PENTOXYIFYLLINE - Names and Identifiers
PENTOXYIFYLLINE - Physico-chemical Properties
Molecular Formula | C13H18N4O3
|
Molar Mass | 278.31 |
Density | 1.1713 (rough estimate) |
Melting Point | 98-100°C |
Boling Point | 421.13°C (rough estimate) |
Solubility | H2O: ≥43mg/mL |
Appearance | solid |
Color | white |
Maximum wavelength(λmax) | ['276nm(lit.)'] |
Merck | 14,7136 |
pKa | 0.50±0.70(Predicted) |
Storage Condition | Sealed in dry,Room Temperature |
Refractive Index | 1.6000 (estimate) |
Physical and Chemical Properties | White needle-like crystals. Melting point 105 °c. Soluble in water, benzene, ethanol, chloroform, ethanol-soluble. Odorless and bitter. |
Use | Used as vasodilator |
PENTOXYIFYLLINE - Risk and Safety
Hazard Symbols | Xn - Harmful
|
Risk Codes | 22 - Harmful if swallowed
|
Safety Description | 36 - Wear suitable protective clothing.
|
WGK Germany | 3 |
RTECS | XH2475000 |
HS Code | 2939590000 |
Toxicity | LD50 orally in mice: 1385 mg/kg (Popendiker) |
PENTOXYIFYLLINE - Standard
Authoritative Data Verified Data
This product is 3, 7-dihydro-3, 7-dimethyl-l-(5-oxohexylpurin-2, 6-dione. Calculated as dried product, the content of C13H18N403 shall not be less than 99.0%.
Last Update:2024-01-02 23:10:35
PENTOXYIFYLLINE - Trait
Authoritative Data Verified Data
- This product is white powder or granules; There is a slight odor.
- This product is soluble in chloroform, soluble in water or ethanol, slightly soluble in ether.
melting point
The melting point of this product (General 0612) is 103 ~ 107C.
Last Update:2022-01-01 11:31:14
PENTOXYIFYLLINE - Differential diagnosis
Authoritative Data Verified Data
- take about 10mg 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.
- take about 10mg of this product, add 5ml of water to dissolve, add 1ml of dilute sulfuric acid, and add several drops of Iodine test solution to generate brown precipitate.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 29).
Last Update:2022-01-01 11:31:14
PENTOXYIFYLLINE - Exam
Authoritative Data Verified Data
acidity
take this product l.Og, add water 50ml to dissolve, immediately add 1 drop of bromothymol blue indicator solution, the solution should be green or yellow, with sodium hydroxide titration solution (0.Olmol/L) titration to slightly blue, consumption of sodium hydroxide titration solution (0.0lmol/L) should not pass 0.2.
clarity and color of solution
take this product l. Add 50ml 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 rule 0902 first method); If it is colored, comparison with yellow No. 1 Standard Colorimetric solution (General 0901 first method) should not be deeper.
bromide
take 0.50g of this product, add 10ml of water to dissolve, add 0.5ml of dilute nitric acid and 1ml of silver nitrate solution, heat to boiling, cool, dilute to 25ml with water, shake, with standard potassium bromide solution 11.0 [per 1ml of standard potassium bromide solution is equivalent to 0.Olmg bromine (Br)], compared with the control solution prepared by the same method, should not be more concentrated.
Related substances
take this product, precision weighing, with solvent [methanol-0.544% potassium dihydrogen phosphate solution (1:1) mixed solution] Dissolved and quantitatively diluted to prepare a solution containing about 1 mg per 1 ml as a test solution; In addition, theobromine control, theophylline control, caffeine control and pentoxifylline control were accurately weighed, A mixed solution containing about 1ug each per 1 ml was prepared by dissolving and quantitatively diluting with a solvent as a reference solution. Test according to high performance liquid chromatography (General 0512). Octyl silane bonded silica gel was used as filler; Mobile phase A was methanol-0.544% potassium dihydrogen phosphate solution (3:7 ), mobile phase B was methanol-0.544% potassium dihydrogen phosphate solution (7:3 ); the detection wavelength was 272MN, and the gradient elution was performed according to the following table. Take the reference solution 20 u1 and inject it into human Liquid Chromatograph. The order of the separated peaks is theobromine peak, theophylline peak, caffeine peak and pentoxifylline peak. The retention time of the pentoxifylline peak is about 12 minutes, the separation degree of the theophylline peak from the caffeine peak should be greater than 4, and the separation degree of the caffeine peak from the pentoxifylline peak should be greater than 10. Then 20ul of the test solution and the reference solution were accurately measured, and the human liquid chromatograph was injected, and the chromatogram was recorded. If there are chromatographic peaks in the chromatogram of the test solution that are consistent with the retention time of theobromine peak, theophylline peak or caffeine peak, the peak area shall be calculated according to the external standard method, and shall not exceed 0.1%; the Peak area of other single impurities shall not be greater than that of pentoxifylline in the control solution (0.1% ) ; The total amount of impurities shall not exceed 0.5%.
loss on drying
take this product, at 60°C under reduced pressure drying to constant weight, weight loss should not exceed 0.5% (General rule 0831).
ignition residue
not more than 0.1% (General rule 0841).
Heavy metals
take l.Og of this product, add 2ml of dilute acetic acid and appropriate amount of water to dissolve into 25ml, check according to law (General Principles 0821 first law), containing heavy metals not to exceed 20 parts per million.
Last Update:2022-01-01 11:31:15
PENTOXYIFYLLINE - Content determination
Authoritative Data Verified Data
take about 0.2g of this product, precision weighing, add 8ml of glacial acetic acid to dissolve, add 32ml of acetic anhydride, according to the potentiometric titration method (General rule 0701), with perchloric acid titration solution (0.1 mol/L) titration, and the results of the titration were corrected with a blank test. Each 1 ml of perchloric acid titration solution (0.1 mol/L) corresponds to 27.83mg of C13H18N403.
Last Update:2022-01-01 11:31:16
PENTOXYIFYLLINE - Category
Authoritative Data Verified Data
Last Update:2022-01-01 11:31:16
PENTOXYIFYLLINE - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update:2022-01-01 11:31:16
PENTOXYIFYLLINE - Pentoxifylline Enteric-coated Tablets
Authoritative Data Verified Data
This product contains pentoxifylline (C13H18N403) should be the label amount of 93.0% ~ 107.0%.
trait
This product is an enteric coated tablet, which shows white color after removing the coating.
identification
This product is ground, weigh an appropriate amount (about 50mg equivalent to pentoxifylline), add chloroform 10ml, shake, filter, and the filtrate is evaporated to dryness on a water bath, the residue was taken according to the test of the identification items (1) and (2) under the pentoxifylline, showing the same reaction.
examination
should be in accordance with the relevant provisions under The tablet item (General rule 0101).
Content determination
Take 10 tablets of this product, remove the coating, precision weighing, fine, precision weighing an appropriate amount (about 0.1g of pentoxifylline), put it in a 100ml measuring flask, add 70ml of water, keep warm in a warm water bath, shake, dissolve pentoxifylline, let it cool, dilute with water until the scale, shake well, filter, and take an appropriate amount of the filtrate accurately, quantitatively dilute with water to make a solution containing about pentoxifylline (lOug) per 1 ml, and measure the absorbance at the wavelength of 274nm by UV-Vis spectrophotometry (General 0401 ), calculated as the absorption coefficient of C13H18N403 is 365.
category, storage
Same as pentoxifylline.
specification
0.lg
Last Update:2022-01-01 11:31:17
PENTOXYIFYLLINE - Pentoxifylline injection
Authoritative Data Verified Data
This product is a sterile aqueous solution of pentoxifylline. The content of pentoxifylline (C13H18N403) shall be between 95.0% and 105.0% of the labeled amount.
trait
This product is a clear colorless liquid.
identification
- take an appropriate amount of this product (about 10mg equivalent to pentoxifylline), add 1 ml of hydrochloric acid and 0.lg of potassium chlorate, and put it in a water bath to evaporate. The residue will appear purple when exposed to ammonia gas. Add several drops of sodium hydroxide test solution, the purple color disappeared.
- (take an appropriate amount of this product (about 10mg equivalent to pentoxifylline), dilute with 5ml of water, add 1 ml of dilute sulfuric acid, and add several drops of Iodine test solution to generate brown precipitate.
- 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.
examination
- the pH value should be 4.0 to 6.5 (General 0631).
- Related substances precision: take this product and quantitatively dilute it with a solvent [methanol-0.544% potassium dihydrogen phosphate solution (151) mixture] to prepare a solution containing about 1mg of pentoxifylline per 1 ml, as a test solution; Another reference theobromine, theophylline control, caffeine control and pentoxifylline control, precision weighing, A mixed solution containing about 2UG each per 1 ml was prepared by dissolving and quantitatively diluting with a solvent as a reference solution. If there are chromatographic peaks in the chromatogram of the test solution with the same retention time as theobromine peak, theophylline peak or caffeine peak, the peak area shall be calculated according to the external standard method, no one shall exceed 0.2% of the labeled amount of pentoxifylline; The peak area of other individual impurities shall not be greater than the peak area of pentoxifylline in the control solution (0.2%); The total amount of impurities shall not exceed 1.0%.
- the bacterial endotoxin of this product is taken and checked according to law (General rule 1143). The amount of endotoxin contained in 1 mg pentoxifylline should be less than 3.0EU.
- 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 octyl silane bonded silicon limb as filler; Methanol-0.544% potassium dihydrogen phosphate solution (48:52) as mobile phase; The detection wavelength was 272nm. Take caffeine reference and pentoxifylline reference, add mobile phase to dissolve and dilute to make solution containing about 50ug per 1 ml, take 20ul, inject into liquid chromatograph, record chromatogram, the degree of separation between the caffeine peak and the pentoxifylline peak should be greater than 5.0, and the theoretical plate number should not be less than 2000 based on the pentoxifylline peak.
- determination precision: take an appropriate amount of this product, quantitatively dilute it with mobile phase to prepare a solution containing pentoxifylline of 50ug per lml, and use it as a test solution. Take 20ul for precision measurement and inject it into the liquid chromatograph, the chromatogram was recorded, and the pentoxifylline reference substance was taken and determined by the same method. According to the external standard method to calculate the peak area, that is.
category
Same as pentoxifylline.
specification
(l)2ml:0.lg (2)5ml:0.lg
storage
light shielding, closed storage.
Last Update:2022-01-01 11:31:17
PENTOXYIFYLLINE - Pentoxifylline and Glucose Injection
Authoritative Data Verified Data
This product is a sterile aqueous solution of pentoxifylline and glucose. The contents of pentoxifylline (C13H18N4O3) and glucose (C6H12O6 • H20) should be 95.0% to 105.0% of the labeled amount.
trait
This product is colorless or almost colorless clear liquid.
identification
- take an appropriate amount of this product (about 50mg equivalent to pentoxifylline), add chloroform 20ml, fully shake, separate the chloroform layer, and put it on a water bath to evaporate, the residue was taken according to the test of identification items (1) and (2) under the pentoxifylline, showing the same reaction.
- take 5ml of this product and slowly drop it into the warm alkaline copper tartrate test solution to generate red precipitate of cuprous oxide.
- 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.
examination
- the pH value should be 4.0 to 6.0 (General 0631).
- Related substances precision: take this product and quantitatively dilute it with a solvent [methanol-0.544% potassium dihydrogen phosphate solution (151) mixture] to prepare a solution containing about 0.4mg of pentoxifylline per 1 ml, as a test solution; Another appropriate amount of theobromine reference, theophylline reference, caffeine reference and pentoxifylline reference, the solvent was added to dissolve and quantitatively dilute to prepare a mixed solution containing about 0.8UG each in 1 ml as a reference solution. If there is a peak with theobromine in the chromatogram of the test solution, the test solution shall be determined according to the method under pentoxifylline related substances except for the sample volume of 5ul, the peak with the same retention time of theophylline peak or caffeine peak shall not exceed 0.2% of the labeled amount of theobromine calculated by the peak area according to the external standard method; Other single impurity peaks (except the 5-hydroxymethylfurfural peak) the area shall not be greater than the peak area of pentoxifylline in the control solution (0.2% ), and the total amount of impurities shall not exceed 1.0%.
- 5-hydroxymethylfurfural take this product as a test solution; Take the appropriate amount of 5-hydroxymethylfurfural reference substance and theobromine reference substance, A mixed solution containing about 10ug each per 1 ml was prepared by dissolving and quantitatively diluting with a solvent under the item of related substances as a reference solution. According to the high performance liquid chromatography (General 0512) determination, with octanosilane bonded silica gel as filler; Mobile phase A is methanol-0.544% potassium dihydrogen phosphate solution (3:7 ), the mobile phase B was methanol-0.544% potassium dihydrogen phosphate solution (7:3 ) ; The detection wavelength was 284mn; The column temperature was 30 ° C.; Gradient elution was performed according to the following table. Take the reference solution 20 u1 and inject it into the liquid chromatograph. The resolution of 5-hydroxymethylfurfural peak and theobromine peak shall meet the requirements. Then, 20 u1 of the test solution and the reference solution were respectively injected into the liquid chromatograph, and the chromatograms were recorded. Calculated by peak area according to external standard method, 0.02% of the labeled amount of glucose shall not be passed.
- take an appropriate amount of heavy metal (about 3g of glucose), put it on a water bath and evaporate it to about 20ml, let it cool, add 2ml of acetate buffer (pH 3.5) and an appropriate amount of water to make it 25ml, inspection by law (General Principles 0821, law I), the content of heavy metals must not exceed 5 parts per million of the amount of glucose marked.
- The osmolality shall be determined according to the law (General 0632), and the millimosmolality shall be 260-32OmOsmol/kg.
- bacterial endotoxin this product, according to the inspection (General 1143), the amount of endotoxin per lm l should be less than 0.50EU.
- others should comply with the relevant provisions under injection (General 0102).
Content determination
- pentoxifylline was determined by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using octyl silane bonded silica gel as filler; Methanol-0.544% potassium dihydrogen phosphate solution (48:52) as mobile phase; The detection wavelength was 272nm. The caffeine control and the pentoxifylline control were taken, dissolved and diluted with the mobile phase to prepare a solution containing about 50ug each per 1 ml. Take 20ul, inject human liquid chromatograph, record chromatogram, the separation degree of caffeine peak and pentoxifylline peak should be greater than 5.0, the theoretical plate number is not less than 2000 according to pentoxifylline peak.
- determination precision: take an appropriate amount of this product and dilute it with mobile phase to prepare a solution containing about 50ug of pentoxifylline per 1 ml, as a test solution, take 20 u1 for precision measurement, injection liquid chromatograph, record chromatogram; Another pentoxifylline reference substance, the same method. According to the external standard method to calculate the peak area, that is.
- glucose the optical rotation was measured at 25 ° C. According to the law (General rule 0621), and multiplied by 2.0852 to obtain a Weight (g) containing C6H12O3 · H20 in of the sample.
category
Same as pentoxifylline.
specification
- 100ml: pentoxifylline 0.lg with glucose 5.0g
- 250ml: pentoxifylline O.lg with glucose 12.5g
- 250ml: pentoxifylline 0.2g Vs. Glucose 13.75G
storage
shading, closed storage
Last Update:2022-01-01 11:31:19
PENTOXYIFYLLINE - Pentoxifylline And Sodium Chloride Injection
Authoritative Data Verified Data
This product is pentoxifylline and sodium gasification of isotonic sterile aqueous solution. The content of pentoxifylline (C13H18N403) and sodium chloride (NaCl) should be 95.0% ~ 105.0% of the labeled amount.
trait
This product is a clear colorless liquid.
identification
- take an appropriate amount of this product (about 10mg equivalent to pentoxifylline), and put it on a water bath to evaporate it. Add 1 ml of hydrochloric acid and 0.lg of potassium chlorate to the residue, and put it on a water bath to evaporate it, after adding several drops of sodium hydroxide solution, the purple color disappeared.
- take an appropriate amount of this product (about equivalent to pentoxifylline lOmg), add 1 ml of dilute sulfuric acid, and add several drops of Iodine test solution, which will generate black precipitate.
- 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.
- This product sodium salt identification (1) of the reaction and gasification identification (1) of the reaction (General 0301).
examination
- the pH value should be 4.5 to 6.0 (General 0631).
- Related substances precision take this product, with solvent [methanol-0.544% potassium dihydrogen phosphate solution (1:1) the solution containing about 0.4mg of pentoxifylline per 1 ml was prepared by quantitative dilution of the mixed solution. The reference substance of theobromine, theophylline, caffeine and pentoxifylline was separately added for precision weighing, the solvent was added to dissolve and quantitatively dilute to prepare a mixed solution containing about 0.8UG each in 1 ml as a reference solution. Determination was performed according to the method under pentoxifylline related substances except that the injection volume was 50u1. If any chromatographic peak in the chromatogram of the test solution is consistent with the retention time of theobromine peak, theophylline peak or caffeine peak, the peak area shall not exceed 0.2% of the labeled amount of pentoxifylline calculated by external standard method; the Peak area of other single unknown impurities shall not be greater than the peak area of pentoxifylline in the control solution (0.2%); The total amount of impurities shall not exceed 1.0%.
- take 0821 of heavy metal, add 2ml of acetic acid buffer solution (pH3.5) and appropriate amount of water to make 25ml, and check according to law (the first method of general rule), containing no more than of heavy metals.
- The osmolality shall be 0632 ~ 320mosmol/kg when the osmolality is determined according to law (General Rule 260).
- bacterial endotoxin this product, according to the law to check (General 1143), the amount of endotoxin per lml should be less than 0.50EU.
- others should comply with the relevant provisions under injection (General 0102).
Content determination
- pentoxifylline was determined by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using octyl silane bonded silica gel as filler; Methanol-0.544% potassium dihydrogen phosphate solution (48:52) as mobile phase; The detection wavelength was 272nm. The caffeine control and the pentoxifylline control were taken, dissolved and diluted with the mobile phase to prepare a solution containing about 50ug each per 1 ml. 204 was injected into the liquid chromatograph, and the chromatogram was recorded. The separation degree between the caffeine peak and the pentoxifylline peak should be greater than 5.0, and the theoretical plate number should not be less than 2000 based on the pentoxifylline peak.
- determination of precision take appropriate amount of this product, quantitative dilution with mobile phase to prepare a solution containing pentoxifylline 50ug per 1 ml, as a test solution, take 20 u1, injection liquid chromatograph, record chromatogram; Another pentoxifylline reference substance, the same method. According to the external standard method to calculate the peak area, that is.
- Take 10ml of sodium chloride, add 40ml of water, add 5ml of 2% dextrin solution, 2ml of 2.5% borax solution and 5~8 drops of fluorescein indicator solution, and use silver nitrate titration solution (0.lmol/L) titration. Each l of silver nitrate titration solution (0.1 mol/L) corresponds to 5.844mg of NaCl.
category
Same as pentoxifylline.
specification
- 100ml: pentoxifylline 0.lg with sodium chloride 0.9g
- 250ml: pentoxifylline 0.lg with sodium chloride 2.25g
- 250ml: pentoxifylline 0.2g with sodium chloride 2.25g
storage
light shielding, closed storage.
Last Update:2022-01-01 11:31:20
PENTOXYIFYLLINE - Pentoxifylline sustained release tablets
Authoritative Data Verified Data
This product contains pentoxifylline (C13H18N4O3) should be 93.0% to 107.0% of the label.
trait
This product is a film-coated tablet, after removing the coating, white or white.
identification
take an appropriate amount of fine powder of this product (about 50mg equivalent to pentoxifylline), add 10ml of chloroform, shake, centrifuge, and take the chloroform solution to dry on a water bath, the residue was identified according to the test (1) and the test (2) under pentoxifylline and showed the same reaction.
examination
- dissolution dissolution of this product, according to the dissolution and release determination method (General 0931 second method), hydrochloric acid solution (9-1000)900ml as the dissolution medium, the rotation speed is 50 rpm, operate according to law. After 2 hours, 6 hours, 12 hours and 16 hours, respectively, take the solution 10ml, filtered, and immediately supplemented with the same temperature, the same volume of dissolution medium, take 3.0ml, L. 0ml, L. 0ml and 1.0ml of the continuous filtrate respectively, put it into a 25ml measuring flask, dilute to the scale with hydrochloric acid solution (9-1000), and shake well, the absorbance was measured at a wavelength of 0401 NM according to ultraviolet-visible spectrophotometry (General rule 351), and the elution amount of each tablet at different times was calculated based on the absorption coefficient of C13H18N403 being. The dissolution amount of each tablet at 2 hours, 6 hours, 12 hours and 16 hours shall be 10% to 30%, 30% to 55%, 50% to 85% and more than 75% of the labeled amount, respectively, the requirements shall be met.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
Take 10 tablets of this product, remove the coating, precision weighing, fine grinding, precision weighing an appropriate amount (about equivalent to pentoxifylline 0.4g ), put it in a 200ml measuring flask, add 100ml of water, keep warm in a warm water bath, shake, dissolve pentoxifylline, let it cool, dilute with water until the scale, shake well, filter, and take an appropriate amount of the filtrate accurately, prepare a solution containing about 10mg pentoxifylline per 1 ml by quantitative dilution with water, shake well, measure the absorbance at the wavelength of 274nm by UV-Vis spectrophotometry (General rule 0401), calculated as the absorption coefficient of C13H18N403 is 365.
category
Same as pentoxifylline.
specification
0.4g
storage
light shielding, sealed storage.
Last Update:2022-01-01 11:31:21
PENTOXYIFYLLINE - Reference Information
NIST chemical information | information provided by: webbook.nist.gov (external link) |
EPA chemical substance information | information provided by: ofmpeb.epa.gov (external link) |
biological activity | Pentoxifylline (BL-191) is a Hemorheology improving agent. Pentoxifylline is an orally active, non-selective phosphodiesterase (PDE) inhibitor with immunomodulatory, anti-inflammatory, hemorheological, antifibrinolytic and antiproliferative effects. Pentoxifylline can be used to study peripheral vascular disease, cerebrovascular disease and other diseases involving local microcirculation defects. |
Target | PDE |
Cell Line:
| MDA-MB-231 cells MDA-MB-231 cells MDA-MB-231 cells MDA-MB-231 cells MDA-MB-231 cells |
Concentration:
| 0.1 mM, 1 mM, 5 mM , 10 mM, 50 mM 0.5 mM 0.5 mM 0.5 mM 0.5 mM |
Incubation Time:
| 24 hours, 48 hours 12 hours, 24 hours, 36 hours 24 hours, 48 hours 24 hours, 48 hours 24 hours, 48 hours |
Result:
| Inhibited cell proliferation in a dose-dependent manner. Induced apoptosis. Induced approximately 20-28% of cell autophagy. Induced G0/G1 phase arrest. Induced high LC3-II/LC3-ratio. Significantly improved the spatial memory and effects were significant different from those of sham-operated and vehicle groups. |
Animal Model:
| Adult male Wistar rats 12-13-weeks-old (250-300 g) |
Dosage:
| 200 mg/kg |
Administration:
| Intraperitoneal injection, at 1hr before and 3 hr after ischemia |
purpose | This product is a vasodilator, which can improve the blood circulation of brain and limbs. Mice oral LD50 was 1385mg/kg. |
production method | by 1, 2-methyl-3-ethoxycarbonyl-5, 6-dihydropyran was obtained by cyclization of 3-bromochloropropane and ethyl acetoacetate at about 80 ℃, the bromination gives 1-bromo-5-hexanone, which is then condensed with the sodium salt of theobromine to give pentoxifylline. |
Last Update:2024-04-09 02:00:10