• Title/Summary/Keyword: Indomethacin

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Effect of Carrier on Dissolution Characteristics of Indomethacin from its Coprecipitates (Indomethacin Coprecipitate 중 Indomethacin 용출(溶出)에 미치는 Carrier의 영향(影響))

  • Ku, Young-Soon;Ahn, Young-Mee
    • Journal of Pharmaceutical Investigation
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    • v.14 no.1
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    • pp.1-10
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    • 1984
  • Effects of water soluble carrier on the dissolution characteristics of indomethacin coprecipitates were investigated. Water soluble carriers used were polyvinylpyrrolidone, dextrose, mannitol and their mixtures of various ratios. The dissolution rates of indomethacin from coprecipitate with ratios of drug-to-carrier, kinds of carrier and ratios of carriers were as follows: 1. The dissolution rates increased proportionally to the ratios of carrier in the case of both single and combined carrier, and the dissolution rate of coprecipitate with the combined carrier was more rapid than that with single carrier. 2. The combined carrier of PVP-dextrose (1 : 2) in the case of the coprecipitate of drug-to carrier (1 : 1) and PVP-dextrose (4 : 1) in the case of the coprecipitate of drug-to carrier (1 : 3) yield the most rapid dissolution rate. 3. The dissolution rate of indomethacin was the most markedly enhanced in the case of the combined carrier of PVP and dextrose.

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Protective Effects of BJS-mix001, in Indomethacin induced Gastric Damages in Rats (BJS-Mix001이 Indomethacin 유발 랫트 위점막 손상에 미치는 영향)

  • Lim, So-Yeon;Byun, Joon-Seok;Kim, Dae-Jun;Kwak, Min-A
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.26 no.2
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    • pp.181-188
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    • 2012
  • The object of this study was to observe the gatro protective effects of BJS-mix001, a mixed herbal formula consisted of 4 herbal drugs Pinelliae Rhizoma : Coptidis Rhizoma : Massa Medicata Fermentata : Ostreae Testa = 1 : 1 : 1 : 1 (g/g) mixtures, which were main component of oriental medicine for treating various digestive diseases, in indomethacin induced gastric damages in rats. Three different dosages of BJS-mix001 (200, 100 and 50 mg/kg) were once orally administered 30 min before indomethacin treatment. Six hrs after indomethacin treatment, changes on the gross lesion scores, fundic histopathology, MPO activity and anti oxidant activities were observed. The results were compared with omeprazole, antioxidant and proton pump inhibitor 10 mg/kg and DA-9601, a standardized extract of the herb Artemisia asiatica 100 mg/kg treated group, respectively. As results of all three different dosages of BJS-mix001 in the indomethacin induced gastric damaged rats, significant decreased gastric damages were detected as compared with the indomethacin treated control rats. BJS-mix001 also strengthened the antioxidative defense systems - decreased the level of lipid peroxidation and catalase activity but increased the level of superoxide dismutase and glutathione contents. BJS-mix001 showed similar gastro protective effects as compared with equal dosage of DA-9601, and BJS-mix001 50 mg/kg showed slighter effects as compared with omeprazole 10 mg/kg, in the present study. The results obtained in this study suggest that BJS-mix001 showed favorable effects in the indomethacin induced gastric damages mediated by strengthening of the antioxidative defense systems.

The effects of indomethacin on distribution and expression of COX-2 and IGF-I in the mandibular condyle of growing dogs (인도메타신투여가 개의 하악두에서 COX-2와 IGF-I의 발현과 분포에 미치는 영향)

  • Nam, Jong-Hyun;Lee, Ki-Soo;Kang, Yoon-Goo
    • The korean journal of orthodontics
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    • v.35 no.5 s.112
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    • pp.351-360
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    • 2005
  • This study aimed to investigate the effects of indomethacin on distribution and expression of COX-2 and IGF-1 in the mandibular condyle ofi growing dogs and to examine the number of chondroclasts around the mineralization zone indomethacin inhibits prostatlandin $E_2$ production in the tissue by inhibiting synthesis of cyclooxygenase 2. Prostaglandin $E_2$ stimulates insulin-like growth factor synthesis. Insulin-like growth factor stimulates growth of mandibular condylar cartilage. Eight mongrel dogs. aged 13-14 weeks, were divided into 4 groups. Group 1 and group 2 were administered indomethacin 2 mg/Kg/day orally two times a day for 7 days and 14 days respectively. Group 3 were administered indomethacin 8mg/Kg/day orally 2 times a day for 14 days, and 4he control group were administered a placebo. The mandibular condyle heads were sectioned in $5{\mu}m$ thickness The specimens were stained with H-E staining. COX-2 immunohistochemical staining and IGF-1 immunohistochemical staining and examined under microscope. After TRAP staining, the number of chondroclasts were calculated The observed results were as follows: Indomethacin inhibited expression and distribution of COX-2 and IGF-1 on the proliferative zone of condylar cartillage. Indomethacin decreased the number of chondroclastes on the mineralization zone by a time-dependent manner (P<0.05). Indomethacin inhibited expression and distribution of IGF-I by a dose and time-dependent manner. These results show that indomethacin inhibited expression and distribution of COX-2 and IGF-1 on the proliferative zone of condylar cartilage and decreased the number of chondroclasts and suggests that when indomethacin is administered for a long time, condyle growth could be delayed.

Pro-Oxidantive Effect of Dehydroepiandrosterone on Indomethacin-Induced Acute Gastritis in Rats

  • Kim, Beom-Gyu;Yim, Sung-Hyuk;Jeong, Seong-Jin;Choi, Yoo-Shin;Nam, Yun-Sung;Jeong, Ji-Hoon;Yun, Sin-Weon;Do, Jae-Hyuk;Lim, Hyun-Muck;Park, Eon-Sub
    • Biomolecules & Therapeutics
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    • v.17 no.1
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    • pp.57-61
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    • 2009
  • This study examined whether or not a pretreatment with dehydroepiandrosterone (DHEA) has an effect on indomethacin-induced gastric mucosal damage. The DHEA group, male Sprague-Dawley rats, was administrated with DHEA orally at a dose of 4 mg/day for one week before inducing gastritis with indomethacin (50 mg/kg, p.o.). Histological assay, lipid peroxidation assay, superoxide dismutase (SOD), glutathione peroxidase (GPx) and Catalase activities were determined. Interestingly, it was found that the DHEA pretreatment attenuated the gastric lesion area induced by indomethacin. Rather, the pretreatment with high dose of DHEA led to submucosal edema, leukocyte infiltration in submucosa and mucosal necrosis. The levels of MDA in the DHEA pretreatment were also higher than those in the rats given with vehicle pretreatment. This suggests that the DHEA pretreatment deteriorates severe inflammation in indomethacin-induced gastritis. DHEA supplementation significantly increased SOD activity in the gastric mucosa. However, the catalase and GPx activities were not altered by DHEA. The co-administration of DHEA with an indomethacin might not offer a protective effect against the acute gastritis induced by indomethacin.

Effect of Water Extract of Ulmi pumilae Cortex on Gastric Ulcer in Rats (유백피(楡白皮) 물 추출물이 흰쥐의 위궤양(胃潰瘍)에 미치는 영향(影響))

  • Lim, Jong-Pil;Cui, Xun
    • Korean Journal of Medicinal Crop Science
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    • v.10 no.3
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    • pp.177-180
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    • 2002
  • Ulmi pumilae Cortex(bark of Ulmus pumila L.), oriental medicine, has been used for the folk remedy of the gastric diseases. In order to investigate antiulcer activities, some experiments for Shay, aspirin-induced and indomethacin-induced gastric ulcers were conducted. The water extract of Ulmi pumilae Cortex(UX) was given intraperitoneally, and the groups of UX 500 and 1,000mg/kg significantly inhibited Shay, aspirin and indomethacin-induced ulcers in rats.

Suppression of Induced Mucin Production from Human Airway Epithelial Cells by Coumarin and Indomethacin (쿠마린과 인도메타신의 억제작용 쿠마린과 인도메타신의 억제작용)

  • Lee, Jae-Woo;Kim, Kil-Dong;Jeon, Byeong-Kyou;Lee, Choong-Jae
    • YAKHAK HOEJI
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    • v.54 no.5
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    • pp.416-421
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    • 2010
  • We examined whether indomethacin, noscapine, coumarin, uridine and betaine affect airway mucin production induced by EGF or TNF-${\alpha}$ from NCI-H292 cells. Cells were pretreated with each agent for 30 min and then stimulated with EGF or TNF-${\alpha}$ for 24 h. Of the five compounds, coumarin suppressed airway mucin production induced by EGF or TNF-${\alpha}$. However, indomethacin suppressed airway mucin production induced by EGF. This result suggests that coumarin and indomethacin can regulate the production of mucin induced by EGF, by directly acting on airway epithelial cells.

Indomethacin Induces Apoptosis in NCI-H1299 Human Lung Carcinoma Cells

  • Kim, Bum-Shik;Kim, Soon-Ae;Kim, Mi-Ja;Lee, Hee-Jae;Park, Seung-Joon;Jung, Jee-Chang;Kim, Chang-Ju;Yim, Sung-Vin;Chung, Joo-Ho
    • The Korean Journal of Physiology and Pharmacology
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    • v.5 no.2
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    • pp.177-181
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    • 2001
  • Recently, nonsteroidal anti-inflammatory drugs (NSAIDs) have been found to be useful in the chemoprevention of colon cancer. To investigate whether indomethacin, an NSAIDs, induces apoptosis and thus assess the possibility of its application in the chemoprevention of human lung cancer, we have performed MTT assay, TUNEL assay, DAPI staining, and flow cytometric analysis using human lung carcinoma cell line NCI-H1299. Through morphological and biochemical analyses, it was demonstrated that NCI-H1299 cells treated with indomethacin (0.5 mM) exhibit classical apoptotic features. These results suggest that indomethacin induces apoptosis in NCI-H1299 cells and that NSAIDs, including indomethacin, may be a useful tool for the chemoprevention of human lung cancer.

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Blunted Indomethacin-Induced Downregulation of Aquaporins by Nitric Oxide Synthesis Inhibition in Rats

  • You, Ju-Hee;Lee, Sung-Su;Bae, Eun-Hui;Ma, Seong-Kwon;Kim, Soo-Wan;Lee, Jong-Un
    • The Korean Journal of Physiology and Pharmacology
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    • v.10 no.4
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    • pp.213-216
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    • 2006
  • The present study was aimed to determine whether nitric oxide (NO) plays a role in the regulation of aquaporin (AQP) channels in the kidney. Male Brattleboro rats ($250{\sim}300\;g$ body weight) were used. The experimental group was treated with $N^G$-nitro-L-arginine methyl ester (L-NAME, 100 mg/L drinking water) for 1 week, and cotreated with indomethacin (5 mg/kg, twice a day, i.p.) for the last two days. Control groups were treated with either L-NAME for 1 week, indomethacin for 2 days, or without any drug treatment. The abundance of AQP1, AQP2 and AQP3 proteins in the kidney was determined by Western blot analysis. Indomethacin downregulated AQP channels, whereas L-NAME by itself showed no significant effects on them. The indomethacin-induced downregulation of AQP2 and AQP3 was significantly blunted in L-NAME-treated rats, while that of AQP1 was not affected. These results suggest that endogenous NO, when stimulated, may downregulate AQP channels that are specifically regulated by AVP/cAMP pathway in the kidney.

Effects of Indomethacin on Development and Hatching of Mouse Embryo (Indomethacin이 생쥐 착상전 배아의 발생 및 부화에 미치는 영향)

  • Cheon, Yong-Pil;Gye, Myung-Chan;Kim, Chung-Hoon;Kim, Moon-Kyoo
    • Clinical and Experimental Reproductive Medicine
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    • v.24 no.1
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    • pp.35-42
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    • 1997
  • The present study was designed to define the role of prostaglandin in the development and hatching of mouse embryo. The effects of indomethacin, an inhibitor of prostaglandin synthesis, on the development and hatching of morula and blastocyst were examined. In early morula stage, embryos were degenerated significantly at 100 ${\mu}M$ and 200 ${\mu}M$ indomethacin. However, the viability of embryos was not influenced by concentration in any other embryonic stages. In all embryonic stages, the hatching was suppressed with concentration dependent manner, but expansion was not suppressed. Particularly, in 84h embryos post hCG injection, the hatching was suppressed significantly compared with post hCG 72h or 96h embryos. When embryos were treated with 100 ${\mu}M$ indomethacin for a specific time (12h) in according to the development stage, the hatching was suppressed all groups. These suppressional effect was decreased as embryonic development stage was progressed. However, the expansion was not affected in all treatment group. This study suggests that hatching-related metabolic substances are synthesized from morula stage and intraembryonic signaling mediated prostaglandin was important for development and hatching of mouse embryo.

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Studies on the effect of Kamikuibitang on the Gastric Ulcer in Rats (가미귀비탕(加味歸脾湯)이 흰쥐의 위궤양(胃潰瘍)에 미치는 영향(影響))

  • Baek, Dong-Jin
    • The Journal of Korean Medicine
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    • v.17 no.2 s.32
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    • pp.277-290
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    • 1996
  • This study was aimed to evaluate the anti-pain effect of Kamikuibitang in acetic acid method and the anti-ulceration effect of Kamikuibitang in indomethacin, aspirin and immobilization stress method in rats. The results were follows; 1. The anti-pain effects of Kuibitang and Kamikuibitang were decreased compared with those of control group. 2. In indomethacin and aspirin method, the anti-ulcerative effects of experimental groups were shown compared with those of control group. 3. In immobilization stress method, the anti-ulcerative effect of experimental groups was significantly shown compared with that of control group. 4. The serum gastrin levels of Kuibitang groups showed very significant decrease in indomethacin-induced and immobilization stress-induced ulcers. The serum gastrin levels of Kamikuibitang groups showed very significant decrease in indomethacin-induced, aspirin- induced and immobilization stress-induced ulcers. 5. The serum $V_{B12}$ levels of Kuibitang groups showed very significant increase in both indomethacin-induced and immobilization stress-induced ulcers. The serum $V_{B12}$ levels of Kamikuibitang groups showed significant increase in aspirin-induced and immobilization stress-induced ulcers whereas very significant increase in indomethacin-induced ulcer. According to the above results, it was concluded that Kamikuibitang had very significant anti-ulceration effect as well as anti-pain effect on gastric ulcer in rats.

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