Acetylspiramycin - Names and Identifiers
Name | Acetylspiramycin
|
Synonyms | spiramycinb spiramycin2 foromacidinb foromacidineb Acetylspiramycin ACETYLSPIRAMYCIN Acetyl Spiramycin Acetylspiramycin (ASPM) 9-o-(5-(dimethylamino)tetrahydro-6-methyl-2h-pyran-2-yl)-leucomycin3-ac 9-O-[(2R,5S,6R)-5-(Dimethylamino)tetrahydro-6-methyl-2H-pyran-2-yl]-3-acetate-leucomycin V (4R,5S,6S,7R,9R,10R,11E,13E,16R)-6-{[(2S,3R,4R,5S,6R)-5-{[(2S,4R,5S,6S)-4,5-dihydroxy-4,6-dimethyltetrahydro-2H-pyran-2-yl]oxy}-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy}-10-{[(2R,5S,6S)-5-(dimethylamino)-6-methyltetrahydro-2H-pyran-2-yl]oxy}-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)oxacyclohexadeca-11,13-dien-4-yl acetate (non-preferred name) (4R,5S,6S,7R,9R,10R,11E,13E,16R)-6-{[(2S,3R,4R,5S,6R)-5-{[(2S,4R,5S,6S)-4,5-dihydroxy-4,6-dimethyltetrahydro-2H-pyran-2-yl]oxy}-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy}-10-{[(2S,5S,6R)-5-(dimethylamino)-6-methyltetrahydro-2H-pyran-2-yl]oxy}-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)oxacyclohexadeca-11,13-dien-4-yl acetate (non-preferred name)
|
CAS | 24916-51-6
|
EINECS | 1312995-182-4 |
InChI | InChI=1/C45H76N2O15/c1-25-22-31(20-21-48)41(62-44-39(51)38(47(10)11)40(28(4)58-44)61-37-24-45(7,53)43(52)29(5)57-37)42(54-12)34(59-30(6)49)23-35(50)55-26(2)16-14-13-15-17-33(25)60-36-19-18-32(46(8)9)27(3)56-36/h13-15,17,21,25-29,31-34,36-44,51-53H,16,18-20,22-24H2,1-12H3/b14-13+,17-15+/t25-,26-,27-,28-,29+,31+,32+,33+,34-,36-,37+,38-,39-,40-,41+,42+,43+,44+,45-/m1/s1 |
Acetylspiramycin - Physico-chemical Properties
Molecular Formula | C45H76N2O15
|
Molar Mass | 885.09 |
Density | 1.21±0.1 g/cm3(Predicted) |
Melting Point | 130-1330C |
Boling Point | 916.7±65.0 °C(Predicted) |
Specific Rotation(α) | D20 -86° |
Flash Point | 508.2°C |
Solubility | DMSO (Slightly, Sonicated), Methanol (Very Slightly, Heated) |
Vapor Presure | 0mmHg at 25°C |
Appearance | Solid |
Color | White to Light Yellow |
pKa | 13.06±0.70(Predicted) |
Storage Condition | Sealed in dry,Store in freezer, under -20°C |
Refractive Index | 1.543 |
Physical and Chemical Properties | White or yellowish powder, bitter, odorless. Slightly soluble in water, soluble in alcohol, chloroform and benzene. The antibacterial spectrum, antibacterial mechanism and indications were similar to erythromycin, and the degree of antibacterial was slightly weak. |
Use | For respiratory infections, pyoderma, scarlet fever, etc |
Acetylspiramycin - Upstream Downstream Industry
Acetylspiramycin - Reference
Reference Show more | 1. Gao Mingkun, Zhang Zhi, Qian Fang. Toxicology, Functional Test and Effect of Mixed Bacteria Preparation (BMX) on Fattening Pigs [J]. Feed Research, 2018, No.485(04):66-71. |
Acetylspiramycin - Standard
Authoritative Data Verified Data
This product is the single acetyl spiramycin 2, single acetyl spiramycin 3, double acetyl spiramycin 2 and double acetyl spiramycin 3 four component mixture. The titer shall not be less than 1200 acetylspiramycin units per lmg calculated on a dry basis.
Last Update:2024-01-02 23:10:35
Acetylspiramycin - Trait
Authoritative Data Verified Data
- This product is white to yellowish powder.
- This product is dissolved in methanol, ethanol, acetone or ether, almost insoluble in water, insoluble in petroleum ether.
Last Update:2022-01-01 11:29:27
Acetylspiramycin - Differential diagnosis
Authoritative Data Verified Data
- this product and the acetylspiramycin standard were taken, and methanol was added to prepare a solution containing 5mg per 1 ml, respectively, as a test solution and a standard solution. According to the thin layer chromatography (General 0502) test, absorb the above two solutions of each lol, respectively, on the same thin layer plate (take silica gel G 0.6g, add 0.lmol/L sodium hydroxide solution 2.5ml, ground into a paste, after mixing, coated on 20cmX5cm glass plate, after drying, put 105X: activation for 30 minutes), with toluene-methanol (9:1) for the development of the agent, after spreading, dry, set iodine vapor color. The position and color of the four main spots displayed by the test solution should be the same as the position and color of the four main spots of the standard solution.
- in the chromatogram recorded under acetylspiramycin component determination, the retention times of the four main component peaks of the test solution should be consistent with the retention times of the four main component peaks of the acetylspiramycin standard solution.
- two items (1) and (2) above can be selected as one item.
Last Update:2022-01-01 11:29:27
Acetylspiramycin - Exam
Authoritative Data Verified Data
loss on drying
take this product, dry to constant weight in 1051C, weight loss shall not exceed 3.0% (General rule 0831).
determination of the composition of the acetyl cockroach is determined by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test with eighteen alkyl silane bonded silica gel as filler; With acetonitrile -0.1 mol/L ammonium acetate solution (60:40)(adjusted to pH 7.2±0.1 with acetic acid) as mobile phase; The detection wavelength was 232nm. Take the standard solution lOul and inject it into human liquid chromatograph. The chromatogram recorded should be consistent with the standard chromatogram.
- the appropriate amount of this product is accurately weighed, and the mobile phase is added to dissolve and quantitatively dilute to prepare a solution containing about 1 mg per 1ml, which is used as the test solution, precise amount of 10u1 injection liquid chromatography, record chromatogram, acetylspiramycin peak order of each component: monoacetylspiramycin 2, monoacetylspiramycin 3, diacetylspiramycin 2 and diacetylspiramycin 3. The peak area shall be measured and calculated according to the following formula, and the content of mono-and diacetylspiramycin (2+3) shall not be less than 35%.
Last Update:2022-01-01 11:29:28
Acetylspiramycin - Content determination
Authoritative Data Verified Data
precision weigh the appropriate amount of this product, add ethanol to dissolve (every 5mg plus ethanol 2ml), quantitative dilution with sterile water to make a solution containing about 1000 units per 1ml, according to the microbiological assay of antibiotics (General 1201).
Last Update:2022-01-01 11:29:28
Acetylspiramycin - Category
Authoritative Data Verified Data
Last Update:2022-01-01 11:29:29
Acetylspiramycin - Storage
Authoritative Data Verified Data
sealed and stored in a cool dark dry place.
Last Update:2022-01-01 11:29:29
Acetylspiramycin - Acetylclarithromycin tablets
Authoritative Data Verified Data
This product containing acetyl spiramycin should be labeled the amount of 90.0% to 110.0%.
trait
This product is sugar-coated tablet or film-coated tablet, after removing the coating, appear white or yellowish.
identification
- take an appropriate amount of the fine powder of this product and add methanol to make a solution containing about 5mg of acetylspiramycin per 1 ml, filter, and take the continued filtrate as the test solution, methanol was added to prepare a solution containing 5mg per 1 ml as a standard solution, and equal volumes of the test solution and the standard solution were mixed and used as a mixed solution. Draw 10 u1 of each of the above three solutions, and identify (1) under the item of acetyl spiramycin. The mixed solution should show four main spots, the position and color of the four main spots displayed by the test solution should be the same as the position and color of the four main spots displayed by the standard solution or mixed solution.
- in the chromatogram recorded under the acetylspiramycin component determination item, the retention times of the four main component peaks of the test solution should be consistent with the retention times of the four main component peaks of the standard solution.
- take an appropriate amount of fine powder of this product (approximately equivalent to acetylspiramycin O.lg), add methanol 10ml, shake, dissolve acetylspiramycin, filter, take the filtrate lml, then methanol solution (1-5) A solution containing 20 tons of acetylspiramycin per 1 ml was prepared by dilution and had an absorption maximum at a wavelength of 232mn as determined by UV-Vis spectrophotometry (General rule 0401).
- two items (1) and (2) above can be selected as one item.
examination
- determination of components of acetyl-C-rotamycin an appropriate amount of fine powder of this product (approximately equivalent to acetyl-spiramycin 0.lg ), Precision weighing, add the mobile phase to dissolve and quantitatively dilute to prepare a solution containing about 1 mg of acetylspiramycin per 1 ml, shake well, filter, and take the continued filtrate as the test solution, containing mono-and diacetylspiramycin (2+3) should not be less than 35%, calculated by the following formula, acetylspiramycin four components of the total content should not be less than 70% of the label.
- dissolution dissolution of this product, according to the dissolution and release determination method (General rule 0931 The first method), hydrochloric acid solution (dilute hydrochloric acid 24ml- 1000ml)900ml as the dissolution medium, the rotation speed is 100 rpm, and the operation is carried out according to law. When the time is 45 minutes, the appropriate amount of the solution is taken, filtered, and the appropriate amount of the filtrate is taken, quantitatively dilute with dissolution medium to make a solution containing about 20mg of acetylspiramycin per 1 ml, and measure absorbance at 232mn wavelength according to UV-visible spectrophotometry (General rule 0401), precise weighing, fine grinding, precise weighing appropriate amount (equivalent to the average tablet weight), plus an appropriate amount of ethanol (every 5mg plus 2ml of ethanol) to dissolve, quantitatively dilute with dissolution medium according to the labeled amount to make a solution containing approximately lOOpg per lm l, filter, and accurately take appropriate amount of filtrate, the dissolution medium was quantitatively diluted to prepare a solution containing about 20mg per LML, which was determined by the same method, and the dissolution amount of each tablet was calculated. The limit is 75% 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 take appropriate amount (about equivalent to acetylspiramycin O.lg ), add ethanol (every 5mg plus 2ml ethanol) to dissolve acetylspiramycin, such as sugar-coated tablets, Take 5 tablets of this product, ground fine, add ethanol (every 5mg plus 2ml ethanol) to dissolve, A solution containing about 1000 units per 1 ml of sterilized water was quantitatively prepared, and the solution was shaken and allowed to stand. An appropriate amount of the supernatant was accurately measured and measured according to the method for acetylspiramycin.
category
same acetylspiramycin.
specification
(1)0g (l 0.2 units) (2) 200,000g (units)
storage
sealed and stored in a cool dark dry place.
Last Update:2022-01-01 11:29:30
Acetylspiramycin - Acetidinomycin capsules
Authoritative Data Verified Data
This product contains acetyl spiramycin should be labeled amount of ~ 110.0%.
trait
The contents of this product are white to yellowish powder or granules.
identification
- take an appropriate amount of the contents of this product, add methanol to make a solution containing about 5mg of acetylspiramycin per 1 ml, filter, and take the continued filtrate as the test solution, methanol was added to prepare a solution containing 5mg per 1 ml as a standard solution, and equal volumes of the test solution and the standard solution were mixed and used as a mixed solution. Draw the above three solutions of each L01, according to the item of acetylspiramycin identification (1) Test, mixed solution should show four main spots, the position and color of the four main spots displayed by the test solution should be the same as the position and color of the four main spots displayed by the standard solution or mixed solution.
- in the chromatogram recorded under the acetylspiramycin component determination item, the retention times of the four main component peaks of the test solution should be consistent with the retention times of the four main component peaks of the standard solution.
- take an appropriate amount of the contents of this product (about 0.lg of acetylspiramycin), add 10ml of methanol, shake, dissolve acetylspiramycin, filter, and take lml of the continuous filtrate, A solution containing 20ul of acetylspiramycin per 1 ml was prepared by dilution with methanol solution (1-5) and had an absorption maximum at a wavelength of 0401 nm as determined by UV-Vis spectrophotometry (general).
- two items (1) and (2) above can be selected as one item.
examination
- weight loss on drying take this product at 105°C; Dry to constant weight, weight loss shall not exceed 4.0% (General rule 0831).
- acetyl spiramycin component determination the content of this product is appropriate (about equivalent to acetyl spiramycin O.lg ), Precision weighing, adding mobile phase to dissolve and quantitatively dilute to prepare a solution containing about 1m acetylspiramycin per 1 ml, shake well, filter, and take the continued filtrate as the test solution, according to the method under the item acetylspiramycin, containing mono-and diacetylclarithromycin (n + m) shall not be less than 35%, calculated by the following formula, the total content of the four components of acetylspiramycin should not be less than 70% of the label amount.
- dissolution dissolution of this product, according to the dissolution and release determination method (General rule 0931 second method), hydrochloric acid solution (dilute hydrochloric acid 24ml- 1000ml)900ml as the dissolution medium, the rotation speed is 50 rpm, and the operation is carried out according to law. When the time is 45 minutes, the appropriate amount of the solution is taken, filtered, and the appropriate amount of the filtrate is taken, the solution containing about 20PG of acetylspiramycin per l of lm was prepared by quantitative dilution with dissolution medium, and the absorbance was measured at the wavelength of 232nm according to ultraviolet-visible spectrophotometry (General rule 0401); take the content under the difference of loading amount, mix evenly, accurately weigh an appropriate amount (equivalent to the average loading of 1 piece), and add an appropriate amount of ethanol (2ml of ethanol per 5mg) to dissolve, quantitatively dilute with dissolution medium according to the labeled amount to make a solution containing about l00Mg per lml, filter, precisely take an appropriate amount of filtrate, quantitatively dilute with dissolution medium to make a solution containing about 20mg per lml, the same method was used to calculate the dissolution of each particle. The limit is 75% and shall be in accordance with the provisions. If the capsule shell swelling does not collapse and lead to non-compliance with the provisions, should be containing 0.32% pepsin 0.lmol/L hydrochloric acid solution as the dissolution medium, re-test.
- others should comply with the relevant provisions under the capsule (General 0103).
Content determination
take the contents under the difference of loading amount, mix evenly, accurately weigh an appropriate amount (about 0.lg of acetocystin), and add ethanol (2ml of ethanol per 5mg) dissolve acetotretinomycin, quantitatively prepare a solution containing about 1000 units per 1 ml of sterilized water, shake well, stand still, and precisely measure an appropriate amount of the supernatant, the assay was carried out according to the method described under the term acetylclarithromycin.
category
The same as acetosideramycin.
specification
(1)0.lg (100,000 units) (2)0.2g (200,000 units)
storage
sealed and stored in a cool dark dry place.
Last Update:2022-01-01 11:29:31
Acetylspiramycin - Reference Information
Indications | Suitable for mild and moderate infections caused by sensitive Staphylococcus, Streptococcus and Streptococcus pneumoniae, such as pharyngitis, tonsillitis, sinusitis, otitis media, periodontitis, acute bronchitis, acute attack of chronic bronchitis, pneumonia, non-gonococcal urethritis, skin and soft tissue infections, and can also be used for sporidiosis, or as an optional drug for the treatment of toxoplasmosis in pregnant women. |
Use | Acetylspiramycin-based macrolide semi-synthetic oral antibiotics, mainly used for Staphylococcus aureus, hemolytic streptococcus, Streptococcus viridans, Pneumococcus, Staphylococcus epidermidis and other bacteria caused by respiratory infections, pyoderma, erysipelas, scarlet fever, pharyngitis, tonsillitis and otitis media. for respiratory infection, pyoderma, scarlet fever, etc. its antibacterial spectrum, antibacterial mechanism and indications are similar to erythromycin |
Effect | Acetylspiramycin is an acetylated derivative of spiramycin and belongs to 16-membered ring macrolides. This product has a good antibacterial effect on gram-positive cocci such as Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, Enterococcus faecalis, etc. For Listeria, Moraxella catarrhalis, Neisseria gonorrhoeae, Campylobacter fetus, Haemophilus influenzae, Legionella pneumophila, Bacillus pertussis, Bacteroides, Perfringens, Propionibacterium acnes, Digestive cocci and Streptococcus, Chlamydia, Mycoplasma, Toxoplasma, Cryptosporidium, etc. also have inhibitory effects. Intestinal gram-negative bacilli are usually resistant. |
biological activity | Acetylspiramycin (ASPM, Spiramycin II, Foromacidin B) is a macrolide antibacterial agent. |
Last Update:2024-04-09 15:16:49