• Polymer(Korea)
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• v.36 no.6
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• pp.699-704
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• 2012

Double-layered polymeric carrier was designed for release control of hydrophilic drug in oral administration. Biopolymeric chitosan and alginate were examined as polar absorbents, poly(D,L-lactide) as a hydrophobic shell, and theophylline and diclofenac sodium as loading drugs. The fabrication of the carriers was prepared in the form of double-layered microsphere for delayed and successively extended release, which consisted of outer shell of poly(D,L-lactide) and inner core of alginate or chitosan with drugs. Morphologies and drug-release behaviors of the carriers were investigated, which were influenced by a combination of polarity between carrier and drug. It was confirmed that the relative polarities of the carriers, the drugs, and the environmental pH affected significantly the drug-release property.

• Journal of Microbiology and Biotechnology
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• v.22 no.2
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• pp.274-282
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• 2012

The object of this study was to assess the efficacy of Polycan from Aureobasidium pullulans SM-2001, which is composed mostly of beta-1,3-1,6-glucan, on osteoarthritis (OA)-induced by anterior cruciate ligament transection and partial medial meniscectomy (ACLT&PMM). Three different dosages of Polycan (85, 42.5, and 21.25 mg/kg) were orally administered once a day for 84 days to male rats a week after ACLT&PMM surgery. Changes in the circumference and maximum extension angle of each knee, and in cartilage histopathology were assessed using Mankin scores 12 weeks after Polycan administration. In addition, cartilage proliferation was evaluated using bromodeoxyuridine (BrdU). As the result of ACLT&PMM, classic OA was induced with increases in maximum extension angles, edematous knees changes, and capsule thickness, as well as decreases in chondrocyte proliferation, cartilages degenerative changes, and loss of articular cartilage. However, these changes (except for capsule thickness) were markedly inhibited in all Polycan- and diclofenac sodium-treated groups compared with OA control. Although diclofenac sodium did not influence BrdU uptake, BrdU-immunoreactive cells were increased with all dosages of Polycan, which means that Polycan treatment induced proliferation of chondrocytes in the surface articular cartilage of the tibia and femur. The results obtained in this study suggest that 84 days of continuous oral treatment of three different dosages of Polycan led to lesser degrees of articular stiffness and histological cartilage damage compared with OA controls 91 days after OA inducement, suggesting that the optimal Polycan dosage to treat OA is 42.5 mg/kg based on the present study.

• The Korean Journal of Pain
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• v.34 no.3
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• pp.262-270
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• 2021

Background: Transient receptor potential vanilloid 1 (TRPV1) is a non-selective cation channel implicated in pain sensation in response to heat, protons, and capsaicin (CAPS). It is well established that TRPV1 is involved in mechanical allodynia. This study investigates the effect of Ononis spinosa (Fabaceae) in CAPS-induced mechanical allodynia and its mechanism of action. Methods: Mechanical allodynia was induced by the intraplantar (ipl) injection of 40 ㎍ CAPS into the left hind paw of male Wistar rats. Animals received an ipl injection of 100 ㎍ O. spinosa methanolic leaf extract or 2.5% diclofenac sodium 20 minutes before CAPS injection. Paw withdrawal threshold (PWT) was measured using von Frey filament 30, 90, and 150 minutes after CAPS injection. A molecular docking tool, AutoDock 4.2, was used to study the binding energies and intermolecular interactions between O. spinosa constituents and TRPV1 receptor. Results: The ipsilateral ipl injection of O. spinosa before CAPS injection increased PWT in rats at all time points. O. spinosa decreased mechanical allodynia by 5.35-fold compared to a 3.59-fold decrease produced by diclofenac sodium. The ipsilateral pretreatment with TRPV1 antagonist (300 ㎍ 4-[3-Chloro-2-pyridinyl]-N-[4-[1,1-dimethylethyl] phenyl]-1-piperazinecarboxamide [BCTC]) as well as the β2-adrenoreceptor antagonist (150 ㎍ butoxamine) attenuated the action of O. spinosa. Depending on molecular docking results, the activity of the extract could be attributed to the bindings of campesterol, stigmasterol, and ononin compounds to TRPV1. Conclusions: O. spinosa alleviated CAPS-induced mechanical allodynia through 2 mechanisms: the direct modulation of TRPV1 and the involvement of β2 adrenoreceptor signaling.

• Applied Chemistry for Engineering
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• v.5 no.3
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• pp.413-418
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• 1994

The synthetic steps of sodium(2-(2, 6-dichlorophenyl)amino)phenylacetate were reduced and increased the yield in each steps. The synthetic process was composed to four steps and 2, 6-dichloroaniline and per catalyst in three lots in 80% yield. The steps of acylation and Friedel-Craft reaction were simplified successfully. The final product, diclofenac was obtained in 97% yield by hydrolyzing 1-(2,6-dichlorophenyl)-2-indolinone which was gained in third step with Claisen-solution.

• Journal of Pharmaceutical Investigation
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• v.37 no.3
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• pp.187-192
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• 2007

A reversed phase HPLC analysis of atorvastatin (AS) standard solution was performed using diclofenac (DF) as internal standard. Column oven temperature, flow rate and the composition of the mobile phase were varied in order to determine a practical system setup using a C18 column and UV detector. Two C18 columns of different length were compared regarding their influence on the AS peak shape. Based on these preliminary experiments a validation study was performed utilizing a C18 column at $62^{\circ}C$ with a mobile phase consisting of sodium phosphate buffer (0.05 M, pH 4.0), methanol and acetonitrile (40:50:10, v/v/v). The detection limit for AS was $0.1{\mu}g/ml$ and inter- and intra-day calibration curves were linear over a concentration range of $0.2-50{\mu}g/ml$. Accuracy and precision were satisfactory in the AS concentration range of $0.5-50{\mu}g/ml$.

• Journal of the Korean Chemical Society
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• v.47 no.3
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• pp.237-240
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• 2003

A synthetic method for the title compounds (2a-o) was carried out. The title compounds (2a-o)were prepared by the condensation of various thioureas and maleic anhydride. Anti-inflammatory activities in vivo were evaluated and compared with standard drug diclofenac sodium. Some compounds showed moderate activity. The structures of all the new compounds were established on the basis of $^1H$ NMR and IR spectral data.

• Bulletin of the Korean Chemical Society
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• v.32 no.7
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• pp.2274-2278
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• 2011

Verapamil is a calcium channel blocker and is classified as a class IV anti-arrhythmic agent. It is used in the control of supra ventricular tachyarrhythmias, and in the management of classical and variant angina pectoris. It is also used in the treatment of hypertension and used as an important therapeutic agent for angina pectoris, ischemic heart disease, hypertension and hypertrophic cardiomyopathy. Verapamil commonly co-administered with NSAIDs (non-steroidal anti-inflammatory drugs) i.e. diclofenac sodium, flurbiprofen, Ibuprofen, mefanamic acid and meloxicam. A simple and rapid RP-HPLC method for simultaneous determination and quantification of verapamil and NSAIDs was developed and validated. The mobile phase constituted of acetonitrile: water (55:45) whose pH was adjusted at 2.7 and pumped at a flow rate of 2.0 mL $min^{-1}$ at 230 nm. The proposed method is simple, precise, accurate, low cost and least time consuming for the simultaneous determination of verapamil and NSAIDs which can be effectively applied for the analysis of human serum.

• Advances in Traditional Medicine
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• v.7 no.3
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• pp.274-279
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• 2007

The crude ethanol extract of leaves of Sonneratia caseolaris Linn. (Sonneratiaceae) was screened for its antinociceptive and antidiarrhoeal activities. The extract produced significant writhing inhibition in acetic acid induced writhing in mice at dose of 250 and 500 mg/kg body weight (P<0.01) comparable to the standard drug diclofenac sodium at the dose of 25 mg/kg of body weight. When tested for its antidiarrhoeal effects on castor oil induced diarrhea in mice, it increased mean latent period and decreased the frequency of defecation significantly at the dose of 500 mg/kg body weight (P < 0.05) comparable to the standard drug loperamide at the dose of 50 mg/kg of body weight. The overall results tend to suggest the antinociceptive and antidiarrhoeal activities of the extract.

• Advances in Traditional Medicine
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• v.7 no.3
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• pp.280-285
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• 2007

The methanol extract of leaves of Bruguiera gymnorrhiza (L.) Lam. (Rhizophoraceae) was screened for its antinociceptive and antidiarrhoeal activities. The extract produced significant inhibition in acetic acid-induced writhing in mice at dose of 250 and 500 mg/kg body weight (P < 0.001), comparable to the standard drug diclofenac sodium at the dose of 25 mg/kg of body weight (P < 0.001). When tested for its antidiarrhoeal effects on castor oil-induced diarrhea in mice, it increased mean latent period (P < 0.02) and decreased the frequency of defecation (P < 0.01) significantly at the dose of 500 mg/kg body weight, comparable to the standard drug loperamide at the dose of 50 mg/kg of body weight. The overall results tend to suggest the antinociceptive and antidiarrhoeal activities of the extract.

• Advances in Traditional Medicine
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• v.3 no.3
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• pp.123-128
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• 2003

Stephania hernandifolia belonging to the family Menispermaceae is the biggest storehouse of diphenylbisbenzylisoquinoline (DBBI) alkaloids. Exhaustive chemical processing of the bulb of S. hernandifolia by the application of modern separation techniques yielded a DBBI alkaloid which was identified as cycleanine using spectroscopic methods (UV, IR, $^1HNMR$. $^{13}CNMR$, Mass). Cycleanine showed significant anti-inflammatory activity against carrageenin induced paw oedema, comparable to that produced by diclofenac sodium, used as standard drug. It exhibited potent analgesic effects against chemical and thermal noxious stimuli. It was also found to possess anticonvulsive activity in the strychnine induced convulsion model.