• Journal of Pharmaceutical Investigation
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• v.27 no.4
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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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• v.27 no.8
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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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• v.14 no.3
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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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• v.8 no.3
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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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• v.29 no.1
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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%.

• Journal of Veterinary Clinics
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• v.10 no.2
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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,

• YAKHAK HOEJI
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• v.34 no.2
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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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• v.47 no.1
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• pp.54-58
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• 2009

Ketoprofen and ibuprofen are non-steroid anti-inflammatory drug(NSAID) that have analgesic and antipyretic properties. (S)-ketoprofen and (S)-ibuprofen have pharmacological activity, while (R)-ketoprofen and (R)-ibuprofen are either inactive or have side effect. The chiral separation of racemic ketoprofen and ibuprofen enantiomers was carried out by using a Kromasil HPLC column. Some chromatographic parameters (selectivity, resolution, number of theoretical plates and ${\Delta}H$) are calculated under different mobile phase compositions of hexane/t-BME/acetic acid and temperatures. The selectivity, resolution and number of theoretical plates were observed high at $25^{\circ}C$ and the composition of hexane/t-BME/acetic acid (80/20/0.1).

• Neonatal Medicine
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• v.18 no.2
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• pp.234-239
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• 2011

Purpose: Ibuprofen is used for prevention and treatment of patent ductus arteriosus as an alternative drug of indomethacin in very premature infants. We aimed to determine the effect of prophylactic ibuprofen on patent ductus arteriosus and clinical outcomes in preterm infants less than 1,250 g. Methods: A retrospective review of 39 preterm infants who were admitted to our neonatal intensive care unit from November 2009 to July 2010 was performed. Patients were divided into a prophylactic group (n=13) and a matched historical control group (n=26), where prophylactic ibuprofen were administrated within 24 hours after birth. The rate of ductal closure, side-effects of drug treatment and clinical outcomes were compared between two groups. Results: Comparison of the prophylactic and control groups revealed no significant differences in the rate of ductal closure (69.2% vs 77.7%, P=0.825) and surgical ligation (23.1% vs 30.8%, P=0.719). Occurrence of bowel perforation was more frequent in the prophylactic group than the control group, but was not significant (30.8% vs 11.5%, P=0.194). The frequency of intraventricular hemorrhage (grade${\geq}$3) and other outcomes did not differ between the groups. Conclusion: Ibuprofen prophylaxis in preterm infants did not decrease the rate of ductal closure, the need for surgical ligation and the incidence of intraventricular hemorrhage. Further studies are needed to investigate the beneficial effect and associated adverse events attributed to ibuprofen prophylaxis.

• Journal of Pharmaceutical Investigation
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• v.27 no.3
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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.