• Title/Summary/Keyword: R-(-)-ibuprofen

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Characteristic behaviors of ozone decomposition and oxidation of pharmaceuticals during ozonation of surface waters in Ulsan (울산시 상수원수에서의 오존분해 특성 및 의약물질 분해 거동 연구)

  • Lee, Hye-Jin;Lee, Hongshin;Lee, Changha
    • 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.

Empirical Equation for Resolution if Ibuprofen Enantiomers by Chiral High-Performance Liquid Chromatography (키랄 고성능 액체 크로마토그래피를 이용하 이부프로펜의 분리도에 관한 실험식)

  • 여미순;노경호
    • KSBB Journal
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    • v.18 no.4
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    • pp.261-265
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    • 2003
  • Ibuprofen was analyzed by chiral high performance liquid chromatography. Retention behaviours of the standard mixtures of ibuprofen were investigated to obtain their acceptable resolution. A chromatographic column (3.9 ${\times}$ 300 mm) was packed by Kromasil CHI-TBB packings (10 $\mu\textrm{m}$) and n-hexane was used as a mobile phase with 0.1% acetic acid and tert-butyl methyl ether. Isocratic elution of ibuprofen at 1.0 $m\ell$/min was performed by changing the mobile phase compositions. The experimental variables affecting the resolution were the compositions of mobile phase and chemical buffer (n-hexane and tert-butyl methyl ether). The resolution between the enantiomers were correlated into the several types of empirical equations including linear form, and their agreements between experimental data and calculated values were examined by the regression coefficient.

Preparation and Characterization of Liquefied Ibuprofen Using Self-Microemulsion Drug Delivery System (SMEDDS) (자가미세유화를 이용한 이부프로펜 액상제제의 제조와 특성)

  • Ahn, Yong-San;Song, Ji-Hee;Kang, Bok-Ki;Kim, Moon-Suk;Cho, Sun-Hang;Rhee, John-M.;Lee, Hai-Bang;Khang, Gil-Son
    • Journal of Pharmaceutical Investigation
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    • v.34 no.1
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    • pp.35-42
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    • 2004
  • Ibuprofen (IBU), is a non-steroidal anti-inflammatory drug, used to treat rheumatoid arthritis, removal of fever and mild to moderate pain. Because of small dosage and very low accumulation in the body, IBU has been used to heal children's fever. However, IBU was very low solubility in a low pH and water (in water $0.03{\sim}2.5$ mg/ml). A nanoemulsion containing IBU by means of self-microemulsion drug delver system (SMEDDS) was prepared in order to enhance the solubility of IBU. The SMEDDS was composed of cosurfactant, oil and surfactant The solubility of IBU in various components such as cosurfactant, oil and surfactant was examined. $Carbitol^{\circledR}\;(386.99{\pm}20.5\;mg/ml)$ as a cosurfactant, $Labrafil^{\circledR}$  M1944CS $(90.16{\pm}1.60mg/ml)$ as an oil and $Cremopher^{\circledR}$  RH-40 $(239.01{\pm}2.8\;mg/ml)$ as a surfactant were used in this study for preparing SMEDDS. Optimized formulation of SMEDDS was obtained by phase diagram which express the section of nanoemulsion formation. The SMEDDS containing IBU had higher dissolution rate than conventional IBU sirups. Thus the SMEDDS was a potential candidate of stable conventional and effective oral dosage form for IBU.

Improved Dissolution Characteristics of Ibuprofen Employing Self-Microemulsifying Drug Delivery System and Their Bioavailability in Rats (자가유화 약물전달시스템을 이용한 이부프로펜의 용출개선 및 흰쥐에서의 생체이용률 평가)

  • Kim, Hyung-Soo;Lee, Sang-Kil;Choi, Sung-Up;Park, Hye-Sook;Jeon, Hyun-Joo;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.32 no.1
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    • pp.27-33
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    • 2002
  • A self-microemulsifying drug delivery system(SMEDDS) composed of Cremophor $EL^{\circledR},\;Labrasol^{circledR}$, and Lauroglycol $FCC^{circledR}$ was prepared for the enhancement of solubility, dissolution rate and bioavailability of ibuprofen(IBP), which is water-insoluble but soluble in oils and surfactants. Phase diagram with various regions including microemulsion area was depicted. The SMEDDS was encapsulated in soft gelatin capsules and their dissolution characteristics in various media were observed in comparison to the generic products commercially available in the market. Soft capsules of SMEDDS formulation showed better dissolution profiles, especially in acidic condition, than the others. For the period of 1 hr dissolution in pH 1.2 medium, it reached over 70% dissolution from soft capsules, compared to less than 40% dissolution from commercial reference tablets. On the other hand, in vivo pharmacokinetic parameters were obtained after oral administrations of different IBP preparations to Sprague Dawley rats. SMEDDS formulation showed higher $C_{max}$ and greater $AUC_{0-5hr}$ than the suspension of reference tablet or IBP powder. Therefore, it is possible to conclude that a newly developed soft capsules employing SMEDDS provides an alternative preparation to improve oral bioavailability of IBP.

Chiral Separation of Non-Steroidal Inflarnrnatory Drugs and Metabolites by Achiral Gas Chromatography as O- Trifluoroacetylated (- )-Menthyl Esters

  • Lee, Yoon-Suk;Paik, Man-Jeong;Kim, Kyoung-Rae
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.396.3-397
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    • 2002
  • Because of the differences in biological and pharmacological properties between enantiomers of chiral acidic non-steroidal antiinflammatory drugs (NSAIDs) in human body. accurate determinations of their optical purities have been in great need. Racemic ibuprofen. tiaprofen. suprofen. flubiprofen and napoxen were reacted with (1R. 28. 5R)-(-)-menthol to convert them to corresponding diastereomeric (1R. 2S. 5R)-(- )-menthyl esters. (omitted)

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Effectiveness of $Myprodol^{(R)}$ in ram Management (통증 조절에 있어서 $Myprodol^{(R)}$의 효과)

  • Shin, Sang-Wook;Lee, Hyun-Sub;Kim, Inn-Se;Baik, Seong-Wan
    • Journal of Hospice and Palliative Care
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    • v.4 no.1
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    • pp.41-46
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    • 2001
  • Background : Many analgesics are used to relieve the pain of various causes. Among these, $Myprodol^{(R)}$, a combination analgesic with codeine, ibuprofen and paracetamol, was recently used as a new analgesics. This study was performed to survey the kinds of diseases, side effects and pain relief effect of $Myprodol^{(R)}$ in clincal practice. Methods : This retrograde study surveyed the medical records of 183 patients treated with $Myprodol^{(R)}$ at Pain Clinic, Pusan National University Hospital. From medical records, the disease entities, the pain characteristics, duration of $Myprodol^{(R)}$ medication, the analgesic effect and side effects were evaluated. Results : $Myprodol^{(R)}$ is used in the treatment of cancer pain (64.3%) and non-cancer pain (35.7%). Among side effects of $Myprodol^{(R)}$ medication, nausea with vomiting, constipation and generalized edema were common in cancer pain, but epigatric pain was common in non cancer pain. $Myprodol^{(R)}$ was more effective in non cancer pain than cancer pain. Conclusions: $Myprodol^{(R)}$ was used in cancer and non-cancer pain patients. In cancer pain patients, $Myprodol^{(R)}$ was effective in early cancer pain but, not effective in advanced cancer. $Myprodol^{(R)}$ was also used and effective in non-malignant benign chest pain, lumbago, post-operative pain.

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Enhancement of Dissolution Rate of Poorly Water-soluble Ibuprofen using Solid Dispersions and Inclusion Complex (고체분산체 및 포접화합물을 이용한 난용성 약물인 이부프로펜의 용출 속도의 증가)

  • Lee, Beom-Jin;Lee, Tae-Sub
    • Journal of Pharmaceutical Investigation
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    • v.25 no.1
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    • pp.31-36
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    • 1995
  • Solid dispersions and inclusion complex were prepared for the enhancement of solubility and dissolution rate of poorly water-soluble ibuprofen(IPF) as a model drug. Polyethylene glycol 4000(PEG4000) and polyvinylpyrrolidone(PVP) were used for the preparation of solid dispersion. $2-Hydroxypropyl-{\beta}-cyclodextrin(2-HP{\beta}CD)$ was also used for the preparation of inclusion complex. The solubility of IPF increased as the concentration of PEG4000, PVP and $2-HP{\beta}CD$ increased. Solubilization capacity of $2-HP{\beta}CD$ was increased about 10 times when compared to PEG 4000 and PVP. The dissolution rate of drug from solid dispersions and inclusion complex in the simulated gastric fluid was enhanced when compared to pure IPF and commercial $BR4^{\circledR}$ tablet as a result of improvement of solubility. In case of solid dispersions, dissolution rate of drug was proportional to polymer concentration in the formulation. The marked enhancement of dissolution rate of drug by inclusion complexation with $2-HP{\beta}CD$ was noted. However, dissolution rate of drug from solid dispersions and inclusion complex in the simulated intestinal fluid was not significant because IPF was readily soluble in that condition. From these findings, water-soluble polymers and cyclodextrin were useful to improve solubility and dissolution rate of poorly water-soluble drugs. However, easiness and reliability of preparation method, scale-up and cost of raw materials must be considered for the practical application of solid dispersion and inclusion complex in pharmaceutical industry.

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Measurement of Optical Purity for Commercially Avialable Dexibuprofen and Ibuprofen Sold in 2013 (2013년도 시판된 Dexibuprofen과 Ibuprofen의 광학 순도 측정)

  • Ryoo, Sang Hyun;Lee, Sang Heon;Seo, Hae Chan;Song, Jung Suk;Ryoo, Dong Hyun;Yu, Jeong Jae;Kim, Hyun Young;Lee, Jae Hwan;Ryoo, Jae Jeong
    • Journal of the Korean Chemical Society
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    • v.58 no.3
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    • pp.277-282
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    • 2014
  • The optical purity of 11 commercial dexibuprofens and 7 ibuprofens sold in Korea in 2013 were examined by chiral HPLC. The Chiralcel OD-H column and LUX-Cellulose-1 column were used as chiral stationary phases and the mixed eluent of hexane:isopropanol:acetic acid as 100:1:0.1 was used as a mobile phase with a flow rate of 1.0 mL/min. Each data was obtained from an average value of at least three different experiments for each sample and the average value of relative standard deviation of them appeared very small, 0.19%. Average optical purity value (97.5%) of eleven commercial dexibuprofens used in this study were smaller than those of 9 years ago (99.2%), but larger than four years ago (95.6%). Enantiomeric ratios of (R)- and (S)-isomers of seven ibuprofen samples used in this experiment were achieved at about 50:50 which was different with the result (44:56) from four years ago.

Preparation and Release Characteristics of Polymer-Reinforced and Coated Alginate Beads

  • Lee, Beom-Jin;Min, Geun-Hong
    • Archives of Pharmacal Research
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    • v.18 no.3
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    • pp.183-188
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    • 1995
  • Polymeric reinforcement and coatings of alginate beads were carried out to control the release rate of drug from alginate beads. A poorly water-soluble ibuprofen (IPF) was selected as a model drug. A commercially available $Eudragit^{\circledR}$ RS100 was also used as a polymer. Effects of polymeric contents, the presence of plasticizers and amount of drug loading on the release rate of drug were investigated. The release rate of drug from alginate beads in the simulated gastric fluid did not occur within 2 h but released immediately when dissolution media were switched to the simulated intestinal fluid. No significant difference of release rate from polymer-reinforced alginate bead without plasticizers was observed when compared to plain (simple) beads. However, the release rate of drug from polymer-reinforced alginate beads was further sustained and retarded when aluminium tristearate (AT) as a plasticizer was added to polymer. However, polyethylene glycol 400 (PEG400) did not change the release rate of drug from alginate beads although PEG400 was used to improve dispersion of polymer and sodium alginate, and plasticize $Eudragit^{\circledR}$ RS100 polymer. The presence of plasticizer was crucial to reinforce alginate gel matrices using a polymer. As the amount of drug loading increased, the release rate of drug increased as a result of decreasing effects of polymer contents in matrices. The significantly sustained release of drug from polymer-coated alginate beads occurred as the amount of polymer increased because the thickness of coated membrane increased so that cracks and pores of the outer surface of alginate beads could be reduced. The sustained and retarded action of polymer-reinforced and coated beads may result from the disturbance of swelling and erosion (disintegration) of alginate beads. From these findings, polymeric-reinforcement and coatings of alginate gel beads can provide an advanced delivery system by retarding the release rate of various drugs.

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Pain Control Effects of $Myprodol^{(R)}$ after Periodontal Surgery and Dental Implant Surgery (치주 수술 및 인공 치아 매식술 후 $Myprodol^{(R)}$의 동통 억제 효과에 대한 연구)

  • Cho, Kyoo-Sung;Lee, Jung-Hoon;Kim, Hyun-Young;Suh, Jong-Gin;Choi, Seong-Ho;Chai, Jung-Kiu;Kim, Chong-Kwan
    • Journal of Periodontal and Implant Science
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    • v.30 no.1
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    • pp.1-11
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    • 2000
  • Although various analgesics have been administrated for postoperative pain control, postoperative pain has not been adequately controlled . The purpose of this study was to evaluate the effects and patient's satisfaction of $Myprodol^{(R)}$(combination analgesics with codeine, ibuprofen, paracetamol) compared to Acetamionphen and placebo drug after periodontal surgery and dental implant surgery. We studied 98 cases of outpatients which were composed of 67 cases of flap operation(which separated to 3 groups: Placebo group(n=25), $Myprodol^{(R)}$ group(n=22), Acetaminophen group(n=20)) and 21 cases of dental implant surgery(which separated to 3 groups : Placebo group(n=10), $Myprodol^{(R)}$ group(n=12), Acetaminophen group(n=9)). We evaluated the postoperative pain(Pain 1), Pain after first drug administraion(Pain 2), the degrees of pain reduction(pain 3), patient's satisfaction for drug, and side-effects. We obtained following results; 1. In Pain 1, making a comparison among groups, there was no significant difference in both cases of flap operation-group and dental implant surgery-group 2. In Pain 2, establishing a comparison among groups, there was no significant difference in flap operation-group, but significant difference was seen between placebo group and $Myprodol^{(R)}$ group in cases of dental implant surgery group(P<0.05). 3. In Pain 3, making a comparison among groups, $Myprodol^{(R)}$ group showed significant differences compared to placebo group and Acetaminophen group in both cases of flap operation group and dental implant surgery group(P<0.05). 4. In patient's satisfactory score, making a comparison among groups, there were significant differences between placebo group and $Myprodol^{(R)}$ group in cases of flap operation group and between $Myprodol^{(R)}$ group and Acetaminophen group in cases of dental implant surgery group(P<0.05). 5. Making a comparison in side-dffect, no significant differrence was seen. Our conclusion is that $Myprodol^{(R)}$ is a effective oral analgesics to the patients who underwent periodontal surgery or implant surgery for it's synergism among three dugs.

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