274-239-6
Doxofylline
CAS: 69975-86-6
Molecular Formula: C11H14N4O4
274-239-6 - Names and Identifiers
| Name | Doxofylline |
| Synonyms | Ansirnar MAXIVENT 274-239-6 Doxofylline DOXOFYLLINE Doxofyliine DOXOPHYLLINE 2-(7'-teofillinmetil)-1,3-diossolano 7-(1,3-dioxolan-2-ylmethyl)-1,3-dimethyl-purine-2,6-dione 7-(1,3-Dioxolan-2-ylmethyl)-3,7-dihydro-1,3-dimethyl-1H-purine-2,6-dione 7-(1,3-dioxolan-2-ylmethyl)-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione 1H-purine-2,6-dione, 7-(1,3-dioxolan-2-ylmethyl)-3,7-dihydro-1,3-dimethyl- DOXOFYLLINE [7-(1,3-DIOXOLAN-2-YLMETHYL)-3,7-DIHYDRO-1,3-DIMETHYL-1H-PURINE-2,6-DIONE] |
| CAS | 69975-86-6 |
| EINECS | 274-239-6 |
| InChI | InChI=1/C11H14N4O4/c1-13-9-8(10(16)14(2)11(13)17)15(6-12-9)5-7-18-3-4-19-7/h6-7H,3-5H2,1-2H3 |
274-239-6 - Physico-chemical Properties
| Molecular Formula | C11H14N4O4 |
| Molar Mass | 266.25 |
| Density | 1.2896 (rough estimate) |
| Melting Point | 144-146°C |
| Boling Point | 409.46°C (rough estimate) |
| Flash Point | 259.3°C |
| Water Solubility | Soluble |
| Solubility | Soluble in water, acetone, ethyl acetate, benzene, chloroform, dioxane, hot methanol or hot ethanol, almost insoluble in ether or petroleum ether. |
| Vapor Presure | 2.49E-10mmHg at 25°C |
| Appearance | Crystallization |
| Color | White to Off-White |
| Merck | 14,3438 |
| pKa | 0.42±0.70(Predicted) |
| Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
| Refractive Index | 1.6000 (estimate) |
| MDL | MFCD00865218 |
| Physical and Chemical Properties | Crystals, melting point 144-145.5 °c. Soluble in water, acetone, ethyl acetate, benzene, chloroform, dioxane, hot methanol or hot ethanol, a few do not dissolve in ether or petroleum ether. Acute toxicity LD50 mice (mg/kg):841 oral, 215.6 intravenous. Acute toxicity LD50 rats (mg/kg):1022.4 oral, 445 intraperitoneal injection. |
| In vitro study | Doxofylline has the activity of a PDE inhibitor and can increase the level of cAMP, so it can be used to treat asthma and COPD. The EC50 value of Doxofylline for inhibiting adenosine-induced relaxation of tracheal smooth muscle was 15 cosy higher than that of aminophylline, and the EC50 value for reducing the negative inotropic effect of adenosine on guinea pig Atria was 15 cosy higher than that of aminophylline. Due to the shortening of the open period and the prolongation of the closing time, Doxofylline can effectively reduce the opening probability of Calcium-activated potassium channels. Compared with theophylline, Doxofylline greatly reduces the affinity for adenosine A 1 and A 2 receptors, which may make it have A better safety profile. In addition, unlike theophylline, Doxofylline does not interfere with calcium influx or antagonize the effects of calcium channel blockers. |
| In vivo study | Doxofylline has been shown to have better efficacy and fewer side effects than theophylline. Doxofylline at 30 mg/kg increased the heart rate of anesthetized cats by 13 beats/min. The effective therapeutic dose of Doxofylline is smaller than that of theophylline, so Doxofylline does not significantly increase the heart frequency and has no arrhythmogenic effect. |
274-239-6 - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37 - Wear suitable protective clothing and gloves. |
| RTECS | XH5135000 |
| HS Code | 29399990 |
| Toxicity | LD50 in mice (mg/kg): 841 orally; 215.6 i.v.; in rats: 1022.4 orally, 445 i.p. (Franzone) |
274-239-6 - Standard
Authoritative Data Verified Data
This product is 7-(1, 3-dioxolan-2-ylmethyl) theophylline. The content of C11H14N4o4 shall be 98.5% ~ 102.0% calculated as dry product.
Last Update：2024-01-02 23:10:35
274-239-6 - Trait
Authoritative Data Verified Data
- This product is white needle-like crystal or crystalline powder; Odorless.
- This product is slightly soluble in water, ethanol or acetone; Slightly soluble in 0.lmol/L hydrochloric acid solution.
melting point
The melting point of this product (General 0612) is 142~145°C.
absorption coefficient
take this product, precision weighing, add 0.1 mol/L hydrochloric acid solution is dissolved and quantitatively diluted to prepare a solution containing about 15ug per 1 ml, and the absorbance is measured at the wavelength of 273nm by ultraviolet-visible spectrophotometry (General rule 0401), the absorption coefficient should be 335-356.
Last Update：2022-01-01 11:53:36
274-239-6 - Differential diagnosis
Authoritative Data Verified Data
- take about 10 mg of this product, add 1 ml of hydrochloric acid and 0.1g of potassium chlorate, and steam dry on a water bath. The residue will appear purple when exposed to ammonia gas.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 941).
Last Update：2022-01-01 11:53:37
274-239-6 - Exam
Authoritative Data Verified Data
acidity
take 0.lg of this product, add 100ml of water to dissolve, and measure according to law (General rule 0631). The pH value should be 5.0~7.0.
clarity and color of solution
take this product O.lg, Add 10ml of water to dissolve, the solution should be clear and colorless; If it is turbid, it should not be more concentrated compared with No. 1 turbidity standard solution (General Principles 0902 first method); If it is colored, it shall not be deeper in comparison with the yellow No. 1 Standard Colorimetric solution (General rule 0901 first method).
bromide
take 0.2g of this product, add 15ml of water, 0.5ml of dilute nitric acid and lml of silver nitrate solution, heat to boiling, cool, dilute to 25ml with water, shake, with standard potassium bromide solution (equivalent to 0.Olmg Br-)llml made 25ml solution must not be more concentrated (0.055%).
Related substances
take an appropriate amount of this product, precision weighing, add acetonitrile-water (15:85) to dissolve and quantitatively dilute to prepare a solution containing about 1 mg per 1 ml as a test solution; another 10 mg of theophylline reference substance was added into a 10ml measuring flask, then acetonitrile-water (15:85) was added to dissolve and dilute to the scale, take 2ml of the sample solution and 2ml of the sample solution, put it in a 100ml measuring flask, dilute it to the scale with acetonitrile-water (15:85), shake it well, and take 5ml of the sample, A 50ml measuring flask was placed, diluted to the mark with acetonitrile-water (15:85) and shaken to serve as a control solution. According to the chromatographic conditions under the content determination item, take 10ul of the control solution and inject it into the liquid chromatograph. The resolution between theophylline peak and doxofylline peak should be greater than 10. The sample solution and the control solution were respectively injected with human liquid chromatograph, and the chromatogram was recorded to 3 times of the retention time of the main component peak. If there is a chromatographic peak in the chromatogram of the test solution that is consistent with the retention time of theophylline peak in the control solution, the peak area shall be calculated according to the external standard method, and shall not exceed 0.2%; the Peak area of other single impurities shall not be greater than that of doxofylline in the control solution (0.2%); The total amount of impurities shall not exceed 0.5%.
residual solvent
N, N-dimethylformamide and ethylene glycol take this product 0.2g, precision weighing, precision adding chloroform 2ml to dissolve, mixing, as a test solution; Take N, N-dimethylformamide 88mg and ethylene glycol 62mg, precision weighing, set in 100ml measuring flask, dilute with chloroform to the scale, shake well, take 5ml, set in 50ml measuring flask, dilute to the scale with chloroform, shake, as a control solution. According to the determination method of residual solvents (General 0861 third method), the capillary column with bonded and modified cross-linked ethylene glycol (or similar polarity) as stationary liquid is used as the chromatographic column, the initial temperature is 60°C, and the maintenance time is 5 minutes, heating to 150°C at a rate of 5°C per minute, and then heating to 200°C at a rate of 50°C per minute for 3 minutes; The temperature of the injection port is 125°C; the detector is a hydrogen flame ionization detector, and the detector temperature is 250 ° C.; The separation degree between the N,N-dimethylformamide peak and the ethylene glycol peak shall meet the requirements. The sample solution and the reference solution were respectively 1u1, injected into the human gas chromatograph, and the chromatogram was recorded. The peak area shall be calculated according to the external standard method and shall comply with the regulations.
methanol, ethanol, dichloromethane and vinyl acetate
take this product 0.5g, precision weighing, top empty bottle, precision add N, N-dimethylacetamide 5ml, sealed, mixed, as a test solution; Take methanol 300mg, 500mg of ethanol, 60mg of dichloromethane and lOOmg of vinyl acetate were accurately weighed, placed in a 100ml measuring flask, diluted to the scale with N, N-dimethylacetamide, and then shaken, dilute to the scale with N, N-dimethylacetamide, shake well, take 5ml precisely, place in a headspace bottle, seal, and use as a reference solution. According to the method for determination of residual solvents (General rule 0861, second method), the capillary column with 6% cyanopropylphenyl-94% dimethyl polysiloxane (or similar polarity) as stationary liquid is used as the chromatographic column, and the initial temperature is 40°C, hold for 5 minutes, raise the temperature to 110°C at a rate of 10°C per minute, then raise the temperature to 200°C at a rate of 5CTC per minute, hold for 5 minutes, and the injection temperature is 200°C, the detector is hydrogen flame ionization detector, and the temperature of the detector is 250°C; The equilibrium temperature of the headspace bottle is 90°C, and the equilibrium time is 30 minutes. Take the reference solution and record the chromatogram, the separation degree between peaks of each component shall meet the requirements. Then the sample solution and the reference solution were injected with headspace, and the chromatogram was recorded. The peak area shall be calculated according to the external standard method and shall comply with the regulations.
loss on drying
take this product, dry to constant weight at 105°C, weight loss shall not exceed 1.0% (General rule 0831).
ignition residue
take l.Og of this product and check it according to law (General rule 0841). The ignition temperature is 500~600°C, and 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 20 parts per million of heavy metal when examined by law (General rule 0821, Law II).
Last Update：2022-01-01 11:53:38
274-239-6 - Content determination
Authoritative Data Verified Data
measured by high performance liquid chromatography (General 0512).
chromatographic conditions and system suitability test
acetonitrile-phosphate buffer (pH 5.8)(15:85) was used as the mobile phase, and the detection wavelength was 273nm; the number of theoretical plates is not less than 2000 based on the doxofylline peak.
assay
precision weigh the appropriate amount of this product, add acetonitrile-water (15:85) to dissolve and quantitatively dilute to make a solution containing about 0.05mg per lml, precision measure 10 u1, note human liquid chromatograph, record chromatogram; Accurately weigh appropriate amount of doxofylline reference substance, add acetonitrile-water (15:85) to dissolve and quantitatively dilute to prepare a solution containing about 0.05mg per 1 ml, same method determination. According to the external standard method to calculate the peak area, that is.
Last Update：2022-01-01 11:53:38
274-239-6 - Category
Authoritative Data Verified Data
bronchodilators.
Last Update：2022-01-01 11:53:38
274-239-6 - Storage
Authoritative Data Verified Data
sealed preservation.
Last Update：2022-01-01 11:53:39
274-239-6 - Doxofylline tablets
Authoritative Data Verified Data
This product contains doxofylline (C11H14N404) should be labeled the amount of 95.0% ~ 105.0%.
trait
This product is white or off-white.
identification
- take an appropriate amount of fine powder of this product (about 20mg equivalent to doxofylline), add 10ml of water, shake, filter, evaporate the filtrate to dryness, add lml of hydrochloric acid and 0.lg of potassium chlorate, and evaporate on a water bath, the residue turned purple when exposed to ammonia gas, and several drops of sodium hydroxide solution were added, and the purple color disappeared.
- take an appropriate amount of the fine powder of this product, add two gas methane to dissolve and dilute to make a solution containing about 10 mg of doxofylline per 1 ml, filter, and take the continued filtrate as the test solution; an appropriate amount of doxofylline reference substance was additionally taken, dissolved and diluted with dimethyl methane to prepare a solution containing about 10 mg per 1 ml as a reference solution. According to the thin layer chromatography (General 0502) test, absorb the above two solutions each 5 u1, respectively, on the same silica gel GF 254 thin layer plate, with two gas methane-cyclohexane-acetone (1:1:1) for the development of the agent, after deployment, dry, set the UV light (254nm) under the inspection, the position and color of the main spot displayed by the test solution should be the same as that of the reference solution.
- take an appropriate amount of the test solution under the item of related substances and dilute it with acetonitrile-water (15:85) to make a solution containing about 0.05mg of doxofylline per 1 ml, as a test solution; An appropriate amount of the doxofylline control was taken, dissolved and diluted with acetonitrile-water (15:85) to prepare a solution containing about 0.05mg per 1 ml as a control solution. According to the chromatographic conditions under the items of related substances, 10 u1 of the test solution and 10 u1 of the reference solution are taken for injection into the human liquid chromatograph respectively, and the chromatograms are recorded, 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.
- take the solution under the content determination item, according to UV-visible spectrophotometry (General 0401), there is a maximum absorption at the wavelength of 273nm, there is minimal absorption at a wavelength of 245Nm.
- two items (2) and (3) above can be selected as one item.
examination
- Related substances take an appropriate amount of fine powder of this product (about equivalent to doxofylline lOOmg), weigh it accurately, put it in a 100ml measuring flask, and add an appropriate amount of acetonitrile-water (15:85), shake to dissolve doxofylline, and dilute to the scale with acetonitrile-water (15:85), shake well, filter, and take the continued filtrate as the test solution; take another 10mg of theophylline reference substance, weigh it accurately, put it in 50ml measuring flask, add acetonitrile-water (15:85) to dissolve and dilute it to the scale, shake it well, 2ml of the sample solution and 1ml of the test solution were accurately measured and placed in the same 200ml measuring flask, diluted to the scale with acetonitrile-water (15:85), and shaken to obtain a control solution. According to the high performance liquid chromatography (General 0512) test, silica gel bonded with eighteen alkyl silane was used as the filler; Acetonitrile-phosphate buffer (pH 5.8)(15:85) was used as the mobile phase; the detection wavelength was 273 nm; The control solution 10u1 was injected into human liquid chromatograph, and the number of theoretical plates was not less than 2000 calculated by doxofylline peak. The separation degree between theophylline peak and doxofylline peak should be greater than 10. 10 u1 of the test solution and the control solution were respectively injected into the liquid chromatograph, and the chromatogram was recorded to 3 times of the retention time of the main component peak. If there is a chromatographic peak in the chromatogram of the test solution that is consistent with the retention time of theophylline peak in the control solution, the peak area shall be calculated according to the external standard method, and 0.2% of the labeled amount shall not be exceeded; the sum of the peak areas of each other impurity shall not be greater than the area of the doxofylline peak in the control solution (0.5%).
- dissolution: according to the dissolution and release determination method (General rule 0931, Method 1), 100 ml of 0.lmol / L hydrochloric acid solution was used as the dissolution medium at RPM, operate according to law, after 30 minutes, take 10ml of solution, filter, take the appropriate amount of filtrate, with 0.1 mol / L hydrochloric acid solution was quantitatively diluted to make a solution containing 15ug doxofylline per 1 ml, and the absorbance was measured at the wavelength of 273nm according to UV-visible spectrophotometry (General rule 0401); take an appropriate amount of doxofylline control, precision weighing, plus 0.1 mol / L hydrochloric acid solution was dissolved and quantitatively diluted to prepare a solution containing about 15ug per 1 ml, which was measured by the same method, and the dissolution amount of each tablet was calculated. The limit is 80% 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 0.15g equivalent to doxofylline), put it in a 200ml measuring flask, add 0.1 mol/L hydrochloric acid solution appropriate amount, fully shake, so that doxofylline dissolution, with 0. Dilute 1 mol/L hydrochloric acid solution to the scale, shake well, filter, take 2ml of continuous filtrate accurately, put it in a 100ml measuring flask, use 0. Dilute the lmol/L hydrochloric acid solution to the scale, shake well, and measure the absorbance at the wavelength of 273mn by UV-Vis spectrophotometry (General rule 0401), precision weighing, add 0.lmol/L hydrochloric acid solution was dissolved and diluted quantitatively to prepare a solution containing about 15ug per lml, which was determined by the same method. It is obtained by calculation.
category
Same as doxofylline.
specification
(1)0.2g (2)0.3g
storage
sealed storage.
Last Update：2022-01-01 11:53:40
274-239-6 - Doxofylline Injection
Authoritative Data Verified Data
This product is a sterilized aqueous solution of doxofylline, containing doxofylline (C11H14N404) should be 95.0% ~ 105.0% of the label amount.
trait
This product is a clear colorless liquid.
identification
- take an appropriate amount of this product (about equivalent to 10mg of doxofylline), put it on a water bath to evaporate, add hydrochloric acid lml and potassium chlorate O.lg, dried on a water bath, leaving light red residue, which turned to purple when ammonia gas was encountered. After adding several drops of sodium hydroxide solution, the purple color disappeared.
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
- take an appropriate amount of this product and dilute it with water to make a solution containing about 15 μl of doxofylline per 1 ml, and measure it by UV-Vis spectrophotometry (General rule 0401), there is a maximum absorption at a wavelength of 273nm and a minimum absorption at a wavelength of 245Nm.
examination
- pH value take 10ml of this product, add 1~2 drops of saturated potassium chloride solution, and check according to law. The pH value should be 4.5~6.5 (General 0631).
- Related substances take this product and dilute it with water to make it contain doxofylline l per lml. 0 mg of the solution was used as a test solution; 1ml was accurately weighed, placed in a 200ml measuring flask, diluted with water to a scale, and shaken to obtain a control solution. According to the chromatographic conditions under the content determination item, 10ul of the test solution and the control solution are respectively injected into the human liquid chromatograph, and the chromatogram is recorded to 2 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 0.2 times (0.1%) 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 (0.5%).
- the bacterial endotoxin of this product is taken and checked according to law (General rule 1143). The amount of endotoxin contained in doxofylline per 1 mg should be less than 0.50EU.
- sterile take this product, by membrane filtration method, inspection according to law (General 1101), should comply with the provisions.
- others should comply with the relevant provisions under injection (General 0102).
Content determination
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler; Acetonitrile-phosphate buffer (pH 5.8)(12:88) as mobile phase; The detection wavelength was 273mn. The number of theoretical plates shall not be less than 2000 based on the doxofylline peak, and the separation degree between the main peak and the adjacent impurity peaks shall be in accordance with the regulations.
- determination of precision take an appropriate amount of this product, diluted with water to prepare each lml containing doxofylline O.lmg solution, as a test solution, take 10ul of precision, inject into the liquid chromatograph, record the chromatogram; Take an appropriate amount of doxofylline reference, precision weighing, water was added to dissolve and quantitatively diluted to make about 0.lmg solution, the same method for determination. According to the external standard method to calculate the peak area, that is.
category
Same as doxofylline.
specification
(l)10ml:0.lg (2)10ml:0.2g (3)20ml:0.3g
storage
sealed storage.
Last Update：2022-01-01 11:53:41
274-239-6 - Doxofylline capsules
Authoritative Data Verified Data
This product contains doxofylline (C11H14N404) should be labeled the amount of 90.0% ~ 110.0%.
trait
The content of this product is white or white powder.
identification
- take an appropriate amount of the content of this product (about 20mg equivalent to doxofylline), add hydrochloric acid lml and potassium chlorate 0.lg, and put it on a water bath to evaporate. The residue will turn purple when exposed to ammonia gas. Add several drops of sodium hydroxide test solution, the purple color disappeared.
- take an appropriate amount of the contents of this product, add methylene chloride to dissolve and dilute to prepare a solution containing 1.0 mg of doxofylline per 1 ml, filter, and take the continued filtrate as the test solution; an appropriate amount of doxofylline control was taken, dissolved and diluted with dichloromethane to prepare a solution containing about 10 mg per 1 ml as a control solution. According to the thin layer chromatography (General 0502) test, draw 5ul of each of the above two solutions, respectively, on the same silica gel GF 2S4 thin layer plate, with two gas methane-cyclohexane-acetone (1:1:1) 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 the same as the main spot of the reference solution.
- take an appropriate amount of the test solution under the item of related substances and dilute it with acetonitrile-water (15:85) to make a solution containing about 0.05mg of doxofylline per 1 ml, as a test solution; An appropriate amount of doxso tea minus control was additionally taken, and acetonitrile-water (15:85) was added to dissolve and dilute to prepare a solution containing about 0.05mg per 1 ml as a control solution. According to the chromatographic conditions under the item of related substances, 10ul of the test solution and the reference solution are respectively injected into the liquid chromatograph, and the chromatograms are recorded, 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.
- take the solution under the content determination item, according to UV-visible spectrophotometry (General 0401), there is a maximum absorption at the wavelength of 273nm, there is minimal absorption at a wavelength of 245Nm.
- two items (2) and (3) above can be selected as one item.
examination
- Related substances take an appropriate amount of the contents of this product (about equivalent to doxofylline lOOmg), weigh it accurately, put it in a 100ml measuring flask, and add an appropriate amount of acetonitrile-water (15:85), shake to dissolve doxofylline, and dilute to the scale with acetonitrile-water (15:85), shake well, filter, and take the continued filtrate as the test solution; Take another 10mg of theophylline control, add acetonitrile-water (15:85) into a 50ml measuring flask, dissolve and dilute to the scale, shake well, and take 2ml and 1 ml of test solution respectively, in the same 200ml measuring flask, dilute to the mark with acetonitrile-water (15:85), shake, as a control solution. According to the high performance liquid chromatography (General 0512) test, silica gel bonded with eighteen alkyl silane was used as the filler; Acetonitrile-phosphate buffer (pH 5.8)(15:85) was used as the mobile phase; the detection wavelength was 273mn. Take the control solution 10u1 and inject it into the liquid chromatograph. The number of theoretical plates shall not be less than 2000 based on the doxofylline peak, and the separation degree between theophylline peak and doxofylline peak shall be greater than 10. 10ul of the test solution and the control solution were respectively injected into the liquid chromatograph, and the chromatogram was recorded to 3 times of the retention time of the main component peak. If there is a chromatographic peak in the chromatogram of the test solution that is consistent with the retention time of theophylline peak in the control solution, the peak area shall be calculated according to the external standard method, and 0.2% of the labeled amount shall not be exceeded; the sum of the peak areas of other impurities shall not be greater than the area of the doxofylline peak in the control solution (0.5%).
- dissolution of this product, according to the dissolution and release determination method (General 0931 first method), with 0.lmol/L hydrochloric acid solution 900ml as the dissolution medium, the rotation speed is 100 revolutions per minute, according to the operation, after 30 minutes, take the solution 10ml, filter, take the appropriate amount of filtrate, with 0.1 mol/L hydrochloric acid solution was quantitatively diluted to make a solution containing 15ug of doxofylline per 1 ml, and the absorbance was measured at the wavelength of 273mn by ultraviolet-visible spectrophotometry (General rule 0401); take an appropriate amount of doxofylline control, precision weighing, plus 0.1 mol/L hydrochloric acid solution was dissolved and quantitatively diluted to prepare a solution containing about 15ug per 1 ml, which was measured by the same method, and the dissolution amount of each particle was calculated. The limit is 80% 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 the contents under the difference of loading amount, mix evenly, weigh an appropriate amount (equivalent to 0.15g of doxofylline) accurately, put it in a 200ml measuring flask, add 0.1 mol/L hydrochloric acid solution appropriate amount, fully shake, so that doxofylline dissolution, with 0. Dilute 1 mol/L hydrochloric acid solution to the scale, shake well, filter, take 2ml of continuous filtrate accurately, put it in a 100ml measuring flask, use 0. Dilute the lmol/L hydrochloric acid solution to the scale, shake well, and measure the absorbance at the wavelength of 273mn by UV-Vis spectrophotometry (General rule 0401), precision weighing, add 0.lmol/L hydrochloric acid solution dissolved and quantitatively diluted into a solution containing about 15ug per lml, determined by the same method and calculated.
category
Same as doxofylline.
specification
0.2g
storage
sealed storage.
Last Update：2022-01-01 11:53:42
274-239-6 - Reference Information
| adverse reactions | regarding the adverse reactions of doxofylline, the instructions are as follows: May cause Nausea, Vomit, epigastric pain, Head Pain, Sleep Initiation and Maintenance Disorders, irritability, tachycardia, premature contraction, tachypnea, hyperglycemia, proteinuria. Such as excessive use will also appear serious arrhythmia, paroxysmal spasm. This is the initial symptoms of poisoning, at this time should be suspended medication, please doctor diagnosis, monitoring blood concentration. But can continue to use after the above signs and symptoms of poisoning disappeared completely. The adverse reactions of doxofylline have been reported in the relevant literature: 1. Allergic reaction: After intravenous drip, the patient developed palpitation, hand and head tremor, and then discontinued. The symptoms disappeared the next day. liver damage: doxofylline 0.3g ns100ml ivgtt, qd, 7 days later, the patient presented with poor appetite, abdominal distension and liver function damage. After 7 days, liver function returned to normal and the above symptoms disappeared. Tip: This product is a derivative of methyl xanthine, and xanthine oxidase (XOD) is an important enzyme in the metabolism of nucleic acid in the body, due to the accumulation of methyl xanthine, a large number of XOD release, the continuous oxidation reaction and the generation of a large number of free radicals aggravate the damage of liver cells on the basis of ischemia and hypoxia. Arrhythmia: doxofylline 0.2g ivgtt and levofloxacin 0.5g ivgtt, qd. The next day, the patient presented with abnormal ECG, frequent ventricular premature beats and atrial premature beats, with ventricular premature bibeat and short ventricular tachycardia at night, with HR 100-130 beats/min. The above symptoms were relieved after 4 days, and ECG returned to normal. It is suggested that the combined use of the two drugs can cause the blood concentration of doxofylline to increase and cause the electrocardiogram to be abnormal. Acute urinary retention: doxofylline tablets 0.2g PO bid was given for reason of bronchial asthma. The patient presented with dysuria the next day. |
| biological activity | Doxofylline (Doxofylline) is a phosphodiesterase inhibitor, a xanthine derivative, used in the treatment of asthma. |
| Target | Value |
| Use | Antiasthmatic antitussive. For bronchial asthma, lung diseases with bronchospasm. Antiasthmatic medicine for antitussive and antiasthmatic |
| production method | theophylline is dissolved in boiling water, sodium hydroxide and 3-chloro-1, 2-propanediol are added, and reflux is carried out. Water was distilled off and then recrystallized from ethanol to obtain compound (I) in a yield of 95%. Compound (I) was dissolved in water, and equimolar HIO4? 2H2O, stirring. The solid was collected by filtration and recrystallized from ethanol to obtain theophylline acetaldehyde in 70% yield. Theophylline acetaldehyde, ethylene glycol and p-toluenesulfonic acid were refluxed and dehydrated in benzene, and the yield was 70%. |
Last Update：2024-04-09 21:32:07
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Product Name: Doxofylline Request for quotationCAS: 69975-86-6
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Mobile: +86-13651600618
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WhatsApp: +8613651600618
Product Name: Doxofylline Request for quotation
CAS: 69975-86-6
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
CAS: 69975-86-6
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
Multiple SpecificationsSpot supply
Product Name: Doxofylline Visit Supplier Webpage Request for quotationCAS: 69975-86-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Multiple Specifications
Product Name: Doxofylline Request for quotationCAS: 69975-86-6
Tel: +86-21-56795779
Email: charles7788@worldyachem.com
Mobile: +86-13651600618
QQ: 2850607228
Wechat: 13651600618
WhatsApp: +8613651600618
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