• Journal of Pharmaceutical Investigation
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• v.32 no.4
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• pp.313-319
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• 2002

Rat skin permeation of various nonsteroidal antiinflammatory drugs (NSAIDs) was investigated in vitro using Franz diffusion cell at $37^{\circ}C$. The effect of various skin permeation enhancers was also observed as a preliminary study of developing transdermal delivery systems of NSAIDs. Lipophilicity of NSAIDs was determined from thε partition coefficient (log P) in 1-octanol/water and 1-octanol/IPB mutual-saturated solutions. The solubility was determined in water, isotonic phosphate buffer (IPB), and propylene glycol (PG) at $37^{\circ}C$. The rat skin permeation rate of acetaminophen, piroxicam, and aceclofenac was almost negligible, although they were saturated in PG. Addition of 1 % permeation enhancer increased the permeation rate of ketoprofen, ketorolac, and diclofenac. However, the skin permeation rate of ibuprofen did not increase with the addition of various enhancers. Among the permeation enhancers testεd, oleic acid was the most effective for various NSAIDs. Based on the daily dose, lipophilicity, and the skin permeation ratε achieved in this study, ketoprofen and ketorolac seem to be the most promising drug candidates for transdermal delivery systems, especially when formulated with unsaturated fatty acids, such as oleic acid.

• YAKHAK HOEJI
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• v.48 no.6
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• pp.317-322
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• 2004

The use of nonsteroidal anti-inflammatory drugs (NSAIDs) is limited by their ability to induce gastrointestinal injury. It has been shown that nitric oxide (NO), similar to pro staglandins (PGs), appears to play an important role in gastric mucosal defence. We hypothesized that NSAIDs contained NO group would be less acutely toxic to the gastric mucosa, but would not interfere with their ability to suppress inflammatory process in rats. We have compared the ulcerogenic and anti-inflammatory effect of CW-501029 (NO-NSAIDs), CW-501027 (NSAIDs) and indomethacin. Both did not change mean blood pressure and heart rates, indicating that they had no side effect on cardiovascular system. We found that CW-501029 increased nitrite/nitrate levels without changing of blood pressure and heart rates. We suggest that it may help gastric mucosal blood flow, the which helps reducing the discomfort in astrointestinal system. Carrageenan-induced PGE2 increase was reduced in a similar tendency when compared CW-501027 or CW-501027 with control in back exudate of rats, but CW-501029 less reduced PGE2 than CW-502027 or indomethacin in gastric tissues. CW-501027 or CW-501029 reduced platelet aggregation. From these results we suggest that CW-501029 may improve the side effect by reduction of short-term gastric injury and less inhibition of PGs synthesis.

• IMMUNE NETWORK
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• v.10 no.3
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• pp.92-98
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• 2010

Background: Nonsteroidal anti-inflammatory drugs (NSAIDs) are widely used to relieve pain, reduce fever and inhibit inflammation. NSAIDs function mainly through inhibition of cyclooxygenase (COX). Growing evidence suggests that NSAIDs also have immunomodulatory effects on T and B cells. Here we examined the effects of NSAIDs on the antigen presenting function of dendritic cells (DCs). Methods: DCs were cultured in the presence of aspirin or ibuprofen, and then allowed to phagocytose biodegradable microspheres containing ovalbumin (OVA). After washing and fixing, the efficacy of OVA peptide presentation by DCs was evaluated using OVA-specific CD8 and CD4 T cells. Results: Aspirin and ibuprofen at high concentrations inhibited both MHC class I and class II-restricted presentation of OVA in DCs. In addition, the DCs generated in the presence of low concentrations of the drugs exhibit a profoundly suppressed capability to present MHC-restricted antigens. Aspirin and ibuprofen did not inhibit the phagocytic activity of DCs, the expression level of total MHC molecules and co-stimulatory molecules on DCs. Ibuprofen rather increased the expression level of total MHC molecules and co-stimulatory molecules on DCs. Conclusion: These results demonstrate that aspirin and ibuprofen inhibit the intracellular processing event of the phagocytosed antigen, and further suggest that prolonged administration of NSAIDs in high doses may impair the capability of DCs to present antigens in asiociation with MHC molecules.

• Maxillofacial Plastic and Reconstructive Surgery
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• v.31 no.6
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• pp.505-509
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• 2009

Purpose: To evaluate the properties of antibiotic and NSAIDs administration before extract of the impacted mandibular third molar. Materials & Methods: No patient showed any sign of pain, inflammation, or swelling at the time of removal. A group of 50 patients was classified in Group 1(preemptive and oral medication was carried out for 3 days postoperatively, N=23) and Group 2(oral medication was carried out for 3 days postoperatively, N=27) subgroups. Clinical and radiologic factors were recorded for each case, and the rationale for assigning the patients to the groups was strictly random. The surgical technique was the same in all cases, and the follow-up period was 1 week. Parameters that were evaluated were infection, swelling, pain and differences in mouth opening. Results: We could not find any significant difference between the 2 groups regarding the evaluated parameters. Conclusion: The results of our study show that antibiotic and NSAIDs administration before the removal of lower third molars does not contribute to a decrease infection, swelling, pain or increase mouth opening. Therefore antibiotic and NSAIDs administration before the removal of lower third molars is not recommended for routine use.

• Journal of The Korean Society of Integrative Medicine
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• v.8 no.4
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• pp.79-92
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• 2020

Purpose : The purpose of this study was to evaluate the prescription pattern of NSAIDs and GPAs in the arthritis patients over 65 years old to prevent the GI adverse events. Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most commonly used agents to treat arthritis, can cause gastrointestinal (GI) adverse effects. Recent guidelines recommend that moderate risk patients who have one or two risk factors, should be prescribed either combination of non-selective NSAID (nsNSAIDs) and gastroprotective agent (GPAs) or selective NSAID alone. Methods : Study population was National Patient Sample of 2011. Number of drugs used were 138 for NSAIDs and 21 for GPAs. Chi-square test was used to compare prescribing patterns. Results : The appropriate prescription rate follows the guideline was 11.2%: co-prescription with nsNSAID and proton pump inhibitor (PPI) or misoprostol was 1.6% and selective NSAID alone was 9.6%. Inappropriate prescription rates were as follows: co-prescription with nsNSAID and Histamine-2 receptor antagonist (H2RA) or antiacid was 53.8% and nsNSAID alone was 35.0%. The appropriate prescription rate among the types of medical institute was 54.4% in tertiary hospital, 31.2% in secondary hospital, and 6.0% in primary hospital. The appropriate prescription rate among the regions was 19.4%, highest in Seoul and 4.2%, lowest in Jeju. The appropriate prescription rate among the medical departments was as follow: 12.2% in orthopaedic surgery, 11.0% in internal medicine, and 7.7% in other departments. Conclusion : This finding suggests the needs to revise the national medical insurance imbursement policy, provide continuing medical education about the guideline of medical doctors.

• Archives of Pharmacal Research
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• v.17 no.5
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• pp.304-308
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• 1994

Among the new series of phenylacetamides, one of capsaicin derivatives, KR-25018 was found to have a very potent analgesic activity. Thus, the phamacological properties of KR-25018 were compared with those of morphine, capsaicin, and nonsteroidal antiinflammatory drugs (NSAIDs). The analgesic activities were evaluated in several animal models, using different stimuli, such as phenylbenzoquinone(PBQ)-induced weithing test, tail-filck test in mice and adjuvant arthritic flexion test in rat. The relationship of phamacological properties of KR-25018 to that of centrally acting opioids was assessed by the blocking test using naloxone. The analgesic potency of the KR-25018 $(MPED_{50}=0.89{\;}p.o.{\;}in{\;}PBQ-induced{\;}weithing{\;}test, {\;}MPED_{50}$=0.61$ s.c. in tail-flick test in mice0, with different action mechanism from morphine and NSAIDs, was comparable to that of morphine.

• Journal of Pharmaceutical Investigation
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• v.26 no.3
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• pp.155-168
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• 1996

The active site of cyclooxygenase was modeled by complementary receptor-cavity mapping procedure using 3D structures of the non-steroidal antiinflammatory drugs (NSAIDs). A total of 50 NSAIDs were chosen as data ligands which compete the same site on the enzyme. Partial atomic charges were estimated, and the energetic differences for various conformations were calculated so as to meet the need for a most efficient overlapping of the probably-equivalent functional groups of the ligand molecules. The structure activity relationships of the NSAIDs, if available, were fully considered throughout the modeling. The overall shape of the model obtained is similar to a boot-without-bottom. Most of inner surface of the cavity appeared as hydrophobic; two polar counterparts except the carboxyl-binding position were found. By this model, some clear explanations could be given on the experimental observations which were not satisfiably understood yet.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.240.1-240.1
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• 2003

Nonsteriodal antiinflammatory drugs(NSAIDs) are widely used to treat pain. fever, and inflammatory conditions including osteoarthritis. However, gastrointestinal (GI) and renal toxicity were related to common NSAIDs limits their usefulness because NSAIDs inhibit not only COX-2 associated with anti-inflammatory activity. but also COX-1 accompanied with side effects in the stomach and kidney. (omitted)

• Journal of Digestive Cancer Research
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• v.8 no.2
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• pp.77-80
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• 2020

Gastric cancer is one of the leading causes of cancer-related deaths worldwide. The increased expression of cyclooxygenase (COX)-2 has been implicated in the development and progression of gastric cancers. A number of recent studies have been published evaluating the chemopreventive effect of aspirin and non steroidal anti inflammatory drungs (NSAIDs) against gastric cancer. Aspirin and NSAIDs use may reduce the risk of gastric cancer incidence and death, whereas other studies have reported contradictory results. Therefore, further study should be needed to clarify the role of aspirin and NSAIDs in the chemoprevention of gastric cancer.

• YAKHAK HOEJI
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• v.44 no.6
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• pp.494-498
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• 2000

Noble 7,7'-substituted (or unsubstituted) 4-oxo-1,1',2,2'-dibenzothiazine-3,3'-dicarboxylic acid methyl ester 1,1,1',1'-tetraoxide 3,4'-yl ethers 2a-h were synthesized through the dehydration of 7-substituted (or unsubstituted) 4-hydroxy-1,2-benzothiazine-3-carboxylic acid methyl ester 1,1-dioxides 1a-h using silver(I) oxide for the development of new nonsteroidal antiinflammatory drugs (NSAIDs). Optimal reaction was proceeded through stirring of distilled acetone using 100 mol% of silver(I) oxide at room temperature for 24-68 hrs.