• The Korean Journal of Pain
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• v.31 no.1
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• pp.39-42
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• 2018

Background: Venipuncture pain is an uncomfortable suffering to the patient. It creates anxiety, fear and dissatisfaction. The ketoprofen transdermal patch is a proven treatment for musculoskeletal and arthritic pain. We planned this study to evaluate the efficacy of the ketoprofen patch to reduce venipuncture pain. Methods: Two hundred adult patients, aged 18-60 years, of either sex, ASA grade I or II, were enrolled. Presuming that therapy would decrease venipuncture pain by 30%, a power calculation with ${\alpha}=0.05$ and ${\beta}=0.80$ required enrollment of at least 24 patients into each group. However, 100 patients in each group were recruited. Group I (Control) received a placebo patch; Group II (Ketoprofen) received a 20 mg ketoprofen patch. A selected vein on the dorsum of the patient's non-dominant hand was cannulated with 18 g intravenous cannula 1 h after the application of the respective patch. Assessment of pain was done by a 10 cm visual analogue scale (VAS) of 0-10, where 0 depicts "no pain" and 10 is "the worst imaginable pain". The venipuncture site was assessed for the presence of skin erythema, swelling and rashes at 12 h, 24 h and at the time of decannulation. Results: Incidence of pain was 100% (94/94) in the control group as compared to 93% (85/91) in the ketoprofen group. The severity of the venipuncture pain was 6 (2) and 2 (2) for control and ketoprofen groups respectively (P < 0.05). Conclusions: Application of a ketoprofen patch at the proposed site of venipuncture one hour before the attempt is effective and safe for attenuating venipuncture pain.

• Biotechnology and Bioprocess Engineering:BBE
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• v.9 no.4
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• pp.285-291
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• 2004

A simulated moving bed (SMB) chromatography system is a powerful tool for preparative scale separation, which can be applied to the separation of chiral compound. We have de-signed our own lab-scale SMB chromatography using 5 HPLC pumps, 6 stainless steel columns and 4 multi-position valves, to separate a racemic mixture of ketoprofen in to its enantiomers. Our design has the characteristics of the low cost for assembly for the SMB chromatography and easy repair of the unit, which differs from the designs suggested by other investigators. It is possible for the flow path through each column to be independently changed by computer control, using 4 multi-position rotary valves and 5 HPLC solvent delivery pumps. In order to prove the operability of our SMB system, attempts were made to separate the (S)-ketoprofen enantiomer from a ketoprofen racemic mixture. The operating parameters of the SMB chromatography were calculated for ketoprofen separation from a batch chromatography experiment as well as by the triangle theory. With a feed concentration of 1 mg/mL, (S)-ketoprofen was obtained with a purity of 96% under the calculated operating conditions.

• Animal Bioscience
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• v.36 no.8
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• pp.1293-1303
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• 2023

Objective: Inflammation and pain management in postpartum hyperprolific sows is currently an important animal welfare issue in the swine industry. The present study investigates effects of ketoprofen treatment on the incidence of post-parturient disorders, feed intake, colostrum yield, piglet colostrum intake, colostrum immunoglobulin G (IgG) and piglet mortality rate during the first 3 days of postnatal life. Methods: In total, 61 Danish Landrace×Yorkshire crossbred sows and their offspring (n = 833) were included in the experiment. The sows were randomly distributed into two groups: i) control (n = 31), sows were treated with tolfenamic acid 2 mg per kg for 2 days postpartum; ii) ketoprofen (n = 30), sows were treated with ketoprofen 3 mg per kg for 2 days postpartum. The farrowing process of the sows was monitored for 24 h daily, and data associated with farrowing were collected. Piglet colostrum intake, sow colostrum yield and colostrum IgG were determined. Results: During the first 3 days postpartum, the incidence of sows that had fever did not differ between control and ketoprofen groups (51.6% and 56.7%, respectively, p = 0.692). Piglet colostrum intake did not differ between control and ketoprofen groups (p = 0.736). However, the proportions of piglets that had inadequate colostrum intake were 71.3%, 22.6%, and 5.4% in those with birth weights of <1.0 kg, 1.0 to 1.29 kg, and ≥1.30 kg, respectively (p<0.001). The piglet mortality rate did not differ between control and ketoprofen groups (p = 0.808). Conclusion: Administration of ketoprofen in postpartum sows for 2 days can control the evidence of post-parturient disorders in sows as effectively as the use of tolfenamic acid. No deleterious effect of ketoprofen was detected on sow colostrum yield, piglet colostrum intake and piglet mortality. Therefore, ketoprofen can be recommended as an alternative anti-inflammatory drug used in postpartum sows.

• Journal of Pharmaceutical Investigation
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• v.32 no.2
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• pp.103-106
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• 2002

A method that describes the determination of the in vitro release of ketoprofen from gels was suggested. The experimental system of the method consists of a Franz diffusion cell, which contains a pH 7.4 phosphate buffer as a receptor medium, and a $70\;{\mu}m$ mesh woven nylon membrane as a diffusion barrier. Under the given condition of the system, the diffusion of ketoprofen across the membrane was rapid enough that the apparent release profile of ketoprofen obtained from the present method could represent the release of the drug from gel preparations. The release of ketoprofen in the present method was reproducible, and the rate increased in proportion to the concentration of ketoprofen in the gel. These suggest that the present method is applicable to the quality evaluation of gel preparations containing ketoprofen.

• Journal of Pharmaceutical Investigation
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• v.33 no.3
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• pp.163-169
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• 2003

In order to develop a film-forming transdermal drug delivery system, polyurethane (PU) based on poly(ethylene glycol) and poly(tetramethylene oxide) was synthesized and characterized. The synthesized PU was blended with Gantrez ES 225 (GT) to improve the adhesion property of film-forming agent to the skin. When film-forming gel formulation containing 3% ketoprofen (KP) was applied, transparent thin film was obtained within 5 minutes and adhered to the skin for 8 hours. In vitro percutaneous absortion studies were performed to determine the rate of ketoprofen absorption through guinea pig skin. A prominent effect of limonene on the skin permeability of ketoprofen was observed among the various skin permeation enhancers investigated. Considering mechanica properties of film and skin permeability of ketoprofen, 2% of limonene was optimal content in the film forming transdermal formulation.

• Biomolecules & Therapeutics
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• v.5 no.4
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• pp.357-363
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• 1997

The effects of formulation variables of topical lotion on the skin permeation of ketoprofen were evaluated using excised rat skins. The formulation variables were the amounts of poloxamer 407, drug and ethanol, and penetration enhancers. The Keshary-Chien diffusion cells were used for the diffusion study. The flux of ketoprofen linearly decreased as the concentration of poloxamer increased from 5% to 15% in the preparation, and linearly increased as the amount of drug increased. Penetration enhancers such as fatty acids and fatty alcohols showed markedly enhancing effects at the level of 5%. Among them, the highest flux was shown in linolenic acid. From these results, optimum formula containing 3% ketoprofen, 5% poloxamer 407, 40% ethanol and 5% linolenic acid having the flux of 537.6 $\mu$g/$\textrm{cm}^2$/hr were noted.

• Journal of Pharmaceutical Investigation
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• v.24 no.2
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• pp.105-108
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• 1994

The ulcerogenic activity of a 3% ketoprofen gel (ID-GEL) after its transdermal application in rats was determined with the Litchfield and Wilcoxon method in reference to the oral administration of ketoprofen in a suspension. The $UD_{50}$ (dose producing ulcers in 50%, of the rats tested) of ID-GEL after its transdermal application was approximately 4 times greater than that after the oral administration of the drug, indicating that the ulcerogenic activity of ketoprofen was much lowered with its transdermal application.

• Archives of Pharmacal Research
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• v.27 no.12
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• pp.1295-1301
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• 2004

The enantiomeric composition tests on flurbiprofen and ketoprofen present in patch products and in urine excretions following patch applications were performed as diastereomeric (R)-(+)- 1-phenylethylamides by achiral gas chromatography and by gas chromatography-mass spectrometry in selected ion monitoring mode. The method for determination of (R)- and (S)-enantiomers in the range from 0.1 to 5.0 ${\mu}$g was linear (r ${\ge}$ 0.9996) with acceptable precision (% RSD ${\le}$5.2) and accuracy (% RE = 0.6 ~ -2.4). The enantiomeric compositions of flurbiprofen in one patch product and of ketoprofen in five different products were identified to be racemic with relatively good precision (${\le}$ 6.4%). The urinary excretion level of (R)-flurbiprofen was two times higher than its antipode, while the comparable excretion levels of (R)- and (S)-enantiomers for ketoprofen were observed.

• Biomolecules & Therapeutics
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• v.6 no.1
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• pp.45-49
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• 1998

The pharmacokinetic properties and antiinflammatory activity of 3% ketoprofen lotion (ID-lotion), formulated with poloxamer 407, were evaluated using rats. For the pharmacokinetic study, the lotion, at the dose of 4.5 mg/kg, was applied on the dorsal skin of rats and the drug concentration in plasma was determined using an HPLC method. As references, ketoprofen suspended in saline was administered orally, and E-lotion, which is a 3% ketoprofen lotion in the Japanese market was applied transdermally. Following the transdermal application of ID-lotion and E-lotion, $C_{max}$ were 316 $\pm$22.3 ng/ml and 163 $\pm$ 12.2 ng/ml, respectively, at the same Tma of 2 hours postdose, while $C_{max}$ and $T_{max}$ after oral administration of the drug were 1,030$\pm$89.1 ng/ml and 0.25 hours, respectively. Relative bioavailabilities of ID-lotion and I-lotion were 69.3% and 34.2%, respectively. The antiinflammatory activity of the two 3% ketoprofen lotions was evaluated with carrageeneninduced edema method after 50 mg of the lotions was applied on the paw of rats. ID-lotion showed 67.6% inhibition of the edema formation, while I-lotion showed 34.\\\\`r%. The calculated ED5o after transdermal application of ID-lotion was 2.5 mg/kg, while that after oral administration was 7.0 mg/kg. Based on these results, the relative equiponderal availability of ID-lotion was 296% compared to the oral administration of ketoprofen.n.n.n.

• KSBB Journal
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• v.29 no.4
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• pp.250-262
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• 2014

A simulation study for finding purity changes of extract and raffinate as well as the best purity of (S)-ketoprofen in simulated moving bed (SMB) was performed with changing parameters of $m_2$ and $m_3$ from triangle theory. Aspen simulator allowed separation process simulation of (R)- and (S)-ketoprofen in SMB and compared 4-bed SMB and 8-bed SMB based on the same Henry constant and mass transfer coefficient. The 4-bed SMB consisted of 4 columns (200 mm of length, 10 mm of diameter) and the 8-bed SMB constructed by 8 columns (100 mm of length, 10 mm of diameter), and therefore total column length was made the same as 800 mm. Considering purities of both (R)-and (S)-ketoprofen, both 4-bed SMB and 8-bed SMB had the best purity when $m_2$ and $m_3$ were on 12.0 and 13.0 in the center of triangle. Taking only (S)-ketoprofen into account, 4-bed SMB as well as 8-bed SMB had the best purity when $m_2$ and $m_3$ were on 10.9 and 12.6 in the left outside triangle, and their purities were 93.3 % for 4-bed SMB and 96.9 % for 8-bed SMB.