OHB), O'Leary index scores, and CPI. In terms of the difference between the groups, there were statistically significant improvement in OHB, O'Leary index scores, and CPI after the education program. Conclusions: The oral health promotion program developed in this study has made a positive contribution to improve the oral health status of NKDs.

Pharmacokinetics and Metabolism of Endothelin Receptor Antagonist: Contribution of Kidneys in the Overall In Vivo N-Demethylation

  • Chong, Sae-Ho;Obermeier, Mary;Humlherys, W.-Griffith
    • Archives of Pharmacal Research
    • /
    • v.26 no.1
    • /
    • pp.89-94
    • /
    • 2003
  • In vivo clearance of BMS-182874 was primarily due to metabolism via stepwise N-demethylation. Despite in vivo clearance approached ca 50% of the total liver plasma flow, BMS-182874 was completely bioavailable after oral administration in rats. Saturable first-pass metabolism and the role of extrahepatic tissue were evaluated as possible reasons for complete oral bioavailability despite extensive metabolic clearance. Pharmacokinetic parameters were obtained after an intravenous and a range of oral doses of BMS-182874 in rats. Bile and urine were collected from bile-duct cannulated (BDC) rats and the in vivo metabolic pathways of BMS-182874 were evaluated. Pharmacokinetics of BMS-182874 were also compared in nephrectomized (renally impaired) vs. sham-operated control rats. Oral bioavailability of BMS-182874 averaged 100%, indicating that BMS-182874 was completely absorbed and the first-pass metabolism (liver or intestine) was negligible. The AUC and C/sub max/ values increased dose-proportionally, indicating kinetics were linear within the oral dose range of 13 to 290 mmole/kg. After intravenous administration of BMS-182874 to BDC rats, about 2% of intact BMS-182874 was recovered in excreta, indicating that BMS-182874 was cleared primarily via metabolism in vivo. The major metabolite circulating in plasma was the mono-N-desmethyl metabolite and the major metabolite recovered in excreta was the di-N-desmethyl metabolite. In vivo clearance of BMS-182874 was significantly reduced in nephrectomized rats. These observations suggest saturable first-pass metabolism is unlikely to be a mechanism for complete oral bioavailability of BMS-182874. Reduced clearance observed in the nephrectomized rats suggests that extrahepatic tissues (e.g., kidneys) may play an important role in the in vivo clearance of xenobiotics that are metabolized via N-demethylation.

The Prevalence of Oral Spirochetes in Korean Adult Periodontitis (한국인 성인성 치주염 환자에서의 구강 스피로헤타의 분포)

  • Kim, Hay-Hyun;Choi, Bong-Kiu;Choi, Seong-Ho;Chai, Jung-Kiu;Kim, Chong-Kwan;Cho, Kyoo-Sung
    • Journal of Periodontal and Implant Science
    • /
    • v.28 no.4
    • /
    • pp.659-678
    • /
    • 1998
  • In the present study, oligonucleotide probes based on 16S rRNA were taken to investigate the diversity of oral spirochetes without culture method. This is the first study that revealed oral spirochetes of both presently cultivable and uncultured oral spirochetes in Korean adult periodontitis patients. Subgingival plaque samples were taken from diseased sites(probing depth ${\geq}6\;mm$, experimental group, n=116) and healthy sites(probing depth${\leq}3mm$, control 1 group, n=28) in 29 patients with adult periodontitis, and from 20 periodontally healthy subjects(probing depth${\leq}3mm$, control 2 group, n=100). Following being examined under phase-contrast microscope, all samples were submitted to dot-blot hybridization after polymerase chain reacton with eubacterial primers. 5 species-specific probes(TVIN, TDEN, TMAL, TSOC, and TPEC) and 7 group-specific probes(TRE I, TRE II, TRE III, TRE IV, TRE V, TRE VI, and TRE VII) were used one by one for the identification of both cultivable and so far uncultivable oral spirochetes. All probes were labeled with digoxigenin(DIG)-ddUTP and detected by chemilumininescence. The following results were obtained. 1. Under phase-contrast microscope, 91.37% and 14.28% of oral spirochetes were observed in the experimental and control 1 groups, respectively. None of oral spirochetes were observed in control 2 group. 2. With universal probe, 98.27%, 46.42%, and 22.0% of oral spirochetes were observed in experimental, control 1, and control 2 groups, respectively. 3. With specific probe, 95.68%, 35.71%, and 19.0% of oral spirochetes were observed in experimental, control 1, and control 2 groups, respectively. 4. With species-specific probes, T. socranskii were recovered in a high percentage of sites(81.89%) examined, followed by T. maltophilum(50.0%), T. vincentii(36.20%), T. denticola(13.79%), respectively. With group- specific probes, TRE IV was recovered in a high percentage of sites(85.34%) examined, followed by TRE II(77.58%), TRE I(56.89%), TRE III(25.86%), TRE VI(5.17%), and TRE V(2.58%), respectively. 5. T. vincentii were only observed in the diseased sites, not in the healthy sites. 6. Neither T. pectinovorum nor group VII oral spirochetes were observed in any sites. The findings warrant further investgations of the recovered spirochetes to elucidate the possible associations of oral spirochetal prevalence in race and types of periodontitis, pathogenesis of T. vincentii and the possible distributional change of oral spirochetes before and after treatments.

  • PDF

Effects of Chronic Nicotine Administration on Salivary Gland in Mice: Immunohistochemical Study

  • Jung, Jung-Woo;Choi, Jae-Kap;Byun, Jin-Seok
    • Journal of Oral Medicine and Pain
    • /
    • v.39 no.3
    • /
    • pp.83-89
    • /
    • 2014
  • Purpose: Chronic nicotine administration induce various effects in whole organs of the body; however, little is known about salivary gland. In the present study, we pursued the links between systemic nicotine and the histomorphological changes of the salivary gland in mice. Methods: Twenty-five C57BL6 mice were allocated into two groups. The control group (n=9) received distilled water only for 8 weeks by gavage. The experimental nicotine group (n=16) was administered nicotine $5{\mu}g/g$ with distilled water. Animals were sacrificed at 8 weeks; then, submandibular glands were excised and processed for histologic evaluation. Volumetric changes in acinar cells were evaluated by H&E staining. The expression of calponin-positive myoepithelial cells and Ki-67-positive proliferating acinar cells were evaluated by immunohistochemistry. Results: The nicotine group showed significantly decreased number of calponin-positive myoepithelial cell process compared with the control group. There were no significant differences in average volume of acinar cell and the number of Ki-67-positive acinar cells between both groups. Conclusions: These findings suggested that chronic nicotine administration may cause decreased function of myoepithelial cells in submandibular glands of mice, and these can partly explain xerostomic conditions in chronic smokers.

Pharmacokinetic Properties and Antiinflammatory Activity of Ketoprofen Lotion (케토프로펜 로오숀의 약물동력학적 특성과 항염증작용)

  • 단현광;배준호;박은석;지상철
    • Biomolecules & Therapeutics
    • /
    • v.6 no.1
    • /
    • pp.45-49
    • /
    • 1998
  • The pharmacokinetic properties and antiinflammatory activity of 3% ketoprofen lotion (ID-lotion), formulated with poloxamer 407, were evaluated using rats. For the pharmacokinetic study, the lotion, at the dose of 4.5 mg/kg, was applied on the dorsal skin of rats and the drug concentration in plasma was determined using an HPLC method. As references, ketoprofen suspended in saline was administered orally, and E-lotion, which is a 3% ketoprofen lotion in the Japanese market was applied transdermally. Following the transdermal application of ID-lotion and E-lotion, $C_{max}$ were 316 $\pm$22.3 ng/ml and 163 $\pm$ 12.2 ng/ml, respectively, at the same Tma of 2 hours postdose, while $C_{max}$ and $T_{max}$ after oral administration of the drug were 1,030$\pm$89.1 ng/ml and 0.25 hours, respectively. Relative bioavailabilities of ID-lotion and I-lotion were 69.3% and 34.2%, respectively. The antiinflammatory activity of the two 3% ketoprofen lotions was evaluated with carrageeneninduced edema method after 50 mg of the lotions was applied on the paw of rats. ID-lotion showed 67.6% inhibition of the edema formation, while I-lotion showed 34.\\\\`r%. The calculated ED5o after transdermal application of ID-lotion was 2.5 mg/kg, while that after oral administration was 7.0 mg/kg. Based on these results, the relative equiponderal availability of ID-lotion was 296% compared to the oral administration of ketoprofen.n.n.n.

  • PDF

Effect of Oral Health Knowledge and Attitude of Caregivers on Oral Health Management of Elderly Inpatients (간병인의 구강보건지식 및 태도가 노인환자의 구강건강관리행위에 미치는 영향)

  • Lim, Hee-Jung;Cho, Han-A
    • The Journal of Korean Society for School & Community Health Education
    • /
    • v.18 no.3
    • /
    • pp.55-68
    • /
    • 2017
  • Objectives: Republic of Korea has entered an aged society, recently. As chronic diseases increase, elderly inpatients has been increasing and they have used caregivers for convenience. Accordingly, this study aims to investigate the oral health knowledge and attitude of caregivers on oral health management of elderly inpatients, which would affect the general health and quality of life. Methods: A survey questionnaire was distributed to the caregiver(n=165), at a neurosurgery or orthopedic hospital inpatient ward in Seoul, Gyeonggi-do from April 1 to 14, 2017. We analyzed the data with descriptive statistics analysis, chi-squared analysis and logistic regression analysis by using SPSS 23.0. Results: The response rate to the questionnaire was 92%. Oral health management provided by caregivers to inpatients in the elderly was prevention of oral diseases(92.8%), tooth brushing (89.5%), use of oral care products(68.4%), denture cleaning(90.8%) and oral cleaning(90.8%). Frequency analysis of oral health management in accordance with the educational needs of caregivers was all confirmed statistically significant(p<0.05). In the logistics regression model, oral health knowledge was significantly associated with low oral cleaning(OR=1.58) and oral health attitude was significantly associated with high denture cleaning(OR=1.29) and oral cleaning(OR=1.28) after adjustment for other covariates including gender, age, certification, education level, ward, working years. Conclusions: It is necessary to expand the scope and improve the quality of education that can change the attitudes and behaviors of the caregivers on the oral health management of the elderly on the basis of the current oral health education.

  • PDF

Oral Health Education Status of Elementary School in Gangwon-Do (강원도 초등학교 구강보건교육 실태)

  • Ryu, Da-Young;Ma, Deuk-Sang
    • Journal of the Korean Society of School Health
    • /
    • v.21 no.1
    • /
    • pp.33-41
    • /
    • 2008
  • Purpose : The purpose of this study was to provide the basic data for p lanning oral health education in elementary schol. Methods conducted using a postal, self-administered questionnaire. A questionnaire containing 19 questions about oral health education which was provided by health teachers in elementary schol was used for data colle ction. Total response rate was 64.3% (119 out of 185). Results : Oral health education except one through textbooks was conduc of which taught oral health themselves. The contents of oral he alth education through special clas was mainly focusing on the tothbrushing method, dental caries, and the use of fluo ride. Acording to the grades clasified by the level of education, the order was the 3rd, 1st, and 2nd grade, which mea ns that the lower grades got more training than the h was acquired through the internet (72.2%), health-related organizations or academies (51.5%). Also, materi als for oral health education were obtained from health-related organizations or academies (67%), self-productio n (49.5%). According to the data during the past 5 years it was found that 13.4% health teachers had oral health-related that more traing neded to be conducted from 89.7% health tea chers. The most dificult problem in oral health education were insufficient time (56.7%). Conclusion : For effective oral health education, there needs a developmen t of targeted goal to achieve a systemic oral health education for each grades as wel as a ned for as health teachers to eficiently acquire knowledge and materials for oral health education, it is necessary to hold regular workshops for health teachers, and develop and distribute appro priate educational materials.

Association between Amalgam Tooth Fillings and Blood Mercury Levels in Children

  • SaKong, Joon;Choi, Youn-Hee;Chung, Sun-Young;Kwon, Ho-Jang;Karmaus, Wilfried;Merchant, Anwar T.;Ha, Mi-Na;Hong, Yun-Chul;Kang, Dong-Mug;Song, Keun-Bae
    • International Journal of Oral Biology
    • /
    • v.36 no.3
    • /
    • pp.123-128
    • /
    • 2011
  • The notion that dental amalgam is a potential source of mercury exposure remains a controversial issue. However, there are few epidemiological analyses that have addressed whether this occurs in children. We aimed in our current study to identify the relationship between dental amalgam filling surfaces and the blood mercury levels in a cohort of 711 South Korean children aged between 8-9 years. Oral examinations were conducted to detect the number of amalgam filling surfaces on the teeth of these individuals. Blood samples were also taken from these children to assess the levels of mercury accumulation in the body. The amalgam filling surfaces were classified into four groups based on their number: 0 (n = 368), 1-5 (n = 219), 6-10 (n = 89), and 11+ (n = 35). The blood mercury levels in the children with more than 10 amalgam surfaces was 0.47 ${\mu}g$/L higher on average than those with no amalgam surfaces after adjusting for the frequency of fish or seafood consumption, age, and gender (P < 0.05). We found from our data that a higher number of dental amalgam fillings correlated with a higher blood mercury level in Korean children. Further studies are needed to investigate whether these elevated mercury levels exert neurotoxic or nephrotoxic effects.

ROENTGENOGRAPHIC STUDY OF NUTRIENT CANALS AND BONE TRABECULAR PATTERN (X선상으로 본 영양관과 골주상구조에 관한 연구)

  • Park Tae Won
    • Journal of Korean Academy of Oral and Maxillofacial Radiology
    • /
    • v.7 no.1
    • /
    • pp.16-18
    • /
    • 1977
  • The purposes of this investigation was to determine the appearance rate of nutrient canals and the aspect of alveolar bone trabecular patterns. 1949 subjects, averages 23 years old, who have normal occlusion were used. The film used in this investigation was full mouth roentgenographic survey. The obtained results were as follows: 1. In the trabecular pattern, coarse form was 35.17% and fine one was 64.14% in both jaws. 2. The appearance rate of nutrient canals was much higher in mandibular anterior segment(89.13%) than in the maxillary posterior segment(0.86%). 3. In the trabecular forms, small trabecular space and horizontal relation appeared in the mandible, and vertical relation in the maxilla.

  • PDF