1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione
Zidovudine
CAS: 30516-87-1
Molecular Formula: C10H13N5O5
1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione - Names and Identifiers
1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione - Physico-chemical Properties
| Molecular Formula | C10H13N5O5 |
| Molar Mass | 283.24 |
| Density | 1.3382 (rough estimate) |
| Melting Point | 113-115 °C (lit.) |
| Boling Point | 410.43°C (rough estimate) |
| Specific Rotation(α) | D25 +99° (c = 0.5 in water) |
| Flash Point | 9℃ |
| Water Solubility | 1-5 g/100 mL at 17 ºC |
| Solubility | Soluble in water (50 mg/ml), DMSO, and methanol. |
| Appearance | White crystal |
| Color | White to Off-white |
| Merck | 14,10123 |
| BRN | 3595791 |
| pKa | pKa 9.53(H2Ot = 25.0±0.1I = 0.00) (Uncertain) |
| Storage Condition | 2-8°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| Sensitive | Light Sensitive & Hygroscopic |
| Refractive Index | 47 ° (C=1, H2O) |
| MDL | MFCD00006536 |
| Physical and Chemical Properties | Melting Point: 106-112°C |
| Use | Used as anti-HIV and antiviral drugs |
1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R40 - Limited evidence of a carcinogenic effect R36/37/38 - Irritating to eyes, respiratory system and skin. R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. |
| Safety Description | S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S36 - Wear suitable protective clothing. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| UN IDs | UN1230 - class 3 - PG 2 - Methanol, solution |
| WGK Germany | 3 |
| RTECS | XP2072000 |
| FLUKA BRAND F CODES | 10 |
| HS Code | 29349990 |
| Hazard Note | Harmful |
| Toxicity | LD50 in male, female mice, male, female rats (mg/kg): 3568, 3062, 3084, 3683 orally; >750 i.v. (all species) (Ayers) |
1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione - Reference
| Reference Show more | 1. [IF=3.69] Yayun Wu et al."Polysaccharides of vinegar-baked radix bupleuri promote the hepatic targeting effect of oxymatrine by regulating the protein expression of HNF4α, Mrp2, and OCT1."J Ethnopharmacol. 2021 Mar;267:113471 |
1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione - Standard
Authoritative Data Verified Data
This product is l-(3-azido-2, 3-dideoxy-B-D-ribofuranosyl)-5-methylpyrimidine -2,4(1H,3H)-Diketone. The content of C10H13N504 shall be between 97.0% and 102.0% based on the water-free content.
Last Update：2024-01-02 23:10:35
1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione - Trait
Authoritative Data Verified Data
- This product is white to light yellow crystalline powder.
- This product is soluble in methanol, N ,N-dimethylformamide or dimethyl sulfoxide, soluble in ethanol, slightly soluble in water.
melting point
The melting point of this product (General 0612) is 122~126°C.
specific rotation
take this product, precision weighing, plus ethanol dissolution and quantitative dilution to make a solution containing about 10 mg per 1 ml, at 25°C, according to the law (General 0621), the specific rotation was 60.5 ° to 63.0 °.
Last Update：2022-01-01 11:53:54
1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione - Differential diagnosis
Authoritative Data Verified Data
- This product is dissolved in water and diluted quantitatively to prepare a solution containing 10ug per lml, which is determined by UV-Vis spectrophotometry (General rule 0401), there is a maximum absorption at a wavelength of 267nm and a minimum absorption at a wavelength of 234mn. The absorption coefficient at a wavelength of 267mn should be 361 to 399.
- 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.
- The infrared absorption spectrum of this product should be consistent with that of the reference product (General rule 0402).
Last Update：2022-01-01 11:53:54
1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione - Exam
Authoritative Data Verified Data
clarity and color of solution
take 0902g of this product and add 10ml of water to dissolve the solution. 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 first method), it shall not be deeper in comparison with the yellow No. 1 Standard Colorimetric solution (General rule 0901 first method).
Related substances
Take 10mg of this product, accurately weigh, put it in 10ml measuring flask, add methanol to dissolve and dilute to the scale, shake, as a test solution; take stavudine 12.5mg in a 25ml measuring flask, add methanol to dissolve and dilute to the scale, shake, as impurity control solution (1); take 10mg of impurity I (3 '-chloro-3'-deoxythymidine) and 10mg of thymidine control, put them in a 10ml measuring flask, dissolve them in methanol, dilute them to the scale, and shake them well, as impurity reference solution (2); Respectively take 1ml of impurity reference solution (1) and 1ml of impurity reference solution (2) in a 100ml measuring flask, and add 1ml of test solution in precision, dilute with methanol to the scale, shake, as a control solution; Precision take the control solution 1ml, 50ml flask, diluted with methanol to the scale, shake, as a sensitivity solution. According to the chromatographic conditions under the content determination item, the sensitivity solution 10u1 is injected into the liquid chromatograph, and the signal-to-noise ratio of the zidovudine peak should be greater than 10; then 10 u1 of the test solution and the control solution are accurately measured, and the human liquid chromatograph is injected respectively, and the chromatogram is recorded to 2.5 times of the retention time of the main component chromatographic peak. If there are impurity peaks in the chromatogram of the test solution, calculated by the peak area according to the external standard method, the content of stavudine shall not exceed 0.5%, and the contents of impurity I and thymine shall not exceed 1.0%. The Peak area of other individual impurities shall not be greater than 0.5 times (0.5%) of the peak area of zidovudine in the control solution, and the total amount of impurities shall not exceed 2.5%. The peak in the chromatogram of the test solution which is smaller than the area of the zidovudine peak in the sensitivity solution is negligible (0.02%).
triphenyl toluene
take this product 10mg, precision weighing, 10ml flask, add methanol dissolved and diluted to the scale, shake, as a test solution; another 10mg of tribenzyl alcohol reference product was accurately weighed, placed in a 10ml measuring flask, dissolved in methanol and diluted to the scale, and then shaken. Then, 1ml was accurately weighed, placed in a 200ml measuring flask, and diluted to the scale with methanol, shake, as a reference solution; Precision take the control solution 1ml, put in 50ml measuring flask, diluted with methanol to scale, shake, as a sensitivity solution. Tested according to high performance liquid chromatography (General 0512). Silica gel bonded with eighteen alkyl silane was used as the filler; Methanol-water (80:20) was used as the mobile phase; The detection wavelength was 215nm. l0ul of the sensitivity solution should be injected into the human liquid chromatograph, and the signal-to-noise ratio of the main component chromatographic peak should be greater than 10. l0ul of the sample solution and the reference solution should be accurately measured and injected into the liquid chromatograph respectively, and the chromatograms should be recorded. If there is a chromatographic peak in the chromatogram of the test solution that is consistent with the retention time of the tribenzyl alcohol peak, the peak area shall be calculated according to the external standard method, and the content of tribenzyl alcohol shall not exceed 0.5%.
residual solvent
methanol, dichloromethane, ethyl acetate, 1, 4-dioxane, pyridine and toluene take this product, precision weighing, and dimethyl sulfoxide dissolved and diluted to make a solution containing 50mg per 1 ml, as a test solution; Another precision weighing methanol, dichloromethane, ethyl acetate, 1, 4-dioxane, pyridine and toluene, with dimethyl sulfoxide quantitative dilution made in each lml containing methanol 150ug, A solution of 30ug of dichloromethane, 250ug of ethyl acetate, 19ug of 1, 4-dioxane, 10ug of pyridine and 44.6ug of toluene was used as a control solution. 5ml of each of the reference solution and the test solution were respectively placed in the headspace bottle and sealed. According to the determination method of residual solvent (General Principle 0861 second method), the capillary column with 6% cyanopropyl phenyl-94% dimethyl polysiloxane (or similar polar) as stationary liquid is used as the chromatographic column, and the temperature is programmed, the initial temperature is 60°C, maintained for 15 minutes, heated to 220°C at a rate of 40°C per minute, maintained for 5 minutes; The temperature of the sample inlet is 210°C, and the temperature of the detector is 250°C; the Headspace bottle equilibration temperature was 105°C and the equilibration time was 30 minutes. Take the reference solution into the headspace, and the separation degree between the peaks of each component shall meet the requirements. The sample solution and the reference solution were sampled by Headspace injection, and the chromatogram was recorded. The peak area shall be calculated according to the external standard method and shall comply with the regulations.
triethylamine, dimethylformamide and dimethyl sulfoxide
take this product, precision weigh, add methanol to dissolve and dilute to make a solution containing 50mg per lml, as a test solution; Another precision weigh triethylamine, N, A solution containing 10ug of triethylamine, 44ug of dimethylformamide and 250ug of dimethylsulfoxide per 1 ml was prepared by quantitative dilution with methanol in an appropriate amount using N-dimethylformamide and dimethylsulfoxide as a reference solution. According to the determination method of residual solvent (General Principle 0861 third method), the capillary column with 6% cyanopropyl phenyl-94% dimethyl polysiloxane (or similar polar) as stationary liquid is used as the column, the initial temperature was 60°C, maintained for 3 minutes, and the temperature was raised to 220°C at a rate of 40°C per minute for 5 minutes. The inlet temperature is 150°C, and the detector temperature is 250°C; The reference solution 1u1 is injected, and the separation degree between peaks of each component shall meet the requirements. Then 1 u1 of the test solution and 1 u1 of the reference solution are accurately measured and injected into the gas chromatograph to record the chromatogram. The peak area shall be calculated according to the external standard method, and the content of triethylamine shall not exceed 0.02%, and the others shall be in accordance with the provisions.
moisture
take this product, according to the moisture determination method (General 0832 first method 1), containing water not more than 1.0%.
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%.
precious metals
The residue left under the item of taking the ignition residue shall not contain more than 10 parts per million of heavy metal when examined by law (General Principles 0821, Law II).
Last Update：2022-01-01 11:53:56
1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione - Content determination
Authoritative Data Verified Data
measured by high performance liquid chromatography (General 0512).
chromatographic conditions and system suitability test
silica gel bonded with eighteen alkyl silane was used as the filler; Methanol-water (20:80) was used as the mobile phase; The detection wavelength was 265nm. Take the appropriate amount of zidovudine control and impurity I control, add methanol to dissolve and dilute to make each 1 ml containing zidovudine lmg and impurity I 0. The mixed solution of Olm is used as the applicable solution of the system, and 10ul is injected into the liquid chromatograph to record the chromatogram. The separation degree of zidovudine peak and impurity I peak should be greater than 2.0.
assay
take about 10mg of this product, weigh it accurately, put it in a 50ml measuring flask, add methanol to dissolve and dilute it to the scale, shake it well, and use it as a test solution, 10u1 was injected into the liquid chromatograph accurately, and the chromatogram was recorded. The zidovudine reference substance was taken and determined by the same method. According to the external standard method to calculate the peak area, that is.
Last Update：2022-01-01 11:53:56
1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione - Category
Authoritative Data Verified Data
antiviral drugs.
Last Update：2022-01-01 11:53:57
1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 11:53:57
1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione - Zidovudine Tablets
Authoritative Data Verified Data
This product contains Zidovudine (C10H13N504) should be 90.0%-110.0% of the label.
trait
This product is a white tablet or film-coated tablet, film-coated tablets after removal of white to light yellow.
identification
- the sample solution in terms of dissolution was taken and measured by ultraviolet-visible spectrophotometry (General rule 0401), which showed that there was a maximum absorption at a wavelength of Nm.
- 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
- Related substances take an appropriate amount of this product's fine powder (about equivalent to zidovudine lOOmg), weigh it accurately, put it in a 100ml measuring flask, add an appropriate amount of mobile phase to dissolve zidovudine and dilute it to the scale, shake it well, filter, take the filtrate as a test solution; Take 1ml of precision, put it in a 100ml measuring flask, dilute to the scale with mobile phase, shake, as a control solution; Take another thymine control, precision weighing, plus mobile phase dissolution and quantitative dilution of the prepared solution containing about 10ug per 1ml, as a reference solution. According to the chromatographic conditions under the content determination item, take the sample solution, the control solution and the reference solution with 10 u1 respectively, and inject the human liquid chromatograph respectively, record the chromatogram of the test solution to 3 times of the retention time of the main component peak. If the peak in the chromatogram of the test solution is consistent with the thymine retention time in the chromatogram of the reference solution, the peak area shall be calculated according to the external standard method, and 1.0% of the labeled amount of zidovudine shall not be exceeded; the Peak area of other individual impurities shall not be greater than the main peak area of the control solution (1.0% ) , and the sum of the peak areas of other impurities shall not be greater than 2 times the main peak area of the control solution (2.0%).
- the dissolution of this product, according to the dissolution and release determination method (General rule 0931 The first method), water 900ml as the dissolution medium, the rotation speed is 10 rpm, according to the law, after 30 minutes, take an appropriate amount of the solution, filter it, take an appropriate amount of the filtrate in a precise amount, and quantitatively dilute it with water to make a solution containing 15ug of zidovudine per 1 ml, which is used as a test solution; in addition, an appropriate amount of zidovudine reference substance was carefully weighed, dissolved with water and quantitatively diluted to prepare a solution containing about 15ug per 1 ml, which was used as a reference 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 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
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler; Methanol-water (30:70) as mobile phase; The detection wavelength was 265mn. 10 mg of impurity I and zidovudine reference product were accurately weighed and placed in a 100ml measuring flask, dissolved with mobile phase and diluted to the scale. Then, shake well, inject 10u1 into human liquid chromatograph, and record the chromatogram. The theoretical plate number is not less than 2000 based on the calculation of the zidovudine peak, and the separation degree of the zidovudine peak from the impurity I peak should be greater than 2.0.
- determination of 20 tablets of this product, precision weighing, fine grinding, precision weighing an appropriate amount (about equivalent to zidovudine lOOmg), put it in a 100ml measuring flask, and add mobile phase to shake to dissolve zidovudine, dilute to the scale with mobile phase, shake, filter, take 10ml filtrate accurately, put it in a 100ml measuring flask, dilute to the scale with mobile phase, shake well, as a test solution, injection of 10u1 into the liquid chromatograph with precision and recording the chromatogram; Accurate weighing of the appropriate amount of zidovudine reference substance, dissolving with mobile phase and quantitatively diluting it into about 0 in 1 ml. lmg solution, the same method for determination. According to the external standard method to calculate the peak area, that is.
category
Same as zidovudine.
specification
(1)0.lg (2)0.3g
storage
light shielding, sealed storage.
Last Update：2022-01-01 11:53:58
1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione - Zidovudine injection
Authoritative Data Verified Data
This product is a sterilized aqueous solution of zidovudine. The content of zidovudine (C10H13N504) shall be between 90.0% and 110.0 of the indicated amount.
trait
This product is colorless to yellowish clear liquid.
identification
- This product is diluted with water to make a solution containing about 10ug per lml, which is determined by ultraviolet-visible spectrophotometry (General rule 0401) and has a maximum absorption at the wavelength of 267nm, there is minimal absorption at a wavelength of 234nm.
- 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 3.5 to 7.0 (General 0631).
- color this product should be colorless; If the color is colored, it should not be deeper compared with the yellow No. 1 Standard Colorimetric liquid (General rule 0901 first method).
- Related Substances: take 5ml of this product, put it in a 50ml measuring flask, dilute it to the scale with methanol, shake it well, and use it as a test solution, add methanol to dissolve in a 10ml measuring flask, dilute to the scale, shake well, take 1ml in a 100ml measuring flask, and add 1ml of test solution, dilute to the scale with methanol, shake, as a control solution; The amount of control solution, diluted 50 times with methanol as a sensitivity solution. According to the chromatographic conditions under the content determination item, the sensitivity solution should be injected into the human liquid chromatograph, and the signal-to-noise ratio of the main component chromatographic peak should be greater than 10; Then the sample solution and the control solution should be accurately measured at 10 u1 respectively, human liquid chromatograph was injected respectively, and the chromatogram was recorded to 2.5 times of the retention time of the main component chromatographic peak. If there are impurity peaks in the chromatogram of the test solution, thymine shall be calculated by the peak area according to the external standard method, and shall not exceed 0.5% of the labeled amount of zidovudine, the Peak area of other single impurities shall not be greater than 0.5 times (0.5%) of the peak area of zidovudine in the control solution, and the sum of each impurity shall not exceed 2.5%. The peak in the chromatogram of the test solution which is smaller than the area of the zidovudine peak in the sensitivity solution is negligible (0.02%).
- the bacterial endotoxin of this product is taken and checked according to law (General rule 1143). The amount of endotoxin contained in zidovudine per 1 mg should be less than 1.0EU.
- 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 eighteen alkyl silane bonded silica gel as filler; Methanol-water (20:80) as mobile phase; The detection wavelength was 265mn. Take the appropriate amount of zidovudine control and impurity I control, add methanol to dissolve and dilute to make each 1 ml containing zidovudine lmg and impurity I 0. The mixed solution of Olmg is used as the applicable solution of the system. 10ul injection liquid chromatograph is used to record the chromatogram. The separation degree of zidovudine peak and impurity I peak should be greater than 2.0.
- the product is quantitatively diluted with methanol to make a solution containing about 0.2mg of zidovudine per 1 ml, which is used as a test solution. 10u1 is injected into the liquid chromatograph with precision and the chromatogram is recorded; another zidovudine reference substance was taken, operated with the same method, and the peak area was calculated according to the external standard method.
category
Same as zidovudine.
specification
(l )10ml:0.lg (2)20ml:0.2g
storage
light shielding, closed storage.
Last Update：2022-01-01 11:53:59
1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione - Zidovudine Capsules
Authoritative Data Verified Data
This product contains Zidovudine (C10H13N504) should be 90.0% ~ 110.0% of the label amount.
trait
This product is a capsule containing white to brown granules or powder.
identification
- the sample solution in terms of dissolution was taken and measured by ultraviolet-visible spectrophotometry (General rule 0401), which showed that there was a maximum absorption at a wavelength of Nm.
- 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 contents under the item of difference in loading amount of related substances should be finely divided and mixed, and a proper amount (about equivalent to zidovudine lOOmg) should be accurately weighed and placed in a 100ml measuring flask, add appropriate amount of mobile phase to dissolve zidovudine and dilute to the scale, shake well, filter, take the continued filtrate as a test solution; Take 1ml of precision, put it in a 100ml measuring flask, dilute to the scale with mobile phase, shake, as a control solution; Take another thymine reference, precision weighing, dissolved and quantitatively diluted with mobile phase to make a solution containing about 10ug per 1ml, as a control solution. According to the chromatographic conditions under the content determination item, take 10ul of the test solution, the control solution and the reference solution, and inject the human liquid chromatograph respectively, record the chromatogram of the test solution to 3 times of the retention time of the main component peak. If the peak in the chromatogram of the test solution is consistent with the retention time of thymine in the chromatogram of the reference solution, the peak area shall be calculated according to the external standard method, the Peak area of other individual impurities not exceeding the labeled amount of zidovudine shall not be greater than the main peak area of the control solution (1.0% ) , and the sum of the peak areas of other impurities shall not be greater than 2 times the main peak area of the control solution (2.0%).
- the dissolution of this product, according to the dissolution and release determination method (General rule 0931 first method), with water as the dissolution medium, the speed is 100 rpm, according to the law, after 30 minutes, take an appropriate amount of the solution, filter it, take an appropriate amount of the filtrate in a precise amount, and quantitatively dilute it with water to make a solution containing 15ug of zidovudine per 1 ml, which is used as a test solution; in addition, an appropriate amount of zidovudine reference substance was carefully weighed, dissolved with water and quantitatively diluted to prepare a solution containing about 15ug per 1 ml, which was used as a reference 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 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
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler; Methanol-water (30:70) as mobile phase; The detection wavelength was 265mn. 10mg of impurity I and 10mg of zidovudine reference product were accurately weighed and placed in a-100ml measuring flask. The mixture was dissolved with mobile phase and diluted to scale. The theoretical plate number is not less than 2000 based on the calculation of the zidovudine peak, and the separation degree of the zidovudine peak from the impurity I peak should be greater than 2.0.
- determination method: the contents under the item of loading amount difference were finely divided and mixed evenly, and an appropriate amount (about 100mg equivalent to zidovudine) was accurately weighed, placed in a 100ml measuring flask, and the appropriate amount of mobile phase was added, shake to dissolve zidovudine, dilute to scale with mobile phase, shake well, filter, take 10ml of continuous filtrate precisely, put it in 100ml measuring flask, dilute to scale with mobile phase, shake well, as a test solution, 10UL is injected into the liquid chromatograph in a precise amount, and the chromatogram is recorded. In addition, an appropriate amount of zidovudine reference substance is accurately weighed, dissolved and quantitatively diluted with mobile phase to make about 0 in 1 ml. lmg solution, the same method of determination, according to the external standard method to calculate the peak area, that is.
category
Same as zidovudine.
specification
(1)0.lg (2)0.25g (3)0.3g
storage
shading, sealed preservation,
Last Update：2022-01-01 11:54:00
1-(3-azido-2,3-dideoxypentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione - Zidovudine and Lamivudine Tablets
Authoritative Data Verified Data
This product contains Zidovudine (C10H13N504) and lamivudine (C8H11N303) should be 90.0% ~ 110.0% of the label amount.
trait
This product is a film-coated tablet, white or off-white after removal of the coating.
identification
- take an appropriate amount of fine powder of this product (about equivalent to zidovudine lOOmg), add 50ml of methanol, fully shake, filter, and take the continued filtrate as the test solution. Another lamivudine and zidovudine control were dissolved and diluted by adding fermentation liquor to prepare a mixed solution containing 1 mg of lamivudine and 2mg of zidovudine per 1 ml as a control solution. According to the thin layer chromatography (General 0502) test, take the above two Solutions 10 u1, respectively, on the same silica gel GF254 thin layer plate, with dichloromethane-methanol-glacial acetic acid (90:10:3) for the development of the agent, expand, dry, set the UV light (254mn) under the inspection, the position and color of the two main spots displayed by the test solution should be consistent with the main spots corresponding to the control solution ^
- (2) in the chromatogram recorded under the content determination item, the retention time of the two main peaks of the test solution should be consistent with the retention time of the two main peaks of the zidovudine and the lamivudine reference solution, respectively.
- two items (1) and (2) above can be selected as one item.
examination
- Related substances the test solution under the content determination item was taken as the test solution. According to the chromatographic conditions under the content determination item, take the sample solution 10 u1 accurately, inject the human liquid chromatograph, and record the chromatogram. If there are impurity peaks in the chromatogram of the test solution, the relative retention time, correction factor, limit and attribution of each impurity peak are calculated according to the following formula.
- dissolution of this product, according to the dissolution and release determination method (General 0931 second method), with 0.900ml of lmol/L hydrochloric acid solution is the dissolution medium, and the rotation speed is 75 RPM. The operation is carried out according to law. After 30 minutes, the appropriate amount of the solution is taken, filtered, and 1ml of the continued filtrate is accurately taken, in a 10ml measuring flask, dilute to the scale with mobile phase, shake well, and use as a test solution; Take the zidovudine reference product about 33.4mg and the lamivudine reference product about 16.7mg, and weigh them precisely, put it in the same lOOml measuring flask, add the dissolution medium to dissolve and dilute to the scale, shake well, take 5ml accurately, put it in the 50ml measuring flask, dilute it to the scale with mobile phase, shake well, as a control solution. Determined by high performance liquid chromatography (General 0512). Silica gel was bonded with eighteen alkyl silane as filler; 0.025mol/L ammonium acetate solution (with glacial acetic acid to adjust the pH value to 4.0 0.1)-methanol (80:20) as mobile phase, the detection wavelength was 270NNU, and 10ul of the test solution and the reference solution were respectively injected into the human liquid chromatograph. The chromatogram was recorded, and the dissolution amount of zidovudine and lamivudine in each tablet was calculated by peak area according to external standard method. The limit shall be 80% of the labeled amount and shall be in accordance with the regulations.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
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; 0.025mol/L ammonium acetate solution (with glacial acetic acid to adjust the pH value to 4.0±0.1) as mobile phase A, methanol was used as mobile Phase B, acetonitrile was used as mobile phase C, and gradient elution was performed according to the following table; The flow rate was 1.0ml per minute; The detection wavelength was 270mn; And the column temperature was 25°C. Take the appropriate amount of zidovudine impurity I, thymidine and thymidine, add 0.025mol/L ammonium acetate solution (pH 4.0±0.1)-methanol (95:5) A solution containing about 0.03mg of zidovudine impurity I, 0.03mg of thymidine and 0.06mg of thymine per 1 ml was prepared by dissolution and dilution as a control solution (1). Take another zidovudine control about 33mg, put it in a measuring flask, Add 10ml of control solution (1), add 0.025mol/L ammonium acetate solution (pH 4.0±0.1)-methanol (95:5) dissolve and dilute to the scale, shake, as a control solution (2). Take 1 bottle of lamivudine impurity mixed reference product (containing cytosine, uracil, lamivudine, salicylic acid and lamivudine impurity I ~ V), add 3ml of reference solution (2), ultrasonic to dissolve, shake, as the system applicable solution, take 10u1 injection liquid chromatograph, record chromatogram. The resolution of lamivudine impurity II peak and lamivudine peak shall meet the requirements, and the resolution of lamivudine peak and thymidine peak shall not be less than 2.0; The resolution of zidovudine peak and zidovudine impurity I peak shall not be less than 2.0.
- determination Method: Take 5 tablets of this product, put them in a 500ml measuring flask, add appropriate amount of water, fully shake to completely disintegrate the tablets, sonicate to dissolve lamivudine and zidovudine, dilute them to the scale with water, and shake them well, filter, Take 5ml of filtrate accurately, put it in a 50ml measuring flask, dilute to the mark with 0.025mol/L ammonium acetate solution (pH 4.0±0.1)-methanol (95:5), as a test solution. Take 10ul for precise measurement, inject human liquid chromatograph, record chromatogram; Take zidovudine reference product about 30mg and lamivudine reference product about 15mg for precise weighing, put in the same lOOml measuring flask, 0.025mol/L ammonium acetate solution (pH 4.0±0.1)-methanol (95:5) was added to dissolve and dilute to the scale, and the solution was shaken to be used as a reference solution and measured by the same method. According to the external standard method to calculate the peak area, that is.
category
antiviral drugs.
storage
sealed storage.
Last Update：2022-01-01 11:54:01
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CAS: 30516-87-1
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Email: sales@tnjchem.com
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Product Name: Zidovudine Visit Supplier Webpage Request for quotationCAS: 30516-87-1
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