• Journal of Pharmaceutical Investigation
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• 제27권4호
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• pp.279-286
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• 1997

In order to formulate 2% ibuprofen solution, the effects of various solublizing agents, such as cosolvents (propylene glycol, polyethylene glycol, glycerin), a complexing agent $(CELDEX{\circledR}\;CH20)$, surfactants $(Poloxamers\;and\;Cremophor{\circledR}\;RH40)$ on the solubility of ibuprofen in aqueous solution were evaluated. Among them, Poloxamer 407 and $Cremophor{\circledR}$ RH40 showed the excellent capacity on the solubilization of ibuprofen. After 2% ibuprofen solution of choice were administered orally to rats, in reference to a 2% ibuprofen syrup in the market, the pharmacokinetic parameters were determined. The absorption rate of ibuprofen from the solution was higher than that from the suspension.

• Archives of Pharmacal Research
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• 제27권8호
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• pp.820-824
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• 2004

An optical purity test was indirectly performed on (S)-ibuprofen as its diastereomeric (R)-(+)-1-phenylethylamide derivative using achiral gas chromatography (GC). The method for the determination of trace (R)-ibuprofen (optical impurity), within the range 1.0 to 50 ng, from a racemic ibuprofen standard was linear (r＝0.9997) with acceptable precision (％ $RSD{\leq}5.3$) and accuracy (％ RE＝0.7~-3.9). Similar results were obtained with the method validation for the quantification of (S)-ibuprofen within the range 0.1 to 2.0 $\mu\textrm{g}$ using a (S)-ibuprofen stan-dard. When applied to seven different commercial (S)-ibuprofen products, their optical purities (98.7~99.1％) were determined with good precision (％ $RSD{\leq}4.0$).

• KSBB Journal
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• 제14권3호
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• pp.273-278
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• 1999

The molecularly imprinted polymers(MIPs) synthesized at various polymerization conditions were examined as ibuprofen receptors in terms of binding characteristics. The 4-vinylpyridine polymers had 1.2 times higher adsorption capability for (S)-(+)-ibuprofen than the methacrylic acid polymers. The methacrylic acid polymers synthesized by UV radiation had 1.9 times higher selectivity for (S)-(+)-ibuprofen compared to those by thermal initiation. Effects of various solvents for binding were also examined in this research. According to the Scatchard analysis, the (S)-(+)-ibuprofen artificial receptors had two different kinds of binding sites for (S)-(+)-ibuprofen while having only single kind of binding site for ketoprofen. The binding sites of (S)-(+)-ibuprofen, n were calculated as 4.3~4.9 $\mu$mol/g and the dissociation constants, $K_D$ were 0.68 mM for the specific binding.

• Mass Spectrometry Letters
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• 제8권3호
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• pp.49-52
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• 2017

Ibuprofen is one of the most popular analgesic and antipyretic drugs. An isotope dilution mass spectrometry method based on LC/MS was developed as a candidate reference method for the accurate determination of ibuprofen in pharmaceutical tablets. Isotope labelled ibuprofen, $ibuprofen-d_3$, was added as an internal standard into sample extracts. Ibuprofen and $ibuprofen-d_3$, was analysed by LC/MS in a selected ion monitoring (SIM) mode to detect ions at m/z 205 and 208, respectively. The repeatability and reproducibility of the developed ID-LC/MS method were tested for the validation and assessment of metrological quality of the method.

• Archives of Pharmacal Research
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• 제29권1호
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• pp.108-111
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• 2006

The economic and effective method for preparation of R-(-)-ibuprofen by diastereomer crystallization was developed. R-(-)-ibuprofen was resolved from racemic ibuprofen by forming R-(-)ibuprofen-R-(+)-$\alpha$-methylbenzylamine diastereomeric salt with R-(+)-$\alpha$-methylbenzylamine and crystallization. The purity of R-(-)-ibuprofen-R-(+)-$\alpha$-methylbenzylamine diastereomeric salt was tested and confirmed using HPLC and $^1H-NMR$ method. The pure diastereomeric salt collected from repeated recrystallization was further fractionated by liquid-liquid extraction to the pure enantiomer without racemization. R-(-)-ibuprofen was recovered producing overall yield of 2.4% with the purity more than 99.97%.

• 한국임상수의학회지
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• 제10권2호
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• pp.203-214
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• 1993

With the use of a rat surgical model, the ability of carboxymethylcellulose and ibuprofen in the reduction of abdominal adhesion was examined. Seventy seven female rats were randomly divided into 7 groups : (1) control, (2) 2% CMC, (3) 3% CMC, (4) ibuprofen 25mg, (5) ibuprofen 50mg, (6) combination of ibuprofen 25mg and 2% CMC and(7) combination of ibuprofen 50mg and 3%, CMC. Following induction of abrasion injuries on ileum, colon and both uterine horns with a surgical blads, the rats in groups (2), (6) were infused with 2% CMC solution singly or in combined Infection of 25 mg/kg of ibuprofen for three consecutive days, the rats In groups (3), (7) were infused with 3% CMC solution singly or In combined Injection of 50mg/kg of ibuprofen for three consecutive days. The rats in groups (4), (5) were injected only with 25 mg or 50 mg/kg of ibuprofen for three consecutive days. After 10 days the abdominal cavities were opened and the appearance of formed adhesion were graded. The changes of body weight, CBC and blood chemicals were also evaluated at 3, 6 and 10 days after operation. In ileum, the rats in the groups (2), (6) and (7) showed less adhesion formation. In colon, there were significant differences(p<0.05) in adhesion formation in all treated groups as compared to control. In both uterine horns, there were significant decrease(p<0.05) of adhesion formation in groups(2), (6) and (7) in comparison with other groups. The increasing rate of body weight was evident in group (3) and fibrinogen concentrations at 6 and 10 days revealed significant decrease (p<0.01) in group (7), whereas there was no consistent change in CBC and blood chemicals. Therefore, it can be sugested that the infusion of 2% CMC solution with or without the injection of 25 mg/kg of ibuprofen and 3% CMC solution with the injection of 50 mg/kg of ibuprofen are effective and safe following abdominal surgery,

• 약학회지
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• 제34권2호
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• pp.126-132
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• 1990

To enhance the activity of ibuprofen, amides of ibuprofen, 1-piperazinyl-2-(4-isobutylphenyl)propionamide(Ibu-P.A.) and 1-(4-methylpiperazinyl)-2-(4-isobutylphenyl)propionamide (Ibu-M.P.), were synthesized and the pharmaceutical properties and the pharmacological activities of the amides were studied. The lipid:water partition coefficients and pKa values were examined in vitro, and the antiinflammatory effect, analgesic effects, acute toxicity, and intestinal absorption were studied for the amides and compared with ibuprofen in vivo. The results are summarized as belows; 1) The lipid:water partition coefficients of Ibu-M.P. were higher than those of ibuprofen. 2) The calculated pKa values of ibuprofen and Ibu-M.P. were 5.49 and 8.66, respectively. 3) The antiinflammatory effects of ibuprofen, Ibu-P.A., and Ibu-M.P. were same intensity, but the duration of the effects of Ibu-P.A. and Ibu-M.P. were longer than that of ibuprofen. 4) The analgesic effect of Ibu-M.P. was more potent than those of ibuprofen and Ibu-P.A. in the acetic acid-induced writhing test. 5) The $LD_{50}$ was 495 mg/kg for ibuprofen, 187 mg/kg for Ibu-M.P., and over 1250 mg/kg for Ibu-P.A.. 6) The absorption rate constants(k) and half-life($t_{1/2}$) were 0.74($hr^{-1}$) and 0.94(hr) for ibuprofen, and 0.72 ($hr^{-1}$) and 0.96 (hr) respectively for Ibu-M.P..

• Korean Chemical Engineering Research
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• 제47권1호
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• pp.54-58
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• 2009

Ketoprofen과 Ibuprofen은 비스테로이드 계통의 진통 및 소염제로서 관절염 등을 위한 진통제나 해열제로 이미 널리 사용되고 있다. 그러나 이 두 물질이 치료약으로 사용될 때 (S)-ketoprofen과 (S)-ibuprofen은 약리학적으로 항염증 작용을 하며 (R)-ketoprofen과 (R)-ibuprofen은 약효가 없거나 부작용을 일으키는 문제점을 가지고 있다. 본 연구에서는 Ketoprofen과 Ibuprofen을 Kromasil HPLC 칼럼을 사용하여 이동상 조성비(hexane/t-BME/acetic acid)와 온도 변화($25{\sim}55^{\circ}C$)가 분리에 미치는 영향을 실험하였다. 분리특성은 선택도, 분리도, 이론단수 그리고 용량인자와 절대온도의 역수사이의 관계에서 계산된 엔탈피 변화 ${\Delta}H$에서 Ketoprofen과 Ibuprofen의 kromasil HPLC column 고정상과의 상호작용의 크기를 열역학적으로 검토하였다. 온도 $25^{\circ}C$, 이동상 조성비(hexane/t-BME/acetic acid) 80/20/0.1에서 선택도, 분리도, 이론단수 엔탈피 수치가 높게 나타났다.

• Neonatal Medicine
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• 제18권2호
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• pp.234-239
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• 2011

목적: 최근 indomethacin의 대체약으로 ibuprofen이 미숙아 동맥관 개존증의 예방과 치료에 사용되고 있다. 본 연구는 1,250g 미만의 미숙아를 대상으로 ibuprofen의 예방적 치료 효과 및 임상 경과를 분석하고자 하였다. 방법: 2009년 11월부터 2010년 7월까지 본원 신생아 중환자실에 입원한 1,250 g 미만의 동맥관 개존증 환아 39명을 대상으로 후향적으로 의무기록을 조사하였다. Ibuprofen의 예방적 투여군(출생 후 24시간 이내에 ibuprofen 투여) 13명에 대해 재태연령과 출생체중을 과거 대응(historical match)하여 대조군 26명으로 분류하였고, 두 군의 동맥관 개존증 빈도, 임상 경과 및 합병증을 분석하였다. 결과: Ibuprofen을 투여한 예방적 투여군과 대조군 간의 동맥관 폐쇄율(69.2% vs 77.7%, P=0.825)은 유의한 차이가 없었고, ibuprofen 치료에 실패하여 동맥관 결찰술을 시행 받은 경우도 두 군간에 유의한 차이가 없었다(23.1% vs 30.8%, P=0.719). 약물과 관련된 부작용으로 위장관 천공이 발생한 경우는 예방적 투여군에서 더 많은 경향을 보였으나 대상수의 부족 등으로 통계적 유의성은 없었다(30.8% vs 11.5%, P=0.194). 뇌실 내 출혈(grade${\geq}$3) 및 다른 미숙아 합병증의 발생률도 두 군간 차이는 없었다. 결론: 미숙아에서 ibuprofen의 예방적인 투여가 동맥관 폐쇄율, 동맥관 결찰술 그리고 고도의 뇌실 내 출혈의 빈도를 감소시키지 못하였다. 향후 예방적 ibuprofen 사용과 관련하여 효과 및 부작용에 대한 더 많은 연구가 되어야 할 것이다.

• Journal of Pharmaceutical Investigation
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• 제27권3호
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• pp.165-171
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• 1997

Ibuprofen, a nonsteroidal antiinflammatory, analgesic and antipyretic drug, has several limitations in clinical application because of low solubility in water and gastrointestinal irritation. Effect of ibuprofen/$2-Hydroxypropyl-{\beta}-cyclodextrin\;(HP{\beta}CD)$ inclusion compound on release of suppository was investigated. Complex formation was confirmed by $^{1}H-\;and\;^{13}C-NMR$ spectroscopy. The release of ibuprofen from suppository base in vitro was significantly increased by the complexation with $HP{\beta}CD$. The release of ibuprofen from hydrophilic base was faster than that from hydrophobic base. In vivo studies, the release rate of ibuprofen from suppository was accelerated after rectal administration in complex form. This results suggested that ibuprofen/$HP{\beta}CD$ complex can be practically used for suppository to have faster effect of ibuprofen with reduced side effect.