• Polymer(Korea)
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• v.25 no.1
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• pp.108-114
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• 2001

Crosslinked poly(glycerol-co-malate)s were synthesized from L-malic acid in Krebs cycle and glycerol. The synthesized polymer was identified by FT-IR spectroscopy. Swelling degrees of the copolymer hydrogels were increased with an increase in pH of the aqueous solution. Hydrolytic behaviors of the crosslinked copolymers were investigated in various pH buffer solutions at 37${\circ}C$. The Hydrolysis of the copolymers proceeded faster with increasing pH of the aqueous solution. Releasing behaviors of the model drug such as diclofenac monosodium salt were also measured in various pH aqueous solutions at 37${\circ}C$. The release concentration of diclofenac monosodium salt from the hydrogel systems was increased with increasing pH. These facts indicate that the unreacted carboxyl and hydroxyl groups in the copolymers are greatly affected by pH in the conditions.

• The Korean Journal of Pain
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• v.32 no.4
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• pp.256-263
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• 2019

Background: Antinociceptive anti-inflammatory drugs have many adverse effects. The goal of this investigation is to study the probable anti-inflammatory and analgesic effects of verapamil and N-acetylcysteine (NAC) in experimental rats. Methods: Adult male Wistar rats were randomly divided into 4 groups in the antinociceptive study, each containing 6 rats; the normal control group, which received saline (1 mL/kg); the diclofenac group, which received diclofenac sodium (5 mg/kg); the NAC group, which received NAC (125 mg/kg); and the verapamil group, which received verapamil (8 mg/kg). In the anti-inflammatory study, 5 groups were used, the 4 previous groups with the addition of an edema control group, received saline and were subjected to formalin test. Hot plate latency time was recorded for antinociceptive evaluation. Paw edema thickness and biochemical parameters were recorded for anti-inflammatory evaluation. Results: Administration of NAC showed significant prolongation of hot plate latency time at 1 hour when compared to the control group while verapamil showed a significant prolongation of hot plate latency time at 1 and 2 hours when compared to the control group and NAC group values. Administration of NAC and verapamil significantly decreased paw edema thickness at 2, 4, and 8 hours when compared to edema control values. Regarding biochemical markers, NAC and verapamil significantly decreased serum nitric oxide synthase, C-reactive protein, and cyclooxygenase-2 levels compared to the edema control value. In accordance, a marked improvement of histopathological findings was observed with both drugs. Conclusions: NAC and verapamil have antinociceptive and anti-inflammatory effects comparable to diclofenac sodium.

• Biomolecules & Therapeutics
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• v.13 no.4
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• pp.246-250
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• 2005

In this study, we tried to investigate whether diclofenac, acetaminophen, nimesulide, acetylsalicylic acid and tumor necrosis factor-alpha (TNF-alpha) significantly affect mucin release from cultured airway goblet cells. Confluent primary hamster tracheal surface epithelial (HTSE) cells were metabolically radiolabeled with $^3H$-glucosamine for 24 hr and chased for 30 min or 24 hr in the presence of each agent to assess the effects on $^3H$-mucin release. The results were as follows: (1) TNF-alpha significantly increased mucin release from cultured HTSE cells during 24 hr of treatment period; (2) However, diclofenac, acetaminophen, nimesulide and acetylsalicylic acid did not affect mucin release, during 30 min of treatment period. Basically, this finding suggests that non-steroidal antiinflammatory drugs (NSAIDs) might not function as a mucoregulator in various inflammatory respiratory diseases showing mucus hypersecretion, although further studies are needed.

• Journal of Pharmaceutical Investigation
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• v.41 no.4
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• pp.211-215
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• 2011

The aim of this study was to develop a stable enteric coated diclofenac sodium (DFS) tablets using Aqua-Polish E without using a subcoat. DFS uncoated tablets were manufactured through the non direct compression process. AquaPolish E white aqueous coating dispersion was used as enteric coating material. This film forming polymer is a mixture of selected polymethacrylic/ethylacrylate copolymers. The stability of the obtained enteric coated tablets was evaluated according to ICH guidelines. No signs of disintegration or cracking was observed when they placed in 0.1N HCl solution (pH1.2), but they were completely disintegrated within 10 minutes when they placed in buffered solution at pH6.8. Dissolution test was also conducted by placing tablets in 0.1 N HCl for 2 hours and then 1 hour in phosphate buffer at pH 6.8. Less than 0.9 % of drug was released in the acidic phase and up to 97% in the basic medium. These findings suggest that aqueous enteric coating with AquaPolish E system is an easy and economical approach for preparing stable DFS enteric coat without the use of a subcoating layer.

• Korean Journal of Clinical Pharmacy
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• v.16 no.1
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• pp.52-56
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• 2006

Aceclofenac, a nonsteroidal antiinflammatory agent of a phenylacetic acid type, has been used for rheumatoid arthritis and osteoarthrits. Although the metabolic pathway of aceclofenc is relatively well-known in vitro, pharmacokinetic profiles of its three major or metabolites are still unclear in human. The present study was designed to investigate pharmacokinetic profiles of the metabolites of aceclofenac, and to evaluate the bioequivalence of the generic preparation of aceclofenac 100 mg tablet. Blood samples were serially collected for a period of 12 hours following a single oral administration of 100 mg aceclofenac in 20 healthy human volunteers. A simple protein precipitation with acetonitrile was employed to purify those substances from plasma. Aceclofenac, diclofenac, 4'-hydroxyaceclofenac and 4'-hydroxy-diclofenac in heparinized plasma were simultaneously measured with flufenamic acid, an internal standard, using HPLC coupled to a tandem mass spectrometer. Time courses of 4'-hydroxydiclofenac, diclofenac and aceclofenac plasma concentrations were clearly revealed, and the pharmacokinetic properties were analyzed. The 90% confidence intervals for the ratios of test/reference for log-transformed AUC and $C_{max}$ lie within 0.80-1.25.

• Journal of Korean Society of Water and Wastewater
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• v.27 no.1
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• pp.39-47
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• 2013

This study demonstrates the oxidative degradation of pharmaceutical compounds during ozonation of surface waters in Ulsan. Diclofenac, carbamazepine, bezafibrate, and ibuprofen were selected as surrogate pharmaceutical compounds, and ozonation experiments were performed using raw waters collected from the Sayeon Dam and the Hoeya Dam in Ulsan. Diclofenac and carbamazepine which have high reactivity with molecular ozone showed higher removal efficiencies than bezafibrate and ibuprofen during ozonation. The addition of tert-butanol, a hydroxyl radical scavenger, increased the removal efficiencies of diclofenac and carbamazepine by increasing the ozone exposure. However, the oxidation of bezafibrate and ibuprofen was inhibited by the presence of tert-butanol due to the suppression of the exposure to hydroxyl radical. The elimination of the selected pharmaceuticals could be successfully predicted by the kinetic model base on the $R_{ct}$ concept. Depending on the experimental condition, $R_{ct}$ values were determined to be $(1.54{\sim}3.32){\times}10^{-7}$ and $(1.19{\sim}3.04){\times}10^{-7}$ for the Sayeon Dam and the Hoeya Dam waters, respectively. Relatively high $R_{ct}$ values indicate that the conversion of $O_3$ into $^{\cdot}OH$ is more pronounced for surface waters in Ulsan compared to other water sources.

• Journal of Veterinary Clinics
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• v.30 no.3
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• pp.159-165
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• 2013

The present study was conducted to evaluate the efficacy of Cinnamomum cassia Blume (CC) extract on the repair of damaged cartilage in a rat model of osteoarthritis (OA) by anterior cruciate ligament transection (ACLT) and medial meniscus resection (MMx). Forty-eight rats were assigned to six groups (n = 8 per group): sham as negative control (NC), positive control (PC), diclofenac sodium (DS, 2 mg/kg), CC 25 mg/kg, CC 50 mg/kg and CC 100 mg/kg groups. Treatments were 12 weeks from 7 days after ACLT + MMx. Loss of cartilage and joint instability were significantly reduced in response to treatment with CC or DS compared to the PC (p < 0.05). CC significantly ameliorated cartilage degradation in a dose-dependent manner as assessed by histological findings (p < 0.01). A reduction in the severity of structural changes and a dose-dependent increase in Safranin-O staining intensity were observed in CC treatments, indicating that cartilage degradation was inhibited. Although DS did not affect the increase in active caspase-3 and cleaved poly(ADP-ribose) polymerase-induced apoptosis during the progression of OA, cells reactive to these apoptotic markers were decreased significantly by CC (p < 0.05). However, treatments with CC or DS did not influence the uptake of 5-bromo-2'-deoxyuridine. The findings suggest that CC can exert a chondroprotective action on OA through anti-inflammatory and anti-apoptotic properties.

• 대한예방의학회:학술대회논문집
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• 2001.10a
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• pp.302-304
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• 2001

• Korean Journal of Clinical Pharmacy
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• v.10 no.3
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• pp.140-144
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• 2000

Reofecoxib는 용량 의존적으로 cyclo-oxygenase-2를 선택적으로 억제한다. 골관절염 환자를 대상으로 하여 이중맹검, 무작위, Western Ontario and McMasters Universi-ties Osteoarthritis Index를 이용하여 평가한 결과, rofecoxib 12.5, 25 mg는 신체적 기능을 크게 향상시키는 것으로 보여졌다. 또한 diclofenac (50 mg, 1일 3회), ibuprofen (800 mg, 1일 3회), nabumetone(1500 mg, 1일 1회)와 유사한 임상효과를 나타내었다. Rofecoxib는 원발성 월경곤란증과 수술 후 치통에 효과적으로 억제하였으며 naproxen sodium과 ibuprofen과 같은 진통 효과를 보였다. Rofecoxib는 안전성 면에서 우수하며 가장 흔한 부작용은 설사, 두통, 오심과 상기도 감염증이다. Rofecoxib 12.5, 25, 50 mg/day를 투여한 골관절염 환자에게서 위장관계 부작용(천공, 궤양, 출혈)은 ibuprofen, diclofenac, nabumetone을 투여한 환자보다 훨씬 낮은 발생빈도를 나타내었다.

• Archives of Plastic Surgery
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• v.39 no.3
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• pp.249-252
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• 2012

Nicolau syndrome is a rare complication of intramuscular injection consisting of ischemic necrosis of skin, soft tissue, and muscular tissue that arises locoregionally. The characteristic pattern is pain around the injection site, developing into erythema, a livedoid dermatitis patch, and necrosis of the skin, subcutaneous fat, and muscle tissue. Three patients were injected with drugs (diclofenac sodium, ketoprofen, meperidine) for pain relief. Three patients complained of pain, and a skin lesion was observed, after which necrosis developed on their buttocks. Each patient underwent debridement and coverage. The wound healed uneventfully. We report three cases of Nicolau syndrome in the buttocks following diclofenac intramuscular injection.