• Biomolecules & Therapeutics
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• 제22권3호
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• pp.260-266
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• 2014

This study evaluated the pharmacokinetic profile and therapeutic efficacy of piroxicam (PX), a long acting non-steroidal anti-inflammatory drug for the treatment of arthritis, following intra-articular (IA) injection in comparison to the pharmacokinetic profile and therapeutic efficacy of PX after intramuscular (IM) injection. In the pharmacokinetic study in rats, systemic exposure and pharmacokinetic parameters of PX after a single IA dose were compared with systemic exposure and pharmacokinetic parameters of PX after administration of the same dose IM (0.6 mg/kg). The anti-inflammatory and analgesic effects of IA PX were evaluated simultaneously in a monoiodoacetate-induced osteoarthritis rat model. The plasma PX concentration rapidly rose following IA injection, and it was comparable to the plasma PX concentration following IM injection, suggesting the rapid efflux of the drug molecule from the joint cavity. However, in the efficacy study, the IA PX administration significantly reduced the knee swelling by reducing the level of prostaglandin $E_2$ in the joint, compared to that following administration of IA vehicle and after administration of the IM PX dose. In addition, we found that the anti-inflammatory and anti-nociceptive efficacies of IA PX were synergistically increased upon co-treatment with hyaluronic acid (HA), a potent agent for the treatment of osteoarthritis, at the weight ratio of 1:1 or 1:2, and these effects were more pronounced than those following administration of HA or PX alone. In conclusion, this study demonstrated the efficacy of the IA use of PX alone and/or in combination with HA in osteoarthritis.

• Journal of Ginseng Research
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• 제40권1호
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• pp.55-61
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• 2016

Background: A number of neurological and neurodegenerative diseases share impaired cognition as a common symptom. Therefore, the development of clinically applicable therapies to enhance cognition has yielded significant interest. Previously, we have shown that activation of lysophosphatidic acid receptors (LPARs) via gintonin application potentiates synaptic transmission by the blockade of $K^+$ channels in the mature hippocampus. However, whether gintonin may exert any beneficial impact directly on cognition at the neural circuitry level and the behavioral level has not been investigated. Methods: In the current study, we took advantage of gintonin, a novel LPAR agonist, to investigate the effect of gintonin-mediated LPAR activation on cognitive performances. Hippocampus-dependent fear memory test, synaptic plasticity in the hippocampal brain slices, and quantitative analysis on synaptic plasticity-related proteins were used. Results: Daily oral administration of gintonin for 1 wk significantly improved fear memory retention in the contextual fear-conditioning test in mice.We also found that oral administration of gintonin for 1 wk increased the expression of learning and memory-related proteins such as phosphorylated cyclic adenosine monophosphate-response element binding (CREB) protein and brain-derived neurotrophic factor (BDNF). In addition, prolonged gintonin administration enhanced long-term potentiation in the hippocampus. Conclusion: Our observations suggest that the systemic gintonin administration could successfully improve contextual memory formation at the molecular and synaptic levels as well as the behavioral level. Therefore, oral administration of gintonin may serve as an effective noninvasive, nonsurgical method of enhancing cognitive functions.

• 대한수의학회지
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• 제61권1호
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• pp.1.1-1.5
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• 2021

A 5-year-old neutered female Dachshund dog presented with a 3-month history of hyperthermia, skin lesions, and shifting lameness. Based on physical examination, blood tests, urinalysis, and radiographs, the dog was diagnosed with systemic lupus erythematosus. Clinical signs improved after administration of prednisolone and cyclosporine but relapsed after the prednisolone was reduced due to side effects. Oral levamisole was commenced and the other immunosuppressants were tapered over a period of 2 months and then stopped. Levamisole was retained as the sole therapy for an additional 2 months. Six months after discontinuation of all treatment, the patient remained in remission.

• The Korean Journal of Physiology and Pharmacology
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• 제1권3호
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• pp.325-335
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• 1997

Evidence for the existance of at least two subclasses of renal adenosine receptors has been presented. N-6-cyclohexyladenosine (CHA) is a relatively selective $A_1$ adenosine agonists, whereas 5'-N-ethylcarboxamidoadenosine (NECA) acts as a preferential agonist of $A_2$ adenoisne receptor. N6-(L-2-phenylisoproryl)-adenosine (PIA) almost unselectively activates both $A_1\;and\;A_2$ adenosine receptors at micromolar concentrations. During the characterization of adenosine receptor in the kidney, we have discovered a novel phenomenon, that is, an intramuscular administration of CHA for 3 days caused a diuresis and a suppression of urinary concentrating ability. To further characterize this novel phenomenon, an intramuscular administration of adenosine and other adenosine angonists, PIA and NECA, and prior treatment of adenosine antagonists, caffeine, theophylline and 1,3-diethyl-8-phenyl-xanthine (DPX) were performed. Systemic administration of CHA, PIA, and NECA for 3 days caused a suppression in heart rate, blood pressure and general motor activity without change in rectal temperature. Systemic administration of CHA, 0.5, 1 and 2 mg/kg/day, for 3 days caused a dose-dependent increase in urine volume and decrease in urinary osmolarity and free water reabsorption. This phenomenon was reversible and repeatable. Administration of adenosine (40 mg/kg/day) produced no apparent effect on the renal function, whereas PIA (2 mg/kg/day) produced an similar effect to CHA on the renal function. Systemic adminstration of NECA, 0.025, 0.05 and 0.25 mg/kg/day, for 3 days caused a dose-dependent increase in urine volume and dose-dependent increases in excreted amount of creatinine, urinary osmolarity and free water reabsorption. These renal effects of adenosine agonist were maximum at second day during the drug administration. In terms of increase in urine volume and the suppression of urinary concentrating ability, NECA was potent than CHA. Prior treatment of caffeine (50 mg/kg/day) or theophylline (50 mg/kg/day) abolished the diuretic effect of CHA, whereas DPX (50 mg/kg/day) did not affect the CHA effect. CHA, 0.5 mg/kg/day, produced no change in plasma renin activity and plasma levels of aldosterone, epinephrine, and norepinephrine. These results suggest that this novel phenomenon produced by an activation of renal adenosine receptors plays an important role in urinary concentrating mechanism.

• 고신대학교 의과대학 학술지
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• 제33권3호
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• pp.468-476
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• 2018

Perioperative anaphylaxis, although rare, is a severe, life-threatening unexpected systemic hypersensitivity reaction. Simultaneous administration of various drugs during anesthesia, the difficulty of communicate with patients in sedation and anesthesia, and coverage of the patient with surgical drapes are considered to be factors that impede early recognition of anaphylactic reactions. It is very important to perform an intradermal skin test because antibiotics are the most common cause of perioperative anaphylaxis. We report a case of negative-intradermal skin test antibiotic anaphylaxis mistaken for local aesthetic systemic toxicity without increase of serum tryptase for confirmative diagnostic biomaker during surgery under brachial plexus block. It is not possible to exclude the danger of anaphylaxis completely, even if it is negative-intradermal skin test and normal tryptase level. Therefore, anesthesiologists should be closely monitored and treated early for antibiotics related hypersensitive reaction, like other medicines during anesthesia.

• Archives of Pharmacal Research
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• 제26권9호
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• pp.768-772
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• 2003

Tween 80 (Polysorbate 80) is a hydrophilic nonionic surfactant commonly used as an ingredient in dosing vehicles for pre-clinical in vivo studies (e.g., pharmacokinetic studies, etc.). Tween 80 increased apical to basolateral permeability of digoxin in Caco-2 cells suggesting that Tween 80 is an in vitro inhibitor of P-gp. The overall objective of the present study was to investigate whether an inhibition of P-gp by Tween 80 can potentially influence in vivo absorption of P-gp substrates by evaluating the effect of Tween 80 on the disposition of digoxin (a model P-gp substrate with minimum metabolism) after oral administration in rats. Rats were dosed orally with digoxin (0.2 mg/kg) formulated in ethanol (40％, v/v) and saline mixture with and without Tween 80 (1 or 10％, v/v). Digoxin oral AUC increased 30 and 61％ when dosed in 1 ％ and 10％ Tween 80, respectively, compared to control (P＜0.05). To further examine whether the increase in digoxin AUC after oral administration of Tween 80 is due, in part, to a systemic inhibition of digoxin excretion in addition to an inhibition of P-gp in the GI tract, a separate group of rats received digoxin intravenously (0.2 mg/kg) and Tween 80 (10％ v/v) orally. No significant changes in digoxin IV AUC was noted when Tween 80 was administered orally. In conclusion, Tween 80 significantly increased digoxin AUC and Cmax after oral administration, and the increased AUC is likely to be due to an inhibition of P-gp in the gut (i.e., improved absorption). Therefore, Tween 80 is likely to improve systemic exposure of P-gp substrates after oral administration. Comparing AUC after oral administration with and without Tween 80 may be a viable strategy in evaluating whether oral absorption of P-gp substrates is potentially limited by P-gp in the gut.

• 경영정보학연구
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• 제10권3호
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• pp.1-20
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• 2008

1990년대 이래 신경 제라는 제목 하에 다양한 경제 사회적 현상들이 관찰되고 논의되어왔다. 문헌에 기록된 대부분의 신경제 현상들은 단편적 일화적으로 묘사되고 있어 신경제의 본질에 대한 논리적이고 체계적인 설명이 부족하다. 본 연구는 시스템 관점에서 신경제 현상의 특성을 분석하였다. 구체적으로 신경제를 하나의 시스템 현상으로 놓고 아래 5가지 시스템적 속성에 대한 답을 구하였다. 1) 신경제 시스템의 구성요소는 무엇이며 그것들은 어떻게 상호 연관되어 있는가? 2) 신경제 시스템은 기능적으로 어떻게 작동하는가? 3) 신경제 시스템에서 생산되는 재화와 서비스는 무엇인가? 4) 신경제가 시스템으로서 가지는 가치는 무엇인가? 5) 신경제 시스템의 총체적 체계적 특성은 무엇인가? 본 연구는 상기 각 시스템 측면에서 신경제가 가지는 핵심 속성을 도출하고, 이를 종합하여 시스템 관점에서의 신경제 이해를 도모하고 있다. 아울러 신경제의 시스템적 특성이 기업의 전략에 시사하는 바가 무엇인지를 논의하고 앞으로의 연구과제들을 제시하고 있다.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.293.2-294
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• 2003

Topical buccal therapy with steroid anti-inflammatory drugs is based on the concept that a high activity of steroids can be produced at the site of administration and, at the same time, the degree of systemic side effects can be minimized or avoided. In this study we developed a new formulation consisting of a mucoadhesive bead for buccal administration of glucocorticoids. (omitted)

• The Korean Journal of Pain
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• 제2권2호
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• pp.167-173
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• 1989

Inadequate pain relief after upper abdominal surgery increases the incidence of pulmonary complications due to the difficulty in coughing and deep breathing. Kvalheim and Reiestad (1984) introduced intrapleural administration of local anesthetic solutions to produce analgesia following cholecystectomy performed through a subcostal incision, unilateral breast surgery and renal surgery. We studied continuous intrapleural administration of bupivacaine and epinephrine, and its effect in controlling pain after cholecystectomy. In 9 patients, an intermittent dosage technique was used. An intrapleural catheter was inserted and 20 ml of 0.5% bupivacaine and 1:100,000 epinephrine was administered. Results were as following: 1) Mean analgesic duration from the initial intrapleural injection to secondary administration of supplementary bupivacaine was 13.5 hours. 2) No specific changes were noted on vital signs and arterial blood gases. 3) Effective analgesia, produced by intrapleural bupivacaine resulted in significant improvement in tidal volume as measured by spirometry. 4) No signs of systemic toxicity and complications were encountered. 5) Intrapleural administration of a local anesthetics after cholecystectomy provides a satisfactory duration of analgesia.

• Journal of Pharmaceutical Investigation
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• 제29권3호
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• pp.179-184
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• 1999

Phannacokinetics of epigallocatechin gallate(EGCG) was studied following i.v. bolus and oral administration in rats. The values of systemic clearance(CL) were $67.9{\pm}5.2$ and $26.5{\pm}1.4\;ml/min/kg$ following i.v. bolus administration of 1 mg and 5 mg EGCG, respectively. The values of volume of distribution at steady state (Vss) were $380{\pm}56$ and $835{\pm}84\;ml/kg$ after i.v. bolus administration of 1 mg and 5 mg EGCG, respectively. The decrease in the value of CL and the increase in the value of $V_{ss}$ as a function of EGCG dose (1 mg to 5 mg) suggest saturable mechanism(s) responsible for the distribution and elimination of EGCG. The fraction absorbed of EGCG after oral and intraduodenal administration of GTC were 13% and 22% of the dose, respectively. This result suggests a considerable degradation or elimination of EGCG in the gastrointestinal absorption after oral administration in rats.