• Journal of Pharmaceutical Investigation
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• 제37권6호
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• pp.349-354
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• 2007

For decades, the various virtues of ${\alpha}-lipoic$ acid (ALA), a natural material synthesized in most cells, have been intensively studied and proved. Recently it was reported that ALA caused significant bodyweight reduction via appetite suppression. Unfortunately, the efficacy requires an administration over 50 mg/kg. The low bioavailability and the short plasma half life of ALA lead us to explore novel pharmaceutical dosage forms using nanoparticles. In this study, the effect of polymeric stabilizers on the bioavailability improvement of ALA nanoparticles was investigated. The reduction of particle size via nano-comminution technology was successful resulting in volume average particle sizes of 320 - 340 nm. The in vitro release rate of ALA did not reflect the decrease of particle size, possibly because of the self polymerization of ALA during nano-comminution. The type of polymeric stabilizers could not affect the release rate either. However, the in vivo food intake results of ALA showed that nano-suspensions were more effective than microparticles or a salt form. The nano-suspension containing polyvinyl pyrrolidone as the primary stabilizer and polyacrylic acid as the secondary stabilizer showed more improved efficacy for 2 hours.

• 한국수산과학회지
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• 제56권3호
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• pp.309-314
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• 2023

Shark populations are constantly decreasing owing to environmental destruction and overfishing; thus, sharks are now at risk of extinction, with 30.5% of species classified as endangered on the International Union for Conservation of Nature's Red List. Sharks are apex predators and keystone species in balancing the marine food chain; their extinction would create an imbalance in the entire marine ecosystem. Assisted reproductive technology is a last resort for protecting animals facing extinction. Here, as a proactive effort toward building a hormone-induced artificial insemination protocol for endangered wild sharks, we identified the possibility of germ cell maturation by administration of GnRH, a commercially produced synthetic salmon gonadotropin-releasing hormone, and calculated its optimum dosage and injection timing. The experiment was conducted on one shark species, Chiloscyllium plagiosum. Injections were administered in 24 h intervals to C. plagiosum females, and 0.2 mL/kg+0.2 mL/kg were the optimal doses. These doses effectively induced maturation and, and ovulation, and oocyte release. Our results confirm that GnRH is a suitable tool for shark hormone-induced artificial insemination and indicate that this method may facilitate the conservation of endangered shark species.

• Journal of Pharmaceutical Investigation
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• 제25권2호
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• pp.109-116
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• 1995

For the administration of narcotic antagonist with short half-life and low patient compliance, the sustained release system using biodegradable matrix is effective. Polyphosphazenes are of considerable interest as biodegradable matrix systems for controlled release of drugs. In this study, biodegradable polyphosphazenes available for the sustained release implantable device were synthesized, and their application was examined. Poly[dichlorophosphazene] was synthesized by solution polymerization method and confirmed with IR spectrum. Poly[bis(ethyl glycinate) phosphazene] and poly[ (diethyl glutamate)-co-(ethyl glycinate)phosphazene] were then produced by substitution of amino acid alkyl esters for chloride side groups. Using these polymers, the implantable devices of 1 mm thickness and $10{\times}10\;mm$ size containing naloxone hydrochloride were prepared and their release and degradation profiles were measured. In the case of poly[bis(ethyl glycinate)phosphazene] with swelling characteristics, degradation rate was slower than the release rate, showing that the release rate is partly dependent on the swelling rate. In contrast, the degradation rate of polyl[(diethyl glutamate)-co-(ethyl glycinate)phosphazene] matrix was identical with release rate of naloxone hydrochloride. On the basis of these results, it is expected that these polymers can be applied to sustained release implantable systems delivering narcotic antagonist.

• Journal of Dental Anesthesia and Pain Medicine
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• 제15권4호
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• pp.213-220
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• 2015

Background: Pediatric dentists face challenges when young patients require a mesiodens extraction. General anesthesia may be a burden to the child as well as the parent due to dental fears and costs. The aim of this study was to evaluate oral and intravenous sedation in the outpatient setting as a safe and effective means of managing patients who require a mesiodens extraction. Methods: Records were reviewed retrospectively to find patients who underwent a mesiodens removal procedure from January 2013 to September 2014 in the Department of Pediatric Dentistry at Ajou University Hospital (Suwon, Gyeonggi-do, Republic of Korea). A total of 81 patients (62 male and 19 female) between 4 and 11 years of age (mean [${\pm}SD$] $81.6{\pm}14.1$ months) were studied, with a mean weight of $22.9{\pm}3.3kg$ (16 kg to 30 kg). Vital signs, sedation drug dosage, and sedation time were studied. Results: Mean doses of $63.7{\pm}2.5mg/kg$ chloral hydrate and $1.36{\pm}0.22mg/kg$ hydroxyzine were used for oral sedation. Nitrous oxide/oxygen was administrated for $40.0{\pm}2.1$ min. The mean dose of midazolam administered intravenously was $0.14{\pm}0.06mg/kg$ ($2.38{\pm}0.97$ times). In all cases, the mesiodens was removed successfully. Conclusions: Intravenous sedation combined with oral sedation and nitrous oxide/oxygen inhalation can be an alternative to general anesthesia when administrated and monitored properly.

• 대한임상독성학회지
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• 제7권2호
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• pp.97-104
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• 2009

Purpose: Antivenin is a standard therapy in snakebite victims. While the required antivenin dose can be easily estimated, based on the initial symptoms, this strategy may be unsuccessful if the initial symptoms progressively worsen. The purpose of this study was to identify the progression rate of the initial symptoms following snakebite and its associated factors. Methods: The medical records of 44 patients treated for snakebite from give the actual dates of the study period were retrospectively examined. Thirty-two of these patients were enrolled. Demographic data, local wound grade and local effect score at initial presentation (G-0 and LES-0, respectively) and 12 hours after admission (G-12 and LES-12, respectively) were reviewed, along with laboratory data. Results: The 32 patients had an average age of $54.0{\pm}14.5$ years and were predominantly male (n=26) and presented mainly during summer. Compared to G-0 and LES-0, re-evaluated G-12 and LES-12 were significantly increased despite initial administration of proper antivenin dosage (p=0.001 and p=0.000, respectively). Total amounts of antivenin correlated with LES-12 (correlation co-efficiency 0.558, p<0.05). However, factors associated with symptom progression were not revealed. Conclusion: Initial snakebite symptoms might progressively worsen within hours despite acceptable initial antivenin therapy. Therefore, re-evaluation within several hours must be considered if when the initial snakebite symptoms are minimal or mild.

• 한국임상약학회지
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• 제28권2호
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• pp.88-94
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• 2018

Background: We strived to evaluate the status of nivolumab use and associated factors on the clinical efficacy of the drug. Methods: The study was retrospectively conducted in patients who had been administered nivolumab at least once at the cancer center of Seoul National University Hospital from June 2015 to April 2017. Data were collected from electronic medical records. A medication-use evaluation was performed based on the American Society of Health-System Pharmacists mediation-use guidelines. Results: Sixty-six of the 74 patients (89.2%) showed indications approved for nivolumab use by the Korean Ministry of Food and Drug Safety (MFDS; n=55) or the US Food and Drug Administration (FDA; n=11). Approximately 73.0% of the patients were administered the approved dose of 3 mg/kg but 25.7% were administered an unapproved fixed dose of 100 mg. The overall response rate was 21.7%, and the response rate of non-small cell lung cancer patients, who accounted for the largest number of indications, was 18.8%. Adverse reactions were found in 90.1% of the patients and were mostly mild (86%). The expression of programmed death-ligand 1 (PD-L1) was analyzed as a factor affecting treatment response (p=0.028, odds ratio [OR]=11.331). Conclusion: PD-L1 expression was found to affect treatment response. However, caution is required while using an unapproved dosage and in the absence of monitoring for effectiveness and safety. Therefore, an effective protocol or instruction manual for the proper use of nivolumab should be considered.

• Mass Spectrometry Letters
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• 제11권4호
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• pp.71-76
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• 2020

While montelukast (ML), a cysteinyl-leukotriene type 1 receptor (CysLT1) antagonist is widely used to treat symptoms of rhinitis or asthma, its formulations are mainly limited to solid preparation due to its instability. Recently, there have been attempts to develop various ML dosage forms, and this situation increases the demand of sensitive and creditable methods to determine ML in various samples such as plasma. Thus, here, a simple and efficient method to determine ML in rat plasma using liquid-liquid extraction (LLE) and multiple reaction monitoring was presented. The mixture of DCM:EtOAc (25:75, v/v), the optimized extract solvent for LLE was found to be effective to extract ML without hydrophilic salts and proteins from the sample with limited volume. Also, the use of zafirlukast, instead of expensive ML-d6, as the internal standard makes the present method economical. The developed method was successfully validated in terms of selectivity, matrix effects (-14.8--6.9%), linearity (r230.998 within 0.5-500 ng/mL), sensitivity (the limit of detection and the lower limit of quantitation, ≤0.5 ng/mL), accuracy (88.4-100.6%), precision (3.0-13.3%), and recovery (80.8-86.3%) by following the FDA guidelines. Finally, the applicability of the validated method to pharmacokinetics (PK) studies was confirmed by the successful determination of PK parameters through it following oral administration of Singulair® granule in rats. Therefore, the present method can contribute to the development of new ML formulations through its performance to determine ML in rat plasma efficiently and sensitively.

• 대한치과의사협회지
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• 제56권1호
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• pp.42-48
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• 2018

INTRODUCTION The most commonly impacted tooth is the third molar. An impacted third molar can ultimately cause acute pain, infection, tumors, cysts, caries, periodontal disease, and loss of adjacent teeth. Local anesthesia is employed for removing the third molar. This study aimed to evaluate the efficacy and safety of 2% lidocaine with 1:80,000 or 1:200,000 epinephrine for surgical extraction of bilateral impacted mandibular third molars. METHODS Sixty-five healthy participants underwent surgical extraction of bilateral impacted mandibular third molars in two separate visits while under local anesthesia with 2% lidocaine with different epinephrine concentration (1:80,000 or 1:200,000) in a double-blind, randomized, crossover trial. Visual analogue scale pain scores obtained immediately after surgical extraction were primarily evaluated for the two groups receiving different epinephrine concentrations. Visual analogue scale pain scores obtained 2, 4, and 6 h after administering an anesthetic, onset and duration of analgesia, onset of pain, intraoperative bleeding, operator's and participant's overall satisfaction, drug dosage, and hemodynamic parameters were evaluated for the two groups. RESULTS There were no statistically significant differences between the two groups in any measurements except hemodynamic factors (P > .05). Changes in systolic blood pressure and heart rate following anesthetic administration were significantly greater in the group receiving 1:80,000 epinephrine than in that receiving 1:200,000 epinephrine ($P{\leq}01$). CONCLUSION The difference in epinephrine concentration between 1:80,000 and 1:200,000 in 2% lidocaine liquid does not affect the medical efficacy of the anesthetic. Furthermore, 2% lidocaine with 1:200,000 epinephrine has better safety with regard to hemodynamic parameters than 2% lidocaine with 1:80,000 epinephrine. Therefore, we suggest using 2% lidocaine with 1:200,000 epinephrine rather than 2% lidocaine with 1:80,000 epinephrine for surgical extraction of impacted mandibular third molars in hemodynamically unstable patients.

• 한국균학회지
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• 제43권3호
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• pp.174-179
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• 2015

버섯을 이용하여 새로운 혈당상승 억제 물질을 개발하여 건강 기능성 식품 소재 산업에 응용하고자 느타리버섯, 노랑느타리버섯, 분홍느타리버섯, 새송이버섯과 잣버섯들의 ${\alpha}$-glucosidase 저해활성을 측정한 결과 잣버섯 자실체의 에탄올 추출물이 가장 높은 ${\alpha}$-glucosidase 저해활성을 보였다. 잣버섯 자실체 분말을 95% 에탄올로 $30^{\circ}C$에서 48시간 추출하였을 때 ${\alpha}$-glucosidase 저해물질이 가장 많이 추출되었고 이 ${\alpha}$-glucosidase 저해물질을 함유한 잣버섯 에탄올 추출물은 일반 쥐와 streptozotocin으로 당뇨를 유발시킨 당뇨 쥐에서 모두 농도 의존적으로 식후 혈당상승 억제 효과를 보였다.

• The Korean Journal of Physiology and Pharmacology
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• 제2권6호
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• pp.661-670
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• 1998

Dopamine has been generally known to exert antinociceptive action in behavioral pain test, such as tail flick and hot plate test, but there appears to be a great variance in the reports on the antinociceptive effect of dopamine depending on the dosage and route of drug administration and type of animal preparation. In the present study, the effects of dopamine on the responses of wide dynamic range (WDR) cells to mechanical, thermal and graded electrical stimuli were investigated, and the dopamine-induced changes in WDR cell responses were compared between animals with an intact spinal cord and the spinal animals. Spinal application of dopamine (1.3 & 2.6 mM) produced a dose-dependent inhibiton of WDR cell responses to afferent inputs, the pinch-induced or the C-fiber evoked responses being more strongly depressed than the brush-induced or the A-fiber evoked responses. The dopamine-induced inhibition was more pronounced in the spinal cat than in the cat with intact spinal cord. The responses of WDR cell to thermal stimulation were also strongly inhibited. Dopamine $D_2$ receptor antagonist, sulpiride, but not $D_1$ receptor antagonist, significantly blocked the inhibitory action of dopamine on the C-fiber and thermal responses of dorsal horn cells. These findings suggest that dopamine strongly suppresses the responses of WDR cells to afferent signals mainly through spinal dopamine $D_2$ receptors and that spinal dopaminergic processes are under the tonic inhibitory action of the descending supraspinal pathways.