• Journal of Pharmaceutical Investigation
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• 제13권1호
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• pp.10-22
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• 1983

The interactions of ${\alpha}-cyclodextrin({\alpha}-CyD)$ and ${\beta}-cyclodextrin({\beta}-CyD)$ with several non-steroidal antiinflammatory drugs were studied on the effects of ${\alpha}-$ and ${\beta}-CyD$ on the solubility of the drugs in aqueous medium. Indoprofen, niflumic acid, alclofenac, and naproxen were chosen as representatives of antiinflammatory drugs. The solubility of all drugs studied increased with the addition of ${\beta}-CyD$, while not with glucose or ${\alpha}-CyD$. The increase of the solubility with ${\beta}-CyD$ was considered due mainly to the formation of inclusion complexes between ${\beta}-CyD$ and drugs. From the solubility data, the apparent stability constants K of the complex could be calculated. Ultraviolet absorption and circular dichroism confirmed the inclusion of indoprofen, niflumic acid and naproxen with ${\beta}-CyD$ in the molar ratio of 1 : 1. Inclusion complexes in solid powder form were obtained by the freeze-drying method and the inclusion formation was confirmed again by infrared, diffential thermal analysis, and X-ray diffraction measurements.

• 생약학회지
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• 제17권3호
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• pp.232-241
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• 1986

The whole plants of Prunella vulgaris (Labiatae) and Thesium chinense (Santalaceae) are used as Hakocho(夏枯草) in the market in Korea. In oriental medicine, these herb drugs are prescribed as a diuretic or antiinflammatory drugs. In order to investigate the efficacy of the plants, the extracts were bioassayed for antiinflammatory action. The water extracts of Prunella Herba and Thesii Herba showed remarkable anti-carrageenin effect and significant inhibition of the swellings in adjuvant arthritis in rats. However, the extracts did not show any inhibition of leucocyte emigration in CMC pouch in rats.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.276.2-276.2
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• 2003

Simultaneous enantioseparation of nine racemic non-steroidal antiinflammatory drugs (NSAIDs) for their accurate chiral discrimination was achieved by cyclodextrin (CO) modified capillary electrophoresis in the normal polarity (NP) mode and in the reversed polarity (RP) mode. The NP mode employed neutral tri-O-methyl-${\beta}$-cyclodextrin (TM${\beta}$CD) as a selector dissolved in MES buffer (PH 6.0). (omitted)

• 약학회지
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• 제26권2호
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• pp.97-103
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• 1982

This paper presents anti-inflammatory effects of nonsteroidal anti-inflammatory drugs and their copper complexes, and the change of content of copper in serum, liver, brain and edema foot induced by 1% carrageenan in rats, and also investigation of stomach hemorrhage. The results were as follows. 1. The content of copper decreased in liver and brain, however, the concentration of copper significantly increased in serum and edema site after carrageenan injection in rats. 2. The content of copper in serum and edema site was decreased after administration of anti-inflammatory drugs. 3. Edema inhibition rate of aspirin was, higher than that of copper (II) aspirinate, but edema inhibition rate of copper complex of naproxen was markedly higher than that of naproxen. 4. Hemorrhage of stomach of copper salicylate was higher than that of sodium salicylate, but hemorrhage of stomach of sodium naproxen was higher than that of copper naproxen.

• Natural Product Sciences
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• 제2권1호
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• pp.1-8
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• 1996

Flavonoids are widely distributed polyphenol compounds in plant kingdom and known to possess varieties of biological/pharmacological activities in vitro and in vivo. A search for antiinflammatory/immunoregulatory flavonoids as potential therapeutic agents has been continued, since serious side effects of currently used nonsteroidal and steroidal antiinflammatory drugs limit their long term uses for the inflammatory disorders. In this reserch, various flavonids were isolated and tested for their in vivo antiinflammatory activity and in vitro inhibitory activity of lymphocyte proliferation. Using a mouse ear edema assay, it was found that certain flavones/flavonols possess mild antiinflammatory activity and a C-2,3-double bond might be essential. Isoflavones were less active. These flavonoids inhibited in vitro lymphocyte proliferation, relatively specific for T-cell proliferation $(IC_{50}=1-10\;{\mu}M)$ and the inhibition was reversible. We have also tested several biflavonoid derivatives, since we recently found that biflavones were phospholipase $A_2$ inhibitors. It was demonstrated that biflavones such as ochnaflavone and ginkgetin inhibited lymphocyte proliferation induced by both concanavaline A and lipopolysaccharide. The inhibition was irreversible in contrast to that of flavones/flavonols. And antiinflammatory activity of biflavonoids are discussed.

• Archives of Pharmacal Research
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• 제24권2호
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• pp.150-158
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• 2001

The activity of nonsteroidal antiinflammatory drugs (NSAIDs) in rheumatoid arthritis is not only due to the inhibition of the production of prostaglandins, which can even have beneficial immunosuppressive effects in chronic inflammatory processes. Since we speculated that these drugs could also act by protecting endogenous proteins against denaturation, we evaluated their effect on heat-induced denaturation human serum albumin (HSA) in comparison with several fatty acids which are known to be potent stabilizers of this protein. By the Mizushimas assay and a recently developed HPLC assays we observed that NSAIDs were slightly less active [$EC_{50}~10^{-5}-10^{-4}$ M] than FA and that the HPLC method was less sensitive but more selective than the turbidimetric assay, i.e. it was capable of distinguishing true antiaggregant agents like FA and NSAIDs from substances capable of inhibiting the precipitation of denatured protein aggregates. In conclusion, this survey could be useful for the development of more effective agents in protein condensation diseases like rheumatic disorders, cataract and Alzheimers disease.

• Journal of Pharmaceutical Investigation
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• 제24권1호
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• pp.17-24
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• 1994

The antiinflammatory and antirheumatic activities of a 3% ketoprofen gel (ID-GEL) were evaluated using carrageenan-induced paw edema method and adjuvant-induced arthritis method, respectively, after its transdermal administration of 50 mg on rat paws in reference to existing transdermal preparations containing 3% ketoprofen and other nonsteroidal antiinflammatory drugs (NSAIDs). The % inhibition of carrageenan-induced edema by ID-GEL was 56.2-65.0%, close to the maximum inhibition obtainable with this model, while the % inhibition by existing 3% ketoprofen gels and other NSAID transdermal preparations were 33.8-47.7% and 18.7-29.2%, respectively. ID-GEL had a pronounced antirheumatic activity in both preventive and curative studies with adjuvant-induced arthritis in rats in respect with the inhibition of edema, arthritis score and weight gain, in reference to existing 3% ketoprofen gel.

• 생약학회지
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• 제32권4호통권127호
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• pp.257-268
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• 2001

Analgesic and antiinflammatory activities of several herbal medicines were investigated in order to develop the antiinflammatory drugs from oriental herbal medicines. 80% Ethanol extracts of Ephedra sinica, Chaenoleles sinensis, Asiasarum siboldi, Nelumbo nucifera, Scolopendra subspinipes mutians, Evodia officinalis, Aremarrhenae asphodeloides, Bufo bufo gargarizans, Gardenia jasminoides, Piper longum, Carthamus tinctorius, Piperus nigrum, Magnolia officinalis and Siegesbeckia glabrescens showed significant inhibitory effects on hyaluronidase, trypsin, and albumin denaturation in vitro. They also decreased the acetic acid-induced pain and vascular permeability induced by histamine in mice.

• 농촌의학ㆍ지역보건
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• 제12권1호
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• pp.102-110
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• 1987

One of the familiar medical facility that most people reach easily in Korea is the drug store. In Korea, it is possible to purchase all kinds of common drugs without physician's prescriptions, which caused some problems. In other words, such treatment without professional supervision has led to medical, social and economical problems. In view of the above, this study is aimed at revealing the actual status of long-term use of drugs in some urban residents. Long-term use of drugs is operationally defined as using certain drugs at least once a week for more than 3 months. This survey took the residents of Guro 6-Dong where was one of the target areas for Community Health Development Project managed by Korea University as a target population. A sample of 1,517 residents was selected by the multistage sampling method. The interview was conducted on September 21st and 22nd in 1985. The object of this study was to compare the result with that of the rural area which was obtained by the same method, tools and research team, prior to this study in 1984. The results were as follows; 1) The age-standardization of the study showed that 97 per 1,000 urban residents were actually on long-term drug use. The prevalance of long-term use is high in accordance with aging and low with education level. 2) Out of 1,000 urban samples the most popular item involved in the long-term drug use was antipyretic-analgesic-antiinflammatory drug (26), and next in order was vitamin (23), antibiotics (13), digestives (10) and antacids (7). In the rural samples as for compare, that was antipyretic-analgesic-antiinflammatory drug (100), antacids (36), digestives (23), adrenocortical hormones (12) etc. 3) With antipyrctic-analgesic-antiinflammatory drugs, 50% of the urban samples were taking for more than a year, whereas such were 82.7% of the rural samples. Using such a high percentage of antipyretic-analgesic-antiinflamatory drugs in the rural residents is probably due to the high prevalence rate of musculo-skeletal diseases. 4) The urban long-term drug users of antipyretic-analgesic-antiinflammatory drugs were influenced mostly by the mass media (43.6%), next in order was pharmacist (35.9%) and physician (10.3%). Comparing with the result from the rural areas the role of mass media was much more influencial in the urban areas. 60% of them consulted with pharmacists, 14.3% with physicians and 25.7% had no history of consultation in the urban samples. 5) Considering the incidence of knowing the possible side-effects of each drug, 28.2% of the urban residents had no recognition about side-effects prior to use antipyretic-analgesic-antiinflammatory drugs. In the rural residents, 29.67o had no knowledge about the side-effects before using the drug. 6) For the solution of the above problems, it is necessary to limit the advertisement of some drugs by the parmaceutical company. And therapeutic drugs which may bring on side effects in case of long-term use should not be sold at drug stores without physician's prescription.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.282.2-283
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• 2003

The carboxylated acidic non-steroidal antiinflammatory drugs (NSAIDs) constitute the principal class of agents for controlling the pain and inflammation of the rheumatic diseases. It is mostly administered as a racemic mixture like most other drugs with asymmetric carbon atoms. However enantiomers of many racemic drug substances have been shown to posses different pharmacological toxicological properties. (omitted)