The chemical name for ketoprofen is 23benzoylphenylpropionic acid with the following structural formula. Ketoprofen drugs and lactation database lactmed ncbi. The objective of the study was to formulate micro particles of a poorly soluble drug ketoprofen with the aid of chitosan in presence of salting out agents. The ketoprofen regular capsule is also used to treat mild to moderate pain, or menstrual pain. Add the ethoxy diglycol to the ketoprofen in the weigh boat and dissolve the powder.
Wu and benet 2005 also assigned ketoprofen to bcs class 1 with regard to its disposition characteristics to estimate permeability. Owing to the lower solubility of the photoproducts, the solution became unclear and then an oily phase was. Formulation and characterization of ketoprofen liquisolid. The excited energy surfaces reveal that the neutral species will not decarboxylate, whereas the deprotonated acid decarboxylates spontaneously in the triplet state, and with an associated 3. Ketoprofen is one of the propionic acid class of nonsteroidal antiinflammatory drugs nsaid with analgesic and antipyretic effects. In the present study a rphplc procedure was developed and validated for the assessment of ketoprofen in human plasma. Drugs az pill identifier supplements symptom checker diseases dictionary media. It is used to reduce swelling and to treat mild to moderate pain.
Solubility and dissolution improvement of ketoprofen by. Pdf enhancement of ketoprofen and ibuprofen solubility and. Solubility enhancement of a poorly aqueous soluble drug. Ketoprofen has been shown not to induce drug metabolizing enzymes. Ketoprofen ktp is an antiinflammatory drug widely used in therapeutics. Ketoprofen extrel caps prescription and dosage sizes information for physicians and healthcare professionals. Nov 09, 2018 ketoprofen is a nonsteroidal antiinflammatory drug nsaid. Ketoprofen polylactidecoglycolide physical interaction.
It is widely used in the management and treatment of patients with. In antiinflammatory models ketoprofen has been shown to have inhibitory effects on prostaglandin and leukotriene synthesis, to have antibradykinin activity. The solubility of ketoprofen in the nonvolatile liquid vehicles glycerin, propylene glycol, tween 80, peg 400 and water was determined. It acts by inhibiting the bodys production of prostaglandin it was patented in 1967 and approved for medical use in 1980. Hbonding seems responsible for the glass transition temperature reduction and the limited solubility. Ketoprofen solubility in organic solvents and aqueous co.
Ketoprofen is mainly excreted in the urine as a glucuronide conjugate. Ketoprofen is a nonsteroidal antiinflammatory drug nsaid used in treatment of. Find patient medical information for ketoprofen oral on webmd including its uses, side effects and safety, interactions, pictures, warnings and user ratings. Improvement of the solubility and dissolution of ketoprofen using natural bile salts mohammed m.
Ketoprofen is a nonsteroidal antiinflammatory drug. As the aim of this study was to enhance the dissolution rate of drug, peg 400 was selected as the suitable nonvolatile solvent in the preparation of ketoprofen liquisolid compacts. This material is provided for educational purposes only and is not intended for medical advice, diagnosis or treatment. Ketoprofen is a propionic acid derivate and nonsteroidal antiinflammatory drug nsaid with antiinflammatory, analgesic and antipyretic effects. Drugcentral is online drug information resource created and maintained by division of translational informatics at university of new mexico. Nonsteroidal antiinflammatory compound that is selective for cox1. The solubility and dissolution rate of poorly watersoluble ketoprofen was. Ketoprofen is nonsteroidal antiinflammatory drug nsaid of propionic acid. The objective of the present research is to enhance the aqueous solubility of the poorly water soluble drug ketoprofen by formulation of solid dispersion systems with the use of gelucire. These drug substances are classified in the class 2 of the fdas biopharmaceutics classification system bcs of drugs fda, 2015 due to their low solubility and high permeability. Ketoprofen is a member of the nonsteroidal antiinflammatory drugs drug class and is commonly used for back pain, fever, frozen shoulder, and others. Solubility of nonsteroidal antiinflammatory drugs nsaids in neat organic solvents and organic solvent mixtures.
Ketoprofen, a widely prescribed analgesic drug which belongs to bcs class ii and exhibit low and variable oral bioavailability due to its poor aqueous solubility. Ketoprofen c16h14o3 cid 3825 structure, chemical names, physical and chemical. Bendazac diklofenak etofenamat felbinak flurbiprofen ibuprofen indometacin ketoprofen naproksen piroksikam suprofen coxinhibirajuci donori azot oksida naprokscinod. Ketoprofen ket 23benzoylphenyl propionic acid figure1 is a nonsteroidal antiinflammatory drug nsaids nonselective cox propionic acid derivative 1. Ketoprofen prices, coupons and patient assistance programs. Ibuprofen, ketoprofen, diclofenac, celecoxib, and etodolac are usually described as practically insoluble in water hydrophobic weakly acidic substances. The objective of the present research is to enhance the aqueous solubility of the poorly water soluble drug ketoprofen by formulation of solid dispersion systems with the use of gelucire 4414 and pvp k30 as a polymer in the formulation. This ketoprofen price guide is based on using the discount card which is accepted at most u. Solubility, the phenomenon of dissolution of solute in solvent to give a homogenous system, is one of the important parameters to achieve desired concentration of drug in systemic circulation for desired anticipated pharmacological response. Orudis ketoprofen capsule food and drug administration. Ketoprofen is a nonsteroidal antiinflammatory drug nsaid used to treat mild to moderate pain, and helps to relieve symptoms of arthritis osteoarthritis and rheumatoid arthritis, such as inflammation, swelling, stiffness, and joint pain.
Ketoprofen is a nonsteroidal antiinflammatory drug nsaid used in treatment of acute pain and chronic arthritis. Ketoprofen is in a class of medications called nsaids. Ketoprofen side effects, dosage, interactions drugs. The nsaids propionic acid derivatives have low water solubility. Ketoprofen, 100 mg, has been tried as a patch to directly deliver the compound to the site of injury.
Micromeritic properties were evaluated for cocrystal exhibiting higher solubility. Effect of different crystallization techniques on the dissolution. Ketoprofen actron is a nonselective nsaid with ic50 of 0. Ketoprofen shows dose linearity over a dose range of 50200 mg. Ketoprofen is one of the propionic acid class of nonsteroidal antiinflammatory drug nsaid with analgesic and antipyretic effects 1. Enhancing aqueous solubility of ketoprofen by fusion.
Ketoprofen drug interactions may also occur with medications such as ibuprofen, warfarin, lithium, and corticosteroids. This approach is useful for the improvement of solubility of poorly soluble drugs. Ketoprofen prevents the action of prostaglandin synthetase. The product is an fdaapproved nonnarcotic, nonsteroidal antiinflammatory agent with analgesic and antipyretic properties. While some drug interactions can cause one or both drugs to lose its effectiveness, others may cause bleeding, kidney damage, stomach ulcers, or other serious side effects. Drugs with higher solubility in the molten peo, when added at higher weight fractions, interfered with. Pdf encapsulation of ketoprofen and ketoprofen lysinate by. There are no known active metabolites of ketoprofen. Chitosan, in handbook of pharmaceutical excipients sixth ed, edited by. There is evidence for topic ketoprofen for osteoarthritis but not other chronic musculoskeletal pain. The solubility results showed that ketoprofen had significantly more solubility in peg 400 as compared with other nonvolatile solvents used in this study. Ketoprofen, tablet, 75 mg1, oral, red pharm drug, inc.
Mechanism of photoinduced decomposition of ketoprofen. Vultures feeding on the carcasses of recently treated livestock suffer acute kidney failure within days of exposure. Patients with reduced renal function may have conversion of the glucuronide conjugate back to the parent drug. Of 40 babies born with persistent pulmonary hypertension of the newborn pphn. Ketoprofen is soluble in organic solvents such as ethanol, dmso. Ketoprofen works by reducing hormones that cause inflammation and pain in the body. Ketoprofen has been linked to a low rate of serum enzyme elevations during therapy and to rare instances of clinically apparent acute liver injury. It exhibits antiinflammatory, analgesic and antipyretic effects. It works by stopping the bodys production of a substance that causes pain, fever, and inflammation.
The prepared ketoprofen cocrystals were characterized by ftir, dsc and xrd. The mechanism of increased dissolution rate of drugs by solid dispersion crystallization. Another opinion is that ketoprofen is a borderline case. Ket being used a nonsteroidal analgesic and antipyretic in argentina in. It serves as an efficient drug to treat ankylosing spondylitis, rheumatoid arthritis and osteoarthritis.
A shift in the ir peaks was observed for all the prepared cocrystals with no presence of additional peaks. Ketoprofen investigated as a drug, hormone, mutagen, primary irritant, and reproductive effector. One to 4 milk samples were collected between the 3rd and 4th dose of ketoprofen. For this purpose mobile phase consisting of methaol. Eighteen women were given ketoprofen 100 mg every 12 hours average 2. Nexcede ketoprofen dosing, indications, interactions.
Ketoprofen is a nonselective cox inhibitor and nonsteroidal antiinflammatory drug. Inspire a love of reading with prime book box for kids discover delightful childrens books with prime book box, a subscription that delivers new books every 1. This emedtv resource lists some of the drugs that may interact with ketoprofen and describes health problems that some drug interactions may cause. Ketoprofen oral route description and brand names mayo. As part of the trusted equine pain and sedation portfolio from zoetis, ketofen is safe and effective against equine pain and. Pharmacology, adverse reactions, warnings and side effects. Physicochemical characterization and in vitro dissolution studies of. Inspire a love of reading with prime book box for kids discover delightful childrens books with prime book box, a subscription that delivers new books every 1, 2, or 3 months new customers receive 30% off your first box. Determination of ketoprofen in human plasma by rphplc. Uvinduced decarboxylation of the nsaid ketoprofen, followed by activation of molecular oxygen or formation of a decarboxylated peroxide adduct, is explored using computational quantum chemistry. Ketoprofen is used to relieve pain from various conditions. Improvement of the solubility and dissolution of ketoprofen.
Only select registry of toxic effects of chemical substances rtecs data is presented here. Ketoprofen oral capsule is available as a generic drug. Use lecithin isopropyl palmitate solution to rinse the weigh boat and help quantitatively transfer the ketoprofen into the syringe. Ketoprofen oral capsule can interact with other medications, vitamins, or herbs you may be taking. Nonsteroidal antiinflammatory drugs, acetaminophen, and cox2 inhibitors. This medicine does not cure arthritis and will help you only as long as you continue to take it. The kinetic study revealed that, the drug release from all formulations followed zero order kinetics. Ketoprofen benzyl alcohol not specified rat 6 mgkgday reproductive toxicity, version. It also reduces pain, swelling, and joint stiffness from arthritis. Do not use in a horse if it has previously shown hypersensitivity to ketoprofen. Ketoprofen was introduced in 1973 in france and the united kingdom for antiinflammatory use.
We do not recommend storing the aqueous solution for more than one day. Natural polymers are used as drug carriers in ionic gelation because of their. Ketoprofen has low solubility in water and it is having dissolution problems. Nonprescription ketoprofen is used to relieve minor aches and pain from headaches, menstrual periods, toothaches, the common cold, muscle aches, and backaches, and to reduce fever. In this paper, ketoprofen and ketoprofen lysinate were used as model drugs in order to investigate release profiles of poorly soluble and very soluble drug from sodium alginate beads manufactured.
The possibility of increased interaction should be kept in mind when orudis ketoprofen doses greater than 50 mg as a single dose or 200 mg of ketoprofen per day are used concomitantly with highly bound drugs. This medication is a nonsteroidal antiinflammatory drug nsaid. List of approved drug products containing ketoprofen in the fda orange book on. Elimination the plasma clearance of ketoprofen is approximately 0. Potential ketoprofen drug interactions involve medications such as ibuprofen, aspirin, and lithium. Ketoprofen cocrystals were evaluated for solubility and dissolution. See what others have said about ketoprofen, including the effectiveness, ease of use and side effects. Ketoprofen is used to treat pain or inflammation caused by arthritis. Ketoprofen inhibits the activity of the enzymes cyclooxygenase i and ii, resulting in a decreased formation of precursors of prostaglandins and thromboxanes. Formulation of a fastdissolving ketoprofen tablet using freeze. Ketoprofen, a propionic acid derivative, is a nonsteroidal antiinflammatory. An interaction is when a substance changes the way a drug works.
This medicine may be used to treat osteoarthritis and rheumatoid arthritis, or painful monthly periods. Ketoprofen orudis, a highly potent and safe nonsteroidal antiinflammatory drug of the propionic acid derivative group, was synthesized in france by rhonepoulenc chemists in 1967, 3 years after the prototype ibuprofen. M for human recombinant cox1 and cox2, respectively target. Ketoprofen is a drug that belongs to a group of medicines called nonsteroidal antiinflammatory drugs, or more precisely to propionic acid derivatives. Cautions federal law restricts this drug to use by or on the order of a licensed veterinarian. Sigmaaldrich offers a number of ketoprofen products. Because the patch facilitates delivery of ketoprofen over a 24hour period, the drug remains continually present in the tissue adjacent to the site of application. Ketoprofen should be used with caution in patients with renal disease, renal impairment, or renal failure.
Pdf solubility and dissolution improvement of ketoprofen by solid. Find patient medical information for ketoprofen bulk on webmd including its uses, side effects and safety, interactions, pictures, warnings and user ratings. Learn about drug interactions between ibuprofen oral and ketoprofen oral and use the rxlist drug interaction checker to check drug combinations. The effect of chitosan in presence of salting out agent predominated drug dissolution rate with the increasing concentrations of chitosan.
Contraindications there are no known contraindications to this drug when used as directed. To enhance the solubility and dissolution rate of poorly water soluble drug ketoprofen, selfmicro emulsifying drug delivery system smedds was developed and evaluated. Synthesis, biological activity and molecular modeling studies of novel cox1 inhibitors. Enhancement of solubility and dissolution of poorly. Ketoprofen is a nonsteroidal antiinflammatory drug with analgesic and antipyretic properties. Ketoprofen is a nonsteroidal antiinflammatory drug nsaid. Be alert for signs of drug induced hepatitis, including anorexia, abdominal pain, severe nausea and vomiting, yellow skin or eyes, skin rashes, flulike symptoms, and musclejoint pain. Ketoprofen ketoprofen dose, indications, adverse effects. The following drug interactions were studied with ketoprofen doses of 200 mgday. Ingredient quantity physical description solubility therapeutic activity ketoprofen 10% wv white powder soluble in alcohol, acetone, chloroform antiinflammatory ethoxy diglycol 20% vv clear, unctuous liquid na solvent.
Brillouin spectroscopy and molecular dynamics simulation data suggest that ketoprofen solubility increases with temperature and nonpolar interactions are responsible for this phenomenon. Ketoprofen is classified as fda pregnancy risk category d drug if used during the third trimester due to the potential for prostaglandin synthetase inhibitors to cause in utero constriction of the fetal ductus arteriosus. Ketoprofen c16h14o3 cid 3825 structure, chemical names, physical and chemical properties. Experiments have found ketoprofen, like diclofenac, is a veterinary drug causing lethal effects in redheaded vultures. The results suggested that lm as a natural solubilizer added promising results in enhancing the solubility and dissolution of the poorly water soluble drugs as kp. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities as well as for the generic development. Ketoprofen fda orange book approved drug product list. The antiinflammatory, analgesic and antipyretic properties of ketoprofen have been demonstrated in classical animal and in vitro test systems.
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