• Journal of Pharmaceutical Investigation
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• v.29 no.1
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• pp.29-36
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• 1999

Aceclofenac is an non-steroidal antiinflammatory drug which has been used in the treatment of rheumatoidal rthritis and osteo-arthritis. In order to decrease the gastric ulcerogenic effects and contol the plasma level of aceclofenac, we have developed the transdermal delivery system of aceclofenac plaster, which were formulated employing matrix polymers of acrylates and penetration-enhancers such as $Lauroglycol^{\circledR}$, $Transcutol^{\circledR}$, oleic acid and linoleic acid. Using Franz diffusion cells mounted with a rat skin, transdermal penetration characteristics of the formulations were evaluated by the HPLC assay of aceclofenac and diclofenac, an active metabolite, in the receptor compartment of pH 7.2 phosphate buffered solution. Skin penetration was increased when the content of aceclofenac increased, showing the flux $(J,\;{\mu}g/cm^2/hr)$ of 0.37 and 2.50 for 2% and 6.75% of the content, respectively. The flux$(J,\;{\mu}g/cm^2/hr)$ from plasters made of $Durotak^{\circledR}$ 87-2074, $Durotak^{\circledR}$ 87-2510 and $Durotak^{\circledR}$ 87-2097 were 2.50, 2.77 and 4.39, respectively. $Durotak^{\circledR}$ 87-2074 showed the lowest penetration due to the carboxylic acid group in the polymer, which might form a strong hydrogen bonding with a secondary amine of aceclofenac. Although both $Durotak^{\circledR}$ 87-2510 and $Durotak^{\circledR}$ 87-2097 are amine-resistant adhesives, $Durotak^{\circledR}$ 872510 showed lower penetration than $Durotak^{\circledR}$ 87-2097 because of the hydroxyl group in $Durotak^{\circledR}$ 87-2510, which might form a weak hydrogen bonding with aceclofenac. These results reveal that the functional group in acrylic polymers would greatly affect the release of aceclofenac from the matrix, which is the rate-limiting step in the penetration of aceclofenac through rat skins. The penetration of aceclofenac from plasters using different penetration-enhancers increased in the following order: Transcutol < linoleic acid < oleic acid. And the flux from the plasters containing oleic acid as a penetrationenhancer was 2.22 times greater than that of creams, which suggest that a newly deveolped aceclofenac plaster could be used in the treatment of rheumatoidal arthritis and osteo-arthritis as an advanced transdermal delivery system.

• Korean Journal of Food Science and Technology
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• v.31 no.3
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• pp.764-770
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• 1999

Antimicrobial activities were assayed through the hot-water extracts from 41 species of medicinal plants against Helicobacter pylori which is known as the ulcerogenic phathogen. Opuntia ficus-indica, Houttuynia cordata, Sinomenium acutum, and Coptis japonica showed the MIC at the concentrations less than 100 ppm, Pulsatilla koreana, Forsythia koreana, Rheum undulatum, and Perilla frutescens less than 200 ppm, Belamcanda chinensis, Arctium lappa, Cassia tora, Citrus tachibana, Siegesbeckia orientalis, and Caesalpinia sappan less than 300 ppm by the 2-fold dilution method. In disc method only three of them were confirmed to have antimicrobial activities which were increased in the order Perilla frutescens, Coptis japonica, Caesalpinia sappan. Three extracts were partitioned with chloroform, ethyl acetate and butanol in sequence and examined for the activity to inhibit H. pylori. The major ativities were observed in ethyl acetate fraction of Caesalpinia sappan, butanol fraction of Perilla frutescens, butanol and chloroform fraction of Coptis japonica. The partitioned fractions were found to have increased antimicrobial activities in all extracts. The experiments in which the extracts were added into urea R broth containing the crude urease derived from H. pylori resulted in the increase of pH and optical density at 560 nm to 8.15 and 1.7 respectively. Urease activity of H. pylori was inhibited over 80% by Caesalpinia sappan, Perilla frutescens, and Coptis japonica, of which Caesalpinia sappan suppressed up to 95%.

• Korean Journal of Food Science and Technology
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• v.35 no.6
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• pp.1182-1187
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• 2003

This study was performed to evaluate the potentiality of Reynoutria elliptica Migo., being used as a folk remedy and a herb medicine for urethritis, cystitis, etc., on growth inhibition of Helicobacter pylori which is known as the ulcerogenic pathogen. The minimum inhibitory concentration (MIC) value of methanol extract from Reynoutria elliptica Migo, was determined to be 120 ppm for H. pylori and urease activity derived from H. pylori was inhibited over 80% by the extract at 2 mg/mL in urea broth. Among various solvent fraction of the methanol extract, the hexane fraction showed a significant inhibitory effect on the growth of H. pylori reducing both its growth and urease activity. Scanning and transmission electron micrographs of H. pylori treated with the methanol extract at 2 mg/mL for 3 hr showed that the cell walls and membranes were disrupted so that the cytoplasmic components were leaked from the body. These results suggest that Reynoutria elliptica Migo. possesses a therapeutic potential on the gastric disease caused by H. pylori.

• Journal of Physiology & Pathology in Korean Medicine
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• v.21 no.6
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• pp.1549-1554
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• 2007

To verify the effects of JAUN-1, which is a water-extracted herbal mixture, on gastroenteric disorders induced by 0.1 percent of iodoacetamide (IA) in rats. We divided four groups, $Na{\&quot;{\i}}ve$ + Distilled Water (DW), 0.1% IA + DW, 0.1% IA + Proton pump inhibitor (Lansoprazole, 5 mg/kg) and 0.1% IA + Herbal mixture (JAUN-1, 50mg/kg) and performed following experimental methods to confirm its advantageous effects against ulcerogenic stomach in rats induced by 0.1% IA; cell cytotoxicity, analysis of lesions score, Hematoxylin & Eosin (H&E) stain, RT-PCR for ${\beta}-actin$, COX-1 and COX-2 and evaluation of intestinal prokinetic activity. No cytotoxicity was elucidated at the concentration of 1, 5, 10, 50, 100, $500\;{\mu}g/ml$ and 1mg/ml JAUN-1 through MTT Assay using by human stomach epithelial AGS cells, respectively. In addition, the JAUN-1 treated group and the lansoprazole treated group significantly decreased in lesions score compared to the DW treated group in the gastritis induced rat model, and results of immunohistochemistry by H&E staining showed that histological recovery in Proton Pump Inhibitor (PPI) and JAUN-1 treated groups rather than the DW administrated group. Another outcome was that ${\beta}-actin$ relative COX-2 expression level was significantly promoted in the DW treated group while ${\beta}-actin$ relative COX-1 expression level was no meaningful change in this rat model. Finally, intestinal prokinetic activity was recovered from low level of prokinetic activity due to 0.1% IA induced gastritis to the similar level of Normal group. These results suggested that JAUN-1 may have beneficial effects against 0.1% IA-induced gastritis rat model through decreasing lesions score, histological recovery, ${\beta}-actin$ relative COX-1, 2 expression level and prokinetic activity.

• Archives of Pharmacal Research
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• v.29 no.7
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• pp.591-597
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• 2006

Aerial parts of Artemisia asiatica (Compositae) have been traditionally used as an oriental medicine for the treatment of inflammatory and ulcerogenic diseases. In the present study, artemisolide was isolated as a nuclear factor $(NF)-{\kappa}B$ inhibitor from A. asiatica by activity-guided fractionation. Artemisolide inhibited $NF-{\kappa}B$ transcriptional activity in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7 with an $IC_{50}$ value of $5.8\;{\mu}M$. The compound was also effective in blocking $NF-{\kappa}B$ transcriptional activities elicited by the expression vector encoding the $NF-{\kappa}B$ p65 or p50 subunits bypassing the inhibitory kB degradation signaling $NF-{\kappa}B$ activation. The macrophages markedly increased their $PGE_2$ and NO production upon exposure to LPS alone. Artemisolide inhibited LPS-induced $PGE_2$ and NO production with $IC_{50}$ values of $8.7\;{\mu}M$ and $6.4\;{\mu}M$, respectively, but also suppressed LPS-induced synthesis of cyclooxygenase (COX)-2 or inducible NO synthase (iNOS). Taken together, artemisolide is a $NF-{\kappa}B$ inhibitor that attenuates LPS-induced production of $PGE_2$ or NO via down-regulation of COX-2 or iNOS expression in macrophages RAW 264.7. Therefore, artemisolide could represent and provide the anti-inflammatory principle associated with the traditional medicine, A. asiatica.