Contraindicated in patients with hypersensitivity to the drug special precautions while taking ketoprofen topical 1. Solubility, dissolution, and partitioning applied physical pharmacy. Enter your mobile number or email address below and well send you a link to download the free kindle app. Ketoprofen should not be used in animals with a known allergy or hypersensitivity to the drug. Buy formulating poorly water soluble drugs aaps advances in the pharmaceutical sciences series book 3. The solubility of ketoprofen in pamam dendrimer solutions in the range 010 mgml was determined at ph 3, 4 and 6 in phosphate buffers 0. The antiinflammatory effects of ketoprofen are believed to be due to inhibition cylooxygenase2 cox2, an enzyme involved in prostaglandin synthesis via the arachidonic acid pathway. Ketoprofen has been linked to a low rate of serum enzyme elevations during therapy and to rare instances of clinically apparent acute liver injury. Summary this chapter considers three application fields important in drug development and drug production. Also, in italy and spain it is available as an overthecounter drug otc under the trade name enantyum.
The solubility of ketoprofen in the nonvolatile liquid vehicles glycerin, propylene. If your doctor has directed you to use this medication, remember that he or she has judged that the benefit to you is greater than the risk of side effects. Ketoprofen fda prescribing information, side effects and uses. Solubility enhancement of a poorly aqueous soluble drug. Indications, dose, contraindications, sideeffects, interactions, cautions, warnings and other safety information for ketoprofen. Fenoprofen has been linked to a low rate of serum enzyme elevations during therapy and to rare instances of clinically apparent acute liver injury. Strategies for the formulation development of poorly soluble drugs. The drug in fdt is characterized by dsc, xrd and sem and evaluated for saturation solubility at ph 1. This medication is a nonsteroidal antiinflammatory drug nsaid. Ketoprofen is used to relieve pain from various conditions. Ketoprofen oral capsule, extended release 200mg drug medication dosage information.
Dexketoprofen is a nonsteroidal antiinflammatory drug nsaid. Dissociation by dilution is considered as major release mechanism of drugs from complex. Dissolution is important for health practitioners because, for drugs to be. Oct 31, 2010 a crucial step in this direction is the determination of the level of drug present in the polymer phase if the latter is fully equilibrated with the pharmaceutical compound in the crystalline state, i. The drug solubility in the nonvolatile solvents is an important parameter in formulation of liquisolid compacts. Avoid contact with eyes, inside the nose, inflamed or broken skin 3. M for human recombinant cox1 and cox2, respectively target. Ketoprofen is a nonsteroidal antiinflammatory drug nsaid. Drugs az pill identifier supplements symptom checker diseases dictionary media. In the pharmaceutical industry, solubility predictions form part of the early stage lead optimisation process of drug. Biochemistry, dissolution and solubility statpearls ncbi bookshelf. This medicine may be used to treat osteoarthritis and rheumatoid arthritis, or painful monthly periods. Ketoprofen oral capsule, extended release 200mg drug. Solubility of ketoprofen in colloidal plga sciencedirect.
Permeability, solubility, dissolution, and charged state of ionizable molecules. Formulating poorly water soluble drugs aaps advances in the. The solubility results showed that ketoprofen had significantly more solubility in peg 400 as compared with other nonvolatile solvents used in this study. Synonyms sodium fenoprofen unii 869607j16q cas number 346911 weight average. Percentage yield, drug content and particle size distribution. Further, this book is designed to provide practical guidance for overcoming formulation challenges toward the end goal of improving drug therapies with poorly. Use of fastum gel from menarini, pregnancy, lactation in childrens and special precautions for fastum gel from menarini, prices of. Various techniques are used for the enhancement of the solubility of poorly soluble drugs which include physical and chemical modifications of.
The compiled solubility data were retrieved primarily from the chemical and pharma. In order to improve the solubility of the drug in water, addition of surface active agents and formation of watersoluble salts were carried out and to enhance dissolution and absorption rate, increasing the wettability and micronization of drug particles has often been used to increase the bioavailability of poorly watersoluble drug molecules. Sigmaaldrich offers a number of ketoprofen products. Ketoprofen is a nonsteroidal antiinflammatory drug. Ketoprofen is one of the propionic acid class of nonsteroidal antiinflammatory drug nsaid with analgesic and. Summary poor aqueous solubility, slow dissolution rate, and low permeability are. Ketoprofen has low solubility in water and it is having dissolution problems. This book is distributed under the terms of the creative commons. Fenoprofen is a propionic acid derivative with analgesic, antiinflammatory and antipyretic properties. These are generally known, easily measured, or easily calculated. Fastum gel from menarini, ketoprofen ketofen to vofane ketoprofen, rs23benzoylphenylpropionic acid chemical formula c16h14o3 is one of the propionic acid class of nonsteroidal antiinflammatory drug nsaid with analgesic and antipyretic effects. Then you can start reading kindle books on your smartphone, tablet, or computer.
Following the administration of capsules or entericcoated tablets in man, 25% to 90% of the drug. The supercritical treatment allows these pharmaceutical formulations to be prepared without the use of any auxiliary agents or organic solvents. Solubility is the maximum concentration of a solute that can dissolve in a solvent at. Ketoprofen actron is a nonselective nsaid with ic50 of 0. 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 lecithin isopropyl palmitate solution 22% vv viscous, tan solution na vehicle, surfactant. Ketoprofen works by reducing hormones that cause inflammation and pain in the body. They are often obtained by coupling crystalline drugs with a biocompatible polymer, such as polyethylene glycol, hydroxypropylmethylcellulose, polyvinylpyrrolidone, etc. Jun 01, 2019 ketoprofen is a nonsteroidal antiinflammatory drug.
It is widely used in the management and treatment of patients with rheumatic disease, but its poor water. In addition, ketoprofen can be used to treat menstrual. An antiinflammatory analgesic and antipyretic highly bound to plasma proteins. Ketoprofen drug information, uses, side effects, chemistry. Preparation and the biopharmaceutical evaluation for the. I wisdom dwell with prudence, and find out knowledge of witty inventions. As greater the solubility, the more would be the drug particles dissolved in the liquid vehicle prior to the adsorption onto the carrier materials. 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. Fenoprofen is a nonsteroidal antiinflammatory drug nsaid used in the treatment of acute pain and chronic arthritis. The problem of low aqueous solubility of natural cds can be addressed by. Pdf solubility and dissolution improvement of ketoprofen. The only inputs used in the gse are the celsius melting point mp and the octanol water partition coefficient kow. Effect of cyclodextrin derivatization on solubility and efficacy of drugs.
Ketoprofen is a nonsteroidal antiinflammatory drug nsaid used in treatment of acute pain and chronic arthritis. The chemical name for ketoprofen is 23benzoylphenylpropionic acid with the following structural formula. It is used to reduce swelling and to treat mild to moderate pain. Prediction of drug solubility by the general solubility. Conversely, a solute can be very soluble, yet require a protracted amount of time to arrive at the final, saturation concentration. Ketoprofen ketoprofen dose, indications, adverse effects. Dissolution studies are carried out and compared with physical mixture pm and pure. It is pharmacologically similar to aspirin, but causes less gastrointestinal bleeding. This emedtv resource lists some of the drugs that may interact with ketoprofen and describes health problems that some drug interactions may cause. The influence of cyclodextrin and ph on the solubility of.
One of the major reasons a drug fails is that it cannot be absorb by the body in a way to have the effect it was intended to have. Learn about the reported side effects, related class drugs, and how these medications will affect your daily lifestyle. Describe the role of drug dissolution from dosage forms in drug. The ketoprofen partition between supercritical co2 and poly. Then you can start reading kindle books on your smartphone, tablet, or computer no kindle device required. The revised general solubility equation gse proposed by jain and yalkowsky is used to estimate the aqueous solubility of a set of organic nonelectrolytes studied by jorgensen and duffy. Ketoprofen by mouth national library of medicine pubmed. This medicine does not cure arthritis and will help you only as long as you continue to take it.
Solubility studies in various nonvolatile solvents. Formulation and characterization of ketoprofen emulgels. Many times drugs work fine when tested outside the body, but when they are tested in the body they fail. If any of these effects persist or worsen, tell your doctor or pharmacist promptly. It is manufactured by menarini, under the tradename keral. 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. Nonsteroidal antiinflammatory drug nsaid structurally related to ibuprofen.
This might be due to increase in the viscosity of polymer around the drug. Sep, 2019 ketoprofen is a nonsteroidal antiinflammatory drug nsaid. Ketoprofen prevents the action of prostaglandin synthetase. Solubility is the property of a solid, liquid or gaseous chemical substance called solute to.
It also reduces pain, swelling, and joint stiffness from arthritis. Various qualitative and quantitative parameters like spray pattern, pump seal efficiency test, average weight per metered dose, and dose uniformity were evaluated. The aim of this study was to investigate the influence of both cyclodextrin and ph on the overall solubility of ketoprofen. The method used for sample preparation was similar for each system, i. It is a propionic acid derivative and is a nonsteroidal antiinflammatory agent nsaia with analgesic and antipyretic properties. Ketoprofen is one of the propionic acid class of nonsteroidal antiinflammatory drug nsaid with analgesic and antipyretic effects 1. Introduction drug delivery systems are pharmaceutical devices able to control the amount of a drug in the human body. Fenoprofen inhibits prostaglandin synthesis by decreasing the enzyme needed for biosynthesis. A veterinarian should be contacted immediately if an overdose is suspected, the symptoms of which can be gi ulcers, renal toxicity, severe laminitis, anorexia, depression, icterus, abdominal swelling, and gastrointestinal and renal effects. Synthesis and antiinflammatory activity of novel ketoprofen and ibuprofen derivatives sadik al mekhlafi 1, hussein alkadi 2 and mohammedi kotb elsayed3 1department of medicinal chemistry, faculty of pharmacy, sanaa university, sanaa, yemen 2department of medicinal chemistry, faculty of medicine, sanaa university, sanaa, yemen.
Permeability funded by the iacp and pba research funds. The impact of stability on the topical penetration of ketoprofen compounded in. The ketoprofen partition between supercritical co2 and. 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. A crucial step in this direction is the determination of the level of drug present in the polymer phase if the latter is fully equilibrated with the pharmaceutical compound in the crystalline state, i. Helps drug discovery professionals to eliminate poorly absorbable molecules.
Drug interactions with ketoprofen oral and labetalol iv. Accurately weighed quantity of formulation was transferred to a 100 ml volumetric flask containing 50 ml of methanol and allowed to stand for 5 h with intermittent sonication to ensure complete solubility of the drug. Fastum gel from menarini, ketoprofen ketofen to vofane. Ketoprofenum pharmacopeia online, drug, pharmaceutical.
Ketoprofen is used to treat pain or inflammation caused by arthritis. Synthesis and antiinflammatory activity of novel ketoprofen. In patients with rheumatoid arthritis, the antiinflammatory action of fenoprofen has been evidenced by relief of pain, increase in grip strength, and reductions in joint swelling, duration of. Jan 01, 2017 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. Cyclodextrin complexation and ph adjustments have been reported as useful tools to increase the solubility of drug. Thermodynamic analysis of the solubility of ketoprofen in. Upset stomach, constipation, diarrhea, dizziness, lightheadedness, drowsiness, loss of appetite, or headache may occur. Learn about drug interactions between ketoprofen oral and labetalol iv and use the rxlist drug interaction checker to check drug combinations. Pranoprofen is a nonsteroidal antiinflammatory drug used in ophthalmology.
Ketoprofen is only found in individuals that have used or taken this drug. Hands should be washed immediately after use pregnancy related. The drug is 99% bound to plasma proteins, mainly to the albumin fraction. Cd were used for the preparation of inclusion complex by shaking method in aqueous. Metabolites as well as the unchanged drug are excreted mainly in the urine. The ketoprofen regular capsule is also used to treat mild to moderate pain, or menstrual pain. Formulation and characterization of ketoprofen liquisolid.
Potential ketoprofen drug interactions involve medications such as ibuprofen, aspirin, and lithium. Calculate the ph of precipitation for weak electrolytes in aqueous and mixed solvent systems. 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. Ultraviolet and visible absorption spectrophotometry 2. Drug delivery systems are pharmaceutical devices able to control the amount of a drug in the human body. It is available in the uk, as dexketoprofen trometamol, as a prescriptiononly drug and in latin america as enantyum, produced by menarini. Polyamidoamine dendrimers used as solubility enhancers of. Determination of drug content the prepared emulgels were tested for the drug content uniformity. Nonsteroidal antiinflammatory compound that is selective for cox1.
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