Drugs ketoprofen

Morita N, Kusuhara H, Nozaki Y, et al. Functional involvement of rat organic anion transporter 2 (Slc22a7) in the hepatic uptake of the nonsteroidal anti-inflammatory drug ketoprofen. Drug Metab Dispos 2005 33 1151-1157. 

Nonsteroidal antiinflammatory drugs (ketoprofen, naproxen, flurbiprofen, indomethacin, ibuprofen) CEC Hypersil C18/SCX, 3 pm Acetonitrile-50 mM Na2HPC>4-water (60 20 20) 210 mm x 50 pm i.d. 138... 

Alternatively, Huntington and Cormier used non-ionic surfactants, including dodecanol and 1,2-dodecanediol, to enhance the delivery of the anionic drug, ketoprofen. Because non-ionic surfactants are not directly affected by the applied electric field, their use may be preferred over ionic surfactants. 

There are few smdies on the in vivo efficacy and irritancy of terpenes used as an enhancer in percutaneous absorption. The percutaneous absorption-promoting effect and skin irritancy of cyclic monoterpenes were investigated in rats and with rabbits, respectively (Okabe etal., 1990). Plasma concentration of the drug (ketoprofen) markedly increased with the addition of the hydrocarbons of cyclic monoterpenes such as trans- -methane and d-limonene. Irritancy of cyclic monoterpenes in rabbits was evaluated using the Draize scoring method. No skin irritation was observed when ethanol-containing hydrocarbons of cyclic monoterpenes (trans-p-menthane and d-limonene) were applied to dorsal skin. 

The release of two chiral drugs, ketoprofen and ricobendazole, from matrix tablets that are produced with two different excipients (a chiral cellulose polymer, HPMC, and an achiral acrylic polymer, Eudragit RL) was investigated by Alvarez et al. [31]. In the case of ketoprofen from... 

Moren J, Francois T, Blanloeil Y, Pinaud M. The effects of a nonsteroidal antiinflammatory drug (ketoprofen) on morphine respiratory depression a double-blind, randomized study in volunteers. Anesth Analg (1997) 85, 400-5. 

The results are in agreement with the recent release study of nonsteroidal drug ketoprofen [6]. Despite the fact that the ketoprofen release was studied by different techniques and therefore the release rate values are not comparable directly, the same tendency was observed. Additionally, it has been shown [34] that incorporation of ketoprofen does not alter the microemulsion system significantly however, its presence prevents the formation of stronger interaction and formation of gel-like structure in water rich region. It was also found out that stronger interactions between microemulsion components in W/O as well in the bicontinuous phase lead to slower ketoprofen release. Because of similar molecule structure of ibuprofen the same could be assumed also for it. We can conclude that release behavior of ibuprofen is influenced with the microstructure and can be predicted to a certain extent, using a combination of several tested methods for physical characterization of microemulsions. 

Oral delivery is desirable due to the ease of administration, lower cost, and increased patient compliance. Despite these advantages, oral delivery of macromolecules is challenging due to low penetration across the intestinal epithelial barrier. To circumvent these barriers, drugs have been attached to mac-romolecular carriers such as dendrimers that can potentially aid in absorption across the intestinal epithelium. PAMAM dendrimers are effectively transported across epithelial barriers (Wiwattanapatapee et al. 2000 El-Sayed et al. 2002 Kitchens et al. 2006). SN-38, a potent anticancer drug, when complexed with PAMAM dendrimers showed increased solubility and uptake by Caco-2 cells (Kolhatkar et al. 2008). Orally administered anti-inflammatory drug ketoprofen in the form of PAMAM complexes (Man et al. 2006) prolonged activity and increased bio availability with a sustained release profile. 

Electropherograms of a urine sample (8 ml) spiked with non-steroidal anti-inflammatory drugs (10 p-g/ml each) after direct CE analysis (b) and at-line SPE-CE (c). Peak identification is as follows I, ibuprofen N, naproxen K, ketoprofen P, flurbiprofen. Reprinted from Journal of Chromatography, 6 719, J. R. Veraait et al., At-line solid-phase exti action for capillary electrophoresis application to negatively charged solutes, pp. 199-208, copyright 1998, with permission from Elsevier Science. 

Ketoprofen, a weak-acid drug, with a pKa 4.12 (25°C, 0.01 M ionic strength), was selected to illustrate Eqs. (7.20) and (7.21) in a series of simulation calculations, as shown in Fig. 7.16. The membrane-buffer apparent partition coefficients /(piii were calculated at various pH values, using the measured constants from... 

At pH 3, ketoprofen is mostly in an uncharged state in solution. The dashed curve in Fig. 7.16 corresponding to pH 3 shows a rapid decline of the sample in the donor well in the first half-hour this corresponds to the membrane loading up with the drug, to the extent of 56%. The corresponding appearance of the sample in the acceptor well is shown by the solid line at pH 3. The solid curve remains at zero for t < xLAG. After the lag period, the acceptor curve starts to rise slowly, mirroring in shape the donor curve, which decreases slowly with time. The two curves nearly meet at 16 h, at a concentration ratio near 0.22, far below the value of 0.5, the expected value had the membrane retention not taken a portion of the material out of the aqueous solutions. 

Figure 7.40 Permeability-pH profiles for ketoprofen under iso-pH conditions for two different PAMPA models unfilled circles = 2% DOPC/dodecane, filled circles = 20% soy lecithin/dodecane. [Reprinted from Avdeef, A., in van de Waterbeemd, H. Lennemas, H. Artursson, P. (Eds.). Drug Bioavailability. Estimation of Solubility, Permeability, Absorption and Bioavailability. Wiley-VCH Weinheim, 2003 (in press), with permission from Wiley-VCH Verlag GmbH.]...

For therapeutic drugs, the highest concentrations in the raw sludge corresponded to the analgesics diclofenac (209 ng g ) and ibuprofen (135 ng g-1), and the sulfonamide antibiotic sulfathiazole (143.0 ng g-1). Next in abundance were the diuretic compounds furosemide (79.9 ng g-1) and hydrochlorothiazide (41.3 ng g-1), and the analgesic ketoprofen (42.4 ng g-1). The remaining PhC were found at concentrations below 40 ng g The list of the 24 detected... 

Mooney et al. [70] investigated the effect of pH on the solubility and dissolution of ionizable drugs based on a film model with total component material balances for reactive species, proposed by Olander. McNamara and Amidon [71] developed a convective diffusion model that included the effects of ionization at the solid-liquid surface and irreversible reaction of the dissolved species in the hydrodynamic boundary layer. Jinno et al. [72], and Kasim et al. [73] investigated the combined effects of pH and surfactants on the dissolution of the ionizable, poorly water-soluble BCS Class II weak acid NSAIDs piroxicam and ketoprofen, respectively. 

Crison, G. L. Amidon. pH and surfactant-facilitated in vitro solubilization and dissolution of ketoprofen, a class II drug. Implications for waiver of bioavailability and bioequivalence studies (Unpublished). 

GI absorption of many poorly soluble drugs depends on small intestinal transit, as demonstrated for ketoprofen, nifedipine, haloperidol, miconazole, and others. Small intestinal transit rate and transit time become important factors in drug absorption, particularly when the ratio of dose to solubility is high and dissolution rate is very slow or when the drug is... 

K. Akira, T. Taira, H. Hasegawa, C. Sakuma, Y. Shinohara, Studies on the Stereoselective Internal Acyl Migration of Ketoprofen Glucuronides Using 13C Labehng and NMR Spectroscopy , Drug Metab. Dispos. 1998, 26, 457 - 464. 

Analysis of non-steroidal anti-inflammatory drugs (ibuprofen, ketoprofen, naproxen, fenoprofen, flurbiproen, and suprofen) Impurity profiling of ketorolac, a chiral nonsteroidal antiinflammatory drug Impurity profiling of a non-steroidal analgesic drug... 

Other inhibitors of COX are collected under the general term nonsteroidal antiinflammatory drugs (NS AlDs). Several of these are available OTC, including ibuprofen (Advil, Motrin), naproxen (Aleve), and ketoprofen (Orudis). About 25 drugs in this class have been approved for use in cliiucal medicine in the United States, including the four just mentioned. Others are available by prescription only. 

NSAiDs (nonsteroidai anti-infiammatory drugs) inhibitors of cyclooxygenase, including aspirin, ibuprofen, and ketoprofen, among many others. 

Oruvail is a proprietary preparation of ketoprofen and Feldene is a proprietary preparation of piroxicam, both of which are non-steroidal antiinflammatory drugs Nootropil is a proprietary preparation of piracetam, which is not a non-steroidal anti-inflammatory drug. Nootropil is indicated as adjunctival treatment in cortical myoclonus. 

Rubefacients act by counter-irritation produced as a result of local vasodilation, resulting in a warm sensation that masks the pain. Counter-irritants should not be applied on broken skin or before or after taking a hot shower. Examples of counter-irritants include salicylates, nicotinates, capsicum, menthol and camphor. Ketoprofen is an example of a non-steroidal anti-inflammatory drug that is available as a topical preparation indicated in painful musculoskeletal conditions. 

Fig. 4.3 CSF concentration/free (unbound) plasma concentration ratios for neutral and basic drugs 1, ritropirronium 2, atenolol 3, sulpiride 4, morphine 5, cimetidine 6, meto-prolol 7, atropine 8, tacrine 9, digoxin 10, propranolol 11, carbamazepine 12, ondansetron 13, diazepam 14, imipramine 15, digitonin 16, chlorpromazine and acidic drugs, a, salicylic acid b, ketoprofen c, oxyphenbutazone and d, indomethacin compared to log D.

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