What Is Indomethacin?

It is suitable for antipyretic and relieving inflammatory pain, so it can be used for acute and chronic rheumatoid arthritis, gouty arthritis and cancer pain (western medicine cancer pain medicine); it can also be used for bursitis, tenosynovitis and joint capsule Inflammation, etc .; can prevent platelet aggregation, so it can prevent thrombosis, but the effect is not as good as acetylsalicylic acid; it has a good antipyretic effect in the treatment of Behcet syndrome; it is particularly effective for Batter syndrome; it is used for biliary colic and ureteral stones The colic caused is effective; it also has a certain effect on migraine and can also be used for menstrual pain.

Indomethacin

It is suitable for antipyretic and relieving inflammatory pain, so it can be used for acute and chronic rheumatoid arthritis, gouty arthritis and

Common name: Indomethacin

Chinese alias: indomethacin, anti-inflammatory indolic acid; indomethacin; Kuboxin; Mitaxin; Yishiding; indoxin; Adidos; sports pie; 2-methyl-1- (4 -Chlorobenzoyl) -5-methoxy-1H-indole-3-acetic acid

English name: Indomethacin methanol solution; indomethacin crystalline; indomethacin usp; indometacin; 1- (4-chlorobenzoyl) -5-methoxy-2-methylindol-3-ylacetic acid; {1-[(4-chlorophenyl) carbonyl] -5- methoxy-2-methyl-1H-indol-3-yl} acetate

CAS number: 53-86-1

EINECS number: 200-186-5

Molecular formula: C19H16ClNO4

Molecular weight: 357.79

Melting point: 155-162 ° C

Boiling point: 499.4 ° C at 760 mmHg

Flash point: 255.8 ° C

Vapor pressure: 8.61E-11mmHg at 25 ° C

Properties: white or light yellow crystalline powder. Almost odorless and odorless.

Solubility: soluble in acetone, slightly soluble in ethanol, ether, chloroform and methanol, slightly soluble in benzene, very slightly soluble in toluene, almost insoluble in water Soluble in sodium hydroxide solution.

Molecular weight: 357.878764 [g / mol]

Molecular formula: C19H16ClNO4
Hydrophobic parameter calculation reference value (XlogP): 4.3

Number of hydrogen-bonded donors: 1
Number of hydrogen bond acceptors: 4
Number of rotatable chemical bonds: 4

Accurate quality: 357.076786
Isotope mass: 357.076786
Topological molecular polar surface area (TPSA): 68.5
Number of heavy atoms: 25
Formal charge: 0

Complexity: 506
Number of isotope atoms: 0
Determine the number of atomic stereocenters: 0
Uncertain number of atomic stereocenters: 0
Determine the number of chemical bond stereocenters: 0
Uncertain number of chemical bond stereocenters: 0
Number of covalent bond units: 1
Number of functional 3d receptors: 4

Functional 3d anion number: 1
Function 3 d ring number: 3
Number of effective rotors: 5
Conformational isomer sampling RMSD: 0.8
Number of CID conformers: 25

Acute and chronic rheumatoid arthritis, gouty arthritis and cancer pain (western medicine cancer pain medicine); can also be used for bursitis, tenosynovitis and arthritis

Oral: 25mg each time at the beginning, 2 or 3 times a day, at meals or immediately after meals (can reduce gastrointestinal adverse reactions). In the treatment of rheumatoid arthritis, if no adverse reactions are seen, it can be gradually increased to 125 to 150 mg per day.

At present, gelatin pills or suppositories are also used to reduce the incidence of gastrointestinal side effects. Suppositories have the characteristics of maintaining a long duration of efficacy. Generally, 10 days is a course of treatment.

1. Common adverse reactions are gastrointestinal reactions (nausea, vomiting, abdominal pain, diarrhea, ulcers, and sometimes cause

Method name: Indomethacin API-Determination of Indomethacin-Neutralization Titration.

Application range: This method uses the titration method to determine the content of indomethacin in the indomethacin drug substance.

This method is applicable to indomethacin APIs.

Principle of the method: After the test sample is dissolved in ethanol, water and a phenolphthalein indicator solution are added, and the titration is performed with a sodium hydroxide titration solution, and the result of the titration is corrected by a blank test. The content of indomethacin is calculated according to the amount of the titration solution used.

Reagents: 1. ethanol

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

3. Phenolphthalein indicator

4. Reference potassium hydrogen phthalate

equipment:

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.

Operation steps: Precisely weigh about 0.5g of the test sample, add 30mL of ethanol, dissolve at low temperature, let cool, add 20mL of water, add 7 ~ 8 drops of phenolphthalein indicator solution, and quickly titrate with sodium hydroxide titration solution (0.1mol / L) And correct the titration results with a blank test. Each 1mL of sodium hydroxide titration solution (0.1mol / L) is equivalent to 35.78mg of C19H16ClNO4.

Note: "Precision weighing" means that the weighed weight should be accurate to one thousandth of the weighed weight. "Precision measurement" means that the accuracy of measuring the volume should meet the accuracy requirements of the volume pipette in national standards.

References: Pharmacopoeia of the People's Republic of China, compiled by the National Pharmacopoeia Committee, Chemical Industry Press, 2005 edition, Part Two, p.254.

(1) This product and

1. Tablets: 25mg each. 2. Gelatin pills: 25mg, 75mg per capsule. 3. Suppositories: 25mg, 75mg, 100mg each. 4. Injection: 1mg, 10mg, 20mg. 5. Cream: 100mg, 10g.

1. Avoid taking indomethacin with fruit juice or refreshing drink: The fruit acid of fruit juice or refreshing drink can easily cause the drug to decompose or dissolve in advance, which is not conducive to the absorption of the drug in the small intestine, which greatly reduces the efficacy of the drug. It has a stimulating effect, and fruit acid can aggravate the stimulation of the stomach wall and even cause gastric mucosal bleeding.

2. Do not take indomethacin before or after drinking: because

1, indomethacin and

I. Allergic reactions: After taking the medicine, it can cause numbness in the mouth, tongue and extremities. Sudden discomfort, headache, nausea, unfavorable language, whole body tremor, uncontrollable, and even fainting. In some cases, systemic vascular edema and rash occur. There are also patients with asthma-like attacks. So if you have allergies and

Numbering	Toxicity type	testing method	Test object	Dosage used	Toxic effect
1	Acute toxicity	oral	Adult woman	10 mg / kg	1. Behavioral toxicity-coma
2	Acute toxicity	oral	Adult male	4286 ug / kg / 2D-I	1. Skin and accessory toxicity-dermatitis (after systemic exposure)
3	Acute toxicity	oral	Adult male	15 mg / kg / 2W-I	1. Hematological toxicity-aplastic anemia
4	Acute toxicity	oral	baby	400 ug / kg / 2D-I	1. Gastrointestinal toxicity-necrosis
5	Acute toxicity	oral	Adult woman	2098 ug / kg / 1D-I	1. Kidney, ureter and bladder toxicity-changes in renal tubules (including acute renal failure, acute tubular necrosis) 2. Kidney, ureter and bladder toxicity-decreased urine output
6	Acute toxicity	oral	Adult male	22500 ug / kg / 3W-I	1. Liver toxicity-hepatitis, fiber (cirrhosis, post-necrotic scar) 2. Liver toxicity-other changes
7	Acute toxicity	oral	Adult male	22500 ug / kg / 3W-I	1. Gastrointestinal toxicity-large gastrointestinal ulcer or bleeding
8	Acute toxicity	oral	Adult male	714 ug / kg	1. Behavioral toxicity-general anesthesia 2. Behavioral toxicity-convulsions or seizure thresholds affected 3. Behavioral toxicity-ataxia
10	Acute toxicity	Intravenous injection	baby	200 ug / kg	1. Hematological toxicity-bleeding
12	Acute toxicity	Rectal injection	Adult male	2586 mg / kg / 3.5YI	1. Eye toxicity-changes in the retina (pigmentation, retinitis, others)
13	Acute toxicity	Multiple ways	Adult male	3557 mg / kg / 5Y-I	1. Eye toxicity-changes in the retina (pigmentation, retinitis, others)
67	Reproductive toxicity	oral	Adult woman	1500 ug / kg, 36 weeks after female conception	1. Reproductive toxicity-abnormal development of the respiratory system 2. Reproductive toxicity-other effects on newborns
68	Reproductive toxicity	oral	Adult woman	1500 mg / kg, 27 weeks after female conception	1. Reproductive toxicity-abnormal development of the cardiovascular circulatory system
69	Reproductive toxicity	oral	Adult woman	12 mg / kg, females 33-34 weeks after conception	1. Reproductive toxicity-stillbirth of newborn
70	Reproductive toxicity	oral	Adult woman	525 mg / kg, after 16-32 weeks of female conception	1. Reproductive toxicity-affecting childbirth 2. Reproductive toxicity-affecting mother 3. Reproductive toxicity-abnormal development of the urinary system
71	Reproductive toxicity	Intravenous injection	Adult woman	18 mg / kg, females 33-34 weeks after conception	1. Reproductive toxicity-steady state abnormal development
72	Reproductive toxicity	Not reported	Adult woman	6 mg / kg, 39 weeks after female conception	1. Reproductive toxicity-abnormal development of the urinary system
73	Reproductive toxicity	Not reported	Adult woman	4 mg / kg, 10 weeks after female conception	1. Reproductive toxicity-abnormal development of the urinary system
74	Reproductive toxicity	Not reported	Adult woman	2 mg / kg, 28 weeks after female conception	1. Reproductive toxicity-abnormal development of the urinary system 2. Reproductive toxicity-abnormal development of the body at steady state
75	Reproductive toxicity	Not reported	Adult woman	12 mg / kg, 32 weeks after female conception	1. Reproductive toxicity-stillbirth of newborn
76	Reproductive toxicity	Not reported	Adult woman	14 mg / kg, 34 weeks after female conception	1. Reproductive toxicity-has other effects on newborns
77	Reproductive toxicity	Multiple ways	Adult woman	22 mg / kg, 33 weeks after female conception	1. Reproductive toxicity-abnormal development of the central nervous system 2. Reproductive toxicity-affecting the Apgar score of newborns (humans only)
78	Reproductive toxicity	Rectal injection	Adult woman	12 mg / kg, 28 weeks after female conception	1. Reproductive toxicity-abnormal development of blood and lymphatic system (including spleen and bone marrow) 2. Reproductive toxicity-abnormal development of the gastrointestinal system 3. Reproductive toxicity-abnormal development of the urinary system