105826-92-4
tropisetron hydrochloride
CAS: 105826-92-4
Molecular Formula: C17H21ClN2O2
105826-92-4 - Names and Identifiers
| Name | tropisetron hydrochloride |
| Synonyms | Novaban SDZ-ICS 930 105826-92-4 Tropisetron HCl Tropisetron hydrochloride Tropiserton Hydrochloride tropisetron hydrochloride 3-TROPANYLINDOLE-3-CARBOXYLATE HYDROCHLORIDE 1H-Indole-3-carboxylic acid (3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester hydrochloride (3-ENDO)-8-METHYL-8-AZABICYCLO[3.2.1]OCT-3-YL 1H-INDOLE-3-CARBOXYLIC ACID ESTER MONOHYDROCHLORIDE |
| CAS | 105826-92-4 |
| EINECS | 630-417-9 |
| InChI | InChI=1/C17H20N2O2.ClH/c1-19-11-6-7-12(19)9-13(8-11)21-17(20)15-10-18-16-5-3-2-4-14(15)16;/h2-5,10-13,18H,6-9H2,1H3;1H |
105826-92-4 - Physico-chemical Properties
| Molecular Formula | C17H21ClN2O2 |
| Molar Mass | 320.81 |
| Melting Point | 283-285°C |
| Boling Point | 448.5°C at 760 mmHg |
| Flash Point | 225°C |
| Water Solubility | Soluble in water |
| Solubility | H2O: >10mg/mL |
| Vapor Presure | 3.09E-08mmHg at 25°C |
| Appearance | Powder |
| Merck | 14,9783 |
| Storage Condition | 2-8°C |
| Sensitive | Sensitive to heat |
| MDL | MFCD00210221 |
| Physical and Chemical Properties | Melting point 283-285°C |
| Use | For the prevention and treatment of tumor chemotherapy and radiotherapy induced Nausea and Vomit reaction |
| In vitro study | Tropisetron is a high affinity ligand for the α7 choline receptor and 5HT3R. Tropisetron has very low affinity for the other nicotine subtypes tested. Tropisetron is a potent and selective serotonin 3(5-hydroxytryptamine3;5-HT 3) receptor antagonist with antiemetic effects, it may be mediated by receptor antagonism in the peripheral region and in the central nervous system. Tropisetron is an early and late potent inhibitor of TCR-mediated T cell activation. Tropisetron specifically inhibited transcription and synthesis of IL-2 of the genes in stimulated T cells. Ttropisetron inhibited NFAT and AP-1 binding to DNA and transcriptional activity. Ttropisetron is a potent inhibitor of PMA and ionomycin-induced NF-(kappa)B activation, but TNF(alpha)-mediated NF-(kappa)B activation is not affected by Ttropisetron. In isolated porcine retinal ganglion cells (RGCs), Tropisetron acts on the α7 nicotinic receptor, providing neuroprotection from glutamate-induced excitotoxicity. Tropisetron acts to reduce p38 MAP kinase levels to inhibit apoptosis. Tropisetron dose-dependently protects retinal ganglion cells (RGCs) from glutamate toxic effects when added to the Culture 1 hour prior to glutamate addition. |
| In vivo study | In DBA/2 mice, Tropisetron(1 mg/kg I. p.) significantly ameliorated deficient inhibition of P20-N40 of the auditory evoked potential. |
105826-92-4 - Risk and Safety
| UN IDs | 2811 |
| WGK Germany | 3 |
| RTECS | NL6012520 |
| HS Code | 29399990 |
| Hazard Class | 6.1 |
| Packing Group | III |
105826-92-4 - Standard
Authoritative Data Verified Data
This product is indole -3-carboxylic acid 1aH,5aH-troppin-3a-alcohol Ester hydrochloride. The content of C17H20N202 • HC1 shall not be less than 99.0% calculated as dry product.
Last Update：2024-01-02 23:10:35
105826-92-4 - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline powder; Odorless.
- This product is soluble in water, slightly soluble in methanol, slightly soluble in ethanol, almost insoluble in chloroform.
Last Update：2022-01-01 14:22:23
105826-92-4 - Introduction
Tropisetron hydrochloride is a potent SR (SR-3) antagonist. It is also a selective, partial agonist at AChR α 7 (α7 nicotinic receptors). Tropisetron hydrochloride is an inhibitor of HTR3.
Last Update：2022-10-16 17:11:45
105826-92-4 - Differential diagnosis
Authoritative Data Verified Data
- take this product, add O. 1 mol /L hydrochloric acid solution dissolved and diluted into solution containing 15ug per 1 ml, according to UV-visible spectrophotometry (General 0401) determination, there is maximum absorption at wavelengths of 230nm and 284nm and minimum absorption at wavelengths of 223nm and 262NM.
- take an appropriate amount of this product, add the mobile phase under the item of related substances to dissolve and dilute to make 0. A solution of 1 mg was used as a test solution; An appropriate amount of tropisetron hydrochloride was taken as a control, and the mobile phase under the item of related substances was added to dissolve and dilute to prepare a solution containing 0.1 mg solution, as a control solution. According to the chromatographic conditions under the item of related substances, 20ul of the test solution and the reference solution are respectively injected into the liquid chromatograph, and the chromatograms are recorded, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the control solution.
- The infrared absorption spectrum of this product should be consistent with that of the reference product (General rule 0402).
- the aqueous solution of this product was chloride identification (1) of the reaction (General 0301).
Last Update：2022-01-01 14:22:23
105826-92-4 - Exam
Authoritative Data Verified Data
acidity
take an appropriate amount of this product, add water to dissolve and dilute the solution containing 10 mg per lml, and determine it according to law (General rule 0631). The pH value should be 5.0~6.5. The clarity and color of the solution take 0.10g of this product, add water to dissolve 5ml, the solution should be clear and colorless; If it is turbid, compared with the No. 1 turbidity standard solution (the general principles of the first method 0902), not more concentrated; in case of color development, it shall not be deeper in comparison with the yellow No. 1 Standard Colorimetric solution (General rules 0901 first method).
Related substances
take this product, add mobile phase to dissolve and dilute to make a solution containing about 1 mg per 1ml as a test solution; Take 1ml for precision measurement and put it in a 500ml measuring flask, dilute to the scale with the mobile phase, shake, and serve as a control solution. Additional tropisetron hydrochloride control, indole -3-carboxylic acid (impurity I) control and indole -3-formaldehyde (impurity II) control, A mixed solution containing 1 mg of tropisetron, 1 lug of impurity and 1 lug of impurity per 1ml was prepared by dissolving and diluting the mobile phase and used as a system-applicable solution. According to the high performance liquid chromatography (General rule 0512) test, with eighteen alkyl silane bonded silica gel as filler, phosphate buffer solution (take potassium dihydrogen phosphate 6.8G, add water 500ml to dissolve, add triethylamine 5ml, dilute to 3.5 ml with water and adjust pH to with phosphoric acid-acetonitrile (80:20) as mobile phase at detection wavelength of 284nm. Take the applicable solution 20 u1 of the system and inject it into human Liquid Chromatograph. The number of theoretical plates shall not be less than 2000 based on tropisetron peak. The resolution of tropisetron peak, impurity I peak and impurity II peak shall meet the requirements. 20 u1 of the test solution and the control solution were respectively injected into the liquid chromatograph, and the chromatogram was recorded to 2.5 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 (0.1%) of the area of the main peak of the control solution, the sum of each impurity peak area shall not be greater than 1.5 times (0.3%) of the main peak area of the control solution.
a-Toprol (impurity III )
take this product 0.2g, precision weighing, precision plus solvent [methanol-dichloromethane solution (1:l) ] 5ml to dissolve, as a test solution; an appropriate amount of a-Tol alcohol reference substance was carefully weighed, dissolved with the above solvent and quantitatively diluted to prepare a solution containing 0.2mg per 1 ml as a reference solution. The appropriate amount of tropisetron hydrochloride reference substance and a-tropicol reference substance was also taken, the above solvent was added, dissolved and diluted to prepare a mixed solution containing 40mg of tromersetron hydrochloride and 0.2mg of a-tropicol per 1 ml, respectively, as a system-applicable solution. According to the thin layer chromatography (General 0502) test, the sample solution, the reference solution and the system applicable solution are accurately drawn 10ul, respectively, on the same silica gel GF254 thin layer plate, methanol-dichloromethane-concentrated ammonia solution (40:60:5) was used as the developing solvent, developed, dried, and sprayed with bismuth potassium iodide solution for color development. The system suitability solution should show two completely separated spots. Test solution such as a-tropicol impurity spots, the color of the main spot compared with the control solution should not be deeper (0.5%).
B-isomer (impurity IV)
take this product, precision weighing, adding mobile phase to dissolve and quantitatively dilute to prepare a solution containing about 1 mg per 1 ml as a test solution; Take an appropriate amount of tropisetron hydrochloride B- isomer reference substance, precision weighing, plus mobile phase dissolution and quantitative dilution to prepare about lug per 1 mL solution, as a reference solution. The appropriate amounts of tropisetron hydrochloride control substance and tropisetron hydrochloride B- isomer control substance were dissolved and diluted with mobile phase to prepare a mixed solution containing 1 mg and lug respectively per 1 ml as a system applicable solution. According to the high performance liquid chromatography (General rule 0512) test, with eighteen alkyl silane bonded silica gel as filler, phosphate buffer solution (take potassium dihydrogen phosphate 6.8g, add water 500ml to dissolve, add triethylamine 5ml, dilute to 3.5 ml with water, adjust pH to with phosphoric acid)-methanol (70:30) as mobile phase, detection wavelength 284mn. 20ul of the applicable solution of the system is injected into the liquid chromatograph, and the number of theoretical plates is not less than 2000 calculated by tropisetron peak. The resolution of tropisetron peak and B- isomer peak shall meet the requirements. Then, 20 u1 of each of the test solution and the reference solution were respectively injected into the liquid chromatograph. If there are chromatographic peaks with the same retention time as B- isomer in the chromatogram of the test solution, the peak area shall be calculated by external standard method, and shall not exceed 0.1%.
residual solvent
take this product about lOOmg, precision weighing, put it in 20ml top-empty bottle, Precision Add 5ml of dimethyl sulfoxide solution [Dimethyl Sulfoxide-water (9:1 )], plus about lg of sodium chloride, as a test solution, seal; Take N-hexane, Tetrahydrofuran, methanol, dichloromethane, ethanol, chloroform, toluene and N, N-dimethylformamide appropriate amount, precision weighing, add dimethyl sulfoxide solution [Dimethyl Sulfoxide-water (9:1 )], dissolve and quantitatively dilute to prepare n-hexane 2.9ug, tetrahydrofuran 7.2ug, methanol 30ug, dichloromethane 6ug, ethanol 50ug per 1 ml, mixed solution of chloroform 0.6ug, toluene 8.9ug,N, N-dimethylformamide 8.8ug, as reference solution, Take 5ml of reference solution in a precise amount, put it in a 20ml headspace bottle, add about lg of sodium chloride, sealed. According to the determination method of residual solvent (General 0861 second method), the capillary column with polyethylene glycol (PEG-20M) (or similar polarity) as stationary liquid is used as the column, and the temperature is programmed, and the initial temperature is 40°C, hold for 8 minutes, ramp to 200°C at a rate of 20°C per minute, hold for 4 minutes, inlet temperature 250°C, split ratio 10:1, detector temperature 250°C. The Headspace bottle equilibration temperature was 85°C and the equilibration time was 25 minutes. The test solution and the reference solution were injected by Headspace, and the chromatograms were recorded. Except that the separation degree between dichloromethane peak and ethanol peak shall not be less than 1.0, the separation degree of peaks of other components shall meet the requirements. The residual amount of N-hexane, Tetrahydrofuran, methanol, dichloromethane, ethanol, trichloromethane, toluene and N ,N-dimethylformamide shall meet the requirements calculated by peak area according to external standard method.
loss on drying
take this product, dry to no weight at 105°C, and lose no more than 0 .5% of weight (General rule 0831).
ignition residue
This product l .O g, inspection according to law (General 0841), residue shall not exceed 0.1%.
Heavy metals
The residue left under the item of taking the ignition residue shall not contain more than 10 parts per million of heavy metal when examined by law (General Principles 0821, Law II).
Last Update：2022-01-01 14:22:25
105826-92-4 - Content determination
Authoritative Data Verified Data
take this product about 0.25g, precision weighing, add glacial acetic acid 10ml, warm to dissolve, add acetic anhydride 70ml, according to the potential titration method (General 0701), with perchloric acid titration solution (0.1 mol/L) titration, and the titration results were corrected with a blank test. Each 1 ml perchloric acid titration solution (0.1 mol/L) corresponds to 32.08mg of C17H20N2O2 • HCl).
Last Update：2022-01-01 14:22:26
105826-92-4 - Category
Authoritative Data Verified Data
5-HT3 receptor antagonist.
Last Update：2022-01-01 14:22:26
105826-92-4 - Storage
Authoritative Data Verified Data
sealed storage.
Last Update：2022-01-01 14:22:26
105826-92-4 - Tropisetron Hydrochloride Injectipn
Authoritative Data Verified Data
This product is a sterile aqueous solution of tropisetron hydrochloride, containing tropisetron hydrochloride as Tropisetron ((C17H20N202), should be 93.0% ~ 107.0% of the label amount.
trait
This product is a clear colorless liquid.
identification
- 5ml of this product was taken, and silicotungstic acid test solution was added dropwise, resulting in white to yellow precipitate.
- 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 and dilute it with water to make a solution containing 10ug tropisetron per 1 ml, and measure it by UV-Vis spectrophotometry (General 0401), there is maximum absorption at wavelengths of 230nm and 284nm, and minimum absorption at wavelengths of 223nm and 262nm.
- This product chloride identification (1) of the reaction (General 0301).
examination
- the pH value should be 4.0 to 6.5 (General 0631).
- clarity and color this product should be clear and colorless. In case of color development, it shall not be deeper in comparison with the yellow No. 1 Standard Colorimetric solution (General rules 0901 first method).
- appropriate amount of related substances should be taken and diluted with mobile phase to prepare a solution containing about 1 mg of tolossetron per lml (lml:5mg specification), or directly take this product (2ml:2mg and 5ml:5mg specification), as a test solution; Precision take 1 ml, 500ml flask, diluted to the scale with mobile phase, shake, as a control solution. The determination was carried out according to the method for related substances of tropisetron hydrochloride. 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 (0.1%) of the area of the main peak of the control solution, the sum of each impurity peak area shall not be greater than 2.5 times (0.5%) of the main peak area of the control solution.
- bacterial endotoxin from this product, according to the determination (General 1143), the amount of endotoxin per 1 mg tropisetron should be less than 20EU.
- sterile take this product, by membrane filtration method, with Staphylococcus aureus as positive control bacteria, according to law inspection (General Principles 1101), should comply with the provisions.
- others should comply with the relevant provisions under injection (General 0102).
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; Phosphate buffer (take potassium dihydrogen phosphate 6.8g, add water 500ml to dissolve, add triethylamine 5ml, dilute to 1000ml with water, the pH value was adjusted to 3.5 with phosphoric acid)-acetonitrile (80:20) as the mobile phase; The detection wavelength was 284nm. Take appropriate amount of tropisetron hydrochloride reference substance, impurity I reference substance and impurity II reference substance, add mobile phase to dissolve and dilute to prepare mixed solution containing tropisetron lmg, impurity I 1ug and impurity II 1ug respectively per lml, as the system applicable solution, take 20u1 injection liquid chromatograph, record chromatogram. The theoretical plate number is not less than 2000 based on the tropisetron peak, and the separation degree between the tropisetron peak, the indole -3-formic acid peak and the indole -3-formaldehyde peak should meet the requirements.
- precision measurement: Take appropriate amount of this product and dilute it quantitatively with water to make a solution containing about 20ul tropisetron per 1 ml, which is used as a test solution, record the chromatogram; Take an appropriate amount of tropisetron hydrochloride reference substance, accurately weigh, add water to dissolve and quantitatively dilute to make a solution containing about 20ug of tropisetron per 1 ml, and determine with the same method. According to the external standard method to calculate the peak area, and the result is multiplied by 0.8864, that is.
category
Same as tropisetron hydrochloride.
specification
calculated by C17H20N202 (l ) lml:5mg (2 )2ml:2mg (3)5ml:5Mg
storage
It was kept in a closed, cool and dark place.
Last Update：2022-01-01 14:22:27
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