Name | Azithromycin dihydrate |
Synonyms | Azithromycin dihydrate AZITHROMYCIN 2-HYDRATE 1-Oxa-6-azacyclopentadecan-15-one, 13-(2,6-dideoxy-3-C-methyl-3-O-methyl-. |
CAS | 117772-70-0 |
EINECS | 641-134-5 |
Molecular Formula | C38H72N2O12·2H2O |
Molar Mass | 785.02 |
Melting Point | 126 C |
Boling Point | 717℃ |
Flash Point | >110°(230°F) |
Appearance | White or nearly white crystalline powder |
Storage Condition | -20℃ |
Refractive Index | -47 |
MDL | MFCD01862248 |
Use | Uses for respiratory tract infections, urinary tract infections, skin and soft tissue infections and sexually transmitted diseases |
Hazard Symbols | Xi - Irritant |
Safety Description | S24/25 - Avoid contact with skin and eyes. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. |
UN IDs | 36/37/38 |
Zhou Yingjie , Zhang Jing , Shi Yaoguo
Abstract:
azithromycin is a macrolide antibiotic used in Community Acquired Infections, including respiratory tract infections (eg, Community Acquired Pneumonia, acute exacerbations of chronic bronchitis, acute pharyngitis and tonsillitis, acute otitis media), urogenital infections (such as Neisseria gonorrhoeae and non-gonococcal urethritis, cervicitis, chancroid) and skin and soft tissue infections [1]. Azithromycin new dihydrate sustained-release oral dry suspension (Zmax), approved in the United States in Community Acquired Pneumonia, is the first single dose for mild or moderate acute bacterial sinusitis (ABS) or (CAP) in adults antimicrobial agents [1-2].
Key words:
azithromycin; Sustained-release dry suspension; pharmacokinetics; Drug interaction; Adverse reaction
DOI:
CNKI:SUN:KGHL.0.2008-04-027
cited:
year:
2008
CN 201510473561
applicant (patent):
Zhejiang Weikang Pharmaceutical Co., Ltd.
inventor:
Abstract:
The present invention belongs to the technical field of medicine, and particularly relates to a azithromycin compound and a soft capsule containing the same. The azithromycin compound provided by the invention is a hydrate crystal, and its molecular formula is: C38H72N2O12 · 3H2O. The azithromycin hydrate crystal provided by the invention is azithromycin trihydrate, and is a new crystalline compound of azithromycin, the new crystalline compound has significantly improved hygroscopicity compared with azithromycin monohydrate of the prior art, and its Hygroscopicity is equivalent to that of azithromycin dihydrate of the prior art, and the dissolution rate and dissolution rate were significantly improved.
Ma Min , Yao Guowei , Deng Yulin
Abstract:
The hydrolysis of two kinds of boric acid esters in the synthesis of azithromycin, namely azithromycin borate (AZMB) and its precursor nitrogen erythromycin borate (AZAB) were compared. The best hydrolysis conditions of AZAB were as follows: under the conditions of pH = 3.0, hydrolysis temperature 30 ℃, hydrolysis time 30 min, the conversion rate was 91.9%. The hydrolysis conditions of AZMB were as follows: pH = 2.0, temperature 30 ℃, reaction time 90 min, the conversion rate 89.3%. The results showed that AZAB was more susceptible to hydrolysis than AZMB. Using Mixed acid of organic acid and inorganic acid instead of inorganic acid in the literature [6] to adjust the pH of hydrolysis can inhibit the acidic degradation reaction of clatin sugar. With erythromycin 6, 9-imine ether as raw material, the total yield of azithromycin dihydrate can reach 85%, and the mass fraction is 98.4% by HPLC analysis.
Key words:
azithromycin azithromycin boronate N-erythromycin N-erythromycin borate hydrolysis
DOI:
10.3321/j.issn:1003-5214.2006.06.010
cited:
year:
2006
Abstract:
for the crystallization process of azithromycin dihydrate, the effects of the initial concentration of crystallization, the flow rate of the dissolving agent and the stirring intensity on the particle size distribution of the crystalline product were investigated, the optimized process parameters were determined as follows: the crystallization temperature was 40 ℃, the initial concentration was 0.32g/g, the stirring rate was 200, and the dropping rate of the dissolving agent was 200 μl/min. Under these conditions, the product with a particle size distribution of about 300 μm to 800 μm and a main particle size of about 580 μm can be obtained, which overcomes the problems of aggregation and uneven particle size distribution of the crystalline product.
Key words:
azithromycin; Dissolution crystallization; Particle size distribution; coalescence
DOI:
10.13353/j.issn.1004.9533.2015.01.008
year:
2015
Zhou Yingjie , Zhang Jing , Shi Yaoguo
Abstract:
azithromycin is a macrolide antibiotic used in Community Acquired Infections, including respiratory tract infections (eg, Community Acquired Pneumonia, acute exacerbations of chronic bronchitis, acute pharyngitis and tonsillitis, acute otitis media), genitourinary infections (eg, Neisseria gonorrhoeae and non-gonococcal urethritis, cervicitis, chancroid) and skin and soft tissue infections [1]. Azithromycin new dihydrate sustained-release oral dry suspension (Zmax), approved in the United States in Community Acquired Pneumonia, is the first single dose for mild or moderate acute bacterial sinusitis (ABS) or (CAP) in adults [1-2]. It has antibacterial activity against Gram-positive bacteria (including Pneumonia Streptococcus), gram-negative bacteria and atypical pathogens causing ABS and CAP in vitro, and has good tissue penetration, treatment of patients with ABS or CAP is therefore effective and well tolerated [1,3-5]. In this paper, the research background, pharmacokinetics, clinical efficacy, indications and adverse reactions of the drug were reviewed, For research and development and clinical reference. I. Research background the efficacy of azithromycin is related to AUC/MIC (area under the blood concentration curve/minimum inhibitory concentration) and is a concentration-dependent antibacterial drug. PK/PD model studies have shown that single dose administration is beneficial to rapidly reduce the bacterial load at the site of infection, thus reducing the spread of drug resistance genes between colonies [6].
, Girard et al [7] for different dosing regimens of azithromycin, I .e., the same dose of a single dose or divided into 2 or 3 doses, in Pneumoniastowed
Key words:
azithromycin sustained-release dry suspension pharmacokinetics drug interaction adverse reaction
year:
2008