• Title/Summary/Keyword: indomethacin

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Dissolution Characterstics of Indomethacin Microcapsules Prepared Using Gelatin-Gum Arabic Complex Coacervation (젤라틴-아리비아고무를 써서 製造한 인도메타신 마이크로캅셀의 용출 특성)

  • Ku, Young-Soon;Kim, Hwa-Yeon
    • YAKHAK HOEJI
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    • v.28 no.4
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    • pp.223-229
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    • 1984
  • Microcapsules of indomethacin were prepared by the complex coacervation technique using gelatin-gum arabic as the wall-forming material. The effects of varying drug-to-matrix ratios and formalization time, and hydroxy propyl cellulose (HPC) added on the release of drug from microcapsules were studied. As the amount of wall-forming material increased, the drug content in the microcapsules decreased and the release of drug from microcapsules was retarded. The drug content was lower in the HPC added microcapsules than that in the microcapsules was retarded. The drug content was lower in the HPC added microcapsules than that in the microcapsules without HPC and the microcapsules with 1:4 drug-to-matrix ratio showed the slowest release. The release rate of the drug from microcapsules with 1:2 drug-to-matrix was delayed according to the increase of formalization time and the microcapsules formalized for 24hr showed ratio the most retardation.

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Crystal Structure of Antiinflammatory Sulindac

  • Koo Chung Hoe;Kim Sang Hern;Shin Wanchul
    • Bulletin of the Korean Chemical Society
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    • v.6 no.4
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    • pp.222-224
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    • 1985
  • The crystal structure of sulindac, $C_{20}H_{17}Fo_3S$, one of the nonsteroid antiinflammatory agents, has been determined by the X-ray diffraction techniques using diffractometer data obtained by the $\varpi-2{\theta}$ scan technique with Cu $$K_{\alpha}$$ radiation from a crystal with space group symmetry Pbca and unit cell parameters a = 8.166(1), b = 18.291(8), c = 23.245(10) ${\AA}.$ The structure was solved by direct methods and refined by full-matrix least-squares to a final R = 0.11 for the 1153 observed reflections. The carboxyl group is nearly perpendicular to the indenyl ring as observed in indomethacin. The dihedral angle between the indenyl and phenyl rings is $35^{\circ}while$ the corresponding angle in indomethacin is $67^{\circ}.$ Crystal packing consists of a hydrogen bond and partial ring stacking between the indenyl rings.

$Luteolin7-O-{\beta}D-glucuronopyranoside$ has the protective effect on gastritis and esophagitis in rats

  • Bae, Ki-Lyong;Yim, Sung-Hyuk;Min, Young-Sil;Park, Joon-Hong;Choi, Hee-Jung;Ham, In-Hye;Hwang, Wan-Kyunn;Sohn, Uy-Dong
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.265.2-265.2
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    • 2002
  • It is well known that flavonoids are the inhibitory effects on inflammations. This study was designed to determine the anti-inflammatory effects of luteolin-7-O-${\beta}$D-glucuronopyranoside (LGC). newly synthesized flavonoids. which was extracted from Salix gilgiana leaves. We investigated the protective action of LGC on reflux esophagitis and gastritis in rats. Esophagitis and gastritis were induced by surgical procedures and the exposure to indomethacin (50 mg/kg), respectively. LGC was injected intraduodenally immediately after the surgical procedures and the exposure to indomethacin (omitted)

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Rosin Microparticles as Drug Carriers: Influence of Various Solvents on the Formation of Particles and Sustained-release of Indomethacin

  • Lee Chang Moon;Lim Seung;Kim Gwang Yun;Kim Do Man;Kim Dong Woon;Lee Hyun Chul;Lee Ki Young
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.9 no.6
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    • pp.476-481
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    • 2004
  • The aim of this study was to formulate a sustained release system for indomethacin (IND) with rosin gum obtained from a pine tree. Rosin microparticles were prepared by a disper­sion and dialysis method without the addition of surfactant. In order to investigate the influence of solvents on the formation of colloidal microparitcles, various solvents like ethanol, DMF, DMAc, and acetone were used. The rosin microparticles containing IND were characterized by X­ray differactometry (XRD) and differential scanning calorimetry (DSC). The morphologies of rosin microparticles observed by scanning electron microscopy (SEM) were spherical. The solvents used to dissolve rosin significantly affected the drug content and drug release rate of IND. The release behaviors of IND from the rosin microparticles were dependent on the drug content and size of the particles. Rosin micorparticles with a higher drug content and of a larger particle size had a slower drug release rate. Also, the IND release rate from the rosin microparticles could be regulated by the rosin content in the microparticles. From these results, rosin microparticles have the potential of being used as a sustained release system of IND.

Experimental Study of Citri Reticulatae Viride Pericarpium extract on the Cerebral Hemodynamics in Rats (청피가 뇌혈류역학에 미치는 실험적 연구)

  • Lee Geum Soo;Jeong Hyun Woo;Lee Won Suk
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.16 no.1
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    • pp.104-110
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    • 2002
  • Citri Reticulatae Viride Pericarpium extract(CRVP) have been used in oriental medicine for many centuries as a therapeutic agent for Soothing the liver and regulating the circulation of qi(疏肝理氣), and promoting digestion and removing stagnated food(消積化滯). The effects of CRVP on the vascular system is not known. The purpose of this Study was to investigate the effects of CRVP on the pial arterial diameter and regional cerebral blood flow(rCBF) in normal rats and ischemic cerebrovascular pathologic model rats. The changes in rCBF was determinated by Laser-Doppler Flowmetry(LDF), and the changes in pial arterial diameter were determinated by video microscopy methods and video analyzer. The results were as follows ; 1. Pial arterial diameter was significantly increased by CRVP in a dose-dependent manner. 2. Pretreatment with L-NNA significantly inhibited CRVP induced increased rCBF and pial arterial diameter. 3. Both the methylene chloride fraction and the hexane fraction of CRVP dose-dependently improved the altered cerebral hemodynamics of cerebral ischemic animal by increasing rCBF. 4. Pretreatment with L-NNA and indomethacin significantly inhibited CRVP(MC) induced increased rCBF. 5. Pretreatment with L-NNA and indomethacin significantly inhibited CRVP(hexane) induced increased rCBF. 6. Pretreatment with CRVP maredly stabilized the changes rCBF and pial arterial diameter during the period of cerebral reperusion. In conclusion, CRVP causes a diverse response of rCBF and pial arterial diameter, and CRVP dose-dependently improved the altered cerebral hemodynamics of cerebral ischemic animal by increasing rCBF and pial arterial diameter. These results suggest that the improvement of cerebral hemodynamics is also mediated by nitric oxide synthase and cyclooxygenase.

Effects of Chlorpyrifos on the Production of Splenic Th Cytokines (비장세포의 Th cytokine 생산에 있어서 chlorpyrifos의 영향)

  • 채병숙
    • Environmental Analysis Health and Toxicology
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    • v.17 no.4
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    • pp.325-332
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    • 2002
  • A helper T(Th)1-mediated response is known to enhance cell -mediated immunity, while a Th2-mediated response is associated with the humoral immunity that if elevated IgE levels and eosinophilia. Prostaglandin (PG)E$_2$results in the decreased capability of Iymphocytes to produce Thl cytokines, with a shift toward a Th2 cytokine response. Chlorpyrifos (CPF) has been reported to impair the blastogenesis and response of T Iymphocytes. CPF also induces delayed febrile effects, which results from the activation of COX -PGE$_2$pathway. The purpose of this study is to determine the effort of CPF on the in vitro production of Th cytokines and the role of PGE$_2$on the CPF-induced production of Th cytokines. Splenocytes obtained from male BALB/c mice were pretreated with CPF(0.1, 1, 10 and 100$\mu$M) in the presence of absence of indomethacin or PGE$_2$for 12 h and then were incubated with concanavalin (Con) A for 48 h. These results showed that CPF remarkedly reduced the production of splenic interleukin (IL)-2 and interferon (IFN)-γ in a dose-dependent manner. CPF significantly increased the splenic IL-4 production at low doses (0.1 and 1$\mu$M) but did not affect at high doses (10 and 100 $\mu$M). Indomethacin reduced the CPF-decreased production of IL-2 and IFN-γ in a dose -dependent manner and significantly attenuated the production of IL-4 increased by CPF 0.1 $\mu$M. High dose of CPF significantly reduced the PGE$_2$-decreased production of IL-2 and IFN-γ, while the PGE$_2$- induced production of IL-4 was significantly enhanced by CPF 1 $\mu$M. These findings suggest that CPF nay down-regulate the immune response of Th 1 type by the suppressed production of IL-2 and IFN-γ, with a shift toward a Th2 cytokine response. The CPF-decreased production of Thl cytokines may not be mediated by endogenous PGE$_2$. Also, CPF may attenuate the exogenous PGE$_2$-decreased Th 1 immune response in a dose--dependent manner but may affect dose-independently the PGE$_2$-induced Th2 immune response.

Effects of Loop Diuretics on Guanylate Cyclase in Rat Medullary Thick Ascending limb of Henle's Loop (흰쥐 헨레고리 수질 비후상행각의 Guanylate Cyclase에 대한 고효능 이뇨제들의 영향)

  • Lee, Seok-Yong;Ro, Kyung-Sik;Kim, Ok-Nyu;Lee, Sang-Bok;Cho, Kyu-Chul
    • The Korean Journal of Pharmacology
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    • v.25 no.1
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    • pp.59-66
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    • 1989
  • To determine the relation between cGMP and ion reabsorption in rat medullary thick ascending limb of Henle's loop (mTALH) the effects of loop diuretics, furosemide and ethacrynic acid, on the guanylate cyclase of rat mTALH were investigated. The interactions between loop diuretics and cyclooxygenase inhibitors, aspirin and indomethacin, on guanylate cyclase of rat mTALH were also investigated. Furosemide and ethacrynic acid increased guanylate cyclase activity and these effects were not inhibited by aspirin or indomethacin. Arachidonic acid potentiated the stimulatory effect of furosemide on guanylate cyclase. These results suggest that furosemide and ethacrynic acid activate guanylate cyclase directly, and in addition, furosemide affects indirectly via prostaglandin. The reabsorption of sodium chloride may be, at least partially, controlled by cGMP in mTALH.

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The Relaxant Activity of Safranal in Isolated Rat Aortas is Mediated Predominantly via an Endothelium-Independent Mechanism - Vasodilatory mechanism of safranal -

  • Razavi, Bibi Marjan;Amanloo, Mojtaba Alipoor;Imenshahidi, Mohsen;Hosseinzadeh, Hossein
    • Journal of Pharmacopuncture
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    • v.19 no.4
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    • pp.329-335
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    • 2016
  • Objectives: Safranal is a pharmacologically active component of saffron and is responsible for the unique aroma of saffron. The hypotensive effect of safranal has been shown in previous studies. This study evaluates the mechanism for the vasodilatory effects induced by safranal on isolated rat aortas. Methods: To study the vasodilatory effects of safranal (0.2, 0.4 and 0.8 mM), we contracted isolated rat thoracic aorta rings by using $10^{-6}-M$ phenylephrine (PE) or 80-mM KCl. Dimethyl sulfoxide (DMSO) was used as a control. The vasodilatory effect of safranal was also evaluated both on intact and denuded endothelium aortic rings. Furthermore, to study the role of nitric oxide and prostacyclin in the relaxation induced by safranal, we incubated the aortic rings by using L-NAME ($10^{-6}M$) or indomethacin ($10^{-5}M$), each for 20 minutes. Results: Safranal induced relaxation in endothelium-intact aortic rings precontracted by using PE or KCl in a concentration-dependent manner, with a maximum relaxation of more than 100%. The relaxant activity of safranal was not eliminated by incubating the aortic rings with L-NAME ($EC_{50}=0.29$ vs. $EC_{50}=0.43$) or with indomethacin ($EC_{50}=0.29$ vs. $EC_{50}=0.35$), where $EC_{50}$ is the half maximal effective concentration. Also, the vasodilatory activity of safranal was not modified by endothelial removal. Conclusion: This study indicated that relaxant activity of safranal is mediated predominantly through an endothelium-independent mechanism.