MeloxicaM, BP
Meloxicam
CAS: 71125-38-7
Molecular Formula: C14H13N3O4S2
MeloxicaM, BP - Names and Identifiers
| Name | Meloxicam |
| Synonyms | Meloxicam MeloxicaM API MeloxicaM, BP MeloxicamUsp27 MeloxicaM (Mobic) Meloxicam (400 mg) 4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-1,1-dioxide-2H-1,2-benzothiazine-3-carboxamide 4-HYDROXY-2-METHYL-N-(5-METHYL-2-THIAZOLYL)-2H-1,2-BENZOTHIAZINE-3-CARBOXAMIDE 1,1-DIOXIDE 4-Hydroxy-2-methyl-N-(5-methyl-1,3-thiazol-2-yl)-2H-1,2-benzothiazin-3-crboxamide 1,1-dioxide 4-Hydroxy-2-Methyl-N-(5-Methylthiazol-2-yl)-2H-benzo[e][1,2]thiazine-3-carboxaMide 1,1-dioxide 4-hydroxy-2-methyl-N-(5-methyl-1,3-thiazol-2-yl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide Sodium 2-methyl-3-[(5-methyl-1,3-thiazol-2-yl)carbamoyl]-2H-1,2-benzothiazin-4-olate 1,1-dioxide |
| CAS | 71125-38-7 |
| EINECS | 615-253-8 |
| InChI | InChI=1/C14H13N3O4S2/c1-8-7-15-14(22-8)16-13(19)11-12(18)9-5-3-4-6-10(9)23(20,21)17(11)2/h3-7,18H,1-2H3,(H,15,16,19) |
| InChIKey | ZRVUJXDFFKFLMG-UHFFFAOYSA-N |
MeloxicaM, BP - Physico-chemical Properties
| Molecular Formula | C14H13N3O4S2 |
| Molar Mass | 351.4 |
| Density | 1.613±0.06 g/cm3(Predicted) |
| Melting Point | 255 °C |
| Water Solubility | practically insoluble in water(0.154 mg/mL), with higher solubility observed in strong acids and bases. |
| Solubility | Soluble in water (22 mg/ml), DMSO (25 mg/ml), DMF, acetone(slightly soluble), ethanol(sli |
| Appearance | Bright yellow powder |
| Color | yellow |
| Merck | 14,5826 |
| pKa | 4.08 in water; 4.24 ± 0.01 in water/ethanol (1:1); 4.63 ± 0.03 in water/ethanol (1:4) |
| Storage Condition | 2-8°C |
| Stability | Stable. Incompatible with strong oxidizing agents. |
| Sensitive | Sensitive to heat |
| Refractive Index | 1.72 |
| MDL | MFCD00868752 |
| Physical and Chemical Properties | Crystallization from dichloromethane, melting point 254 °c (decomposition). pKa:4.08 water; 4.24±0.01 water-ethanol (1:1);4.63±0.03 water-ethanol (1:4). Acute toxicity LD50 mice (mg/kg):470 oral. |
| Use | For the treatment of rheumatoid arthritis, painful osteoarthritis |
MeloxicaM, BP - Risk and Safety
| Risk Codes | R22 - Harmful if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. R25 - Toxic if swallowed |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S60 - This material and its container must be disposed of as hazardous waste. S36/37 - Wear suitable protective clothing and gloves. |
| UN IDs | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS | DL0702000 |
| HS Code | 29349990 |
| Hazard Class | 6.1 |
| Packing Group | III |
| Toxicity | LD50 orally in mice: 470 mg/kg (Trummlitz, 1980) |
MeloxicaM, BP - Reference
| Reference Show more | 1. Song Yanbo, Zhao Guishan, Ru Xiaofei, Hou Xiaolin, Mengzhou, Li Xinjie, Meng Qingrong, Wang Xiaodong. Preparation of artificial antigen and polyclonal antibody of indomethacin [J]. Animal husbandry and veterinary medicine 2019 51(10):44-48. 2. [IF = 3.535] Hui Jiang et al."Determination of lipid-water partition coefficient of neutral and ionic drugs by lipid chromatography." Electrophoresis. 2021 Aug;42(14-15):1436-1449 3. [IF = 3.935] Hui Jiang et al."Preparation of covalently bonded lipid capilary column and its application in evaluation of drug membrane permeability." J Pharmaceut Biomed. 2022 Feb;209:114513 |
MeloxicaM, BP - Nature
Open Data Verified Data
yellow crystalline powder. Melting point 254 °c (decomposition). Slightly soluble in chloroform, slightly soluble in dilute hydrochloric acid, dilute aqueous sodium hydroxide solution, almost insoluble in water. pK. 4.24 soil 0.01 water-ethanol (1:1); 0.03 soil water-ethanol (1 1 4).
Last Update：2024-01-02 23:10:35
MeloxicaM, BP - Preparation Method
Open Data Verified Data
4-hydroxy -2-methyl -2H-1,2 benzothiazole-3-carboxylic acid methyl ester -1,1-= oxide and 2-amino -5-methyl thiazole were refluxed in xylene to give meloxicam.
Last Update：2022-01-01 09:09:28
MeloxicaM, BP - Standard
Authoritative Data Verified Data
This product is 2-methyl-4-hydroxy-n-(5-methyl-2-thiazolyl)-2H-l, 2-benzothiazine-3-carboxamide -1,1-dioxide. Calculated as dried product, containing no less than 98.5% of C14H13N304S2.
Last Update：2024-01-02 23:10:35
MeloxicaM, BP - Trait
Authoritative Data Verified Data
- This product is yellowish to yellowish or yellowish green to yellowish green crystalline powder; Odorless.
- This product is dissolved in dimethylformamide, slightly soluble in acetone, slightly soluble in methanol or ethanol, and almost insoluble in water.
Last Update：2022-01-01 14:19:11
MeloxicaM, BP - Use
Open Data Verified Data
developed by Boedriger Ingelheim, launched in South Africa in 1996. Non-steroidal anti-inflammatory drugs. For the symptomatic treatment of rheumatoid arthritis and painful osteoarthritis.
Last Update：2022-01-01 09:09:29
MeloxicaM, BP - Differential diagnosis
Authoritative Data Verified Data
- take about 30mg of this product, put it in a test tube, burn, the gas generated can make the wet lead acetate test paper black.
- take about 10mg of this product, add 5ml of chloroform to dissolve, add 1 drop of ferric chloride test solution, shake, after placing, the chloroform layer is light purple red.
- take this product, add 0.1 mol /L sodium hydroxide solution is dissolved and made into a solution containing about 7ug per 1 ml, which has the maximum absorption at the wavelengths of 270nm and 362nm as determined by ultraviolet-visible spectrophotometry (General rule 0401), there is minimal absorption at a wavelength of 312mm.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 998).
Last Update：2022-01-01 14:19:11
MeloxicaM, BP - Safety
Open Data Verified Data
mouse oral LD50: 470mg/kg.
Last Update：2022-01-01 09:09:29
MeloxicaM, BP - Exam
Authoritative Data Verified Data
clarity of the solution
take 2.5g of this product, add 50ml of dimethylformamide to dissolve, and the solution should be clear.
Related substances
take this product, Add alkaline methanol solution (take 40% methanol solution, add 0.4mol/L sodium hydroxide solution 6ml, mix evenly) dissolve and dilute to prepare a solution containing about 1 mg per 1 ml, as a test solution, 1 ml was accurately measured, placed in a 100ml measuring flask, diluted to a scale with the above alkaline methanol solution, and shaken to obtain a control solution. Test according to high performance liquid chromatography (General 0512). Silica gel bonded with eighteen alkyl silane was used as filler, and methanol -0.lmol/L ammonium acetate solution (1:1) was used as mobile phase. The detection wavelength was 270Nm. The number of theoretical plates is not less than 2000 based on the meloxicam peak. 20ul of the control solution and the test solution were injected into the liquid chromatograph respectively, and the chromatogram was recorded to 6 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than 0.5 times (0.5%) the area of the main peak of the control solution, and the sum of the areas of each impurity peak shall not be greater than the area of the main peak of the control solution (1.0%).
residual solvent
take the right amount of this product, precision weighing, plus O. 1 mol/L sodium hydroxide solution was dissolved and prepared to contain meloxicam in about 0.lg of the solution, as the test solution; Another ethanol, N,N-dimethylformamide, Tetrahydrofuran, dichloromethane, toluene and xylene each appropriate amount, precision weighing, with O. 1 mol/L sodium hydroxide solution is made into a mixed solution containing about 0.5mg of ethanol, 0.088mg of N,N-dimethylformamide, 0.072mg of tetrahydrofuran, 0.06mg of dichloromethane, 0.089mg of toluene and 0.217mg of xylene per 1 ml, as a control solution. 10ml of each of the reference solution and the test solution were accurately measured and placed in the headspace bottle and sealed. According to the test for determination of residual solvents (General rule 0861 second method), the capillary column with 6% cyanopropylphenyl-94% dimethylpolysiloxane (or similar polarity) as stationary liquid is used as the column; The initial temperature is 40 ℃, maintain 8 minutes, at a rate of 30°C per minute to 150°C, maintain 10 minutes; Injection port temperature is 230°C; Detector temperature is 250°C; Headspace bottle equilibrium temperature is 100°C, the equilibration time was 30 minutes. Take the reference solution into the headspace, the separation degree between the peaks of each component shall meet the requirements. Then the reference solution and the test solution were injected into the headspace, and the chromatogram was recorded. The residual amount of ethanol, N,N-dimethylformamide, Tetrahydrofuran, dichloromethane, toluene and xylene shall be calculated by peak area according to external standard method.
chloride
take anhydrous sodium carbonate 2G, spread on the bottom and around the Crucible, take this product l. Put it on anhydrous sodium carbonate, wet it with a small amount of water, dry it, burn it with small fire to make it ash completely, let it cool, add appropriate amount of water to dissolve it, filter it, wash the Crucible and filter with water, combine filtrate and wash solution, add water to make 20ml, shake well, take 1ml of filtrate, add Dropwise nitric acid to make neutral, add 1 drop of nitric acid, shake well, heat in a water bath at 75-85°C, remove hydrogen sulfide, cool, add 1% sodium carbonate solution Dropwise to make it neutral, add water to make it 0801, and check it according to law (general rule), not more concentrated (0.1%) than the control solution made from of standard sodium chloride solution.
loss on drying
take this product, dry to constant weight at 105°C, weight loss shall not exceed 0.5% (General rule 0831).
ignition residue
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
Heavy metals
The residue left under the item of taking the ignition residue shall not contain more than 10 parts per million of heavy metals and shall be inspected according to law (General rule 0821 second law).
arsenic salt
take 1.0g of this product, add lg of calcium hydroxide, mix well, add 2ml of water Dropwise, mix well, dry, burn with small fire to charring, and then burn at 500~600°C to ash, cold, add hydrochloric acid 5M l and water 23ml, according to the law inspection (General Principles 0822 The first law), should comply with the provisions (0.0002%).
Last Update：2022-01-01 14:19:12
MeloxicaM, BP - Content determination
Authoritative Data Verified Data
take this product about 0.4g, precision weighing, precision plus sodium hydroxide titration solution (0.1 mol/L)25ml, dissolved at a slight temperature, cooled, added with 100ml of neutral ethanol (neutral to the indicator solution of bromothymol blue), added with 10 drops of indicator solution of bromothymol blue, titration with hydrochloric acid titration solution (0/1 mol/L), and the results of the titration with blank test correction. Each 1 ml of sodium hydroxide titration solution (0.1 mol/L) corresponds to 35.14mg of C14H13N304S2.
Last Update：2022-01-01 14:19:13
MeloxicaM, BP - Category
Authoritative Data Verified Data
antipyretic analgesic, non-steroidal anti-inflammatory drugs.
Last Update：2022-01-01 14:19:13
MeloxicaM, BP - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 14:19:13
MeloxicaM, BP - Meloxicam Tablets
Authoritative Data Verified Data
This product contains meloxicam (C14H13N3O4S2) should be 90.0% ~ 110.0% of the label amount.
trait
This product is light yellow or yellow or film-coated tablets, after removing the film-coated pale yellow or yellow.
identification
- take an appropriate amount of the fine powder of this product (about 15mg of meloxicam), add chloroform (10ml) to shake to dissolve meloxicam, filter, add 3 drops of ferric chloride solution to the filtrate, shake, after placement, it showed light purple-red color.
- take the sample solution under the content determination item of this product and measure it by UV-Vis spectrophotometry (General rule 0401), with maximum absorption at 270mn and 362nm wavelength, there is minimal absorption at a wavelength of 312nm.
- take an appropriate amount of the fine powder of this product (about 20mg of meloxicam), add 10ml of trichloromethane, dissolve meloxicam by ultrasonic oscillation, filter, and take the continued filtrate as the test solution, add chloroform to dissolve and dilute to prepare solution containing 2mg per 1 ml as a reference solution, according to thin layer chromatography (General 0502) test, take the above two Solutions 10 u1, on the same silica gel GF254 thin layer plate, respectively, with chloroform-methanol-diethylamine (60:5:7.5) as the developing solvent, spread out, dry, put under UV light (254nm) for inspection, the position and color of the main spot displayed by the test solution should be consistent with the main spot of the control solution.
- take an appropriate amount of the fine powder of this product and the reference substance of meloxicam, and add alkaline methanol solution (take 40% of methanol solution and add 6mL of 0.4mol/L sodium hydroxide solution, mix well) dissolve and dilute to make about O per 1 ml. lmg solution, as the test solution and the reference solution, according to the related substances under the chromatographic conditions, record chromatogram. The retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the control solution.
- two items (3) and (4) above can be selected as one item.
examination
- Related substances take the fine powder of this product, Add alkaline methanol solution (take 40% methanol solution 100ml, add 0.4mol/L sodium hydroxide solution 6ml, mix well) dissolve and dilute to make a solution containing about 1 mg per 1ml, filter, and take the filtrate as the test solution; Take 1ml for precision measurement and put it in a 100ml measuring flask, as a control solution, it was diluted to the scale with the above basic methanol solution and shaken. If there are impurity peaks in the chromatogram of the test solution, except for the chromatographic peaks whose relative retention time is less than 0.30, the single impurity peak area shall not be greater than 0.5 times (0.5%) of the main peak area of the control solution, and the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%).
- Content uniformity take 1 tablet of this product, put it in a 100ml measuring flask, add 0.0941 of 1 mol/L sodium hydroxide solution, according to the method under the content determination item, from the "ultrasonic oscillation to dissolve meloxicam", according to the law, the determination shall comply with the regulations (general).
- dissolution the dissolution of this product was determined according to the dissolution and release determination method (General rule 0931 second method), and the dissolution medium was 7.4 phosphate buffer (pH), and the rotation speed was 75 revolutions per minute, according to the law, after 45 minutes, take the solution, filter, take the filtrate as the test solution; Another meloxicam control about 20mg, precision weighing, 100ml flask, add 0.lmol/L sodium hydroxide solution 10ml, ultrasonic to dissolve, then dilute to the scale with dissolution medium, shake well, take 2ml accurately, put it in 50ml measuring flask (7.5mg specification) or 25ml measuring flask (15mg specification), dilute to the scale with dissolution medium, shake, as a reference solution; Take the above two solutions, the absorbance was measured at a wavelength of 0401 nm by ultraviolet-visible spectrophotometry (general), and the elution amount of each tablet was calculated. The limit is 75% of the labeled amount and shall be in accordance with the provisions.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
Take 20 tablets of this product, precision weighing, fine grinding, precision weighing an appropriate amount (about equivalent to meloxicam 7.5mg), put it in a 100ml measuring flask, add 0.1 mol/L sodium hydroxide solution 10ml and methanol 40ml, sonicated to dissolve meloxicam, let it cool, diluted with methanol to the scale, shake, filter, Take 5ml of continued filtrate with precision, in a 50ml measuring flask, use 0. Dilute 1 mol/L sodium hydroxide solution to the scale, shake well, as the test solution, according to UV-visible spectrophotometry (General 0401), at the wavelength of 362nm absorbance; another appropriate amount of meloxicam reference substance was accurately weighed, dissolved and quantitatively diluted with the same method to make a solution containing about 7.5ug per lml, which was determined with the same method. It is obtained by calculation.
category
Same as meloxicam.
specification
(1)7.5mg (2)15mg
storage
light shielding, sealed storage.
Last Update：2022-01-01 14:19:14
MeloxicaM, BP - Meloxicam Dispersible Tablets
Authoritative Data Verified Data
This product contains meloxicam (C14H13N304S2) should be 90.0% ~ 110.0% of the label amount.
trait
This product is a light yellow tablet.
identification
- take an appropriate amount of the fine powder of this product (equivalent to 15mg of meloxicam), add 10ml of three gas methane to shake the meloxicam to dissolve, filter, add 3 drops of ferric chloride test solution to the filtrate, shake, after placement, it showed light purple-red color.
- take the test solution under the content determination item, according to ultraviolet-visible spectrophotometry (General rule 0401), there is a maximum absorption at the wavelength of 270mn and 362mn, there is minimal absorption at a wavelength of 312nm.
- take an appropriate amount of meloxicam powder (equivalent to meloxicam 20mg), add chloroform 10ml, sonicate meloxicam to dissolve, filter, take the continued filtrate as the test solution; Take meloxicam control, A solution containing 2mg per 1 ml was prepared by dissolving and diluting with chloroform as a control solution. According to the thin layer chromatography (General 0502) test, absorb the above two solutions of 10 u1, respectively, on the same silica gel GF254 thin layer plate, with chloroform-methanol-diethylamine (60:5:7.5) for the development of the solvent, expand, dry, set the UV lamp (254mn) to view, the position and color of the main spot of the test solution should be consistent with the main spot of the reference solution.
- take the fine powder of this product and the reference substance of meloxicam, Add alkaline methanol solution (take 40% methanol solution, add 6mL of 0.4mol /L sodium hydroxide solution, mix well) dissolve and dilute to make meloxicam in about 1 ml. 1 mg solution, as the test solution and the control solution, according to the related substances under the chromatographic conditions test, record the chromatogram. The retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the control solution.
- two items (3) and (4) above can be selected as one item.
examination
- Related substances take the fine powder of this product, Add alkaline methanol solution (take 40% methanol solution 100ml, add 0.4mol/L sodium hydroxide solution 6ml, mix well) dissolve meloxicam and dilute it to make a solution containing about 1 mg per 1ml, filter it, and take the continued filtrate as a test solution; Take 1ml for precision measurement and put it in a 100ml measuring flask, as a control solution, it was diluted to the scale with the above-mentioned basic solvent and shaken. The determination was carried out according to the method for related substances of meloxicam. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be more than 0.30 times (0.5) of the area of the main peak of the control solution, except for the chromatographic peak whose relative retention time is less than 0.5%, the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%).
- Content uniformity take 1 tablet of this product, put it in a 100ml measuring flask, and add O. About 70ml of 1 mol/L sodium hydroxide solution, according to the method under the content determination item, from the "ultrasonic dissolution of meloxicam", according to the law, shall comply with the provisions (General 0941).
- dissolution the dissolution of this product was determined according to the dissolution and release determination method (General rule 0931 second method), and the dissolution medium was 7.4 phosphate buffer (pH), and the rotation speed was 50 revolutions per minute, according to the law, after 30 minutes, take the solution, filter, take the filtrate as the test solution; Another meloxicam control about 20mg, precision weighing, 100ml flask, add O. 1 mol/L sodium hydroxide solution 10ml, dissolved by ultrasound, diluted to scale with dissolution medium, shake well, take 2ml accurately, put it in 50ml measuring flask, dilute to scale with dissolution medium, shake well as a control solution. The absorbance of each of the above two Solutions was measured at a wavelength of 0401 nm by ultraviolet-visible spectrophotometry (general), and the elution amount of each tablet was calculated. The limit is 75% of the labeled amount and shall be in accordance with the provisions.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
Take 20 tablets of this product, precision weighing, fine grinding, precision weighing appropriate amount (about equivalent to meloxicam 7.5mg), put it in a 100ml measuring flask, add O. 1 mol/L sodium hydroxide solution about 70ml, sonicated meloxicam dissolution, let cool, with O. Dilute 1 mol/L sodium hydroxide solution to the scale, shake well, filter, Take 5ml of continuous filtrate accurately, put it in 50ml measuring flask, use 0. Dilute 1 mol/L sodium hydroxide solution to the scale, shake well, as the test solution, according to UV-visible spectrophotometry (General 0401), at the wavelength of 362nm absorbance; another meloxicam control, precision weighing, plus 0.1 mol/L sodium hydroxide solution was dissolved and quantitatively diluted to prepare a solution containing about 7.5ug per 1 ml, which was determined by the same method. It is obtained by calculation.
category
Same as meloxicam.
specification
7.5mg
storage
light shielding, sealed storage.
Last Update：2022-01-01 14:19:15
MeloxicaM, BP - Meloxicam Tablets
Authoritative Data Verified Data
This product contains meloxicam (C14H13N304S2) should be 90.0% ~ 110.0% of the label amount.
trait
The content of this product is light yellow or yellow particles or powder.
identification
- take an appropriate amount of the content of this product (about 15mg equivalent to meloxicam), add chloroform 10ml to shake to dissolve meloxicam, filter, add 3 drops of ferric chloride solution to the filtrate, shake, after placement, it showed light purple-red color.
- take the test solution under the content determination item, according to ultraviolet-visible spectrophotometry (General rule 0401), there is a maximum absorption at the wavelength of 270nm and 362nm, there is minimal absorption at a wavelength of 312nm.
- take an appropriate amount of the content of this product (about 20mg equivalent to meloxicam), add chloroform 10ml ultrasound to dissolve meloxicam, filter, and take the filtrate as the test solution, A solution containing 2mg per 1 ml was prepared by dissolving and diluting with chloroform as a control solution. According to the thin layer chromatography (General 0502) test, absorb the above two solutions of 10 u1, respectively, on the same silica gel GF254 thin layer plate, with chloroform-methanol-diethylamine (60:5:7.5) for the development of the solvent, expand, dry, set the UV lamp (254nm) to view, the position and color of the main spot of the test solution should be consistent with the main spot of the reference solution.
- take the content of this product fine powder and meloxicam reference, Add alkaline methanol solution (take 40% methanol solution, add 0.4mol/ L sodium hydroxide solution 6ml, mix well) dissolve and dilute to make meloxicam in about 1 ml. 1 mg solution, as the test solution and the control solution, according to the related substances under the chromatographic conditions test, record the chromatogram. The retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the control solution.
- two items (3) and (4) above can be selected as one item.
examination
- Related Substances: take the fine powder of the contents of this product and add alkaline methanol solution (take 40% ml of 0.4mol / L sodium hydroxide solution for 6ml, mix well) dissolve meloxicam and dilute it to prepare a solution containing about 1 mg per 1ml as a test solution. Take 1ml of meloxicam in a 100ml measuring flask and dilute to the scale with the above alkaline methanol solution, as a control solution. If there are impurity peaks in the chromatogram of the test solution, except for the chromatographic peaks whose relative retention time is less than 0.30, the single impurity peak area shall not be greater than 0.5 times (0.5%) of the main peak area of the control solution, and the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%).
- Content uniformity take 1 capsule of this product, put the content in a 100ml measuring flask, and use a small amount of O. Wash the capsule shell with 1 mol/L sodium hydroxide solution, incorporate the wash solution into the measuring flask, and add O. About 70ml of 1 mol/L sodium hydroxide solution, according to the method under the content determination item, from the "ultrasonic dissolution of meloxicam", according to the law, shall comply with the provisions (General 0941).
- dissolution the dissolution of this product was determined according to the dissolution and release determination method (General rule 0931 method 1), and the dissolution medium was 7.4 phosphate buffer (pH 100), and the rotation speed was rpm, according to the law, after 30 minutes, take the solution, filter, take the filtrate as the test solution; Another meloxicam control about 20mg, precision weighing, 100ml flask, add O. 1 mol/L sodium hydroxide solution 10ml, dissolved by ultrasound, diluted to scale with dissolution medium, shake well, take 2ml accurately, put it in 50ml measuring flask, dilute to scale with dissolution medium, shake, as a reference solution; Take the above two solutions, according to UV-visible spectrophotometry (General rule 0401), absorbance at the wavelength of nm, respectively, to calculate the amount of dissolution of each particle. The limit is 75% of the labeled amount and shall be in accordance with the provisions.
- others should comply with the relevant provisions under the capsule (General 0103).
Content determination
Take 20 capsules of this product, weigh it precisely, pour out the contents, grind it finely, weigh it properly (about 7.5mg equivalent to meloxicam), put it in a 100ml measuring flask, add 0.1 mol/L sodium hydroxide solution about 70ml, sonicated meloxicam dissolved, let cool, with 0. Dilute 1 mol/L sodium hydroxide solution to the scale, shake well, filter, Take 5ml of continuous filtrate accurately, put it in 50ml measuring flask, use 0. Dilute 1 mol/L sodium hydroxide solution to the scale, shake well, as the test solution, according to UV-visible spectrophotometry (General 0401), at the wavelength of 362nm absorbance; another meloxicam control, precision weighing, plus 0.1 mol/L sodium hydroxide solution was dissolved and quantitatively diluted to prepare a solution containing about 7.5ug per 1 ml, which was determined by the same method. It is obtained by calculation.
category
Same as meloxicam.
specification
7.5mg
storage
light shielding, sealed storage.
Last Update：2022-01-01 14:19:16
MeloxicaM, BP - Reference Information
| EPA chemical substance information | information provided by: ofmpeb.epa.gov (external link) |
| analgesic anti-inflammatory drugs | meloxicam a non-steroidal antipyretic analgesic anti-inflammatory drugs, not hormonal drugs, with strong anti-inflammatory, analgesic and antipyretic effect, which selectively inhibits the activity of cyclooxygenase-2 (COX-2), thereby blocking the synthesis of prostaglandins, the inhibition of prostaglandin biosynthesis in inflammatory sites is stronger than that in gastric mucosa or kidney, and is safer than other NSAIDs. It is mainly used to relieve the symptoms of osteoarthritis, painful osteoarthritis, rheumatoid arthritis and ankylosing spondylitis. |
| Overview | meloxicam (meloxicam), chemical name 4-hydroxy-2-methyl-n-(5-methyl-2-thiazolyl)-2H-1, 2-benzothiazine-3-carboxamide 1,1-dioxide, a non-steroidal anti-inflammatory drug. It was first launched in South Africa in 1996 by the German company Boehringer Ingelheim. It has analgesic, anti-inflammatory and antipyretic effects, and is clinically applicable to the symptomatic treatment of rheumatoid arthritis and painful osteoarthritis. The mechanism of action of non-steroidal anti-inflammatory drugs is to prevent the synthesis of inflammatory prostaglandins (PGs) and the like by inhibiting cyclooxygenase (COX). Cyclooxygenase (COX) is a membrane-bound serum protein and glycoprotein that catalyzes the oxidation of arachidonic acid (AA) to prostaglandin G2(PGG2) and the reduction from PGG2 to pgh2. There are two isoforms of COX: The cyclooxygenase-1 (COX-1)-structural enzyme and the cyclooxygenase-2 (COX-2)-PGG2-inducible enzyme. The inducible enzyme COX-2 is induced by inflammatory regulation and is involved in the regulation of the inflammatory response; Whereas the structural enzyme COX-1 is required for normal physiological processes and is present in most tissues, its function is to synthesize PG to regulate the normal physiological activity of cells, protect the digestive tract mucosa, support the microcirculation in the kidney and protect other organs from damage. Among the cyclooxygenase (COX) selective inhibitors of many different NSAIDs, meloxicam selectively inhibits COX-2, while diclofenac, piroxicam, indomethacin non-steroidal anti-inflammatory drugs or the same both inhibit COX, or inhibition of COX-1 than inhibition of COX-2. Meloxicam is safe in gastrointestinal tract and less toxic to kidney, which is due to its weak inhibition of COX-1. Fig.1 inflammatory reaction mechanism |
| pharmacological action | 1. Analgesic effect and other non-steroidal anti-inflammatory drugs, meloxicam is mainly used for mild to moderate chronic dull pain, such as neuralgia, Arthralgia. It has a strong and lasting analgesic effect on inflammatory pain in experimental rats. In male Lewis rats with experimental RA, the dose was 0.063 to 0 .5mg · kg-1, once a day, oral administration for 21 days, not only on the hind paw swelling and bone and cartilage damage, but also has a strong and lasting analgesic effect on inflammatory pain, oral doses up to 10mg · kg-1 had no effect on the central nervous system, similar to indomethacin, meloxicam had no analgesic effect on visceral pain. Antipyretic effect of meloxicam can reduce the body temperature of fever, but almost no effect on normal body temperature. For example, within the anti-inflammatory dose range, meloxicam had no effect on normal body temperature in rats, but reduced yeast-induced by Fever. Fever, respectively ip injection of meloxicam 0.1,0.3 or 0.5mg · kg-1, 2 times a week found that has obvious cooling effect, the best antipyretic dose was 0.3mg · kg-1. Twice a week. 3. Anti-inflammatory effects in animal models of inflammation (mainly including carrageenan, White Clay-induced edema in the hind paw of rats implanted cotton ball model of rat granuloma; carrageenan-induced pleurisy and liquid paraffin-adjuvant M. Tuberculosis-induced arthritis model), meloxicam showed strong anti-inflammatory activity. For carrageenan-induced pleurisy, unlike indomethacin, meloxicam reduces pleurisy secretion and inhibits leukocyte migration. In pleurisy in rats, the action of meloxicam is to inhibit the biosynthesis of prostaglandin E2(PGE2), which is 2 times that of piroxicam and 8 times that of diclofenac, respectively. In peritonitis in mice, meloxicam was 2 times more inhibitory than piroxicam and 10 times more inhibitory than diclofenac. Oral administration of meloxicam, piroxicam, diclofenac or tenidap once daily to male Lewis rats with experimental RA were observed for hind paw enlargement, bone and cartilage damage in hind paws, increase in spleen weight, erythrocyte sedimentation rate, and changes in serum protein components. It was found that the above drugs could inhibit the same inhibitory effect of the hind paw enlargement and the secondary reaction caused by the mouse hind paw enlargement, and the dose of the drug was twice as high as that of meloxicam, the doses of diclofenac and tenucleotide were 3.5 and 60 times higher than that of meloxicam, respectively. The daily dose of meloxicam required to inhibit bone and cartilage damage caused by RA is lower, and Piroxicam is four times that of meloxicam. Doses of diclofenac and tenidaph, which inhibit swelling of the hind paws in rats, had little effect on bone and cartilage damage. The dose of piroxicam was 3 to 4 times higher than that of meloxicam in the treatment of RA in rats. However, diclofenac and tenidaph did not produce comparable effects. |
| pharmacokinetics | The drug is well absorbed by oral and rectal administration, and the drug has no effect on absorption when eating. The bioavailability is 89%, the onset time after oral administration is 30 minutes, and the drug concentration of 7.5mg and 15mg orally is proportional to its dose. To achieve a steady-state blood concentration of 3 to 5 days, continuous treatment of more than 1 years in patients with drug concentration and the first time into a stable state of the patient. The concentration of its penetration into the inflammatory synovial membrane is about 50% of the blood concentration, and the plasma protein binding rate is> 99%, and its half-life is 20 hours. This product is metabolized in the liver, and the metabolites are inactive. 50% are excreted by the kidney, and the remaining 50% are excreted by the feces. |
| synthesis | There are many methods for the synthesis of meloxicam. With commercially available sodium saccharin (without purification and drying) as the starting material, by condensation with methyl chloroacetate in DMF to produce 2,2 in the refluxing solution of sodium methoxide in methanol to give 3, after N-methylation, the obtained 4 is reacted with 2-amino-5-methylthiazole to obtain crude product 1, and then recrystallized from 1, 2-dichloroethane to obtain a pure product with a content of ≥ 99%, the overall yield was 48.6%. 3-oxo-1, 2-benzisothiazole-2-acetic acid methyl ester 1, 1-dioxide (2)1000ml three-necked flask was added with DMF(410ml), sodium saccharin (1.0g, 162.8 mol, commercially available, containing water of crystallization) was added under magnetic stirring, and after being substantially dissolved, methyl chloroacetate (1.5g, mol) was added. The mixture was gradually heated to reflux (bath temperature 130-140°C) and reacted for 3H. After cooling to room temperature, the reaction mixture was added to cold water (820mL) with stirring, and a white solid was immediately precipitated. Suction filtration, water (100ml x 3). After vacuum drying (60°C) a white solid 2 was obtained. 4-hydroxy-2h-1, 2-benzothiazine-3-carboxylic acid methyl ester 1, 1-dioxide (3)250 ml three-necked flask was added with anhydrous methanol (60ml), sodium metal (6.5g,0.28mol) was then added portionwise, after complete dissolution of the sodium (which can be heated slightly), and the mixture was stirred electrically and heated to a bath temperature of 110-120°C. Powdered 2(18g,0.07mol) was immediately added quickly in one portion while stirring vigorously (care was taken to prevent flushing out), and the reaction was instantaneous to give a yellow-orange slurry. The oil bath was removed, and then ice (72g) -concentrated hydrochloric acid (28ml) mixture was added, stirred, and cooled to below 10°C in an ice water bath to precipitate a white solid, which was suction filtered and washed with water, vacuum drying (60°C) gave a white solid 3. 4-hydroxy-2-methyl-2h-1, 2-benzothiazine-3-carboxylic acid methyl ester 1, 1-dioxide (4)250ml three-necked flask was added with ethanol (72ml), with magnetic stirring, 3(14.4g,56.47mmol) was added followed by a solution of sodium hydroxide (3.16g) in water (72ml). After the reaction was exothermic and the solid was completely dissolved, the temperature was lowered to 20 ° C. Or lower, and then dimethyl sulfate (11.81g , 93.74mmol) was added dropwise (keeping the internal temperature not higher than 25 ° C.). After several minutes, a large amount of solid was precipitated and reacted at about 25 ° C. For 15 hours. It was cooled to below 10°C, suction filtered, and washed with 50% ethanol to obtain white solid 4. Fig.2 synthesis of meloxicam |
| Use | for rheumatoid arthritis, rheumatoid arthritis, osteoarthritis, soft tissue injury pain, etc. (2015-11-23) Non-steroidal anti-inflammatory drugs. For the treatment of osteoarthritis, rheumatoid arthritis. drugs for arthritis and rheumatoid arthritis. for the treatment of rheumatoid arthritis, painful osteoarthritis cyclooxygenase-2 inhibitors for the symptomatic treatment of rheumatoid arthritis, painful osteoarthritis |
| adverse reactions | may occur dyspepsia, Abdominal Pain, Nausea, Diarrhea, elevated liver enzymes, dizziness, Head Pain, rash, anemia. There are occasional edema, elevated blood pressure, mild blood creatinine or urea nitrogen abnormalities, acute renal failure, gastric ulcer, gastric bleeding, gastric perforation, leukopenia and thrombocytopenia. |
| note | 1. Allergic to non-steroidal anti-inflammatory drugs, active peptic ulcer, severe liver dysfunction, pregnant and lactating women, under the age of 15 disabled. 2. History of upper digestive tract and is using anticoagulants, liver and kidney insufficiency in elderly patients with caution, if peptic ulcer or gastrointestinal bleeding should stop using this product. 3. Regular examination of liver and kidney function during medication, especially in elderly patients over 65 years of age. |
| drug interaction | 1. Concomitant use of oral anticoagulants, heparin and thrombolytic agents may increase the risk of bleeding. 2. The combination of this product and lithium salt can increase the plasma concentration of lithium, and the plasma lithium level should be monitored. 3. This product combined with methotrexate, can enhance the blood toxicity of the latter, should monitor the blood and liver function. 4. The combination of this product and cyclosporine can increase the renal toxicity of the latter through the indirect effect of renal prostaglandin, and the renal function should be determined regularly. 5. This product can reduce the effect of hypoglycemic drugs and antihypertensive drugs taken at the same time, so it is advisable to monitor and adjust the dosage of medication. No drug-drug interactions related to pharmacokinetics were observed with concomitant use of antacids, cimetidine, digoxin and furosemide. |
| production method | 4-hydroxy-2-methyl-2h-1, 2-benzothiazine-3-carboxylic acid methyl ester 1,1-dioxide and 2-amino-5-methylthiazole were refluxed in xylene to give meloxicam in 74% yield. |
| category | toxic substances |
| toxicity grade | high toxicity |
| Acute toxicity | oral-rat LD50 84 mg/kg; Oral-mouse LD50: 470 mg/kg |
| flammability hazard characteristics | combustible, fire discharge of nitrogen oxides, sulfur oxides spicy stimulus smoke |
| storage and transportation characteristics | The warehouse is low temperature, ventilated and dry, and stored separately from food raw materials; custody of specialized institutions |
| extinguishing agent | water, carbon dioxide, dry powder, sand |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-09 19:05:13
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