• Title/Summary/Keyword: Nonsteroidal anti-inflammatory drug

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Preparation and Characterization of Microemulsion containing Ibuprofen (Ibuprofen이 함유된 Microemulsion의 제조 및 평가)

  • 양재헌;김영일;김현주;정규호
    • YAKHAK HOEJI
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    • v.45 no.6
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    • pp.634-640
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    • 2001
  • Ibuprofen is one of the nonsteroidal anti-inflammatory drugs (NSAID) and has shown antiinflammatory; antipyretic, and analgesic activity in both animals and humans. But it causes gastric mucosal abnormalities including edema, erythema, and submucosal petechial hemorrhages and erosin in human. In addition, based on the pharmaceutical point of view the compression and dissolution ability of ibuprofen is known as poor. Therefore we studied to develop novel formulation containing water-insoluble drug, ibuprofen, using microemulsion consisting of surfactant, oil phase, and water phase was prepared for the purpose of increasing its bioavilability The physicochemical properties such as particle size, dissolution rate, solubility of ibuprofen in the system were determined. After oral administration of ibuprofen containing the microemulsion system, to Sprague-Dawley rats, pharmacokinetic parameters were also obtained. For the formulation in the study, oleic acid, linoleic acid, and several kinds of glycerides and triglycerides were used as an oil phase with several surfactants. Diethylene glycol monoethyl ether (Transcuto $l^{ }$) or saturated polyglycolized glycerides (Labrafil $^{ }$)as surfactant was used, the domain of microemulsion was wide. The diameter of o/w microemulsion was ranged from 90 to 220 nm. Microemulsion, prepared with unsatulated polyglycolized glycerides (Labrafil $^{ }$) and the 2 : 1 molar mixture of diethylene glycol monoethyl ether (Transcuto $l^{ }$)/polyoxyethylene(4) lauryl ether (Bri $j^{ }$ 30) , is expected to be promising system that increased the bioavilability of ibuprofen.ibuprofen.

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Mechanism of Naproxen-Induced Antidiuretic Response in Dog (나프록센의 항이뇨작용 기전)

  • 고석태;이한구;유강준
    • YAKHAK HOEJI
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    • v.39 no.3
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    • pp.314-328
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    • 1995
  • This study was attempted to investigate the mechanism of retention of sodium and water by naproxen which is a drug among nonsteroidal anti-inflammatory drugs in dogs. Napoxen, when given intravenously in doses ranging from 30 mg to 100 mg/kg, elicited antidiuresis accompanied vath the decrease of osmolar clearance(Cosm) and amounts of sodium excreted in urine(E$_{Na}$), with the increase of sodium reabsorption rate in renal tubule(R$_{Na}$) and ratio of potassium against sodium (K/Na). Naproxen infused into a renal artery in doses ranging from 1.0mg to 3.0mg/kg/min produced both diuretic action in infused kidney and antidiuretic action in control kidney. Naproxen injected into carotid artery in doses ranging from 10.0 mg to 30.0 mg/kg exhibited antidiuretic action. Changes of renal function in the circumstances of above two antidiuresis were the same with aspect of intravenous naproxen. Antidiuretic action of naproxen injected into carotid artery was not affected by renal denervation, was blocked by pretreatment with i.v. arachidonic acid, prostaglandin precursor, or i.v. indomethacin, cyclooxygenase inhibitor. Naproxen injected into carotid artery abolished the diuretic action of i.v. spironolactone, aldosterone antagonist, and i.v. spironolactone blocked the antidiuretic action of naproxen given into carotid artery. The results suggest that naproxen produced antidiuresis, and sodium and water retention through the central system, the mechanism being related to the prostaglandin biosynthetic inhibition and aldostercfne like action.

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Aseptic Meningitis after a Lumbar Epidural Steroid Injection -A case report- (요부 경막외 스테로이드 주입 후 발생한 무균성 수막염 -증례 보고-)

  • Hwang, Byeong Mun;Leem, Jung Gil
    • The Korean Journal of Pain
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    • v.18 no.1
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    • pp.52-55
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    • 2005
  • Complications following a well conducted epidural steroid injection are rare. A 50-year-old man developed a headache and neck stiffness 2 days after a lumbar epidural steroid injection. Under the impression of aseptic meningitis, fluid and nonsteroidal anti-inflammatory drug therapy was started immediately after cerebrospinal fluid (CSF) sampling. The CSF was turbid, and revealed a white blood cell count, protein, glucose and pressure of $550/{\mu}l$ (98% lymphocyte), 107.9 mg/dl, 48 mg/dl (serum 113 mg/dl) and $17cmH_2O$, respectively. The CSF stain and culture, and antibody test and polymerase chain reaction for pathogens were negative. A computed tomography (CT) scan of the brain revealed no abnormality, and a chest roentgenogram and the results of the neurological examination were normal. Under the impression of aseptic meningitis, the condition was managed conservatively, without antibiotics. Seven days later, the clinical symptoms had improved, and the patient discharged.

Total Ankylosis by Heterotopic Ossification in an Adolescent Anterior Trans-olecranon Fracture Dislocation: A Case Report

  • Kim, Beom-Soo;Song, Kwang-Soon;Bae, Ki-Cheor;Lee, Si-Wook;Um, Sang-Hyun;Cho, Chul-Hyun
    • Clinics in Shoulder and Elbow
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    • v.22 no.3
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    • pp.154-158
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    • 2019
  • The incidence of heterotopic ossification in adolescents appears to be lower than in adults. There exist very few reports of heterotopic ossification with total bony ankylosis in child or adolescent populations. We describe a case of total bony ankylosis of the elbow secondary to heterotopic ossification, in a 14-year-old female. Total ankylosis of the elbow at 45 degrees of flexion was noted 6 months postsurgery, and complete surgical excision of the heterotopic mass was performed. After an additional one-time dose of radiation therapy and nonsteroidal anti-inflammatory drug medication, full range of motion was obtained without any recurrence or other complications, up to the last follow-up of 30 months.

Meclofenamate Suppresses MUC5AC Mucin Gene Expression by Regulating the NF-kB Signaling Pathway in Human Pulmonary Mucoepidermoid NCI-H292 Cells

  • Jiho Ryu;Kyung-il Kim;Rajib Hossain;Misoon Lee;Jin Tae Hong;Hyun Jae Lee;Choong Jae Lee
    • Biomolecules & Therapeutics
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    • v.31 no.3
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    • pp.306-311
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    • 2023
  • The current study aimed to reveal the potential effect of meclofenamate, a nonsteroidal anti-inflammatory drug, on the gene expression of airway MUC5AC mucin. Human pulmonary mucoepidermoid NCI-H292 cells were pretreated with meclofenamate for 30 min and stimulated with phorbol 12-myristate 13-acetate (PMA) for 24 h. Thereafter, the effect of meclofenamate on the PMA-induced nuclear factor kappa B (NF-kB) signaling pathway was assessed. Meclofenamate inhibited glycoprotein production and mRNA expression of MUC5AC mucins induced by PMA by inhibiting the degradation of inhibitory kappa Bα (IkBα) and NF-kB p65 nuclear translocation. These results suggest meclofenamate suppresses mucin gene expression by regulating NF-kB signaling pathway in human pulmonary epithelial cells.

Endoscopic Diagnosis and Treatment of Benign Small Bowel Stricture (양성 소장협착의 내시경적 진단과 치료)

  • Jinsu Kim
    • The Korean Journal of Medicine
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    • v.99 no.4
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    • pp.199-205
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    • 2024
  • Benign small bowel strictures can occur in association with various conditions, including small bowel Crohn's disease, nonsteroidal anti-inflammatory drug-induced enteritis, ischemic enteritis, intestinal tuberculosis, radiation enteritis, postoperative adhesions, and anastomotic strictures. Benign small bowel strictures are classified into two categories, low-grade and high-grade. Low-grade small bowel strictures involve a partial reduction of the internal diameter of the small intestine, causing slight obstruction of the passage of food and digestive fluids without significant bowel obstruction symptoms. By contrast, high-grade small bowel strictures involve a severe narrowing of the intestinal lumen, leading to marked obstruction of the passage of food and digestive fluids and pronounced bowel obstruction symptoms. Small bowel strictures can be diagnosed using various methods, including abdominal plain radiography, abdominal computed tomography, computed tomography enterography, magnetic resonance enterography, balloon-assisted enteroscopy, and abdominal ultrasound. Each diagnostic method has unique advantages and disadvantages as well as differences in diagnostic specificity and sensitivity. Therefore, even if small bowel strictures are not observed using a single imaging technique, their presence cannot be completely excluded. A comprehensive diagnosis that combines clinical information from multiple diagnostic modalities is necessary. Therapeutic approaches for managing small bowel strictures include medical therapy, endoscopic balloon dilation using balloon-assisted enteroscopy, and surgical methods such as strictureplasty and segmental resection. Endoscopic balloon dilation, in particular, can help reduce complications associated with repeated surgeries for strictures.

A Drug-Induced Liver Injury by Western Medication (양약으로 유발된 약인성 간손상 환자 임상보고)

  • Son, Chang-gue
    • The Journal of Internal Korean Medicine
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    • v.36 no.1
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    • pp.69-75
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    • 2015
  • Objectives : To investigate the clinical features of drug-induced liver injury (DILI) and traditional Korean medicine (TKM) -based management. Methods : A female patient diagnosed with DILI caused by Western drugs had been treated with Oriental therapies, then the subjective clinical outcome and biochemical parameters were monitored. Results : A 73-year-old female had taken Western drugs (nonsteroidal anti-inflammatory and skeletal muscle relaxants) for about 3 months, and complained of severe abdominal discomfort and tiredness. Her RUCAM score was 9, which met the criteria for DILI (AST 90 IU/L, ALT 100 IU/L, ALP 191 IU/L, and GGT 614 IU/L). She was treated with herbal drugs, moxibustion, and acupuncture, and her symptoms completely resolved, with normalized hepatic enzymes within two weeks. Conclusions : This case report provides a clinical characteristic for a typical DILI caused by Western medicine, and shows an example of a TKM-based application.

Results of 6 Month Short Course Chemotherpay for Pulmonary Tuberculosis with 2SHRZ/4HR (6개월 단기 항결핵 화학요법의 성적)

  • Lee, Hyang-Ju;Min, Chul-Hong;Lee, Sun-Woo;Park, In-Won;Choi, Byoung-Whui;Hue, Sung-Ho
    • Tuberculosis and Respiratory Diseases
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    • v.38 no.2
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    • pp.93-98
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    • 1991
  • A clinical trial was made on 76 patients with pulmonary tuberculosis to determine the effectiveness and acceptibility of 6 month 2SHRZ/4HR antituberculosis regimen. Out of 76 patients, 13 patients (17.1%) dropped out and 11 patients (14.5%) were excluded due to drug resistance. In 3 patients (3.9%), regimen was changed due to adverse effects. Treatment failure rate was 2.0% in 50 patients. One patient, who had far advanced lesion, was treated longer than 6 months due to failure of sputum conversion. The most common adverse effect was arthralgia, which was controlled by the administration of allopurinol and nonsteroidal anti-inflammatory drug. In conclusion, 2SHRZ/4HR for 6 months was effective regimen in treating the newly-diagnosed patients with tuberculosis, but change of the regimen and duration might be carefully considered by the severity of the lesion and adverse effect of the drug But further study will be needed to evaluate not only the efficacy and efficiency of 6 month chemotherapy but also relapse rates.

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Formulation Design and Evaluation of Ketorolac Tromethamine Hydrogel for Transdermal Delivery System (경피흡수를 위한 케토롤락 하이드로겔의 제제설계 및 평가)

  • Cho, In-Sook;Lee, Gye-Won;Lee, Jong-Hwa;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.33 no.1
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    • pp.21-28
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    • 2003
  • Ketorolac tromethamine(KT) is a nonsteroidal agent with potent analgesic and moderate anti-inflammatory activity. The lipid-water partition coefficient of KT was evaluated and KT gel was formulated as a gel containing different pH, different concentrations of polymer (poloxamer 407, carbopol 941), propylene glycol, ethanol and various enhancers. The resulting KT gels were evaluated with respect to their viscosity, in vitro drug permeation rate through hairless mouse skin and stability. In n-octanol and chloroform, the lipid-water partition coefficient of KT was the highest at pH 4 phosphate buffer. The apparent viscosity of KT gel increased with an increase in gel pH, polymer and enhancer concentration. But the apparent viscosity of KT gel decreased with an increase in ethanol concentration. The permeation rate of KT through hairless mouse skin from gels different pH was maximum at pH 4 which is close to KT $pK_{a}$ 3.54. The permeation rate decreased with an increase in polymer, propylene glycol concentration. But the permeation rate increased with an increase in ethanol. The increase of drug concentration from 1 to 3% induced linear increase in permeation rate. The best enhancer was the combination of $Labrasol^{\circledR},\;Transcutol^{\circledR}$, oleic acid and l-menthol. In the accelerated stability test(25, 40 and $50{\circ}C$), pH 5 gel was most stable and pH 4 gel was most unstable for 90 days.

Solubilization of Talniflumate in Microemulsion Systems (마이크로에멀젼을 이용한 탈니플루메이트의 가용화)

  • Lee, Gye-Won;Cho, Young-Ho;Kim, Hak-Hyung;Kim, Sock-Young;Kim, Do-Kyun;Kim, Eun-Hea
    • Journal of Pharmaceutical Investigation
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    • v.38 no.3
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    • pp.171-176
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    • 2008
  • Talniflumate is a nonsteroidal anti-inflammatory drug (NSAID), which has been used treat of rheumatoid diseases, is insoluble in water, therefore it has low bioavailability after oral administration. The purposes of this study were to prepare O/W or W/O microemulsions for solubilization of poorly water soluble drug, talniflumate and to formulate into other dosage form. For this purpose, we made O/W or W/O microemulsion with oil(soybean oil, IPM), surfactant (Cremophor $EL^{(R)}$, Tween 80) and water or propylene glycol and evaluated solubility of talniflumate. The microemulsion systems were very stable and showed transmittance above 95% without flocculation or aggregation. Especially, the solubility of talniflumate in the formulation B-1 containing 18% of isopropyl myristate and 71% of tween 80 was 10 times higher than that of other O/W microemulsions. The addition of propylene glycol and N-methylglutamine to the fomulation B-1 showed excellent capacity on the solubilization of talniflumate and the percentage was almost 2.0%. These results suggest that the microemulsion system may be promising for the solubility improvement of talniflumate.