• Journal of Oral Medicine and Pain
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• v.39 no.3
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• pp.96-99
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• 2014

Purpose: The objective of this retrospective pilot study was to evaluate the effectiveness of Gabapentin in patients with primary burning mouth syndrome (BMS). Methods: Ten subjects were diagnosed with primary BMS (8 women and 2 men). The mean age was 60.1 years. They had clinical examination to exclude local factors such as the presence of Candida species, xerostomia, lichen planus, etc. They also underwent hematological examination to exclude secondary BMS due to systemic disorders. Pain was assessed by patients on an 11-point numerical rating score system (0 to 10). Gabapentin was administered at a starting dose of 300 mg/day, slowly titrated up to maximum of 1,800 mg/day. All patients were treated for 4 weeks. Results: One half of the patients (n=5) obtained reduction in pain over the treatment period. Four patients reported no reduction in pain symptoms. One patient reported that symptoms were worsening. The average pain score before the treatment was 6.3 and after the treatment was 5.25. No significant relationship was detected between pretreatment and posttreatment pain score. Only one patient noted mild side effect (dizziness). Conclusions: This retrospective pilot study provides no preliminary evidence that Gabapentin has effect in the management of BMS. However, further research (well-designed, randomized, and controlled trial with large sample) would be needed to investigate the efficacy of Gabapentin in treatment of BMS.

• Journal of Nutrition and Health
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• v.25 no.5
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• pp.351-359
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• 1992

This study was conducted to compare the effects of perilla oil or corn oil on lipid peroxidation and eicosanoid productions which are associated with the promotion of carcinogenesis. in liver or blood in rats. Male Sprague-Dawley8 weaning rats were fed on semisynthetic diets containing 15%(w/w) beef fat(BF). corn oil(CO) or perilla oil(PO) Three weeks after the half of rats in each diet group were injected with a single dose of 50mg 2-acetylaminofluorene (AAF)/Kg BW hepatocarcinogen intraperitoneally 3 times at 2-day interval and all of the rats were sacrificed after 8 weeks from the first injection. The rats fed on different dietary fats without 2-AAF treatment had not different MDA produc-tion and conjugated diene content in liver microsome. CO+AAf group had significantly higher conjugated diene content than BF+AAF and PO+AAF groups. and lower glucose-6-phospha-tase activity than BF+AAF group But PO+AAF had similar conjugated diene content to BF+AAF group and significantly lower MDA production than BF+AAF and CO+AAF groups. The hepatic mocrosomal lipid peroxidation was slightly greater in CO group than in PO group though perilla oil(P/S=9.67) has much more polyunsaturated fatty acids than corn oil(P/S=2.92) PG E2 level in liver and TX B2 level in plasma were significantly higher in CO group than in BF and PO groups. TX B2 level was lowered in CO and BF groups by 2-AAF treatment. These results reach to the contclousion than the type of dietary fatty acid as well as the P/S ratio has effect on hepatic microsomal lipid peroxidation and eicosanoid production and perilla oil or linolenic acid(n3) might be less effective on lipid peroxidation or PG E2 and TX B2 mediated tumor promotion than corn oil or linoleic acid(n6).

• Journal of Pharmaceutical Investigation
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• v.38 no.1
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• pp.73-78
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• 2008

To evaluate the bioequivalence of two ramipril formulations, a standard 2-way randomized cross-over study was conducted in twenty-six healthy male Korean volunteers. A single oral dose of 10 mg of test formulation $Ramiprin^{(R)}$ (tablet) or reference formulation Tritace $Protect^{(R)}$ (tablet) was administered with one-week washout period. Plasma concentrations of ramipril were assayed over a period of 12 hr with a well validated method using liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS). The values of area under the plasma concentration-time curve, from time zero to last sampling time $(AUC_t)$ and from time zero to time infinity $(AUC_{inf})$ were $77.45{\pm}44.78\;and\;78.96{\pm}45.64$ for test, and $70.30{\pm}42.27\;and\;71.99{\pm}43.55ng\;hr/mL$ for reference formulation, respectively. Similarly, maximum concentration $(C_{max})$ and elimination half-life $(t_{1/2})$ were $65.61{\pm}19.96ng/mL$ and $2.15{\pm}0.75hr$ for test, and $63.63{\pm}25.50ng/mL$ and $2.16{\pm}0.73hr$ for reference formulations, respectively. Time to reach maximum concentration $(T_{max})$ for the test and the reference, were $0.51{\pm}0.22hr\;and\;0.52{\pm}0.18hr$, respectively. The parametric 90% confidence intervals on the mean of the differences between the two formulations (test-reference) of the log-transformed values of $AUC_t\;and\;C_{max}$ were 1.03 to 1.19 and 0.98 to 1.17, respectively. The overall results indicate that the two formulations are bioequivalent and can be prescribed interchangeably.

• Biomolecules & Therapeutics
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• v.10 no.1
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• pp.37-42
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• 2002

Brain drug targeting through the blood-brain barrier (BBB) in vivo is possible with peptidornirnetic monoclonal antibodies that undergo receptor-mediated transcytosis through the BBB. Monoclonal antibody to the rat transferrin receptor, such as the OX26 was studied in rats as a transport vector through BBB on the transferrin receptor. But, OX26 is not an effective brain delivery vector in mouse. In the present studies, rat monoclonal antibody, 8D3 to the mouse transferrin receptor were evaluated for brain drug targeting vector intransgenic mouse model. Pharrnacokinetic parameters in plasma and organ uptakes were determined at varioustimes after i.v. bolus injection of [$^{}125}I$] 8D3 in Balb/c mice. Brain uptake of [$^{}125}I$] 8D3 was also studied with an internal carotid artery perfusioncapillary depletion method. After i.v. injection of [$^{}125}I$] 8D3, plasma concentrations declined biexponentially with elimination half lift of approximately 2.2 hours. Brain uptake of [$^{}125}I$] 8D3 was $0.50{\pm}0.09$ persent of injected dose per g brain after 2 hours i.v. injection. After perfusion 5 min the apparent volume of distibution of [$^{}125}I$] 8D3 in brain was $22.3 {\mu}l/g,$ which was 4.8 fold higher than the intravascular volume. These studies indicate rat monoclonal antibody to the mouse transferrin receptor, 8D3 may be used for brain drug targeting vector in mice.

• The Korean Journal of Nuclear Medicine
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• v.26 no.2
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• pp.355-359
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• 1992

The $^{67}Ga$ has somewhat long physical and biological half livies with 78 hours and 600 hours respectively, so we can get $^{67}Ga-scan$ images for 3 or more days after once injection of $^{67}Ga$. Furthermore $^{67}Ga$ scan would be useful to search some residual tumors after surgical removal of the tumors trapped with $^{67}Ga$. However $^{67}Ga$ bound with plasma proteins would be delayed in plasma clearance as approximately 10% of the dose remains in the plasma at 24 hours. If the remained $^{67}Ga$ in the plasma is redistributed into the surgical wound, we wouldn't evaluate the degree of the tumor remained after surgery. So the authors examined the amounts of the remained blood $^{67}Ga$ and the redistribution of the blood $^{67}Ga$ into the artificial wound with S or more centimeters in the diameter at the neck and chest of the rabbits. The results were as follows; 1) The $^{67}Ga$ remained in the plasma were 12%, 5.7%, 4.2% at 24, 48 and 72 hours after $^{67}Ga$ injection respectively. 2) The blood $^{67}Ga$ were redistributed into the artificial wound with 5.9% at 48 hours and 6.9% at 72 hours after $^{67}Ga$ injection.

• Journal of Veterinary Clinics
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• v.4 no.2
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• pp.473-481
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• 1987

This experiment was performed in order to establish a proper method to determine the half life of indocyanine green(ICG T$\frac{1}{2}$) and its fractional clearance rate(KICG) and investigate the applicability of indocyanine green ( ICG ) excretion test in hepatotoxicity experiment in Korean black goats. The results were as follows : 1. Maximum absorbance of ICG in plasma was at 810 nm in this experiment. 2. The coefficient of correlation between the results obtained by standard method and potassium cyanide method was 0.99 and the regression equation between two methods was y=0.9996 x＋0.0065. 3. As the disappearance curve of ICG plotted in semi-log graph revealed linear pattern at least for 6 minutes after injection, the postinjection blood samples were decided to collect at 2 and 6 minutes after ICG injection. 4. ICG T$\frac{1}{2}$ and KICG values were not affected by dose level of ICG. 5. When 0.25 mg of ICG per kg body weight was administered the normal data of ICG T$\frac{1}{2}$ and KICG in Korean black goa were 1.468${\pm}$0.197 minutes(mean${\pm}$SD) and 0.482${\pm}$0.076/minutes respectively. 6. After administration of carbon tetracholride. the ICG T$\frac{1}{2}$ started to increase acutely from day 1, revealed the peak at day 3, and then returned almostly but not completely to preinjection level at day 14. The ICG T$\frac{1}{2}$ value was suggested to be a sensitive indicator of hepatic injury in Korean black goats.

• Biomolecules & Therapeutics
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• v.23 no.5
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• pp.449-457
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• 2015

The present study was aimed to investigate the effects of MB12662, a synthetic dunnione compound, on cisplatin-induced vomiting reflexes and intestinal, renal, immune system, and hematopoietic toxicities in ferrets and mice, respectively. Male ICR mice were orally administered MB12662 (5, 10, 25 or 50 mg/kg) for 10 days, during which intraperitoneally challenged with cisplatin (3.5 mg/kg) from day 4 to 7, and sacrificed on day 10 for the pathological examination. Male ferrets were orally administered MB12662 (25, 50 or 100 mg/kg) for 7 days, subcutaneously challenged with cisplatin (5 mg/kg), and monitored for vomiting reflexes and survival of the animals. Four-day injection of cisplatin (3.5 mg/kg) to mice caused body weight loss and degeneration and atrophy of intestinal villi, reducing villi/crypt ratio to a half level of control animals. Cisplatin also induced renal and hepatic toxicities, and depletion of splenocytes and bone marrow progenitor cells. The systemic toxicities including decreased villi/crypt ratio, immune system atrophy, splenocyte depletion, and decreased cellularity in bone marrow were improved by MB12662. Cisplatin (5 mg/kg) induced retching and emetic responses of ferrets, which were remarkably attenuated by MB12662 in a dose-dependent manner. All the ferrets pretreated with MB12662 survived the challenge of cisplatin, in comparison with 40% mortality in vehicle-treated animals, and blood parameters of nephrotoxicity and hepatotoxicity were markedly recovered. It is expected that MB12662 could be a candidate for the body protection against burden, including emesis, of chemotherapeutic agents.

• Biomolecules & Therapeutics
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• v.15 no.3
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• pp.187-191
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• 2007

This study was conducted to compare the bioavailability of two brands of atenolol (50 mg) tablets, which are a generic product of $Ditent^{\circledR}$ (Daewon Pharmaceutical Co., Ltd., Korea) and an innovator product $Tenormin^{\circledR}$ (Hyundai Pharm. Ind. Co., Ltd., Korea), in 20 healthy Korean male volunteers. The volunteers received a single 50 mg dose of each atenolol formulation according to a randomized, two-way cross-over design. The washout period between treatments was 1 week. Plasma samples were obtained over a 24-hour interval, and atenolol concentrations were determined by HPLC with a fluorescence detector. From the plasma atenolol concentration vs. time curves, the following parameters were compared: area under the plasma concentration-time curve ($AUC_{0-24}$), peak plasma concentration ($C_{max}$), time to reach peak plasma concentration ($T_{max}$), and terminal first order elimination half-life ($t_{1/2}$). No statistically significant difference was obtained between the $T_{max}$ values, and the logarithmic transformed $AUC_{0-24}$ and $C_{max}$ values of the two products. The 90% confidence interval for the ratio of the logarithmically transformed AUC and $C_{max}$ values of $Ditent^{\circledR}$ over those of $Tenormin^{\circledR}$ were calculated to be between 0.85 and 1.04, and 0.89 and 1.07, respectively; both were within the bioequivalence limit of 0.80-1.25. The mean of $T_{max}$ in $Tenormin^{\circledR}$ group was 3.1 hour, and that in Ditent$^{\circledR}$ group was 3.2 hour. The values of $t_{1/2}$ between the two products were found comparable, and the mean values were 5.2 hour in the both products. Based on these results, it was concluded that $Ditent^{\circledR}$ was comparable to $Tenormin^{\circledR}$ in both the rate and extent of absorption, indicating that $Ditent^{\circledR}$ was bioequivalent to the reference product, $Tenormin^{\circledR}$.

• Mass Spectrometry Letters
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• v.7 no.3
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• pp.69-73
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• 2016

High-resolution quadrupole-Orbitrap mass spectrometry (HRMS), with high-resolution (> 10,000 at full-width at half-maximum) and accurate mass (< 5 ppm deviation) capabilities, plays an important role in the structural elucidation of drug metabolites in the pharmaceutical industry. ML106, a derivative of imidazobenzimidazole, decreased melanin content and tyrosinase activity in a dose-dependent manner. Here, we investigated the phase 1 metabolic pathway of ML106 using HRMS in human liver microsomes (HLMs) and recombinant cDNA-expressed cytochrome P450 (CYP). After the incubation of ML106 with pooled HLMs and recombinant cDNA-expressed CYP in the presence of NADPH, five phase 1 metabolites, including three mono-hydroxylated metabolites (M1-3) and two di-hydroxylated metabolites (M4 and M5), were investigated. The metabolite structures were postulated by the elucidation of protonated mass spectra using HRMS. The CYP isoforms related to the hydroxylation of ML106 were studied after incubation with recombinant cDNA-expressed CYP. Here, we identified the phase 1 metabolic pathway of ML106 induced by CYP in HLMs.

• Journal of Korean society of Dental Hygiene
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• v.14 no.4
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• pp.601-608
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• 2014

Objectives : The purpose of the study is to examine the apoptotic effects of Pseudomonas aeruginosa exotoxin A(PEA) in squamous cell carcinoma(SCC) 25 cells. Methods : Cell growth reduction and apoptosis induced by PEA were confirmed by WST-1 assay, Hoechst 33258 staining, flow cytometry analysis, and Western blot assay. Results : The PEA treatment decreased the cell viability in a dose and time dependent manner: control; $100{\pm}0^e$(p<0.01), 0.1875 nM; $87{\pm}4.36^d$(p<0.01), 0.375 nM; $82{\pm}0.58^d$(p<0.01), 0.75 nM; $72{\pm}1.67^c$(p<0.01), 1.5 nM; $51{\pm}1.53^{bc}$(p<0.01), 7.5 nM; $31{\pm}1.20^{ab}$(p<0.01), 15 nM; $26{\pm}0.67^a$(p<0.01), control; $100{\pm}0^a$(p<0.05), 24 h; $51{\pm}1.53^b$(p<0.05), 48 h; $16{\pm}0.5^c$(p<0.05), 72 h; $12{\pm}1.67^d$%(p<0.05). The PEA was observed on SCC 25 cells with the half maximal inhibitory concentration(IC50) value of 1.5 nM at 24 hours. The PEA treated SCC 25 cells demonstrated several types of apoptotic indications, such as nuclear condensation, the increase of sub G1, and the cleavage of PARP-1 and DFF 45. Conclusions : PEA showed anti-cancer activity against SCC 25 cells via apoptosis. PEA may potentially contribute to human oral cancer treatment.