This study was carried out to compare the bioavailability of $Ceclex^{(R)}$ (test drug, cefaclor 250 mg/capsule) with that of $Ceclor^{(R)}$ (reference drug) and to estimate the pharmacokinetic parameters of cefaclor in healthy Korean adult. The bioavailability was examined on 20 healthy volunteers who received a single dose (250 mg) of each drug in the fasting state in a randomized balanced 2-way crossover design. After dosing, blood samples were collected for a period of 6hours. Plasma concentrations of cefaclor were determined using HPLC with UV detection. The pharmacokinetic parameters $(AUC_{0-6hr},\;C_{max},\;T_{max},\;AUC_{int},\;K_e,\;t_{1/2},\;Vd)$ F, and CL/F) were calculated with non-compartmental pharmacokinetic analysis. The ANOVA test was utilized for the statistical analysis of the $T_{max},\;log-transformed\;AUC_{0-6hr}\;log-transformed\;C_{max},\;t_{l/2},\;V_d/F$, and CL/F. The ratios of geometric means of AUC0-6hr and $C_{max}$ between test drug and reference drug were $103.2\%\;(6.74\;{\mu}g{\cdot}hr/ml\;vs\;6.53{\pm}g{\cdot}hr/ml)\;and\;100.4\%\;(4.85\;{\mu}g\ml\;vs\;4.82\;{\mu}g/ml)$, respectively. The $T_{max}$ of test drug and reference drug were $0.9\pm0.38\;hr\;and\;0.83\pm0.34$ hrs, respectively. The $90\%$ confidence intervals of mean difference of logarithmic transformed $AUC_{0-6h},\;and\;C_{max}$ were log $0.98{\sim}log$ 1.08 and log $0.88{\sim}log1.15$, respectively. It shows that the bioavailability of test drug is equivalent with that of reference drug. The estimated half-life of this study was longer $(1.21\pm0.27\;hrs\;vs\;0.5-1\;hr)$, the Vd/F was larger $(68.89\pm25.72L$ vs 24.9L), and the CL/F was higher $(38.62\pm7.09\;L/hr$ vs 24.9 L/hr) than the previously reported values.
Using the $Methionine-2-C^{14}$, the metabolism of methionine to the experimental rats on rice diet was studied comparing with that to the rats on stock diet in this paper. The National Institute of Health strain of weaning albino rats were housed into the individual cages deviding into 2 groups, the rice diet (RD) group and the stock diet (SD) group, and fed on rice diet and stock diet respectively for 10 weeks. On the day of experiment, the rats were parenterally administered. the $methionine-2-C^{14}$ solution after fasting over night. And then the rats were sacrificed by ether anesthesia by time being of one, three, six, and twelve hours each and the organs, pituitary gland, pancreas, spleen, liver, and kidney, were taken out for the determinations of radioactivities. And also the excretion of radioactivities through urine were determined by time being. The radioactivities were determined by Autoscaler SC-51 using the planchets. The results of radioactivities of urine excretion were shown at table 3 and the results of radioactivities distibutions in the organs by time being after parenteral administration of $methionine-2-C^{14}$ were shown table 4 in the original paper. According to the results, the following are summarized; 1. The growth experiment result of rats on. rice diet and stock diet were same as shown by the previous workers indicating significant growth inhibition at the rice diet group. 2. Due to the result of radioactivity excretion through urine after administration of $methionine-2-C^{14}$, it might he considered that methionine in the rice diet seems to be limited. However, it seems to be not 주 mostly limited. 3. And due to the results of radioactivity distribution in the organs by time being, the radioactivity in the liver tissue showed appearently higher readings at this methionine study compared with the results at the lysine study shown by HAW and his co-worker. This might be interpreted, though it is not clear, that liver might require methionine as a deficient amino acid at the tissue because methionine is limited at the rice diet.
Kim In-Jae;Kim Min-Ja;Yun Tae;Park Sung-Gue;Lee Woo-Young;Hong Seong-Su;Hwang Bang-Yeon;Nam Sang-Young
Korean Journal of Plant Resources
/
v.18
no.3
/
pp.505-511
/
2005
This study was carried out to obtain the basic information for quality changes according to degree of exposed sunlight after harvest of aerial part in Saururus chinensis Baill. Top part harvested was exposed to sunlight from 0 to 3 hours with 1-hour interval, and was dried at $50^{\circ}C$ hot air. The values were higher at shorter time of sunlight exposure, while the opposite is the true to the a values. The b and c values were high at 2-hour exposure before drying. Those were higher at shorter time of sunlight exposure after drying, but showed opposite tendency in tang-jeon. The contents of rutin and quercitrin, and astringency were greater at shorter time of sunlight exposure. Preference of quality and tang-jeon showed similar tendency with those.
Fakhri, Sajad;Jafarian, Safoora;Majnooni, Mohammad Bagher;Farzaei, Mohammad Hosein;Mohammadi-Noori, Ehsan;Khan, Haroon
The Korean Journal of Pain
/
v.35
no.1
/
pp.33-42
/
2022
Background: Cupressus arizonica Greene is a coniferous tree with great importance in fragrance and pharmaceutical industries. Essential oils from C. arizonica (EC) have shown potential antioxidant, and anti-microbial activities. This study aimed at investigating the anti-nociceptive and anti-inflammatory effects/mechanisms of EC. Methods: The EC was evaluated for anti-nociceptive and anti-inflammatory activities on male Wistar rats using a formalin test and carrageenan-induced paw edema, respectively. Also, we pre-treated some of the animals with naloxone and flumazenil in the formalin test to find out the possible contributions of opioid and benzodiazepine receptors to EC anti-nociceptive effects. Finally, gas chromatography/mass spectrometry (GC/MS) analysis was used to identify the EC's constituents. Results: EC in intraperitoneal doses of 0.5 and 1 g/kg significantly decrease the nociceptive responses in both early and late phases of the formalin test. From a mechanistic point of view, flumazenil administration 20 minutes before the most effective dose of EC (1 g/kg) showed a meaningful reduction in the associated anti-nociceptive responses during the early and late phases of the formalin test. Naloxone also reduced the anti-nociceptive role of EC in the late phase. Furthermore, EC at the doses of 1, 0.5, and 0.25 g/kg significantly reduced paw edema from 0.5 hours after carrageenan injection to 4 hours. GC/MS analysis showed that isolated EC is a monoterpene-rich oil with the major presence of α-pinene (71.92%), myrcene (6.37%), δ-3-carene (4.68%), β-pinene (3.71%), and limonene (3.34%). Conclusions: EC showed potent anti-nociceptive and anti-inflammatory activities with the relative involvement of opioid and benzodiazepine receptors.
Jawarishe Jalinoos (JJ) is an orally used formulation available in semisolid dosage form, prepared with powdered plant materials mixed in honey or sugar syrup. It has many admirable pharmacological effects and used in Unani medicine to treat various acute and chronic disorders since ancient times. The ICH Harmonised Tripartite Guideline stated that photostability testing should be an essential part of stability testing to confirm that light exposure does not result in an unacceptable change in drugs substance and finished products. To date, the effect of light on JJ is not studied, in this study photostability evaluation of JJ was carried out. The test sample was manufactured with genuine ingredients in the in-door pharmacy of the National Institute of Unani Medicine. JJ was packed in two transparent polyethylene terephthalate airtight containers. The first sample was analysed at zero-day and the second sample was placed in a stability chamber subjected to light challenge with an overall illumination of 1.2 million lux hours combined with near ultraviolet energy of 200-watt hours per square meter by using option 2, along with 30±2℃ temperature and relative humidity 70±5%. Analysis of both finished products showed no considerable changes in organoleptic characters. Less than 5% variation was observed in physicochemical parameters. HPTLC fingerprinting showed justifiable variation. Microbial load and specific counts were within the limit prescribed by WHO. As no unacceptable changes were noted in JJ subjecting to light challenge, it is concluded that JJ is a photostable Unani compound formulation.
Dam Hee Kang;Ok Hwa Kang;Hee-Sung Chae;Dong Yeul Kwon
Korean Journal of Pharmacognosy
/
v.54
no.2
/
pp.72-79
/
2023
MRSA is Staphylococcus aureus resistant to β-lactam antibiotics, and is a worldwide infectious disease. Even with the discovery of new antibiotics, resistance develops rapidly, so new alternatives are needed. Jakyakgamcho-tang (JGT) is a combination of Jakyak and Gamcho, and has been mainly used as an antispasmodic and analgesic in oriental medicine. This study was conducted to find out whether there is an effect on MRSA in relation to the anti-inflammatory effect of JGT and the antibacterial effect of Jakyak and Gamcho found in previous studies. In this study, in order to investigate the antibacterial activity of JGT and the combined effect of existing antibiotics, after extracting JGT with 70% EtoH, the disc diffusion method, minimum inhibitory concentration (MIC), drug combination effect (FICI), and time-kill analysis (Time-kill assay), metabolic inhibition, Western blot and qRT-PCR analysis were used to confirm the antibacterial activity mechanism of MRSA of JGT. As a result of the experiment, all of MRSA showed antibacterial activity in JGT's disc diffusion method, and the MIC was 250-1000 ㎍/mL. When existing antibiotics and JGT were combined with drugs, most had synergy or partial synergy. In addition, it was confirmed that the degree of bacterial growth was suppressed over time when simultaneous administration for 24 hours. JGT showed a synergistic effect when administered together with the ATPase-inhibitor DCCD, suggesting that it affected the inhibition of ATPase. As a result of observing the expression of PBP2a, and hla protein in the JGT-treated group and the untreated control group through wstern blot, it was confirmed that the protein expression of the JGT-treated group was significantly suppressed, and the expression levels of mecA, mecR1 and hla genes were also suppressed during JGT treatment. was observed by qRT-PCR. Combining the results of the experiment, it can be seen that JGT has antibacterial activity in MRSA, and when combined with existing antibiotics, the effect was increased compared to treatment with the drug alone. This suggests that JGT can be an alternative to treatment for antibiotic resistance of MRSA.
Journal of the Korean Applied Science and Technology
/
v.26
no.2
/
pp.103-109
/
2009
Chemicals for cosmetics, including skin, the skin absorbs some of the research in the field of science or pharmacy recently, about the environment and the health of the heightened interest in skin absorption. Many other human attributes and absorption evaluation studies are underway in various areas. This study were used rats and carried out to find out the effects of commercial permanent wave products to skin which are composed with thioglycolic acid and bases. Results were as follows. Permanent wave penetrated to 3 hours later with steady state in skins and was not significant changeable after 20hr later. In case of neutralizer with thioglycolic acid lag time and permeability coefficient in healthy skin were 3.32hr and $0.101{\mu}g/cm^2/hr$, in old skin were 3.08hr and $0.117{\mu}g/cm^2/hr$, and in wounded skin were 3.02hr and $0.166{\mu}g/cm^2/hr$. In conclusion, lag time and permeability coefficient in old skin and wounded skin were faster than healthy skin. In vivo, We were studied to general time and method of permanent wave. We found out that fine wrinkle and rash of skin were changeable in the case of treating with permanent wave drugs than normal skin.
This study was aimed to design and formulate the moisture-activated patches containing ofloxacin and lidocaine for antibacterial and local anesthetic action. The solubility of lidocaine at $32^{\circ}C$ in various vehicles decreased in the rank order of PG $759.5{\pm}44.5\;mg/mL$ > PGL > IPM > PEG 300 > PEG 400 > Ethanol > PGMC > DGME > PGML > OA > $Captex^{\circledR}\;300$ > $Captex^{\circledR}\;200$ > water $(4.0{\pm}0.1\;mg/mL)$. Ofloxacin revealed very low solubility, which the highest solubility was obtained from PEG 400 $(18.7{\pm}6.3\;mg/mL)$ among the vehicles used. The addition of lactic acid increased the solubility of ofloxacin dramatically; the solubility at 5% lactic acid was $133.7{\pm}9.7\;mg/mL$. As $2-hydroxypropyl-{\beta}-cyclodextrin$ was added at the concentrations of 40, 80, 120, 160 and 200 mM, the solubilities of lidocaine and ofloxacin were enhanced up to three and two times, respectively, with concentration-dependent pattern. Gel intermediates for filmtype patches were prepared with mucoadhesive polymer, viscosity builders, lidocaine or ofloxacin at pH values from 5 to 7. Gels were cast onto a release liner and dried at room temperature. Dried patch was attached onto an adhesive backing layer, thus forming a patch system. Patches containing a single drug component were characterized by in vitro measurement of drug release rates through a cellulose barrier membrane. The release study was carried out at $37^{\circ}C$ using a Franz-type cell. Receptor solutions were isotonic phosphate buffers (pH 7.4). Samples $(100\;{\mu}L)$ were taken over 24 hours and quantitated by a verified HPLC method. The releases from all tested were proportional to the square root of time. The release rates were 0.9, 157.3 and $281.7\;{\mu}g/cm^{2}/min^{1/2}$ for the lidocaine patches and 19.8,37.2 and $50.7\;{\mu}g/cm^{2}/min^{1/2}$ for the ofloxacin patches at the concentrations of 0.3, 0.5 and 1 %, respectively. The release rates were dose dependent in both drug patches $(R^{2}\;=\;0.9077\;for\;lidocaine;\;R^{2}\;=\;0.9949\;for\;ofloxacin)$ and those were also thickness-dependent $(R^{2}\;=\;0.9246\;for\;lidocaine;\;R^{2}\;=\;0.9512\;for\;ofloxacin)$.
This study was conducted in an attempt to grasp the health problems and environmental situation of the farmers and their vinyl houses. The study was done between Aug. 10, 1995 and Sep. 10, 1995, for one month period. with two hundred and nine vinyl house cultivation farmers chosen at random as subjects in five areas in and around Kim Chun City. The following are the results of the study carried out through direct interviews and surveys with the subjects : 1. The career of farming on vinyl house facilities by sex(male vs female) averages 17.29 and 15.08 years is shorter than that of general farmer's average of 31.24 and 25.58 years(P<0.05). Hours of labor between the two are silimar : monthly labor hours for vinyl house farmers are average 28 and 27.52 days. longer than the general farmers' average of 26.57 and 25.95 hours respectively. 2. The comp aints of physical symptoms among the vinyl house farmers range from lumbago, shoulder pain dullness in the limbs and dizziness, which show no remarkable differences from those of general farmers. 3. The frequency of application of chemicals on vinyl house forming for a period of one year averages 23.79, three times as often as the general farmer's average or 8.36(P<0.05). In the addiction rate of chemicals, too, the vinyl house farmer stowed a higher percentage of $9.09\%$ over the general farmer's $1.24\%$(P<0.01). 4. In temperature, humidity and disconfort indices of in and outside of the vinyl house, room temperature is on an average $34.6{\pm}5.05^{\circ}C,\;11.7^{\circ}C$ higher than that of outside, while in humidity inside was lower than outside by $10.6\%$ point, $65.9\%$ over $76.5\%$. The discomfort index was higher inside by $83{\pm}4.61\;vs\;70.64{\pm}5.61$. 5. The status of physical treatment over the past one year shows : for vinyl house farmers-physiotheraphy$(43.06\%)$, pharmacy$(24.04\%)$, clinic(18.66%), herbal medicine(574%) : for general farmers-pharmacy$(34.16\%)$, Physiotherapy$(27.33\%)$, Clinic$(18.63\%)$, Folk Medicine$(11.18\%)$ (P<0.01).
To find biologically active components of the higher fungi of Korea, the carpophores of Auricularia polytricha, a well-known edible mushroom, were extracted with 0.14 M NaCl solution. The extract was successively fractionated by adding ammonium sulfate at various concentrations, and the respective precipitates were separated by centrifugation, then dialyzed and freeze-dried. When a does of 60 mg/kg of each was injected i.p. into ICR mice, the fraction which precipitated at 20% ammonium sulfate showed the highest toxicity, killing seven out of seven mice within two days. The fraction obtained at 40% ammonium sulfate showed the second highest toxicity. The two fractions were named auritoxin I and II after the genus name. However, they Nere shown to have nearly identical composition by physicochemical and 6.8% protein. The polysaccharide moiety was found to have 12.3% $\alpha$-linkage and 87.7% $\beta$-linkage and to be a heteromannoglucan consisting of 45.1% glucose, 435 mannose and 11.0% xylose. The protein moiety contained ten amino adids. The molecular weight of the toxin was $1.5\times10^6$ dalton by Sepharose CL-4B gel filtration. The modian lethal doses of auritoxin in mice were 56.4, 157.2 and 454.6 mg/kg by i.p., s.c. and p.o.administrations, respectively. The signs of intrxication were convulsion during the first 30 minutes after the injection, coma or sleeping within an hour, termor, lacrimation, nasal bleeding congestion, and death in 24 hours. Smong the various organs, the spleen was found to be enlarged remarkably. Human platelet aggregation was inhibited by the addition of auritoxin. The activity of malic dehydrogenase in vitro was inhibited by the toxin.
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