• 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.

• 약학회지
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• 제52권5호
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• pp.394-401
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• 2008

In order to access the suppressive effects of piroxicam (PX) and hydrolyzed products of Scutellariae Radix (PSH) on arthritis, we investigated whether PSH gel could suppress the progression of collagen-induced arthritis. PX, one of nonsteroidal anti-inflammatory drugs has been used in the systemic and topical treatment in a variety of inflammatory conditions. Scutellariae Radix, one of the herbal medicines, was used for the purpose of anti-inflammatory and anti-bacterials. For the purpose of transdermal absorption of the hydrogel preparations, two classes of hydrogels (PX, PSH) were formulated with carbomer 940, diethylene glycol monoethyl ether, polyethylene glycol-8-glyceryl caprylate/caprate and triethanolamine. In carrageenan-induced edema in rat hind paws, inhibition of foot swelling was more increased in PSH than PX hydrogel. Rheumatoid factors including serum IgG, IgM and collagen specific antibody were present much lower in PSH gel treated mice than control. Histological examination revealed that PSH hydrogel inhibited infiltration of inflammatory cells into affected paw joint, compared with control. The PSH hydrogel would be a suitable preparation to increase transdermal treatment for anti-inflammatory effects on collagen-induced arthritis.

• 대한임상약리학회:학술대회논문집
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• 대한임상약리학회 1995년도 정기총회 및 추계학술대회
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• pp.67-67
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• 1995

• The Korean Journal of Physiology and Pharmacology
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• 제10권1호
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• pp.45-50
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• 2006

Melittin-induced pain model has been known to be very useful for the study of pain mechanism. Melittin-induced nociceptive responses are reported to be modulated by the changes in the activity of excitatory amino acid receptor, calcium channel, spinal serotonin receptor and extracellular signaling-regulated kinase. The present study was undertaken to investigate the role of cyclooxygenase (COX) in the melittin-induced nociception. Changes in mechanical threshold, flinchings and paw thickness were measured before and after intraplantar injection of melittin in the rat hind paw. Also studied were the effects of intraperitonealy administered diclofenac (25 mg & 50 mg/kg), piroxicam (10 mg & 20 mg/kg) and meloxicam (10 mg & 20 mg/kg) on the melittin-induced nociceptions. Intraplantar injection of melittin caused marked reduction of mechanical threshold that was dose-dependently attenuated by non-selective COX inhibitor (diclofenac) and selective COX-1 inhibitor (piroxicam), but not by COX-2 inhibitor (meloxicam). Melittin-induced flinchings were strongly suppressed by non-selective COX and COX-1 inhibitor, but not by COX-2 inhibitor. None of the COX inhibitors had inhibitory effects on melittin-induced increase of paw thickness (edema). These experimental findings suggest that COX-1 plays an important role in the melittin-induced nociceptive responses.

• 대한한방부인과학회지
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• 제26권1호
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• pp.1-24
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• 2013

Objectives: The object of this study was to observe the protective effect of Gamijipaesan aqueous extracts(GJS), which has been traditionally used in Korean medicine in obstetrics & gynecological fields as anti-infectious and anti-inflammatory agents, against mastitis induced by Staphylococcus aureus infection in a rat model through antibacterial, antiinflammatory, immunomodulatory, and anti-oxidant effects. Methods: Antibacterial activities of GJS against S. aureus were detected using standard agar microdilution methods, with the effects on the bacterial invasion and intracellular killing of individual test materials in human mammary gland carcinoma cell(MCF-7) and murine macrophages(Raw 264.7) at MIC1/2, MIC and MIC2 concentration levels. In addition, the effects on the cell viability, nitric oxide(NO), tumor necrosis factor(TNF)-${\alpha}$ and interleukin (IL)-6 productions of LPS activated Raw 264.7 cells. The changes on the mammary tissue viable bacterial numbers, myeloperoxidae(MPO), inducible nitric oxide synthetase(iNOS), TNF-${\alpha}$ and IL-6 contents were observed in the S. aureus in vivo intramammary infectious rat model. The anti-bacterial and anti-inflammatory effects were compared with ciprofloxacin and piroxicam, respectively in the present study. Results: MIC of GJS and ciprofloxacin against S. aureus were detected as $0.860{\pm}0.428$ (0.391-1.563) mg/ml and $0.371{\pm}0.262$(0.098-0.782) ${\mu}g/ml$, respectively. In addition, GJS and ciprofloxacin were also showed marked dosage-dependent inhibition of the both bacterial invasion and intracellular killing assays using MCF-7 and Raw 264.7 cells at MIC1/2, MIC and $MIC{\times}2$ concentrations, respectively. $ED_{50}$ against LPS-induced cell viabilities and NO, TNF-${\alpha}$ and IL-6 releases of GJS were detected as 0.72, 0.04, 0.08 and 0.11 mg/ml, and as 19.04, 4.18, 5.37 and 4.27 ${\mu}g/ml$ in piroxicam, respectively. 250 and 500 mg/kg of GJS also inhibit the intramammary bacterial growth, MPO, iNOS, TNF-${\alpha}$ and IL-6 contents in S. aureus in vivo intramammary infected rats, respectively. GJS 500 mg/kg showed quite similar antibacterial and anti-infectious effects as compared with ciprofloxacin 40 mg/kg and also showed similar anti-inflammatory effects as piroxicam 10 mg/kg, in S. aureus in vivo intramammary infectious models. Conclusions: The results obtained in this study suggest that over 250 mg/kg of GJS showed favorable anti-infectious effects against S. aureus infection in a rat model through their antibacterial, anti-inflammatory, immunomodulatory and anti-oxidant effects and therefore expected that GJS can be used as alternative therapies, having both anti-inflammatory and anti-infectious activities. However, more detail mechanism studies should be conducted in future with the efficacy tests of individual herbal composition of GJS and the screening of the biological active compounds in individual herbs. In the present study, GJS 500 mg/kg showed quite similar anti-infectious effects were detected as compared with ciprofloxacin 40 mg/kg treated rats, and also GJS shows quite similar anti-inflammatory effects as compared with piroxicam 10 mg/kg in S. aureus in vivo intramammary infectious rats, but ciprofloxacin did not showed any anti-inflammatory effects, and piroxicam did not showed anti-infectious effects in this study.

• 대한치과교정학회지
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• 제35권1호
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• pp.60-68
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• 2005

부정교합의 평가는 질적, 양적인 면에서 모두 평가되어야 한다. 이는 부정교합의 경중도의 평가뿐만 아니라 이의 치료가 얼마나 어려운가를 반영할 수 있는 치료의 난이도로 발전되어야 한다. 이러한 부정교합의 경중도와 치료의 난이도를 객관적이고 효율적으로 측정하기 위한 방법의 개발이 필요하다. 이는 치과 교정학에서 치료의 효과 및 효율의 평가에서 치료난이도를 반영하는 부정교합 경중도 측정을 가능하게 하여 교정치료의 양적 그리고 질적 평가를 가능하게 할 것이다. 본 연구는 부정교합의 객관적 정량분석을 위한 연구로써 객관적 부정교합의 경중도와 주관적 치료 난이도를 측정하고 이들간의 상관관계를 연구하고자 하였다. 이를 위하여, 100쌍의 교정용 치아모형을 이용하여 경험 있는 8명의 치과교정의가 주관적인 치료의 난이도를 평가하기 위하여 치료의 어려움과 예상치료기간을 추정하였으며. 객관적인 부정교합의 경중도를 측정하기 위하여 저자는 동료평가등급 지수 (PAR index) 를 사용하여 각 부정교합의 구성요소 별 경중도를 계측하였다. 이들간의 상관관계의 조사에서 객관적으로 계측한 부정교합의 경중도와 평가단의 치료 예상난이도 사이에는 유의한 관련성이 있었으며. 특히 상악 전치부 배열, 구치부교합, 수평피개도, 수직피개도 그리고 정중선 일치도에서 높은 상관성을 보였다 본 연구를 통하여 객관적으로 계측된 부정교합의 경중도가 치과 교정의사가 느끼는 주관적 치료 난이도에 미치는 영향을 조사할 수 있으며. 이는 치료의 주관적 난이도를 내포하는 새로운 국내형 교합지수 개발에 도움이 될 것으로 사료된다회된 법랑질 깊이가 유의성 있게 감소하였다. (p<0.05). 접착레진으로 부착된 군 (Group 4)은 법랑질 탈회가 거의 나타나지 않았다. 이상의 연구결과는 교정치료 시 법랑질 탈회 가능성을 줄이기 위해서 브라켓 부착 시 실런트 레진의 도포가 유용함을 시사하였다..5\;{\mu} g/mL)\;piroxicam(3.5\pm0.3\l{\mu}g/mL)$,으로 유의성이 있었으며(p<0.05), 흡수 속도상수는 piroxicam-$\beta$-cyclodextrin$(3.00\pm0.49\;h^{-1}), \;piroxicam(1.80\pm0.21\;h^{-1})$이었다(p<0.1). 이상의 결과에서, piroxicam-$\beta$-cyclodextrin정은 piroxicam 확산정과 비교하여 흡수되는 정도는 서로 비슷하지만 흡수 초기의 혈장농도 및 흡수속도상수에서 보다 빠른 약동학적 특성을 나타내었다.삼차원 입체조형치료를 받은 환자에 대해서는 앞으로 추적 관찰이 좀 더 필요할 것으로 생각된다. 앞으로 국소관해를 높이기 위한 방사선치료방법과 전신적 전이율의 감소를 위한 항암요법에 관한 연구가 필요할 것으로 생각된다.다. MD-BED $Gy_3$는 직장합병증 발생과의 관계는 통계적으로 유의하였고, 방광합병증과는 유의하지 않았다. 직장합병증과의 연관성은 MD-BED $Gy_3$보다 개별 환자의 직장전벽 총 선량 BED값인 R-BED $Gy_3$가 훨씬 더 높았다

• 대한한방부인과학회지
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• 제26권1호
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• pp.41-58
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• 2013

Objectives: The object of this study was to observe the in vitro anti-bacterial and anti-inflammatory effects of three single aqueous herbal extracts(Trichosanthes Semen, Gardeniae Fructus, and Angelicae Dahuricae Radix), traditionally used for treating various gynecological diseases including mastitis in Korea, against Staphylococcus aureus and lipopolysaccharide(LPS)-activated Raw 264.7 cells. Methods: Anti-bacterial activities of three single aqueous herbal extracts against S. aureus were detected using standard agar microdilution methods. In addition, the effects on the cell viability, $PGE_2$, NO, TNF-${\alpha}$, IL-$1{\beta}$ and IL-6 productions of LPS activated Raw 264.7 cells. The anti-bacterial and anti-inflammatory effects were compared with lincomycin and piroxicam, respectively in the present study. Results: MIC of three single aqueous herbal extracts against S. aureus were detected as over 25, $4.063{\pm}2.096$ and $1.641{\pm}0.972$ mg/ml, respectively. MIC of lincomycin was detected as $0.469{\pm}0.297{\mu}g/ml$ at same conditions. In addition, $ED_{50}$ against LPS-induced cell viabilities and cytokine releases of three single aqueous herbal extracts were as follows - cell viability: 7.635, 13.761, 6.986 mg/ml, NO production : 4.808, 22.015, 2.949 mg/ml, $PGE_2$ production : 3.040, 4.312, 0.821 mg/ml, TNF-${\alpha}$ production : 9.563, 54.931, 1.240 mg/ml, IL-$1{\beta}$ production : 1.362, 1.801, 0.534 mg/ml, IL-6 production : 0.371, 0.797, 0.202 mg/ml, respectively. $ED_{50}$ of piroxicam against LPS-induced cell viabilities, NO, $PGE_2$, TNF-${\alpha}$, IL-$1{\beta}$ and IL-6 were detected as 35.179, 6.552, 1.162, 7.273, 7.101 and 5.044 ${\mu}g/ml$, respectively at same conditions. Conclusions: The results of the study showed anti-bacterial effects against S. aureus in the order of Gardeniae Fructus and Angelicae Dahuricae Radix aqueous extracts, except for Trichosanthes Semen. They also showed anti-inflammatory effects against LPS-activated Raw 264.7 cells in the order of Angelicae Dahuricae Radix, Trichosanthes Semen, and Gardeniae Fructus aqueous extracts. These three herbs are expected to be great substitutes to reduce side-effect of lincomycin and piroxicam, if the amount of those three single aqueous herbal extracts is adjusted appropriately.

• Archives of Pharmacal Research
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• 제22권1호
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• pp.44-47
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• 1999

Three 1,2-benzothiazine derivatives were synthesized, and their analgesic / anti-inflammatory efficacy and their effect s of gastric irritation were evaluated. Among the three compounds, 39 exhibited the most potent anlagesic action, but the effect was weaker than that of piroxicam. Nonetheless, the compound showed 4 times more potent analgesic action with less gastric damage than did ibuprofen. These compounds did not show anti-inflammatory effect at an oral dose of 5 mg/kg.

• Bulletin of the Korean Chemical Society
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• 제26권11호
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• pp.1771-1775
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• 2005

An efficient and environment friendly method has been described for the synthesis of various 2-alkyl-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxides starting from N-alkylation of sodium obenzosulfimide in an ionic liquid for the first time. Ring cleavage and ring closure of the resulting product were achieved in a single step in a cost effective solvent (methanol) followed by N-alkylation of resulting alkyl 4-hydroxy-2H-1,2-benzothiazine-3-carboxylate in ionic liquid while boron triflouride was used as a catalyst along with molecular sieves in carboxamide formation step.

• 대한수의학회지
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• 제57권3호
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• pp.205-208
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• 2017

Study purposes were to evaluate ultrasonographic characteristics of transitional cell carcinoma (TCC) and quantitate bladder tumor size in dogs. Heterogeneous mass, wall involvement, and broad-based attachment were significantly associated with TCC, but not prominently the trigone region. Mass size evaluation revealed a significant correlation between progressive disease (PD) in TCC patients with piroxicam therapy. Largest diameter of target lesion/body weight (cm/kg) ratio showed a high mean value in PD. A value > 0.3 was associated with PD with 83% sensitivity and 66% specificity. The results suggest that ultrasonography can provide evidence for diagnosing and predicting a prognosis for TCC.