What Is Ketoprofen?

Ketoprofen is a chemical that is a white crystalline powder; it is odorless or almost odorless. Very soluble in methanol, easily soluble in ethanol, acetone or ether, almost insoluble in water. Melting point is about 93-96 ° C. It is an arylalkanoic acid compound. With analgesic, anti-inflammatory and antipyretic effect. The anti-inflammatory effect is stronger than ibuprofen, with less side effects and low toxicity. Oral easily absorbed from the gastrointestinal tract. After one dose, about o. Peak plasma concentrations can be reached in 5 to 2 hours. t 1/2 is 1.6 to 1.9 hours. Strong binding to plasma proteins in blood. The excretion rate from urine within 24 hours is 30% to 90%. It is mainly excreted as glucuronic acid conjugate. It is used for rheumatoid arthritis, rheumatoid arthritis, osteoarthritis, joint hardening spondylitis and gout.

Drug Name: Keto ibuprofen
Alias: Ketoprofen
Foreign name: ketoprofen

Main indications: Rheumatoid arthritis, rheumatoid arthritis, osteoarthritis, etc.
Adverse reactions: Bowel, stomach upset or rash, headache, tinnitus
Main medication contraindications: Caution for pregnant and lactating women

Ketoprofen Basic Information

Chinese name: Keto ibuprofen

Chinese alias: ketoprofen; -methyl-3-benzoyl phenylacetic acid; dexketoprofen; (+)-(S) --benzoyl-phenylacetic acid; (S)-(+) -Ketoprofen; dexketoprofen; dexketoprofen

English name: ketoprofen

English alias: Ketoprofen, 98%; 2- (3-benzoylphenyl) propionic acid; (S)-(+)-ketoprofen; S-(+)-Ketoprofen; S) -ketoprofen; Dexketoprofen; p-Bromothioanisole; (2S) -2- (3-benzoylphenyl) propanoic acid ^[1]

CAS: 22071-15-4; 22161-81-5

EINECS: 244-759-8

Molecular formula: C16H14O3

Molecular weight: 254.2806

Ketoprofen physical and chemical properties

Melting point: 93-96 & ordm; C

Property description: Appearance: white or off-white crystalline powder, anti-inflammatory analgesic. Quality index: Content: 98.5-1050 Heavy metal: 10ppm Loss on drying: 0.5 Sulfate: 0.1

Ketoprofen method

Ketoprofen-determination of ketoprofen-neutralization titration

Ketoprofen application range

This method uses neutralization titration to determine the content of ketoprofen (C16H14O3).

This method is applicable to the determination of ketoprofen.

Ketoprofen method principle

Take an appropriate amount of test product, dissolve it with neutral ethanol (significantly neutral to phenolphthalein), use phenolphthalein as the indicator solution, and titrate with sodium hydroxide titration solution (0.1mol / L). Each 1mL of sodium hydroxide titration solution (0.1mol / L) is equivalent to 25.43mg of C16H14O3, which is calculated.

Reagent:

1. Water (newly boiled to room temperature)

Neutral ethanol

3. Sodium hydroxide titration solution (0.1mol / L)

4. Phenolphthalein indicator liquid

5. Reference potassium phthalate

Ketoprofen sample preparation

1. Sodium hydroxide titration solution (0.1mol / L)

Preparation: Take an appropriate amount of sodium hydroxide, add water and shake to dissolve it into a saturated solution. After cooling, place it in a polyethylene plastic bottle and let it stand for several days. Take 5.6mL of a clear saturated sodium hydroxide solution, add freshly boiled cold water to 1000mL, and shake well.

Calibration: Take about 0.6g of standard potassium hydrogen phthalate dried to constant weight at 105 ° C, weigh it accurately, add 50mL of freshly boiled cold water, shake it to dissolve it as much as possible, add 2 drops of phenolphthalein indicator solution, When this solution is titrated, when the end point is reached, potassium hydrogen phthalate should be completely dissolved and titrated until the solution becomes pink. Each 1mL of sodium hydroxide titration solution (0.1mol / L) is equivalent to 20.42mg of potassium hydrogen phthalate. Calculate the concentration of this solution based on the consumption of this solution and the amount of potassium hydrogen phthalate taken.

Storage: Put it in a polyethylene plastic bottle and keep it in a sealed container. There are 2 holes in the plug. One glass tube is inserted into the hole. One tube is connected to the soda lime tube. One tube is used to suck out the liquid.

Phenolphthalein indicator

Take 1 g of phenolphthalein and add 100 mL of ethanol to dissolve.

Ketoprofen steps

Take about 0.5g of this product, accurately weigh, add 25mL of neutral ethanol (phenolphthalein indicator solution is neutral), add 3 drops of phenolphthalein indicator solution, and titrate with sodium hydroxide titration solution (0.1mol / L).

Note 1: "Precision weighing" means that the weighed weight should be accurate to one thousandth of the weight. Precision requirements.

Note 2: "Determination of moisture" uses the drying method, taking 2 to 5 g of the test sample, and spreading it in a flat weighing bottle that is dry to constant weight, the thickness does not exceed 5 mm, and the loose test sample does not exceed 10 mm. Open the bottle cap and dry at 100 ~ 105 ° C for 5 hours. Place the cap on the dryer, cool it for 30 minutes, and weigh it precisely. Then dry it at the above temperature for 1 hour, cool, and weigh until two times in a row. The difference in weighing does not exceed 5 mg. Calculate the moisture content (%) in the test product based on the weight lost. ^[2]

Ketoprofen usage

Oral: 50mg each time, 150mg a day. 3 to 4 times; or 100mg each time, 3 times a day, and later changed to 2 times a day. To avoid gastrointestinal irritation, take it after meals and swallow the entire capsule.

Ketoprofen indications

The anti-inflammatory effect is stronger than ibuprofen, with less adverse reactions and low toxicity. Oral easily absorbed from the gastrointestinal tract. It is used for rheumatoid arthritis, rheumatoid arthritis, osteoarthritis, joint hardening spondylitis and gout.

Ketoprofen instructions

[] Ketoprofen [Note]

Adverse reactions are similar and mild to ibuprofen and are generally tolerable. Mainly gastrointestinal reactions. A small number of people develop drowsiness, headaches, and palpitations. Patients with gastric and duodenal ulcers are contraindicated.

[Formulation] Enteric-coated capsules: 25 mg per capsule; 50 mg.

Ketoprofen adverse reactions

This product is well tolerated and has low side effects. It is usually caused by intestinal and gastric discomfort or rash, headache, and tinnitus.

Ketoprofen precautions

Patients with gastrointestinal disease who are cautious and who have a history of bronchial asthma may cause bronchospasm, and patients who use anticoagulants should monitor their prothrombin time at all times. Use with caution in pregnant women and lactating women. Use with caution, overdose may cause headache, vomiting, drowsiness, and hypotension can disappear on its own.

[Other names] Ibuprofen, Ibuprofen, and Rage.

[Indications] The analgesic and anti-inflammatory mechanism of this product has not been fully clarified, and it may play a local role in inflammatory tissues by inhibiting the synthesis of prostaglandins or other stimulating transmitters.

This product is suitable for antipyretic and relieves moderate pain such as arthritis, neuralgia, muscle pain, headache, migraine, dysmenorrhea, toothache, cold and flu symptoms.

[Adverse reactions] Occasionally mild indigestion, rash, gastrointestinal ulcers and bleeding, elevated aminotransferase.

[Precautions]

(1) People who are allergic to aspirin or other non-steroidal anti-inflammatory drugs have cross-allergic reactions to this product.

(2) Use with caution in pregnant and lactating women.

(3) Use with caution in patients with asthma, cardiac insufficiency, hypertension, hemophilia and other bleeding disorders, peptic ulcers, and renal insufficiency.

[Contraindications]

(1) Those who are severely allergic to aspirin or other steroid drugs are contraindicated.

(2) Disabled in patients with nasal polyps syndrome and angioedema.

[Warning] If you experience gastrointestinal bleeding, liver and kidney damage, vision impairment, blood abnormalities, and allergic reactions during medication, you should immediately stop the medication and go to the hospital for a doctor.

[medicine interactions]

(1) Alcohol and concurrent use with other non-steroidal anti-inflammatory drugs can increase gastrointestinal side effects and also cause the risk of ulcers.

(2) When used with aspirin or other salicylic acid drugs, the efficacy cannot be increased, and the incidence of gastrointestinal side effects and bleeding tendency increases.

(3) Used with anticoagulant drugs to increase the risk of bleeding.

(4) This product can enhance the effect of antidiabetic drugs; reduce the antihypertensive effect of antihypertensive drugs; the same use with corticosteroids can significantly reduce the symptoms of inflammation.

(5) Should not be used with methotrexate to prevent poisoning.

(6) When used with probenecid, verapamil and nifedipine, pay attention to reducing the dose; when using it with digoxin, pay attention to adjusting the dose of digoxin.

[] Ketoprofen [Dosage and Administration]

Oral: 200 mg per adult, 1 to 3 times a day, up to 800 mg per day; slow release agents can be 300 mg each time, 1 to 2 times a day.

Children 1 to 3 times a day, 20 to 30 mg for children under 1 year of age; 60 mg for 1 to 3 years of age; 100 mg for 4 to 6 years of age; 150 mg for 7 to 9 years of age; 180 mg once; 200 mg each over 12 years.

Topical: 5%, 3 times a day.

[Formulation] Tablet, sustained release tablet, sustained release capsule, granule, oral solution, suppository, cream, tincture, compound.

[Pharmacokinetics] Oral absorption is easy, absorption slows down when taken with food, but absorption does not decrease. Taken with antacids containing aluminum and magnesium does not affect absorption. The plasma protein binding rate was 99%. After taking the drug, the blood concentration reached a peak in 1.2-2.1 hours, and the dosage was 200 mg. The blood concentration is 22-27g / ml, 23-45g / ml when 400mg is used, and 43-57g / ml when 600mg is used. T1 / 2 is usually 1.8-2 hours after a single administration. After 5 hours of taking the drug, the concentration of synovial fluid is equal to the concentration of blood drug, and the concentration of synovial fluid is higher than the plasma concentration within the next 12 hours. This product is metabolized in the liver, 60% -90% is excreted by the urine through the kidney, 100% is excreted within 24 hours, of which about 1% is the original form, and some are excreted with feces.

[Pharmacology and toxicology] Ibuprofen is an effective cyclooxygenase inhibitor with antipyretic, analgesic and anti-inflammatory effects.

[Specifications] 0.3g

[Storage] shading, store in a cool and dry place.

Ketoprofen drug interactions

(1) Alcohol and concurrent use with other non-steroidal anti-inflammatory drugs can increase gastrointestinal side effects and also cause the risk of ulcers.

(2) When used with aspirin or other salicylic acid drugs, the efficacy cannot be increased, and the incidence of gastrointestinal side effects and bleeding tendency increases.

(3) Used with anticoagulant drugs to increase the risk of bleeding.

(5) Should not be used with methotrexate to prevent poisoning.

(6) When used with probenecid, verapamil and nifedipine, pay attention to reducing the dose; when using it with digoxin, pay attention to adjusting the dose of digoxin.

Ketoprofen Safety Information

Safety instructions: S26: In case of contact with eyes, rinse immediately with plenty of water and take to a doctor.

S45: If you have an accident or feel unwell, go to your doctor for help immediately (preferably bring the product container label).

Dangerous goods mark: T: Toxic substance

Danger category code: R25: Toxic if swallowed.

R36 / 37/38: Irritating to eyes, respiratory tract and skin.

Dangerous Goods Transport Number: UN2811