ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME)
roxithromycin
CAS: 80214-83-1
Molecular Formula: C41H76N2O15
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Names and Identifiers
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Physico-chemical Properties
| Molecular Formula | C41H76N2O15 |
| Molar Mass | 837.05 |
| Density | 1.25±0.1 g/cm3(Predicted) |
| Melting Point | 111-118?C |
| Boling Point | 864.7±75.0 °C(Predicted) |
| Specific Rotation(α) | D25 -77.5 ±2° (c = 0.45 in chloroform) |
| Flash Point | >110°(230°F) |
| Water Solubility | Soluble in water to 18µg/ml |
| Solubility | Easily soluble in ethanol or acetone, more soluble in methanol or ether, almost insoluble in water. |
| Vapor Presure | 7.17E-35mmHg at 25°C |
| Appearance | White crystalline powder |
| Merck | 14,8276 |
| pKa | pKa 9.27±0.01(H2Ot = 25.0I = 0.15 (KCl)) (Uncertain) |
| Storage Condition | Sealed in dry,2-8°C |
| Refractive Index | 1.535 |
| MDL | MFCD00214389 |
| Physical and Chemical Properties | White crystalline powder, odorless, bitter taste. Soluble in ethanol or acetone, more soluble in methanol or ether, a few insoluble in water. [Α] D23-77.5 ° ± 2 °(C = 0.45, chloroform). |
| Use | For a new generation of macrolide antibiotics |
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| RTECS | KF4990000 |
| HS Code | 29415000 |
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Upstream Downstream Industry
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Reference
| Reference Show more | 1. Liu Jiang, Liu Yuan, Li Yingchun, Tang Hui, Wu Binbing. Preparation and characterization of erythromycin surface molecularly imprinted polymers by two-step distillation-precipitation polymerization [J]. Chinese Journal of Polymer Science 2014(12):1635-1642. 2. Zhang Yuxiang, Wei Jianping, Song Zihan, et al. Distribution and control of cold-tolerant bacteria in frozen chicken [J]. Modern Food Science and Technology 2020 v.36;No.247(03):146-155. 3. Wang Xiaoji, Tang Hui, Li Yingchun, etc. Preparation and evaluation of erythromycin molecularly imprinted polymer microspheres by multi-step swelling suspension polymerization [J]. China Pharmacy, 2013, 024(013):1197-1200. 4. Chen Xiaojuan, Liu genqi, Ren genrui, etc. Study of sulfadimidine molecularly imprinted two-dimensional photonic crystal hydrogel sensor [J]. Journal of Chemistry of universities, 2018, 29 (2):212-218. 5. Li manxiu, Hu Xuena, Jia Zuoli, etc. Determination of roxithromycin by ionic liquid-enhanced fluorimetry [J]. Chinese Journal of antibiotics, 2015, 40(011):841-844. 6. Huang Hao, Zhu Yuen, Li Hua, et al. Effect of humic acid dosage on the degradation of Tylosin in chicken manure [J]. Journal of Shanxi Agricultural Sciences, 2020, v.48;No.408(02):116-119. 7. Gao Min-jun, Liu genqi, Xue Yafeng, Chen Xiaojuan, Shi Weijiang, Fan Xiaodong. Study on erythromycin molecularly imprinted two-dimensional photonic crystal hydrogel sensor [J]. Journal of Analytical Chemistry, 2017,45(05):727-733. 8. Li Xiaodan, Cong Jinpeng, Yu Jie, et al. Effect and mechanism of Yiqi huatan Tongluo method on pulmonary fibrosis in rats [J]. Journal of Qingdao University (Medical Sciences), 2019. 9. Zhang Lu Dan, Lu Peng, Pi Jia Xin, Yan Hong Li, Zhang Yu, Xie Jia Rong, Liu Zhi Dong. Pharmacokinetics of cyclic ester erythromycin nanocrystals administered by pulmonary spray in rats [J]. Journal of Drug Evaluation Research, 2021,44(04):762-766. 10. Chen Shu-Xin, Wang Jing, He Shi-Chong, Liu Yan-Zheng, Feng Huajun, Mu Peng-Qian. Determination of 17 antibiotics in water by ultra performance liquid chromatography-tandem mass spectrometry [J]. China Environmental Monitoring, 2020,36(06):119-126. 11. Han, Qizhi, et al.. "Ecobiology 29.5 (2020): 625-633. 12. Chunxi Zhao, Yang Jiao, He Gao, Yaling Yang, Hong Li, N, S co-doped carbon dots for temperature probe and the detection of tetracycline based on the inner filter effect, Journal of Photochemistry and Photobiology A: Chemistry, Volume 367, 2018, Pages 137- 13. [IF=7.312] Yuanyuan Zhang et al."Transformation of antibacterial agent roxithromycin in sodium hypochlorite disinfection process of different water matrices."Sep Purif Technol. 2019 Apr;212:528 14. [IF=6.291] Jiahua Guo et al."Transcriptomic analysis suggests the inhibition of DNA damage repair in green alga Raphidocelis subcapitata exposed to roxithromycin."Ecotox Environ Safe. 2020 Sep;201:110737 15. [IF=3.679] Yunlei Cao et al."A sulfamethoxazole molecularly imprinted two-dimensional photonic crystal hydrogel sensor."Soft Matter. 2021 May;17(19):4969-4978 16. [IF=2.823] Han Qizhi et al."Involvement of oxidative stress in the sensitivity of two algal species exposed to roxithromycin."Ecotoxicology. 2020 Jul;29(5):625-633 17. [IF=2.19] Jianping Wei et al."Distribution of cold-resistant bacteria in quick-frozen dumpling and its inhibition by different antibacterial agents."J Food Process Pres. 2020 Sep;44(9):e14710 18. [IF=6.498] Jingyun Shi et al."Groundwater antibiotics and microplastics in a drinking-water source area northern China: Occurrence, spatial distribution, risk assessment, and correlation."Environ Res. 2022 Jul;210:112855 19. [IF=2.896] Zhongqi Xu et al."Simultaneous separation of 12 different classes of antibiotics under the condition of complete protonation by capillary electrophoresis coupled contactless conductivity detection."Anal Methods-Uk. 2021 Dec ;: |
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Nature
Open Data Verified Data
white crystalline powder, odorless, bitter.
Soluble in ethanol or acetone, more soluble in methanol or ether, almost insoluble in water.
Last Update：2024-01-02 23:10:35
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Quality standards-Chinese Pharmacopoeia 2005 edition
Open Data Verified Data
The content of roxithromycin (C41 H76 Nz Ois) shall not be less than 94, calculated as anhydrous. 026; PH value should be 8.0~10.0(0.lg the product is soluble in 150mL water); There is a beauty of substances should comply with the provisions; Containing water not over 3. 0%; Ignition residue should not exceed 0.1%; Heavy metal should not exceed 0. 001%; Abnormal toxicity should be consistent with the provisions.
Last Update：2022-01-01 08:52:37
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Standard
Authoritative Data Verified Data
This product is 9-[O [(2-methoxyethoxy) methyl] oxime] erythromycin. According to the anhydrous and solvent-free calculation, containing roxithromycin (C41H76N2O15) shall not be less than 94.0%.
Last Update：2024-01-02 23:10:35
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline powder; Odorless f is slightly hygroscopic.
- This product is soluble in ethanol or acetone, soluble in fermentation broth, slightly soluble in acetonitrile, almost insoluble in water.
specific rotation
take this product, precision weighing, plus anhydrous ethanol dissolution and quantitative dilution of about 20mg per lml solution, according to the law (General 0621), the specific rotation was from -82 ° to -87 °.
Last Update：2022-01-01 13:35:38
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Preparation Method
Open Data Verified Data
erythromycin is reacted with hydroxylamine hydrochloride in triethylamine and methanol to form oxime, and then with methoxyethoxymethyl chloride in acetone to obtain roxithromycin.
Last Update：2022-01-01 08:52:38
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Differential diagnosis
Authoritative Data Verified Data
- 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 control (Spectrum set 786). In case of inconsistency, take lg of this product, put it in a 10ml test tube with a stopper, add 2ml of 80% acetone solution, heat and shake to dissolve, and naturally cool or crystallize in an ice bath, if the crystal is pasty or flocculent, re-heating and dissolving and then recrystallizing, Suction filtration, take the residue and dry it under reduced pressure at 60°C.
Last Update：2022-01-01 13:35:38
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Use
Open Data Verified Data
developed by Rousel Uelaf, Inc., France, was launched in France in October 1987. A semisynthetic new generation of macrolide antibiotics, antibacterial spectrum is similar to erythromycin, but the effect is 6 times stronger than erythromycin, bioavailability is high. The majority of respiratory pathogens such as hemolytic Streptococcus, Streptococcus Pneumonia, Haemophilus influenzae, Pneumonia Mycoplasma and Staphylococcus aureus have better antibacterial effect. For respiratory tract infection, such as Pneumonia, acute bronchitis, skin and soft tissue infection, chronic bronchitis acute infection, atypical Pneumonia and genitourinary system infection, has good therapeutic effect and tolerance, adverse reaction is smaller than erythromycin.
Last Update：2022-01-01 08:52:38
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Exam
Authoritative Data Verified Data
alkalinity
take this product O.lg, add water 150mU shake to make a suspension containing about 0.7mg per lml, and determine according to law (General rule 063l),pH value should be 8.0~10.0.
Related substances
take this product, add mobile phase to dissolve and dilute to make about 2.0 mg of solution, as a test solution; Take 1ml of precision, put it in a 100ml measuring flask, dilute it with mobile phase to the scale, shake, as the chromatographic conditions under the determination of the content of the control solution, the sample solution and the control solution are accurately measured by 20ul, and the human liquid chromatograph is injected respectively, the chromatogram was recorded to 4 times the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, except for the peak of N, N-dimethylformamide (determined by the same method with 0.001% N, N-dimethylformamide solution prepared by mobile phase, positioned according to retention time), the single impurity peak area shall not be greater than the main peak area of the control solution (1.0%), and the sum of each impurity peak area shall not be greater than 4 times (4.0%) of the main peak area of the control solution, peaks less than 0.1 times the main peak area of the control solution in the chromatogram of the supply solution are negligible.
residual solvent
methanol, acetone, triethylamine and dichloromethane take about 0.2g of this product, precision weighing, top empty bottle, precision plus dimethyl sulfoxide 5ml to dissolve, sealed, as a test solution; accurately weigh the appropriate amount of methanol, acetone, triethylamine and dichloromethane, and quantitatively dilute with dimethyl sulfoxide to make a mixed solution containing about 0.12mg of methanol, 0.20mg of acetone, 0.013mg of triethylamine and 0.024mg of dichloromethane per 1 ml, precision take 5M l in the top empty bottle, sealed, as a reference solution. 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 the stationary liquid is the column; The initial temperature is 40°C, hold for 5 minutes, at a rate of 30°C per minute to 200°C for 15 minutes; The detector temperature is 250°C; The sample inlet temperature is 230°C; The headspace bottle equilibrium temperature is 105°C, the equilibration time was 30 minutes. Take the reference solution into the headspace, record the chromatogram, and the separation degree between the peaks of each component shall meet the requirements. The test solution and the reference solution were injected into the headspace, and the chromatograms were recorded. The residual amount of triethylamine should not exceed 0.032% based on the peak area calculated by the external standard method, the residual amount of two gas methane shall be in accordance with the regulations.
N,N-dimethylformamide
precision weigh appropriate amount of this product, add dimethyl sulfoxide to dissolve and quantitatively dilute to make a solution containing about 50mg per 1 ml, as the sample solution I precision weigh appropriate amount of N, N-dimethylformamide, A solution containing about 45ug of N, N-dimethylformamide per 1 ml was prepared by quantitative dilution with dimethyl sulfoxide as a control solution. According to the determination method of residual solvent (General 0861 third method), the capillary column with 6% cyanopropylphenyl-94% dimethyl polysiloxane (or similar polarity) as the stationary liquid is the column: the initial temperature is 120°C, maintain for 4 minutes, at a rate of 30°C per minute to 200°C, maintain for 5 minutes; Detector temperature is 250°C; Sample inlet temperature is 25O °C; accurately take 1.0 u1 of the test solution and the reference solution, respectively inject human gas chromatography, record the chromatogram, and calculate the peak area according to the external standard method. The residual amount of N ,N-dimethylformamide should comply with the regulations.
moisture
take this product, according to the moisture determination method (General 0832 first method 1), the water content shall not exceed 3.0%.
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 burning residues shall be inspected according to law (General Principles 0821, Law II) and shall not contain more than 10 parts per million of heavy metals.
Last Update：2022-01-01 13:35:39
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Content determination
Authoritative Data Verified Data
measured by high performance liquid chromatography (General 0512).
chromatographic conditions and system suitability test
silica gel bonded with octylsilane was used as the filler, and 0.067mol/L ammonium dihydrogen phosphate solution (adjusted to pH 6.5 with triethylamine)-acetonitrile (65:35) was used as the mobile phase; the detection wavelength was 210mm. Appropriate amount of roxithromycin standard and erythromycin standard was taken, dissolved and diluted with mobile phase to prepare mixed solution containing about 1 mg in each lml, and 20u1 was injected into human liquid chromatograph, the retention time of the roxithromycin peak is about 14 minutes, and the degree of separation from the erythromycin peak should be not less than 15.0, the resolution between roxithromycin peak and impurity peak with relative retention time of about 0.95 shall be not less than 1.0, and the resolution between impurity peak with relative retention time of about 1.2 shall be not less than 2.0.
assay
take the appropriate amount of this product, precision weighing, plus mobile phase dissolution and quantitative dilution made from each lml containing about l. 0 mg of the solution, as the test solution, the precision of 20u1 injection of human liquid chromatography, record the chromatogram. Another roxithromycin reference substance, the same method for determination. According to the external standard method to calculate the peak area, that is.
Last Update：2022-01-01 13:35:40
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Category
Authoritative Data Verified Data
macrolide antibiotics.
Last Update：2022-01-01 13:35:40
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Storage
Authoritative Data Verified Data
sealed and stored in a dry place.
Last Update：2022-01-01 13:35:40
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Roxithromycin for suspension
Authoritative Data Verified Data
This product containing roxithromycin (C41H76N2015) should be labeled amount of 90.0% ~ 110.0%.
trait
This product is powder; Fragrance.
identification
- take 1ml of the test solution under Item (2) of identification, add 5 drops of concentrated sulfuric acid, and the solution is dark green in color within 1 minute,
- take an appropriate amount of fine powder of this product, add anhydrous ethanol to dissolve and dilute to make a solution containing about 5mg of roxithromycin per 1 ml, filter, the continued filtrate was taken as the test solution f, and an appropriate amount of roxithromycin control was taken, dissolved and diluted with absolute ethanol to prepare a solution containing about 5mg per 1 ml as the control solution. The above two kinds of solutions were mixed in equal amounts as a mixed solution. According to the thin layer chromatography (General 0502) test, absorb the above three solutions of 10 u1, respectively, on the same silica gel G thin layer plate, with toluene-dichloromethane-diethylamine (50:40:7) for the development of the solvent, the solvent was spread out, dried, sprayed with a color developing agent (2.5g of phosphomolybdic acid, 50ml of glacial acetic acid and 2.5ml of sulfuric acid were added to dissolve, and shaken well), and then heated at 105 ° C. For several minutes. The main spot displayed by the mixed solution should be a single spot, and the position and color of the main spot displayed by the test solution should be the same as that of the reference solution or the mixed solution.
- 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.
- two items (2) and (3) above can be selected as one item.
examination
- alkalinity take an appropriate amount of this product (about equivalent to 15mg of roxithromycin), add 10ml of water to dissolve, shake, and determine according to law (General rule 0631), and the pH value should be 7.0~9.0.
- loss on drying: Take appropriate amount of the product and dry under reduced pressure at 80°C to constant weight. The weight loss shall not exceed 2.0% (General rule: 0831).
- dissolution of this product, according to the dissolution and release determination method (General 0931 second method), with acetate buffer solution (pH 5.5)(take O.04mol/ L sodium acetate solution, adjust the pH value to 5.5 with glacial acetic acid) 900ml as dissolution medium (50mg specification dissolution medium 600ml,25mg specification dissolution medium 500ml), rotation speed is 50 rpm, operate according to law, after 30 minutes, take the appropriate amount of solution, filter, take the filtrate, according to the method under the content determination item; Take the appropriate amount of roxithromycin reference, precision weighing, the dissolution medium is added and dissolved and quantitatively diluted to prepare a solution containing about 0.08mg (25mg of 0.05mg) per 1 ml, which is measured by the same method, and the dissolution amount of each bag is calculated. The limit is 80% of the labeled amount and shall be in accordance with the provisions.
- other than sedimentation volume ratio (single dose package), should comply with the relevant provisions under the item of oral suspension (General Principle 0123).
Content determination
The contents under the item of difference in loading volume were extracted, and then the appropriate amount (equivalent to 50mg of roxithromycin) was accurately weighed, then quantitatively dilute with mobile phase to make a solution containing about 0.5mg of roxithromycin per lml, filter, and take the continued filtrate as the test solution, the mobile phase was added to dissolve and quantitatively dilute to prepare a solution containing about 0.5mg per 1 ml as a control solution. According to the method under the item of roxithromycin, obtained.
category
Same as roxithromycin.
specification
(l)25mg (2)50mg (3)75mg
storage
light-shielded, sealed, and stored in a dry place.
Last Update：2022-01-01 13:35:41
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Roxithromycin tablets
Authoritative Data Verified Data
This product containing roxithromycin (C41H76N2015) should be labeled amount of 90.0% ~ 110. 0%.
trait
This product is white or white-like tablets or film-coated tablets, white or white-like after removing the coating.
identification
- 1 ml of the test solution under identification (2) was taken, and 5 drops of concentrated sulfuric acid were added. The color of the solution was dark green within 1 minute.
- take an appropriate amount of fine powder of this product, add anhydrous ethanol to dissolve and dilute to prepare a solution containing roxithromycin 25mg per 1 ml, filter, and take the continued filtrate as the test solution; an appropriate amount of roxithromycin reference substance was additionally taken, dissolved and diluted with absolute ethanol to prepare a solution containing about 25mg per 1 ml as a reference solution. The above two kinds of solutions were mixed in equal amounts as a mixed solution. According to the thin layer chromatography (General 0502) test, absorb the above three solutions each 2 u1, respectively, on the same silica gel G thin layer plate, with toluene-dichloromethane-diethylamine (50:40:7) for the development of the solvent, the solvent was spread out, dried, sprayed with a color developing agent (2.5g of phosphomolybdic acid, 50ml of glacial acetic acid and 2.5ml of sulfuric acid were added to dissolve, and shaken well), and then heated at 105 ° C. For several minutes. The main spot displayed by the mixed solution should be a single spot, and the position and color of the main spot displayed by the test solution should be the same as that of the reference solution or the mixed solution.
- 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.
- 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 (if it is a film-coated tablet, remove the film coating), add the mobile phase to dissolve and dilute to make about 1 ml of roxithromycin 2.0 mg of the solution, filtration, take the filtrate, according to the method under the item of roxithromycin determination, except with the peak relative retention time of 0.30 before the peak of roxithromycin, the single impurity peak area shall not be greater than 1.5 times (1.5%) of the main peak area of the control solution, and the sum of each impurity peak area shall not be greater than 4.5 times (4.5%) of the main peak area of the control solution.
- dissolution of this product, according to the dissolution and release determination method (General 0931 first method), with acetate buffer (pH 5.5)(0.04mol/L sodium acetate solution, adjust the pH value to 5.5 with glacial acetic acid) 100 as the dissolution medium (50mg specification, the amount of dissolution medium is 600ml), the rotation speed is rpm, operate according to law, after 45 minutes, take the appropriate amount of solution, filter, take the filtrate as the test solution, according to the method under the content determination item, take the appropriate amount of roxithromycin reference, precision weighing, the dissolution medium was added and dissolved and quantitatively diluted to prepare a solution containing about 0.16mg ( 75mg and 50mg of 0.08mg) per 1 ml, and the dissolution amount of each tablet was calculated by the same method. 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 10 tablets of this product, precision weighing, fine grinding, precision weighing appropriate amount (about 50mg equivalent to roxithromycin), add appropriate amount of mobile phase, ultrasonic 20 minutes to help dissolution, after quantitative dilution with mobile phase, prepare about roxithromycin l per 1 ml. 0mg of the solution was filtered, and the continued filtrate was taken as a test solution, which was measured according to the method under the item of roxithromycin.
category
Same as roxithromycin.
specification
(l)50mg (2)75mg (3)150mg
storage
sealed and stored in a dry place.
Last Update：2022-01-01 13:35:42
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Roxithromycin Capsules
Authoritative Data Verified Data
This product containing roxithromycin (C41H76N2015) should be labeled amount of 90.0% ~ 110.0%.
trait
The contents of this product are white or off-white powder and granules.
identification
- 1ml of the test solution under identification (2) was taken, and 5 drops of concentrated sulfuric acid were added, and the color of the solution was dark green within 1 minute.
- take an appropriate amount of the contents of this product, add anhydrous ethanol to dissolve and dilute to prepare a solution containing roxithromycin 25mg per 1 ml, filter, and take the continued filtrate as the test solution; an appropriate amount of roxithromycin reference substance was additionally taken, dissolved and diluted with absolute ethanol to prepare a solution containing about 25mg per 1 ml as a reference solution. The above two kinds of solutions were mixed in equal amounts as a mixed solution. According to the thin layer chromatography (General 0502) test, draw 2ul of each of the above three solutions, respectively, on the same silica gel G thin layer plate, with toluene-dichloromethane-diethylamine (50:40:7) for the development of the solvent, the solvent was spread out, dried, sprayed with a color developing agent (2.5g of phosphomolybdic acid, 50ml of glacial acetic acid and 2.5ml of sulfuric acid were added to dissolve, and shaken well), and then heated at 105 ° C. For several minutes. The main spot displayed by the mixed solution should be a single spot, and the position and color of the main spot displayed by the test solution should be the same as that of the reference solution or the mixed solution.
- 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.
- 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, add the mobile phase to dissolve and dilute to prepare about roxithromycin per 1 ml. 0 mg of the solution, filtration, take the filtrate, according to the method under the item of roxithromycin determination, except with the peak relative retention time of 0.30 before the peak of roxithromycin, the single impurity peak area shall not be greater than 1.5 times (1.5%) of the main peak area of the control solution, and the sum of each impurity peak area shall not be greater than 4.5 times (4.5%) of the main peak area of the control solution.
- dissolution of this product, according to the dissolution and release determination method (General 0931 first method), with acetate buffer (pH 5.5)(0.04 mol/ L sodium acetate solution, adjust the pH value to 5.5 with glacial acetic acid) 100 as the dissolution medium (50mg specification, the dissolution medium is 600ml), the rotation speed is rpm, operate according to law, after 45 minutes, take appropriate amount of solution, filter, the filtrate was taken and determined according to the method under the item of content determination, the dissolution medium was added and dissolved and quantitatively diluted to prepare a solution containing about 0.16mg ( 75mg and 50mg of 0.08mg) per 1 ml, which was measured by the same method, and the dissolution amount of each particle was calculated. The limit is 75% of the labeled amount and shall be in accordance with the provisions. In case of non-compliance, Trypsin (containing not less than 0.08 activity units of trypsin, not less than 1.1 activity units of pancreatic amylase and not less than 0.4 activity units of pancreatic lipase per lml) acetate buffer (pH 5.5) as the dissolution medium, according to the above method to re-test, should comply with the provisions.
- others should comply with the relevant provisions under the capsule (General 0103).
Content determination
The contents under the item of difference in loading volume were extracted, and then the appropriate amount (about 50mg of roxithromycin) was accurately weighed, the appropriate amount of mobile phase was added, and the dissolution was assisted by ultrasound for 20 minutes, after quantitative dilution with mobile phase, prepare about roxithromycin l per 1 ml. 0mg of the solution was filtered, and the continued filtrate was taken as a test solution, which was measured according to the method under the item of roxithromycin.
category
Same as roxithromycin.
specification
(l)50mg (2)75mg (3)150mg
storage
shading, sealing, storage in a dry place ^
Last Update：2022-01-01 13:35:43
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Roxithromycin granules
Authoritative Data Verified Data
This product containing roxithromycin (C41H76N2015) should be labeled amount of 90.0% ~ 110.0%.
trait
This product is suspended particles; Or coated particles, white or white after removal of the coating.
identification
- 1 ml of the test solution under identification (2) was taken, and 5 drops of concentrated sulfuric acid were added, and the color of the solution was dark green within 1 minute.
- take an appropriate amount of the contents of this product, grind it, add anhydrous ethanol to dissolve and dilute it to make a solution containing about 5mg of roxithromycin per 1 ml, filter it, and take the continued filtrate as the test solution; another roxithromycin control substance was taken, dissolved and diluted with absolute ethanol to prepare a solution containing about 5mg per 1 ml as a control solution. The above two kinds of solutions were mixed in equal amounts as a mixed solution. According to the thin layer chromatography (General 502) test, absorb the above three solutions of 10 u1, respectively, on the same silica gel G thin layer plate, with toluene-dichloromethane-diethylamine (50:40:7) for the development of the solvent, expand, dry, spray with color developer (take phosphomolybdic acid 2.5g, add 50ml of glacial acetic acid, sulfuric acid 105 ml to dissolve, shake well), and then heat at °C for several minutes. The main spot displayed by the mixed solution should be a single spot, and the position and color of the main spot displayed by the test solution should be the same as that of the reference solution or the mixed solution.
- 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.
- two items (2) and (3) above can be selected as one item.
examination
- weight loss on drying this product shall be dried at 105°C to constant weight, and the weight loss shall not exceed 2.0% (General rule 0831).
- dissolution of this product, according to the dissolution and release determination method (General 0931 second method), with acetate buffer (pH 5.5) (0.04mol/L sodium acetate solution, adjust the pH value to 5.5 with glacial acetic acid) 900ml as dissolution medium (50mg specification dissolution medium 600ml,25mg specification dissolution medium 500ml), rotation speed is 50 rpm, operate according to law, after 30 minutes, take the appropriate amount of solution, filter, take the filtrate, according to the method under the content determination item, take the appropriate amount of roxithromycin reference, precision weighing, add the above dissolution medium to dissolve and quantitatively dilute to make a solution containing about 0.16mg(75mg and 50mg specification is 0.08mg; 25mg specification is 0.05mg) per 1 ml, the dissolution of each bag was calculated. The limit is 80% of the labeled amount and shall be in accordance with the provisions. (For non-coated granules)
- take this product, according to the dissolution and release determination method (General 0931 first method) test, with hydrochloric acid solution (l -lO00)900ml is dissolution medium (50mg of dissolution medium is 600ml,25mg of dissolution medium is 500ml), the rotation speed is 100 rpm, operated according to law, after 45 minutes, take appropriate amount of solution, filter, take the continued filtrate as the test solution, and determine it according to the method under the content determination item, and take the appropriate amount of roxithromycin reference substance, add the above dissolution medium to dissolve and quantitatively dilute to make a solution containing about 0.16mg(75mg and 50mg specification is 0.08mg ;25mg specification is 0.05mg) per 1 ml, which is determined by the same method, the dissolution of each bag was calculated. The limit is 70% of the labeled amount and shall be in accordance with the provisions. (For coated granules)
- others should comply with the relevant provisions under The granule (General Principle 0104).
Content determination
The contents under the item of difference in loading volume were extracted, and then the appropriate amount (about 50mg of roxithromycin) was accurately weighed, the appropriate amount of mobile phase was added, and the dissolution was assisted by ultrasound for 20 minutes, then quantitatively dilute with mobile phase to make a solution containing about 0.5mg of roxithromycin per lml, filter, and take the continued filtrate as the test solution, the mobile phase was added to dissolve and quantitatively dilute to prepare a solution containing about 0.5mg per 1 ml as a control solution. According to the method under the item of roxithromycin, obtained.
category
Same as roxithromycin.
specification
(l)25mg (2)50mg (3)75mg (4)150mg
storage
sealed and stored in a dry place.
Last Update：2022-01-01 13:35:45
ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME) - Reference Information
| EPA chemical substance information | information provided by: ofmpeb.epa.gov (external link) |
| Introduction | roxithromycin is the most commonly used broad-spectrum anti-inflammatory drug, is a member of the broad-spectrum antibacterial drug family; Common name is Roxithromycin Capsules, erythromycin Enteric-coated Tablets, Roxithromycin Dispersible Tablets, roxithromycin dry suspension. Commonly used in Streptococcus pyogenes caused by pharyngitis and tonsillitis, a variety of inflammation caused by sensitive bacteria. Roxithromycin is a semi-synthetic 14-membered ring macrolide antibiotic. Its mechanism of action is similar to erythromycin, the antibacterial effect in vivo is 1-4 times stronger than erythromycin, the effect on Gram-positive bacteria is slightly worse than erythromycin, the effect on legionella pneumophila is stronger than erythromycin, the effect on Pneumonia chlamydia, pneumonia Mycoplasma, Ureaplasma urealyticum antimicrobial effect and erythromycin similar or slightly strong. Roxithromycin is a semi-synthetic macrolide antibiotic. This product can penetrate the bacterial cell membrane, through the inhibition of bacterial protein synthesis and achieve antibacterial effect. |
| pharmacokinetics | a single oral dose of 150mg,2 H peak plasma concentration. The drug absorption decreased after eating. This product is highly fat-soluble, if taken with milk is well absorbed. The concentration in tissues and body fluids was significantly higher than that of erythromycin. Very low in breast milk. Mainly through the feces and urine in the original form of discharge, but also some of the sugar metabolism. The half-life of this product is 8.4~15.5 hours. Renal insufficiency half-life extension, but generally do not need to adjust the dose. In patients with severe alcoholic cirrhosis, the half-life is extended by two times, and the interval time of administration needs to be adjusted. |
| pharmacological action | This product can penetrate the bacterial cell membrane, close to the donor ("P" position) reversibly binding to the 50s subunit of the bacterial ribosome, blocking the binding of the transfer RNA to the "P" position, and also blocking the polypeptide chain from the acceptor position ("A" position) transfer to the "P" position, and thus bacterial protein synthesis is inhibited, thus playing an antibacterial role. It is characterized by rapid entry into macrophages, alveolar cells, neutrophils. In vitro studies have confirmed that roxithromycin has A broad antibacterial spectrum against various streptococci (including Type A, B, C and Pneumonia streptococci, except Type G and Enterococcus), Pneumonia streptococci, Staphylococcus aureus, staphylococcus aureus (except MRSA), Staphylococcus epidermidis, Legionella pneumophila, Haemophilus ducreis, Chlamydia trachomatis, Pneumonia Mycoplasma, oral or vaginal anaerobes have almost the same antibacterial activity as erythromycin, sinococcus catarrhalis is highly sensitive to roxithromycin, and also has inhibitory effect on campylobacter, Bordetella pertussis, Haemophilus influenzae, Mycobacterium tuberculosis and diphtheria bacillus, and has no antibacterial activity against other gram-negative bacteria. In vivo antibacterial activity of this product was significantly stronger than erythromycin, and chlamydia, Mycoplasma, Ureaplasma urealyticum, Treponema pallidum and Legionella infection curative effect is remarkable. Of Helicobacter, Neisseria gonorrhoeae, meningococcus, Bordetella pertussis and other weak role. Some bacteria have cross resistance to erythromycin and this product. |
| indication | This product is suitable for pharyngitis and tonsillitis caused by Streptococcus pyogenes, sinusitis, otitis media, acute bronchitis and acute attack of chronic bronchitis caused by sensitive bacteria, pneumonia caused by mycoplasma or Pneumonia chlamydia Pneumonia; Infections of the genitourinary system (urethritis and cervicitis) caused by Chlamydia trachomatis; Infections of the skin and soft tissues and other parts of the body caused by sensitive bacteria; also used for non-specific and gonococcal genital infections. Infection caused by legionella. Pediatric infection. roxithromycin is characterized by acid resistance and good oral absorption, T1/2 is 12 to 14 hours, more than 6 times higher than erythromycin. Wide distribution in the body, the upper and lower respiratory tract, genital tract and skin can reach a high concentration and maintain a long time. Most are metabolized in the body. evaluation of clinical application of roxithromycin: the clinical and bacteriology of chlamydia urethritis and cervicitis was 93% ~ 97% Recovery Rate. The curative effect on genital infection was similar to that of doxycycline, and Recovery Rate of skin infection was more than 90%, the effective rate of treatment of respiratory tract infection was 83% and 50%, Pneumonia and the effective rate of dental infection was 79% and 85%. |
| note | 1. There is cross resistance between this product and erythromycin. 2. It is contraindicated for those who are allergic to this product. 3. Should not be combined with ergotamine and dihydroxy ergotamine. |
| Use | macrolide antibiotics, derivatives of erythromycin, antibacterial spectrum and erythromycin similar, but the effect is 6 times stronger than erythromycin, high bioavailability. For respiratory tract infections, such as Pneumonia, acute bronchitis, chronic bronchitis acute infection, atypical Pneumonia, and genitourinary system infections, skin and soft tissue infections, have good therapeutic effect and tolerance, the adverse reaction was smaller than that of erythromycin. as a new generation of macrolide antibiotics This product is a new generation of macrolide antibiotics, mainly used for Gram-positive bacteria, anaerobic bacteria, chlamydia and Mycoplasma. Its antibacterial effect in vitro is similar to that of erythromycin, and its in vivo effect is 1-4 times stronger than that of erythromycin. Pharmacological effects and indications 1, a strong killing effect on Gram-negative bacteria, some Gram-negative bacteria (meningococcus, Neisseria gonorrhoeae, influenza bacilli, pertussis, Brucella) and spirochete, Pneumonia Mycoplasma, Rickettsia, legionella is sensitive to Mycoplasma and chlamydia. 2. Antibacterial mechanism: it binds to the 50s subunit of the bacterial control protein body, and inhibits the synthesis of the protein by blocking the transfer of the peptide and the displacement of the MRNA. 3, the oral absorption of good, quick, bioavailability and blood concentration were stronger than erythromycin. According to the report, the peak concentration of oral 6.6 mg is as high as 7.9~0.2 ug/ml, while erythromycin is only 0.4 ~ ug/ml under the same conditions. Roxithromycin is mainly distributed in body fluids and tissues, It has a high and long-lasting tissue concentration and cell concentration, and has a half-life of up to 12h, while erythromycin has only 1.5~2.0h. 4, in the medical clinic for drug-resistant Staphylococcus aureus and hemolytic streptococcus caused by the preferred drug, veterinary clinical for the treatment of penicillin-resistant, Staphylococcus aureus caused by serious infections, Pneumonia, metritis, chronic respiratory diseases of poultry, etc. 5, the product is mainly used for the treatment of chronic respiratory diseases of livestock and poultry, livestock and poultry Staphylococcus and Streptococcus disease, chlamydia, spirochosis (swine dysentery), Transmissibility pleurisy, rhinitis and so on. 6, indications for: Avian neck swelling, local heat, pain, Dyspnea, nose and mouth white foam, mucous membrane and skin cyanosis and other symptoms. |
| production method | erythromycin is used as raw material, hydroxylamine hydrochloride is reacted with triethylamine and methanol to form oxime, it is then reacted with methoxyethoxymethyl chloride in acetone to give roxithromycin. |
Last Update：2024-04-09 02:00:12
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Product Name: Roxithromycin Visit Supplier Webpage Request for quotationCAS: 80214-83-1
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Product Name: Roxithromycin Visit Supplier Webpage Request for quotationCAS: 80214-83-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: Roxithromycin Visit Supplier Webpage Request for quotationCAS: 80214-83-1
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Multiple SpecificationsSpot supply
Product Name: Roxithromycin Visit Supplier Webpage Request for quotationCAS: 80214-83-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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Raw Materials for ERYTHROMYCIN 9-(-O-[2-METHOXYETHOXY]METHYLOXIME)