The aim of this study is to develop a physiologically based pharmacokinetic (PBPK) model in intra-abdominal infected rats, and extrapolate it to human to predict moxifloxacin pharmacokinetics profiles in various tissues in intra-abdominal infected human. 12 male rats with intra- abdominal infections, induced by Escherichia coli, received a single dose of 40 mg/kg body weight of moxifloxacin. Blood plasma was collected at 5, 10, 20, 30, 60, 120, 240, 480, 1440 min after drug injection. A PBPK model was developed in rats and extrapolated to human using GastroPlus software. The predictions were assessed by comparing predictions and observations. In the plasma concentration versus time profile of moxifloxcinin rats, $C_{max}$ was $11.151{\mu}g/mL$ at 5 min after the intravenous injection and $t_{1/2}$ was 2.936 h. Plasma concentration and kinetics in human were predicted and compared with observed datas. Moxifloxacin penetrated and accumulated with high concentrations in redmarrow, lung, skin, heart, liver, kidney, spleen, muscle tissues in human with intra-abdominal infection. The predicted tissue to plasma concentration ratios in abdominal viscera were between 1.1 and 2.2. When rat plasma concentrations were known, extrapolation of a PBPK model was a method to predict drug pharmacokinetics and penetration in human. Moxifloxacin has a good penetration into liver, kidney, spleen, as well as other tissues in intra-abdominal infected human. Close monitoring are necessary when using moxifloxacin due to its high concentration distribution. This pathological model extrapolation may provide reference to the PK/PD study of antibacterial agents.
Journal of the Korea Organic Resources Recycling Association
/
v.8
no.3
/
pp.104-111
/
2000
The study war carried out to evaluate the characteristics of inorganic phosphate factions in soil mixed with paper mill sludge compost(PMSC). The experiments were conducted by an incubation test. For the incubation test, application rates of PMSC to soil were 0, 2, 8, and 16%. Water content of the samples mixed with PMSC were adjusted to 10% and 15% and incubating temperatures of the samples were kept at $4^{\circ}C$ and $30^{\circ}C$, respectively. The results can be concluded as follows; pH increased depending on the higher rates of PMSC application to the soil during the incubation tests, because calcium content was $4.9cmol_c/kg$ and contents of nutrients were high. When the application rates of PMSC were increased Saloid-P and Fe-P decreased, while Al-P and Ca-P in soil increased during the incubation tests.
To investigate effects of the shared living on nutrient intakes,250 college male students who were living alone (104 men) or sharing accommodation with friends (134 men) were participated. Their average age was 22.6 years, their average height was 171.8 cm, their average weight was 65.6 kg and their average Body Mass Index (BMI) was 22.2. The caloric intakes of the men living alone or sharing accommodation were 55.9% and 72.5% of the Korean Recommended Dietary Allowance (RDA), respectively. The decreased caloric level of the group living alone seemed to be due to their decreased protein and fat consumption as compared to that of the group sharing accommodation. The group living alone consumed increased amounts of fiber for breakfast and half the carbohydrates, but more fat (p < 0.05) in snacks than the group sharing accommodation. The daily carbohydrate : protein : fat (C : P : F) ratio averaged 58.6 14.1 27.3, which is a lower carbohydrate and a higher fat ratio than the Korean recommended ratio. However, the group living alone was closer to the Korean recommended ratio than the group sharing accommodation. The food intake habits were evaluated as being poorer in the group living alone as compared to the group sharing accommodation, less frequent consumption of fried / pan-fried dishes, and fruits / juices, but more frequent consumption of instant / processed foods. In comparing the eating patterns of the two groups, the group living alone showed better eating habits, such as more“breakfast eating”and less“snacking in the morning, afternoon or late at night”whereas the group sharing accommodation showed better eating habits such as less“picky eaters”and less “eating out”. In the group living alone, their lower caloric intake was assumably due to their fewer side dishes, however they showed higher eating frequencies of instant i processed foods. Since the lifestyle of living alone seems to grow gradually among young men, we strongly recommend dietary education for them.
Objectives : Samhwangsasim-tang (SHSST) is a traditional Korean medication, which has been used in Korea for treatment of hypertension and chest pain. Hyperlipidemia and inflammation could influence hypertension and chest pain. This study investigated whether and how SHSST reduces the hyperlipidemia and inflammation related to high-cholesterol diet-induced obesity in rats. Methods : Mice were divided randomly into four groups: the normal diet group, high-cholesterol diet group, low dose treatment group supplemented with 30% ethanol extract of SHSST (L) and high dose treatment group supplemented with 80% ethanol extract of SHSST (H). L and H groups were orally administered with SHSST at the dose of 50mg/kg a day respectively and others were administered with the same volume of physiological saline. Results : Administration of SHSST resulted in a decrease in serum levels of total cholesterol and low-density lipoprotein. Expression of hepatic genes(SREBP2, LXR, LDLR, and HMG-CoA) related with cholesterol metabolism was also suppressed. In addition, SHSST decreased the expression of inflammation-related gene (TNF-${\alpha}$, IL-6, ICAM-1, VCAM-1, TGF-${\beta}1$ and fibronectin). Histological examinations also showed that the size of the adipocytes was smaller in the SHSST treated group than in the high-colesterol diet group. In an in vitro study, SHSST inhibited the production of nitric oxide in a concentration-dependent manner. Conclusions : This study indicates that SHSST has anti-hyperlipidemia and anti-inflammatory effects. It may also suggest that SHSST may be alternative therapy for treatment of hyperlipidemia and its complications.
This study was performed to determine the composition of phenolic substances contained in the leaves of Cirsium setidens (Compositae), validate the high-performance liquid chromatography (HPLC) method, and determine the in vivo sedative effect of the main component pectolinarin. Six phenolic compounds isolated from C. setidens were spectroscopically identified as chlorogenic acid (1), hyperoside (2), 3,4-di-O-caffeoylquinic acid (3), caffeic acid methyl ester (4), linarin (5), and pectolinarin (6) and then used as standard compounds for HPLC analysis. HPLC proved to be precise, accurate, and sensitive for the simultaneous analysis of the phenolic substances. In particular, six compounds showed good regression ($R^2$ > 0.999) within test ranges and recovery was in the range of 95.4 - 104.8%. The content of pectolinarin was considerably higher (156.48 mg/g) than those of other phenolic substances including the other flavone glycoside, linarin (18.99 mg/g). The contents of other phenolic substances, in order, were chlorogenic acid (8.41 mg/g), 3,4-di-O-caffeoylquinic acid (5.74 mg/g), hyperoside (4.33 mg/g), and caffeic acid methyl ester (0.51 mg/g). Oral administration with compound 6 (10 and 20 mg/kg) enhanced the sleeping time induced by pentobarbital in mice, indicating that it has a sedative effect.
Jang, Mee;Chung, Kun Ho;Ji, Young Yong;Lim, Jong Myung;Kang, Mun Ja;Choi, Guen Sik
Journal of Radiation Protection and Research
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v.41
no.2
/
pp.101-104
/
2016
Background: To protect the public from natural radioactive materials, the 'Act on safety control of radioactive rays around living environment" was established in Korea. There is an annual effective dose limit of 1 mSv for products, but the activity concentration limit for products is not established yet. Materials and Methods: To suggest the activity concentration limits for consumer goods containing NORM, in this research, we assumed the "small room model" surrounding the ICRP reference phantom to simulate the consumer goods in contact with the human bodies. Using the Monte Carlo code MCNPX, we evaluate the effective dose rate for the ICRP reference phantom in a small room with dimension of phantom size and derived the activity concentration limit for consumer goods. Results and Discussion: The consumer goods have about 1600, 1200 and $19000Bq{\cdot}kg^{-1}$ for $^{226}Ra$, $^{232}Th$ and $^{40}K$, and the activity concentration limits are about six times comparing with the values of building materials. We applied the index to real samples, though we did not consider radioactivity of $^{40}K$, indexes of the some samples are more than 6. However, this index concept using small room model is very conservative, for the consumer goods over than index 6, it is necessary to reevaluate the absorbed dose considering real usage scenario and material characteristics. Conclusion: In this research, we derived activity concentration limits for consumer goods in contact with bodies and the results can be used as preliminary screening tool for consumer goods as index concept.
Eighteen water buffalo calves of Nili-Ravi breed (about 15 months age and of $147{\pm}12$ kg average body weight and mixed sex) were used with six animals on each treatment. All the animals were fed long wheat straw for ad libitum intake as the basal ration. Animals in group-I were supplemented with ad libitum amount of urea molasses block having cotton seed meal (CSMB) while the animals in group-II were supplemented with ad libitum urea molasses block containing sunflower seed meal (SFMB) and group III animals were supplemented with a fixed amount of commercial concentrate feed (CCF). The experiment lasted for a period of 80 days (April to June). Results revealed a significantly decreased total feed intake (wheat straw+supplements) in group-III ($1,666{\pm}52$ g/h/d) as compared to group I ($2,299{\pm}194$ g/h/d) and group-II ($2,193{\pm}230$ g/h/d). Average daily supplement intakes were $891{\pm}87$; $666{\pm}104$ and $593{\pm}0$ grams per head in group I, II and III, respectively. Supplement intakes among groups were different (p<0.05). Average daily body weight gains (g/h) were $214{\pm}25$, $174{\pm}23 $and $183{\pm}24$ for group I, II and III, respectively. Feed conversion ratio (FCR) was found to be $10.74{\pm}1.12$, $12.60{\pm}0.88$ and $9.90{\pm}1.33$ grams for group No. I, II and III, respectively. The economic net benefit of live weight gain of calves were 7.63, 6.11 and 7.33 rupees/h/d for group No. I, II and III, respectively. Thus SFM can replace CSM and urea molasses blocks can replace commercial concentrates as supplement to basal ration of wheat straw.
BACKGROUND: The purpose of this study was to investigate the effects of clothianidin on the soil in terms of clothianidin dissipation and degradation to evaluate its safety in order to provide an analytical foundation for clothianidin and the 5 metabolites related to it. METHODS AND RESULTS: High-performance liquid chromatography(HPLC) was used to separate clothianidin and its metabolites in this study. In soil, after suppressing dissociation-proned ions with weak alkalic $NH_4OH$ and extracting the metabolites with methanol, clothianidin, Methylaminoimidazole(MAI), Methylnitroguanidine(MNG), Thiazolylmethylurea(TZMU) and Thiazolylnitroguanidine(TZNG). Thiazolylmethylguanidine(TMG) were extracted with the addition of neutral $NH_4OAC$ to increasing the intensity of ions. Compounding elements were separated by using Hydrometrix ($ChemElut^{TM}$) and ion-exchanging Solid-phase extraction(SPE) Strong cation-exchanger(SCX) and C18 were used. The recovery rates of clothianidin and 5 metabolites in soil and water ranged from 87.4% to 104.3%. A standard deviation of our analysis for the soil and water samples were less than 5%. CONCLUSION: Well accepted detection limits for clothianidin and 5 metabolites in soil samples based on a dissipation analysis is 0.005 mg/kg and 0.001 mg/L in water samples. The dissipation concentration of this study was decided to be enough to evaluate the dissipation levels of clothianidin and its metabolites.
A study on the effect of diethylcarbamazine (DEC) (Supatonin) against Brugia malayi infection was conducted on Cheju Island in September 1965. A total of 182 persons living in a village of Aiwol Myun, Bukcheju-Gun was examined for microfilaraemia. Microscopic examination of smears of $20{\mu}l$ of blood revealed a microfilaria positivity rate of 28.5%. At the end of September 1965, 34 confirmed microfilaria positive cases were treated with DEC at a daily dosage of 5mg/kg body weight. A full course of 12 days of drug administration divided of two rounds for 6 days each was used. The first round of treatment was given under a strict supervision of the author in order to observe carefully side-effects of the drug. The second round of treatment was given in January 1966. The microfilaria density in $20{\mu}l$ of blood of those who received the drug was checked four times; before the treatment, during the first round of the treatment, 2 weeks and 4 months after the completion of the first round. The pre-treatment mean microfilaria density of 104.6 diminished to nearly zero (only two cases with one microfilaria respectively) 2 weeks after the first round and again slightly rose up to 0.5 four months after the first round. These results indicate that DEC (Supatonin) is highly effective to eliminate the microfilaria of B. malayi. However, severe side-effects, e.g. fever (average $38.6^{\circ}C$, maximum $39.7^{\circ}C$), headache, backache and seldom abdominal discomfort etc. were observed. There were two cases of withdrawal from the scheme due to refusal.
Physiological reactions of 24 six months old (22.7 kg. body weight) Barki ram lambs, to hot summer conditions, as influenced by asbestos shading at Maryout area were studied. Animals (12 shaded and 12 Unshaded) developed hyperthermia during summer as their rectal temperature (RT) and respiration rate (RR) were always higher (p<0.01) than normal. Asbestos shading caused higher (p<0.05) RT and RR ($39.5^{\circ}C$ and 69.9 r.p.m. vs. 39.2 and 45.7 r.p.m.) of rams at morning (6-8 a.m.) which became lower ($39.9^{\circ}C$ and 104.3 r.p.m. vs. $40.1^{\circ}C$ and 120.5 r.p.m.) in afternoon (2-4 p.m.) as compared to sun exposure. Shading also resulted in higher hematocrit value (PCV) (35.3% vs. 33.0%) and lower (p<0.05) daily weight gain (128.57 vs. 131.43 g). Diurnal (p<0.01) and monthly (p<0.05) RT and RR changes were closely associated with air temperature (AT) fluctuations. Monthly variation (p<0.05) in PCV was evident. Puberty was reached one month later in the shaded as compared to the unshaded group (265 vs. 232.3 day, respectively). It is concluded that asbestos shading prevents efficient heat dissipation to the sky by hyperthermic rams during summer nights. Construction materials for animal shelters are of extreme practical importance.
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