Esanbutol
ethambutol dihydrochloride
CAS: 1070-11-7
Molecular Formula: C10H24N2O2.2ClH
Esanbutol - Names and Identifiers
| Name | ethambutol dihydrochloride |
| Synonyms | Esanbutol Ethambutol hcl ETHAMBUTOL HCL USP Ethambutol Hydrochlorid Ethambutol Hydrochloride ethambutol dihydrochloride (2S,2'S)-2,2'-(ethane-1,2-diyldiimino)dibutan-1-ol 2,2'-(1,2-Ethanediyldiimino)bis-1-butanol dihydrochloride (R)-2,2'-(1,2-Ethanediyldiimino)bis-1-butanol dihydrochloride [S-(R*,R*)]-2,2'-(Ethylenediimino)dibutan-1-ol dihydrochloride (S,S)-N,N'-Bis(1-hydroxy-2-butyl)ethylenediaMine Dihydrochloride Emb, 2,2μ-(1,2-Ethanediyldiimino)bis-1-butanol dihydrochloride (2S,2'S)-2,2'-(ethane-1,2-diyldiimino)dibutan-1-ol dihydrochloride 1-Butanol, 2,2'-(1,2-ethanediyldiimino)bis-, hydrochloride (1), (2S,2'S)- (2S,2'S)-2,2'-(Ethane-1,2-diylbis(azanediyl))bis(butan-1-ol) dihydrochloride |
| CAS | 1070-11-7 |
| EINECS | 213-970-7 |
| InChI | InChI=1/C10H24N2O2.ClH/c1-3-9(7-13)11-5-6-12-10(4-2)8-14;/h9-14H,3-8H2,1-2H3;1H/t9-,10-;/m0./s1 |
Esanbutol - Physico-chemical Properties
| Molecular Formula | C10H24N2O2.2ClH |
| Molar Mass | 277.23 |
| Melting Point | 198-200°C |
| Boling Point | 376.2°C at 760 mmHg |
| Specific Rotation(α) | D25 +7.6° (c = 2 in water) |
| Flash Point | 181.3°C |
| Water Solubility | Slightly soluble in water |
| Solubility | DMSO 56 mg/mL Water 56 mg/mL Ethanol <1 mg/mL |
| Vapor Presure | 3.35E-07mmHg at 25°C |
| Appearance | White powder |
| Color | white |
| Merck | 14,3720 |
| Storage Condition | 2-8°C |
| MDL | MFCD00216025 |
| In vitro study | Ethambutol directly affects two polymers, arabinogalactan (AG) and lipoarabinomannan (LAM) in Mycobacterium smegmatis. In M. In smegmatis, Ethambutol completely inhibits the synthesis of arabinan and inhibits the synthesis of AG, most likely due to the release of arabinan from bacteria by more than 50% of the cells after Ethambutol treatment, no galactosomes are released. Ethambutol mainly targets the emb B gene product in Anti-M. avium. Ethambutol causes mutations in 60% of the emb gene in drug-resistant mutant strains of tuberculosis. Ethambutol is effective against growth-active mycobacteria-like microorganisms, including M. tuberculosis. Almost all strains of M. tuberculosis and M. kansasii and some M. Aviumcomplexes (MAC) are sensitive to Ethambutol. In Vitro, Ethambutol is effective against M. tuberculosis (H37Rv) with MIC of 0.5 μg/ml. Ethambutol is effective in treating mycobacterial infected macrophages. When M. tuberculosis infected macrophages, treated with 6 μg/ml Ethambutol, after 3 days of treatment, the log CFUs was 4.17, while the value of the control group was 4.8. The MICs for M. avium (MTCC 1723) and M. smegmatis (MTCC 6) were 15 μg/ml and 0.18 μg/ml, respectively. |
| In vivo study | Ethambutol is effective in animal models. Oral administration of 100 mg/kg Ethambutol for 15 days, intravenous injection once a week for 5 weeks, compared with the untreated group, will cause a lower CFU(4.59 to 5.07). |
Esanbutol - Risk and Safety
| Risk Codes | R61 - May cause harm to the unborn child R36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S53 - Avoid exposure - obtain special instructions before use. S22 - Do not breathe dust. 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.) S36/37 - Wear suitable protective clothing and gloves. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 3 |
| RTECS | EL3854000 |
| HS Code | 29419000 |
| Hazard Class | IRRITANT |
Esanbutol - Reference
| Reference Show more | 1. [IF=7.46] Ying Zhang et al."A polydopamine-polyethyleneimine/quantum dot sensor for instantaneous readout of cell surface charge to reflect cell states."Sensor Actuat B-Chem. 2020 Dec;324:128696 |
Esanbutol - Standard
Authoritative Data Verified Data
This product is [2R,2[S-(R1 ,R2 )]-R]-( +)2,2 '-(l, 2-ethylenediimino)-Bis-1-butanol dihydrochloride. The content of C10H24N202 • 2HC1 shall not be less than 98.5% calculated on a dry basis.
Last Update：2024-01-02 23:10:35
Esanbutol - Trait
Authoritative Data Verified Data
- This product is white crystalline powder; Odorless or almost odorless; Slightly hygroscopic.
- This product is very soluble in water, slightly soluble in ethanol, very slightly soluble in chloroform, almost insoluble in ether.
specific rotation
take this product, precision weighing, adding water to dissolve and quantitatively dilute to make a solution containing about 0.10g per lml. When measured at 25 ° C. According to the law (General rule 0621), the specific rotation is 6.0 ° to 7.0 °.
Last Update：2022-01-01 14:19:40
Esanbutol - Differential diagnosis
Authoritative Data Verified Data
- take about 20mg of this product, add 2ml of water to dissolve, add 2-3 drops of copper sulfate test solution, shake well, and add 2-3 drops of sodium hydroxide test solution to show dark blue.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 311).
- This product is chloride identification reaction (General 0301).
Last Update：2022-01-01 14:19:41
Esanbutol - Exam
Authoritative Data Verified Data
acidity
take this product, add water to make a solution containing 50mg per lml, according to the law (General 0631),pH value should be 3.4~4.0. (+) 2-aminobutanol (impurity T) take this product, add methanol to dissolve and dilute to make a solution containing about 50mg per 1 ml as a test solution; Take (+) the appropriate amount of 2-aminobutanol reference substance was dissolved and diluted with methanol to make a solution containing about 0.5mg per 1 ml as a reference solution; The appropriate amount of ethambutol hydrochloride reference substance and (+) 2-aminobutanol reference substance was also taken, methanol was added to dissolve and diluted to prepare a mixed solution containing about 5mg of ethambutol hydrochloride and 0.5mg of (+) 2-aminobutanol per 1 ml as a system-applicable solution. According to the thin layer chromatography (General 0502) test, absorb 2 u1 of each of the above two solutions, respectively point on the same silica gel G thin layer plate, with methanol-water-concentrated ammonia solution (75:15:10) for the development of the solvent, expand, dry, heated at 110°C for 10 minutes, cool, spray with ninhydrin solution (ninhydrin 1.0g, add 50ml of ethanol to dissolve, then add 10ml of glacial acetic acid, shake well) and heat at 110°C for 5 min. Two clearly separated spots should be shown in the system suitability solution chromatogram. If the test solution shows impurity spots corresponding to the control solution, the color of the test solution should not be deeper (1.0%) than the main spot of the control solution.
Related substances
new system for clinical use. Take about 20mg of this product, accurately weigh, put it in a 20ml measuring flask, add about 10ml of acetonitrile and 0.5ml of triethylamine, sonicate for 5 minutes to dissolve, dilute to scale with acetonitrile, shake well, take 4ml, put it in 10ml measuring flask, add (R)-( + )- a-methylbenzyl isocyanate 15u1, plug, shake, keep warm in a water bath at 70°C for 20 minutes, let it cool, shake well, and use it as a test solution. Take 1 ml in a precision volume, put it in a 200ml measuring flask, dilute it to the scale with acetonitrile, and shake well, as a control solution. According to high performance liquid chromatography (General 0512) determination, with eighteen alkyl silane bonded silica gel as filler; Mobile phase A is methanol-water (50:50 ) , mobile phase B is methanol, the linear gradient elution was carried out as follows; The detection wavelength was 215nm. The column temperature was 40°C. Take ethylamine-factory alcohol system applicable reference product about 4mg, precision weighing, put 10ml measuring flask, Precision Add acetonitrile 4ml and triethylamine 100ul ultrasonic 5 minutes to dissolve, Precision Add (R)-( + )-a-methylbenzyl isocyanate 15 u1, 70°C water bath for 20 minutes, cool, shake, take 10u1 injection human liquid chromatograph, record chromatogram, the retention time of the ethambutol derivative peak is about 14 minutes, and the degree of separation of the ethambutol derivative peak from the impurity II derivative peak at a relative retention time of about 1.3 should be greater than 4.0. The sample solution and the control solution of 10 u1 were respectively injected into the human liquid chromatograph, and the chromatogram was recorded. In the chromatogram of the test solution, if there are impurity peaks in the relative retention time of ethambutol derivative 0.75~1.5, the peak area of impurity II derivative shall not be more than 2 times (1.0%) of the main peak area of the control solution, other single impurity peak area shall not be greater than 0.2 times (0.1%) of the main peak area of the control solution, and the sum of each impurity peak area shall not be greater than 2 times (1.0%) of the main peak area of the control solution, any impurity peak less than 0.1 times the main peak area of the control solution in the chromatogram of the test solution is negligible.
loss on drying
take this product, dry to constant weight at 105°C, weight loss shall not exceed 0.5% (General rule 0831).
ignition residue
not more than 0.1% (General rule 0841).
Heavy metals
take 1.0g of this product, add 2ml of acetate buffer (pH 3.5) and appropriate amount of water to dissolve it into 25ml, and check it according to law (General Principles 0821 first method), heavy metals should not be more than 10 parts per million.
Last Update：2022-01-01 14:19:42
Esanbutol - Content determination
Authoritative Data Verified Data
take about 0.2g of this product, weigh it accurately, put it in a 50ml measuring flask, add 20ml of water to dissolve, add 1.8ml of copper sulfate test solution, and add 7ml of sodium hydroxide test solution while shaking, dilute to the scale with water, shake, centrifuge (4500 rpm), take the supernatant 10ml, add ammonia-ammonium chloride buffer (pH 10.0)(take ammonium chloride 70g, add water 300ml to dissolve, add 100ml of concentrated ammonia solution, dilute to 1000ml with water, adjust the pH value to 10.0 with concentrated ammonia solution) 10ml and water 100ml, add 0.15ml of test solution in Cu-PAN, and use ethylenediamine tetraacetic acid disodium titration solution (O.Olmol/L) titration to the solution from blue-purple through light red to light yellow, and the results of the titration were corrected with a blank test. Each 1 ml of ethylene diamine tetraacetic acid disodium titration solution (O.Olmol/L) corresponds to 2.7723mg of C10H24N2O2 · 2HC1.
Last Update：2022-01-01 14:19:43
Esanbutol - Category
Authoritative Data Verified Data
anti-tuberculosis drugs.
Last Update：2022-01-01 14:19:43
Esanbutol - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 14:19:43
Esanbutol - Ethambutol Hydrochloride Tablets
Authoritative Data Verified Data
This product contains ethylamine hydrochloride alcohol (Cl0H24N202 • 2HC1) should be 95.0% ~ 105.0% of the label amount.
trait
This product is a white tablet or a film-coated tablet, and the film-coated tablet is White after removing the coating.
identification
- take an appropriate amount of fine powder of this product (about 0.lg of ethambutol hydrochloride), add 10ml of water, shake to dissolve ethambutol hydrochloride, filter, take 2ml of filtrate, add 2-3 drops of copper sulfate solution, and shake well, 2-3 drops of sodium hydroxide solution was added, which showed dark blue.
- take an appropriate amount of fine powder of this product (about 0.05g of ethambutol hydrochloride), add 5ml of methanol, dissolve ethambutol hydrochloride by ultrasound, filter, and volatilize the filtrate to dryness, the infrared absorption spectrum of the residue should be consistent with that of the control (Spectrum set 311).
- 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
- (+) 2-aminobutanol (impurity I) take an appropriate amount of the fine powder of this product, add methanol to dissolve ethylamine hydrochloride T alcohol and dilute it to make a solution containing about 50mg of ethambutol hydrochloride in 1 ml, filter it, the continued filtrate was taken as the test solution. Another impurity [reference substance, dissolved with methanol and diluted to make a solution containing about 0.5mg per 1 ml as a reference solution; Another alcohol reference substance from ethylamine hydrochloride factory and an appropriate amount of impurity I reference substance, A solution containing about 5mg of ethambutol hydrochloride and 10.5mg of impurities per 1 ml was prepared by dissolving and diluting with methanol as a system-suitable 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 ethyl acetate-glacial acetic acid-hydrochloric acid-water (11:7:1:1) for the development solvent, about 10cm was developed, taken out, dried, dried at 105°C for 30 minutes, allowed to cool, sprayed with ninhydrin test solution, and heated at 105°C for 30 minutes. System applicability the solution should show two clearly separated spots. If the test solution shows impurity spots corresponding to the reference solution, the color should not be deeper (1.0%) compared with the main spot of the reference solution..
- new system of related substances in clinical use. Take an appropriate amount of fine powder of this product (about 0.2g of ethambutol hydrochloride), put it in a 20ml measuring flask, add water and ultrasound to dissolve ethambutol hydrochloride and dilute it to the scale, shake well, filter, and take 2ml of filtrate with precision, put it in a 20ml measuring flask, dilute with acetonitrile to scale, shake well, take 4ml, add 100ul triethylamine,(R)-( + )-G-methylbenzyl isocyanate 15ul and mix well, it was heated in a water bath at 70 ° C. For 20 minutes and allowed to stand for cooling as a test solution; 1ml was accurately weighed, placed in a 200ml measuring flask, diluted to a scale with acetonitrile, and shaken well to serve as a control solution. According to the method for the determination of related substances in ethambutol hydrochloride. If there is a chromatographic peak in the chromatogram of the test solution that is consistent with the retention time of the impurity II derivative of ethambutol hydrochloride, its area shall not be more than 2 times (1.0%) of the area of the main peak of the control solution, the Peak area of other single impurities with relative retention time between 0.75 and 1.5 shall not be greater than 0.2 times (0.1%) of the main peak area of the control solution, the sum of each impurity peak area shall not be greater than 2 times (1.0%) of the main peak area of the control solution. The peaks in the chromatogram of the test solution which were 0.1 times smaller than the main peak area of the control solution were ignored.
- 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 45 minutes, 5ml of the solution was taken, filtered, and the filtrate was taken as a test solution, which was measured according to the method under the content measurement item. The dissolution amount of each tablet was calculated by the peak area according to the external standard 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
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler; Ammonium acetate/copper acetate solution (50g of ammonium acetate and 0.2g of copper acetate, dissolved in water and diluted to 1000ml, the pH value was adjusted to 5.0 with glacial acetic acid)-methanol (88:12) as mobile phase; The detection wavelength was 270nm; The column temperature was 40°C. The reference solution 10H1 was injected into the liquid chromatograph, and the chromatogram was recorded. The ethambutol peak tailing factor should not be greater than 1.6.
- determination Method: Take 20 tablets of this product, accurately weigh and grind, accurately weigh an appropriate amount of fine powder (about 0.25g equivalent to ethambutol hydrochloride), put it in a 100ml measuring flask, and add water and ultrasound to dissolve ethambutol hydrochloride, cool, dilute to the scale with water, shake well, filter, Take 5ml of filtrate accurately, put it in a 50ml measuring flask, dilute to the scale with water, shake well, as a test solution, accurately weigh the appropriate amount of ethambutol hydrochloride reference substance, add water to dissolve and quantitatively dilute to prepare a solution containing about 0.25mg per 1 ml, which is determined by the same method. According to the external standard method to calculate the peak area, that is.
category
with ethambutol hydrochloride.
specification
0.25g
storage
light shielding, sealed storage.
Last Update：2022-01-01 14:19:44
Esanbutol - Ethambutol Hydrochloride Capsules
Authoritative Data Verified Data
This product contains ethambutol hydrochloride (C10H24N202 • 2HC1) should be 90.0% ~ 110.0% of label amount.
trait
The content of this product is white crystalline powder.
identification
- take about 20mg of the content of this product, add 2ml of water to dissolve, add 2~3 drops of copper sulfate test solution, shake well, and add 2~3 drops of sodium hydroxide test solution to show dark blue.
- take an appropriate amount of the content of this product (about 0.05g of ethambutol hydrochloride), add 5ml of methanol, ultrasonic dissolve ethambutol hydrochloride, filter, and volatilize the filtrate to dryness, the infrared absorption spectrum of the residue should be consistent with that of the control (Spectrum set 311).
- 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
- (+) 2-aminobutanol (impurity I) accurately weigh the appropriate amount of the contents of this product, add methanol to dissolve ethambutol hydrochloride and dilute it to make a solution containing about 50mg of ethambutol hydrochloride per 1 ml, and filter it, the continued filtrate was taken as the test solution. In addition, an appropriate amount of reference substance of impurity I was accurately weighed, dissolved with methanol and quantitatively diluted to make a solution containing about 0.50mg per 1 ml, which was used as a reference solution; An appropriate amount of reference substance of ethambutol hydrochloride and reference substance of impurity I was taken, A solution containing about 5mg of ethambutol hydrochloride and 0.5mg of impurity I in 1 ml was prepared by adding methanol as a system suitability solution. According to the thin layer chromatography (General 0502) test, absorb the above three solutions each 2u1, respectively, on the same silica gel G thin layer plate, with ethyl acetate-glacial acetic acid-hydrochloric acid-water (11:7:1:1) for the development solvent, about 10cm was developed, taken out, dried, dried at 105°C for 30 minutes, allowed to cool, sprayed with ninhydrin test solution, and heated at 105°C for 30 minutes. System applicability the solution should show two clearly separated spots. If the test solution shows impurity spots corresponding to the reference solution, the color should not be deeper (1.0%) compared with the main spot of the reference solution..
- new system of related substances in clinical use. Take an appropriate amount of the content of this product (about 0.2g of ethambutol hydrochloride), put it in a 20ml measuring flask, add water and ultrasound to dissolve ethambutol hydrochloride and dilute to the scale, shake, filter, take 2ml of the filtrate with precision, put it in a 20ml measuring flask, dilute it to the scale with acetonitrile, shake it well, take 4ml precisely, add triethylamine 100 u1,(R)-(+ )-a-methylbenzyl isocyanate 15ul, the mixture was mixed well, heated in a water bath at 70°C for 20 minutes, and allowed to cool, and used as a test solution. Take 1ml accurately, put it in a 200ml measuring flask, dilute it to the scale with acetonitrile, shake it well, and use it as a control solution; Measure it according to the method under the item of ethambutol hydrochloride related substances. If there is a chromatographic peak in the chromatogram of the test solution that is consistent with the retention time of the impurity II derivative of ethambutol hydrochloride, its area shall not be more than 2 times (1.0%) of the area of the main peak of the control solution, the Peak area of other single impurities with relative retention time of 0.75~1.5 shall not be greater than 0.2 times (0.1%) of the main peak area of the control solution, the sum of each impurity peak area shall not be greater than 2 times (1.0%) of the main peak area of the control solution. The peaks in the chromatogram of the test solution which were 0.1 times smaller than the main peak area of the control solution were ignored.
- 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; Ammonium acetate/copper acetate solution (50g of ammonium acetate and 0.2g of copper acetate, dissolved in water and diluted to 1000ml, the pH value was adjusted to 5.0 with glacial acetic acid)-methanol (88:12) as mobile phase; The detection wavelength was 270nm; The column temperature was 40°C. Take the reference solution 10u1 injection human liquid chromatography, record chromatogram, ethambutol tail factor should be less than 1.6.
- determine the contents under the item of loading difference, mix evenly, weigh an appropriate amount (about 0.25g equivalent to ethambutol hydrochloride) accurately, put it in a 100ml measuring flask, add water to dissolve ethambutol hydrochloride, cool, dilute to the scale with water, shake well, filter, Take 5ml of filtrate accurately, put it in a 50ml measuring flask, dilute to the scale with water, shake well, as a test solution, A 10ul injection liquid chromatograph was accurately measured, and the chromatogram was recorded. An appropriate amount of ethambutol hydrochloride reference substance was accurately weighed, dissolved with water and quantitatively diluted to prepare a solution containing about 0.25mg per 1 ml, which was determined by the same method. According to the external standard method to calculate the peak area, that is.
category
anti-tuberculosis drugs.
specification
0.25g
storage
light-shielded, sealed, and stored in a dry place.
Last Update：2022-01-01 14:19:45
Esanbutol - Reference Information
| Biological activity | Ethambutol 2HCl (CL40881) is an anti-mycobacterial bacteriostatic agent that interferes with cell wall formation by inhibiting arabinosyltransferase. |
Last Update：2024-04-10 22:29:15
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Product Name: ethambutol dihydrochloride Request for quotation
CAS: 1070-11-7
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
CAS: 1070-11-7
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
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Product Name: Ethambutol Hydrochloride Visit Supplier Webpage Request for quotationCAS: 1070-11-7
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