• Journal of Korean Society of Environmental Engineers
• /
• v.32 no.2
• /
• pp.219-226
• /
• 2010

In order to evaluate a removal characteristic of chloramphenicol, salicylic acid and ketoprofen according to dose of oxidants, $Cl_2$, $O_3$ and $O_3/H_2O_2$ are used as oxidants in this study. In case of that $Cl_2$ is used for oxidizing harmaceuticals, chloramphenicol, salicylic acid and ketoprofen is not removed entirely at $Cl_2$ dose rang of 0.5~5.0 mg/L for 60 min. However, removal tendency of salicylic acid is so obviously at $Cl_2$ dose higher than 1.0 mg/L. In addition, as $Cl_2$ dose and contact time increase, the removal rate of salicylic acid is enhanced. When $O_3$ is used as oxidant, chloramphenicol and ketoprofen is not eliminated at $O_3$ dose range of 0.2~2.0 mg/L. On the contrary, 30~70% of salicylic acid is removed at $O_3$ dose of 1.0~5.0 mg/L. Only 30% removal of salicylic acid is achieved at contact time of 5 min, however, the removal rate is enhanced remarkably at contact time over 10 min. In experiments using $O_3/H_2O_2$ as an oxidant, we can find that $O_3/H_2O_2$ is much more effective than $O_3$ only for removal of 3 pharmaceuticals, and the efficiency is raised according to increase of $H_2O_2$ dose. On reaction rate constant and half-life of 3 pharmaceuticals depending on $Cl_2$, $O_3$ and $O_3/H_2O_2$ dose, experiments using $O_3/H_2O_2$ show that oxidation of pharmaceuticals is less effective as the $H_2O_2/O_3$ ratio increases to above pproximately 1.0 related to reaction rate constant. An oxidation of salicylic acid by $Cl_2$ and $O_3$ particularly has a comparatively high reaction rate constant comparing $O_3/H_2O_2$, and thus salicylic acid is easily eliminated in oxidation processes.

• Archives of Pharmacal Research
• /
• v.10 no.1
• /
• pp.25-28
• /
• 1987

(+)-Ketoprofen was obtained form resolution with (S) (+)-2-amino-1-butanol and its absolute configuration was determined to be (S) by chemical correlation with (S) (+)-ethyl hydratropate using Beckmann rearrangement as a key step.

• Proceedings of the PSK Conference
• /
• 2002.10a
• /
• pp.410.2-411
• /
• 2002

Ketoprofen (KP), a potent analgesic and non-steroidal anti-inflammatory drug, has some disadvantages such as gastro-intestinal irritation. short half-life (1.5-4 hour) in plasma and low solubility in aqueous solution. In order to minimize these disadvantages. we have recently prepared a KP prodrug, KP-polyethylene glycol conjugate (KPEG750, PEG Mw=750), and investigated its pharmacokinetic behavior. anti-inflammatory and analgesic effect. (omitted)

• Journal of Veterinary Clinics
• /
• v.31 no.3
• /
• pp.220-222
• /
• 2014

A 14 year-old Shih-tzu was referred to the Veterinary Medical Teaching Hospital of Chungnam National University with a history of foreign body ingestion and vomiting. The vomitus contained ketoprofen plaster, which is used for orthopedic analgesia in humans. Supportive care and gastrointestinal (GI) protective agents were administered, including famotidine, misoprostol, sucralfate, omeprazole, and fluid therapy. However, the clinical signs worsened, and anemia, melena, leukocytosis, and azotemia developed. The patient was diagnosed with GI hemorrhage and underwent a whole blood transfusion followed by barium sulfate administration. After administering barium sulfate as a GI protectant, the clinical signs improved, and the patient was discharged.

• The Korean Journal of Pain
• /
• v.12 no.2
• /
• pp.211-216
• /
• 1999

Background: Transdermal fentanyl patch (TDFP) is a simple, noninvasive analgesic with continuous effect. The aim of this study was to evaluate the postoperative analgesic effect of TDFP. Methods: Sixty healthy patients undergoing cesarean section were divided into 3 groups. Postoperative pain was controlled with different methods; Group I: application of TDFP-$25{\mu}g/hr$, Group II: intramuscular injection of ketoprofen; Group III: continuous epidural block. Pain scores (numerical rating scale, NRS), number of patients who needed additive ketoprofen injections and side effects were recorded at 8, 20, 32, 44 hours postoperatively. Results: There was no significanant difference in pain score between Group I and Group II. The numbers of patients who need additive ketoprofen injections were lower in group I than group II. Pruritis (25%), nausea/vomiting (10%), leg numbness (40%) was experienced in group III, but not in Group I & II. Conclusions: TDFP-$25{\mu}g/hr$ for postoperative pain control is simpler and more convinient than intramuscular injection of analgesics.

• Journal of Pharmaceutical Investigation
• /
• v.26 no.4
• /
• pp.245-256
• /
• 1996

Solid lipid nanoparticles (SLN) have been developed as a new drug delivery system. Although many particulate drug carriers, such as microsphere, liposome, niosome, emulsion, etc. have been introduced, they have some disadvantage; low efficiency of incorporation and stability, lack of reproducibility, and so on. Meanwhile, SLN as a new drug delivery system is known to entrap rugs with a high efficiency and a good reproducibility. Moreover, small size SLN can circulate in blood for a prolonged time. Although many preparation methods were introduced, microfluidization method is recommended to be the most useful. This study was attempted to prepare and evaluate ketoprofen-incorporated SLNs (keto-SLN), which were prepared by two methods, ultrasonication and microfluidization. Keto-SLN was evaluated by measurement of particle size and zeta potential, efficacy of entrapment, sedimentation volume, in virto release pattern. The mean particle size was about $0.1\;{\mu}m$, and the size was dependent on the type and the amount of emulsifier. Zeta potential was negative, $-9{\sim}-13mV$ and entrapment efficacy was very high and stability was good for at least 60 days in the respect of particle size and sedimentation volume ratio. Analgesic effect was also determined as well as pharmacokinetic parameters. The former was comparable to that of that of ketoprofen loaded suspension (keto-sus) and the latter revealed that consistent with the delayed release of keto-SLN. $T_{max}$ was longer than keto-sus. Therefore, keto-SLN was favourable dosage forms in the field of drug delivery system such as anti-cancer, analgesics and anti-inflammatory agents.

• 한국생물공학회:학술대회논문집
• /
• 2001.11a
• /
• pp.652-655
• /
• 2001

The comparative study of enzymes that catalyze a similar reactions but have different substrate spectrum and/or stereospecificity is a powerful approach to understanding the reaction mechanism between the relative enzymes, and it was also an useful tool to cloning the related enzyme, without the typical cloning from DNA library of genomic pools. For this purpose, we conducted an approach that the comparison at the molecular and protein level of esterases, from various sources including a previously identified (S)-stereospecific esterase of Pseudomonas sp. ES1. As expected, we found an esterase family genes that shared a high similarity at the protein and genetic level in the identical genus Pseudomonad. The striking structural and biochemical identity strongly suggested the family genes to be an identical one. We, hence, aligned the family genes and designated a degenerated primer for PCR-cloning using six Pseudomonas strains as templates. As a result, a recombinant esterase from Pseudomonas fluorescens KCTC 1767 was cloned and high-level expressed with high selectivity to (R,S)-ketoprofen ethyl ester. The enzyme exhibited a high ester-hydrolyzing activity to (S)-ketoprofen but did not hydrolyzed the opposite stereoisomer. Further characteristics were discussed in our presentation.

• 한국생물공학회:학술대회논문집
• /
• 2002.04a
• /
• pp.445-448
• /
• 2002

The Pseudomonas fluorescens KCTC 1767, a selected and identified as potential candidate for stereo-specific resolution of rac-ketoprofen ethyl ester, was systematically investigated in order to induce the high level expression and detailed characterization of the expressing enzyme esterase. We cloned the esterase gene from chromosomal DNA of Pseudomonas fluorescens KCTC 1767 by PCR with two synthetic primers that desinged for simple purification. The recombinant esterase from Pseudomonas fluorescens KCTC 1767 exibited a high conversion rate and enantioselectivity to the (S)-ketoprofen ethyl ester as expected. The enzyme was easily purified to homogeniety by using a metal chelating affinity chromatography as a protein with poly histidine taq, and thus obtained 0.6 mg of protein from a 100 mL culture broth in a single step. The purified enzyme was steadily stable at the pH range from 7.0 to 10. The activity was also retained to be about 70% after the preincubation at $40^{\circ}C$ but over $50^{\circ}C$ lost the activity completely. The molecular mass of the esterase was estimated to be about 43 kDa on SDS-PAGE, and an identical result was also shown in gel filteration chromatography. The specific activity was calculated 27 mM/mg-protein/min by using the rac-ketoprofen ethly ester as a substrate.

• YAKHAK HOEJI
• /
• v.45 no.5
• /
• pp.506-512
• /
• 2001

Ketoprofen (KP) was formulated as a transdermal patch using the percutaneous penetration enhancers sorbitan monmmleate(SMO), polyvinylpyrrolidone(PVP). The control patch without penetration enhancers showed a KP flux of 8.9$\pm$0.75$\mu\textrm{g}$/$\textrm{cm}^2$/h The flux was increased in proportion to the concentration of SMO added. Furthermore, lag times were decreased upon addition of SMO. Conversely; the skin flux of KP was decreased in proportion to the concentration of PVP added. Pharmacokinetic parameters including $C_{max}$, $T_{max}$, and AUC were increased when SMO was added. However, $C_{mas}$ significantly decreased by the addition of PVP. $T_{max}$ was not significantly different in 2%, 4%, and 8% PVP patches. Patches containing 4% PVP showed the highest AUC value (19.158$\mu\textrm{g}$.h/ml). We found that the effectiveness of the two percutaneous penetration enhancers for topical KP patches was similar, with the addition of appropriate amounts of HPC modifying both skin flux and lag time of KP in the patches. In conclusion, it is possible to manufacture KP patches exhibiting high AUC, high skin flux, and short lag time using percutaneous penetration enhancers of SMO and PVP.

• Journal of Pharmaceutical Investigation
• /
• v.22 no.1
• /
• pp.17-29
• /
• 1992