丙硫异烟胺 (BP88 和 BP88 & SPECIAL STANDARD)
Prothionamide
CAS: 14222-60-7
Molecular Formula: C9H12N2S
丙硫异烟胺 (BP88 和 BP88 & SPECIAL STANDARD) - Names and Identifiers
| Name | Prothionamide |
| Synonyms | 1321th PROTIONAMIDE Protionamide Prothionamide PROTHIONAMIDE Isothionicotinamide Propylthioisonicotinamide 2-propyl-4-pyridinecarbothioamid 2-propyl-4-thiocarbamoylpyridine 2-propyl-4-pyridinecarbothioamide 2-propylpyridine-4-carbothioamide |
| CAS | 14222-60-7 |
| EINECS | 238-093-7 |
| InChI | InChI=1/C9H12N2S/c1-2-3-8-6-7(9(10)12)4-5-11-8/h4-6H,2-3H2,1H3,(H2,10,12) |
丙硫异烟胺 (BP88 和 BP88 & SPECIAL STANDARD) - Physico-chemical Properties
| Molecular Formula | C9H12N2S |
| Molar Mass | 180.27 |
| Density | 1.1015 (rough estimate) |
| Melting Point | 140-143°C |
| Boling Point | 310.4±44.0 °C(Predicted) |
| Flash Point | 141.5°C |
| Solubility | Soluble in ethanol, methanol, ether, and chloroform. Insoluble in water., Soluble in eth |
| Vapor Presure | 0.000601mmHg at 25°C |
| Appearance | Crystalline powder |
| Color | Yellow |
| Merck | 14,7891 |
| pKa | 12.14±0.29(Predicted) |
| Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
| Refractive Index | 1.5300 (estimate) |
| MDL | MFCD00464119 |
| Use | With inhibition of tuberculosis, high concentration of bactericidal effect |
丙硫异烟胺 (BP88 和 BP88 & SPECIAL STANDARD) - Risk and Safety
| RTECS | NS0650000 |
| Hazard Class | IRRITANT |
| Toxicity | LD50 in mice, rats (g/kg): 1.0, 1.32 orally (Il'in) |
丙硫异烟胺 (BP88 和 BP88 & SPECIAL STANDARD) - Reference
| Reference Show more | 1. [IF=2.363] Li Xie et al."A sensitive EZMTT method provides microscale, quantitative and high-throughput evaluation of drug efficacy in the treatment of Mycobacterium tuberculosis infectious diseases."J Microbiol Meth. 2021 Feb;181:106136 |
丙硫异烟胺 (BP88 和 BP88 & SPECIAL STANDARD) - Standard
Authoritative Data Verified Data
This product is 2-propylthioisonicotinamide. The content of C9H12N2S calculated as dry product shall not be less than 99.0%.
Last Update：2024-01-02 23:10:35
丙硫异烟胺 (BP88 和 BP88 & SPECIAL STANDARD) - Trait
Authoritative Data Verified Data
- This product is yellow crystal or crystalline powder; Micro special odor.
- This product is dissolved in methanol, ethanol or acetone, slightly soluble in ether, almost insoluble in water.
melting point
The melting point of this product (General 0612) is 139~143°C.
Last Update：2022-01-01 11:35:10
丙硫异烟胺 (BP88 和 BP88 & SPECIAL STANDARD) - 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.
- take this product, dissolve and dilute with ethanol to make a solution containing about 20ug per lml, and measure by UV-Vis spectrophotometry (General 0401), there is a maximum absorption at a wavelength of 291nm.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 69).
Last Update：2022-01-01 11:35:10
丙硫异烟胺 (BP88 和 BP88 & SPECIAL STANDARD) - Exam
Authoritative Data Verified Data
acidity
take 2.0g of this product, add ethanol 20ml, slightly heat dissolve, add water 20ml, cool, shake to precipitate the crystal, add 2 drops of Cresol red indicator solution, use sodium hydroxide titration solution (0.lmol/U titration, consumption of sodium hydroxide titration solution (0.lmol/L) not over 0.20.
Related substances
operation in the dark. Take this product, add mobile phase to dissolve and dilute to make about 0.1 mg of the solution was used as a test solution; 1ml was accurately weighed, placed in a 100ml measuring flask, diluted to the scale with the mobile phase, and shaken to obtain a control solution. According to the chromatographic conditions under the content determination item, 20ul of each of the test solution and the control solution are accurately measured and injected into the human liquid chromatograph respectively, and the chromatogram is recorded to 3 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than 0.5 times (0.5%) of the area of the main peak of the control solution, the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%).
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
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
Heavy metals
The residue left under the item of taking the ignition residue shall not contain more than 20 parts per million of heavy metal when examined by law (General rule 0821, Law II).
Last Update：2022-01-01 11:35:11
丙硫异烟胺 (BP88 和 BP88 & SPECIAL STANDARD) - Content determination
Authoritative Data Verified Data
measured by high performance liquid chromatography (General 0512).
chromatographic conditions and system suitability test
silica gel bonded with octa-alkyl silane was used as filler, and 0.2mol/L sodium dihydrogen phosphate solution (adjusted to pH 3.0 with phosphoric acid)-acetonitrile (80:20) was used as mobile phase; the detection wavelength was 282nm. The number of theoretical plates shall not be less than 5000 calculated from the peak of propylthioisicotinamide.
assay
take this product, precision weighing, add mobile phase dissolution and quantitative dilution to make a solution containing about 50ug per lml, as a test solution, take 20 u1 for precision, injection of human liquid chromatograph, record chromatogram; Another reference substance of propylthioisicotinamide, the same method for determination. According to the external standard method to calculate the peak area, that is.
Last Update：2022-01-01 11:35:12
丙硫异烟胺 (BP88 和 BP88 & SPECIAL STANDARD) - Category
Authoritative Data Verified Data
anti-tuberculosis drugs.
Last Update：2022-01-01 11:35:12
丙硫异烟胺 (BP88 和 BP88 & SPECIAL STANDARD) - Storage
Authoritative Data Verified Data
sealed storage.
Last Update：2022-01-01 11:35:12
丙硫异烟胺 (BP88 和 BP88 & SPECIAL STANDARD) - Protionamide Enteric-coated Tablets
Authoritative Data Verified Data
This product contains propylthioisonicotinamide (C9H12N2S) should be 90.0% to 110.0% of the label amount.
trait
This product is an enteric-coated tablet, which shows yellow color after removing the coating.
identification
- 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.
- take an appropriate amount of the fine powder of this product, dissolve it with ethanol and dilute it to make a solution containing about 20ug of propylthioisicotinamide per lml, filter it and take the filtrate, there is an absorption maximum at a wavelength of 0401 nm as determined by UV-Vis spectrophotometry (general).
examination
- the related substances were protected from light. Take an appropriate amount of fine powder of this product, add the mobile phase to dissolve and dilute to make about 0.1 mg of the solution was filtered, and the continued filtrate was taken as a test solution; 1ml was accurately measured, placed in a 100ml measuring flask, diluted to the scale with the mobile phase, and shaken to obtain a control solution. Test according to the method under prothioisonicotino-related substances. If there are impurity peaks in the chromatogram of the test solution, the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%).
- dissolution of this product, according to the dissolution and release determination method (General 0931 second method 2), the speed is 75 rpm, the dissolution of phosphate buffer (pH 6.8) (containing 0.05% sodium dodecyl sulfate) was used as the dissolution medium. The filtrate under the acid elution amount was taken as the test solution (1), and the filtrate under the buffer solution elution amount was taken as the test solution (2). Another 10mg of the reference substance of propylthioisonicotinamide was added into a 100ml measuring flask, dissolved with 10ml of methanol, diluted to the scale with the above phosphate buffer solution, and then shaken to form the reference solution. The sample solutions (1) and (2) and the reference solution were respectively taken and measured according to the method under the content measurement item, and the dissolution amount of each tablet was calculated. The amount of dissolution in the acid should be consistent with the regulations; The limit of dissolution in the buffer is 70% of the labeled amount, which should be consistent with the regulations.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
Take 20 tablets of this product, remove the coating, precision weighing, fine grinding, precision weighing appropriate amount (about 0.lg equivalent to propylthionicotinamide), put it in a 100ml measuring flask, add mobile phase to dissolve propylthioisonicotinamide and dilute to the scale, shake well, filter, Take 5ml of continuous filtrate precisely, put it in 100ml measuring flask, dilute to the scale with mobile phase, shake well, as a test solution, according to the method under the item of determination of the content of propylthioisonicotinamide, it is obtained.
category
Same as propylthioisonicotinamide.
specification
0.lg
storage
light shielding, sealed storage.
Last Update：2022-01-01 11:35:13
丙硫异烟胺 (BP88 和 BP88 & SPECIAL STANDARD) - Reference Information
| Pharmacological effects | Prothioisonicotinamide is a derivative of isonicotinic acid. Its mechanism of action is unknown and may have an inhibitory effect on peptide synthesis. The effect of this product on Mycobacterium tuberculosis depends on the drug concentration at the infection site. It only has antibacterial effect at low concentration, and has bactericidal effect at high concentration. This product has partial cross-resistance to ethionine. |
| pharmacokinetics | propylsulifinamide is absorbed rapidly and completely in the gastrointestinal tract after oral administration. 90% drugs are absorbed, and the blood drug concentration can reach a high peak within 1~2 hours. it is widely distributed in body tissues and body fluids, can cross the blood-brain barrier into cerebrospinal fluid, and can also enter the fetal circulation through the placental barrier. The drug concentration in each tissue and body fluid is almost equal to the blood drug concentration, and the effective drug concentration can be maintained for more than 6 hours with a half-life of 3 hours. Most of them are metabolized in liver and excreted in urine. 1% are prototype, 5% are active metabolites, and the rest are inactive metabolites. |
| Indications | Prothioisonicotinamide is only effective against mycobacteria. This product is combined with other anti-tuberculosis drugs for tuberculosis patients who are ineffective after first-line drugs (such as streptomycin, isoniazid, rifampicin and ethambutol). |
| adverse reactions | 1. higher incidence: depression (central nervous system toxicity), diarrhea, loss of appetite, stomachache, stomach discomfort, vomiting (gastrointestinal disorders). 2. Less incidence: gait instability or numbness, acupuncture sensation, burning sensation, hand and foot pain (peripheral neuritis), mental confusion or other mental changes (central nervous system toxicity), eyes or skin yellow (jaundice, hepatitis). 3. The incidence rate is very small: blurred vision or vision loss, combined with or without eye pain (optic neuritis), menstrual disorders or fear of cold, decreased libido (men), dry and rough skin, hypothyroidism, Joint pain, stiffness and swelling. |
| use | has the effect of inhibiting tuberculosis bacteria, high concentration bactericidal effect has the effect of inhibiting tuberculosis bacteria, high concentration bactericidal effect. |
Last Update：2024-04-09 21:21:28
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Product Name: Prothionamide Visit Supplier Webpage Request for quotationCAS: 14222-60-7
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CAS: 14222-60-7
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Tel: +86-18821248368
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