AKOS 92111
Venlafaxine Hydrochloride
CAS: 99300-78-4
Molecular Formula: C17H28ClNO2
AKOS 92111 - Names and Identifiers
| Name | Venlafaxine Hydrochloride |
| Synonyms | EFFEXOR Venlift AKOS 92111 VENLAFAXINEHCL Venlafaxine HCl D,L-VENLAFAXINE Venlaffaxine HCL VenlfaxineHydrochloride Venlafaxine Hydrochloride D,L-VENLAFAXINE, HYDROCHLORIDE 1-[2-(DIMETHYLAMINO)-1-(4-METHOXYPHENYL)ETHYL]CYCLOHEXANOL, HCL 1-[2-(DIMETHYLAMINO)-1-(4-METHOXYPHENYL)ETHYL]CYCLOHEXANOL HYDROCHLORIDE (RS)-1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol hydrochloride 1-[2-DIMETHYL AMINO)-1-(4-METHOXYPHENYL)ETHYL]CYCLOHEXANONE HYDROCHLORIDE (+) N,N-dimethyl-2-p-methoxyphenyl-2-(1-hydroxycyclohexyl) ethylamine hydrochloride |
| CAS | 99300-78-4 |
| EINECS | 619-421-1 |
| InChI | InChI=1/C17H27NO2.ClH/c1-18(2)13-16(17(19)11-5-4-6-12-17)14-7-9-15(20-3)10-8-14;/h7-10,16,19H,4-6,11-13H2,1-3H3;1H |
| InChIKey | QYRYFNHXARDNFZ-UHFFFAOYSA-N |
AKOS 92111 - Physico-chemical Properties
| Molecular Formula | C17H28ClNO2 |
| Molar Mass | 313.86 |
| Melting Point | 207-209°C |
| Flash Point | 9℃ |
| Solubility | Soluble in water (>25 mg/ml), and DMSO (50 mM) |
| Appearance | powder |
| Color | white |
| Merck | 14,9946 |
| Storage Condition | 2-8°C |
| Sensitive | Sensitive to light |
| MDL | MFCD03658865 |
| Use | An inhibitor of ST and SLC6A2. |
| In vitro study | Venlafaxine has a low potential to inhibit CYP2D6 substrate metabolism compared to several widely used SSRIs, such as imipramine and desipramine, and also inhibits the metabolism of several other major human hepatocyte P450s substrates. Venlafaxine inhibits binding to human norepinephrine (NE) and serotonin (5-HT) transporters with K (I) values of 2480 nM and 82 nM,K (I) than 30. Venlafaxine blocked p-chloramphetamine and 6-hydroxydopamine-induced monoamine depletion with ED(50) values of 5.9 mg/kg and 94 mg/kg, respectively. |
| In vivo study | Venlafaxine induced dose-dependent analgesia with an ED50 of 46.7 mg/kg in mice. In mice, Venlafaxine-induced analgesia was significantly inhibited by naloxone,nor-BNI, and naltrindole, but not by β-FNA or naloxonazine, implying that κ-and δ-opioid receptor mechanisms are involved. In rats with fully developed neuropathy, Venlafaxine reversed hyperalgesia. Venlafaxine also appears to have a mild non-specific analgesic effect, which increases the thermal stimulation of foot constriction latency (PWL) in the prosthesis. |
AKOS 92111 - Risk and Safety
| Risk Codes | R36/37/38 - Irritating to eyes, respiratory system and skin. R36 - Irritating to the eyes R39/23/24/25 - R23/24/25 - Toxic by inhalation, in contact with skin and if swallowed. R11 - Highly Flammable |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S37/39 - Wear suitable 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. S16 - Keep away from sources of ignition. S7 - Keep container tightly closed. |
| UN IDs | UN1230 - class 3 - PG 2 - Methanol, solution |
| WGK Germany | 3 |
| RTECS | GV8872760 |
| HS Code | 29225090 |
AKOS 92111 - Reference
| Reference Show more | 1. Wan Guangsheng, Li Jingyu, Liu Lili, et al. Effect of tianfoshen on oxaliplatin-induced neurotoxicity in rats [J]. Shi Zhen, National Medicine, 2018, 029(002):301-304. |
AKOS 92111 - Standard
Authoritative Data Verified Data
This product is (±)-l-[2-(N,N-dimethylamino)-l-(4-methoxyphenyl) ethyl] cyclohexanol hydrochloride. The content of C17H27N02 • HC1 shall not be less than 98.5% calculated on a dry basis.
Last Update：2024-01-02 23:10:35
AKOS 92111 - Trait
Authoritative Data Verified Data
- This product is white crystal or crystalline powder; Odorless.
- This product is soluble in water, soluble in ethanol, almost insoluble in ether; Soluble in dilute hydrochloric acid.
Last Update：2022-01-01 14:20:40
AKOS 92111 - Differential diagnosis
Authoritative Data Verified Data
- take about 10mg of this product, add about 0.5 of citric acid-acetic anhydride solution, shake well, put it in a boiling water bath and heat it for several minutes to show blood red.
- take this product, add water to dissolve and dilute to make a solution containing about 20ug per lml, and measure by UV-Vis spectrophotometry (General 0401), there is an absorption maximum at a wavelength of 225Nm.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 1265).
- the aqueous solution of this product can identify the reaction of (1) (General rule 0301).
Last Update：2022-01-01 14:20:41
AKOS 92111 - Exam
Authoritative Data Verified Data
acidity
take 0.50g of this product, Add 10ml of water to dissolve, and measure according to law (General rule 0631). The pH value should be 4.0~6.0.
Related substances
take this product, add the mobile phase to dissolve and make a solution containing about 1 mg per 1 ml, as a test solution; Take an appropriate amount, A solution containing about 10% per 1 ml was prepared as a control solution by quantitative dilution with mobile phase. Tested according to high performance liquid chromatography (General 0512). With octanosilane bonded silica gel as filler; With ethyl-cured -0. The mobile phase was 1 mol/L potassium dihydrogen phosphate solution (25:75); The detection wavelength was 225nm; The number of theoretical plates was not less than 2000 according to the peak of venlafaxine hydrochloride. Take 10 u1 of the test solution and the control solution respectively, inject the human liquid chromatograph, record the chromatogram to 4 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 0.1 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 0.2 times (0.2%) of the main peak area of the control solution.
residual solvent
take this product about 0. LG, precision weighing, top empty bottle, precision plus 50% N, N-dimethylformamide solution to dissolve, sealed, as a test solution; weigh the appropriate amount of methanol, ethanol, ether, acetone, isopropanol, dichloromethane, N-hexane, ethyl acetate, Tetrahydrofuran, cyclohexane and toluene with 50% N, the N-dimethylformamide solution was quantitatively diluted to contain methanol 0.15mg, ethanol 0.25mg, acetic acid 0.25mg, acetone 0.25mg, isopropanol 0.25mg, dichloromethane 0.03mg, N-hexane 0.0145mg, 0.25mg of ethyl acetate, 0.036mg of tetrahydrofuran, 0.194mg of toluene and 0.0445mg of mixed solution, 2ml of which was precisely weighed, placed in a headspace bottle, sealed, and used as a reference solution. According to the test for determination of residual solvents (General Principle 0861 second method), a capillary column with 6% cyanopropylphenyl-94% dimethylpolysiloxane (or similar polarity) as stationary liquid is used as the column; The initial temperature is 40°C, hold for 10 minutes, raise to 140 ° C at a rate of 10 ° C per minute, then raise to 220 ° C at a rate of 30 ° C per minute for 2 minutes; Inlet temperature at 200 ° C; the temperature of the detector is 25CTC; The equilibrium temperature of the headspace bottle is 80 ° C, and the equilibrium time is 30 minutes. The reference solution is sampled in the headspace and the chromatogram is recorded. Then the sample solution and the reference solution were injected with headspace, and the chromatogram was recorded. The residual amount of methanol, ethanol, diethyl ether, acetone, isopropanol, dichloromethane, n-hexane, ethyl acetate, Tetrahydrofuran, cyclohexane and toluene shall be in accordance with the provisions calculated by the peak area according to the external standard method.
loss on drying
take this product, dry to constant weight at 105°C, weight loss shall not exceed 1.0% (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 14:20:42
AKOS 92111 - Content determination
Authoritative Data Verified Data
take this product about 0.2g, precision weighing, add glacial acetic acid 10ml and acetic anhydride 30ml dissolved, according to the potential titration method (General rule 0701), with perchloric acid titration solution (0.1 mol/L) titration, and the results of the titration were corrected with a blank test. Per 1 ml of perchloric acid titrant (0.1 mol/L) corresponds to 31.39mg of C17H27N02 • HCL.
Last Update：2022-01-01 14:20:42
AKOS 92111 - Category
Authoritative Data Verified Data
antidepressants.
Last Update：2022-01-01 14:20:42
AKOS 92111 - Storage
Authoritative Data Verified Data
sealed and stored in a dry place.
Last Update：2022-01-01 14:20:43
AKOS 92111 - Venlafaxine hydrochloride capsules
Authoritative Data Verified Data
This product contains venlafaxine hydrochloride (C17H27N02 • HCl) should be 90.0% to 110.0% of the label children.
trait
The content of this product is white powder.
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 control solution.
- take an appropriate amount of the contents of this product, add water to dissolve and dilute to a solution containing about 20ug venlafaxine hydrochloride per 1 ml, filter, and measure the filtrate by UV-Vis spectrophotometry (General rule 0401), there is an absorption maximum at a wavelength of 225Nm.
- take an appropriate amount of the contents of this product, add water to dissolve, filter, filtrate chloride identification (1) of the reaction (General 0301).
examination
- relevant substances: take an appropriate amount of fine powder of this product, dissolve it with mobile phase, dilute it to a solution containing about 1 mg venlafaxine hydrochloride per 1ml, filter it, and take the continued filtrate as the test solution; take 1ml of precision, 100ml flask, diluted with mobile phase to scale, shake, as a control solution. 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%).
- the dissolution of this product, according to the dissolution and release determination method (General rule 0931 first method), water 900ml as the dissolution medium, the speed of 75 rpm, according to the law, after 30 minutes, take the solution, filter, take the continued filtrate as the test solution (25mg specification), or take the appropriate amount of the continued filtrate, quantitatively dilute with water to make a solution containing 28ug of venlafaxine hydrochloride per 1 ml as a test solution (50mg specification); Take an appropriate amount of reference substance of venlafaxine hydrochloride, water was added to dissolve and quantitatively diluted to prepare a solution containing about 28ug per 1 ml as a control solution. Take 10 u1 of each of the reference solution and the test solution, and inject the liquid chromatograph. According to the method under the content determination item, the determination is carried out according to law. According to the external standard method, the dissolution amount of each particle was calculated by the peak area. The limit is 70% of the labeled amount and shall be in accordance with the provisions.
- 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 octanosilane bonded silica gel as filler; Acetonitrile-O. 1 mol/L potassium dihydrogen phosphate solution (25:75) is the mobile phase; The detection wavelength is 225nm; The number of theoretical plates is not less than 20000 based on the peak of venlafaxine .
- determine the contents under the item of loading difference, mix evenly, accurately weigh appropriate amount (about 5mg equivalent to venlafaxine hydrochloride), put it in a 50ml measuring flask, and add appropriate amount of mobile phase, shake to dissolve venlafaxine hydrochloride, dilute to the scale with mobile phase, shake, filter, take the filtrate as the test solution, and inject 10u1 into the liquid chromatograph to record the chromatogram; in addition, an appropriate amount of venlafaxine hydrochloride reference substance was accurately weighed, dissolved and quantitatively diluted with mobile phase to make about O in 1 ml. lmg solution, the same method for determination. According to the external standard method to calculate the peak area, that is.
category
Same as venlafaxine hydrochloride.
specification
(l)25mg (2)50mg
storage
sealed and stored in a dry place.
Last Update：2022-01-01 14:20:44
AKOS 92111 - Venlafaxine hydrochloride sustained-release tablets
Authoritative Data Verified Data
This product contains venlafaxine hydrochloride (C17H27N02 • HCI) should be the label amount of 90.0% ~ 110.0%.
trait
This product is a film-coated tablet, white or off-white after removal of 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 control solution.
examination
- appropriate amount of fine powder under the content determination item of related substances is taken, dissolved and diluted with mobile phase to prepare a solution containing about 1 mg venlafaxine hydrochloride per 1 ml, filtered, and the continued filtrate is taken as the test solution; take 1 ml accurately, put it in a 100ml measuring flask, dilute it to the scale with mobile phase, shake it well, and use it as a control solution. 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%).
- the dissolution of this product, according to the dissolution and release determination method (General rule 0931 second method), water 500ml as the dissolution medium, the speed of 50 rpm, according to the law, after 1 hour, 4 hours, 6 hours, 8 hours, 12 hours, respectively, take the solution 10ml, and immediately add the same temperature, the same volume of dissolution medium, filtered, take the filtrate, according to UV-Vis spectrophotometry (General rule 0401), the absorbance was measured at 274nm wavelength respectively; The appropriate amount of venlafaxine hydrochloride was accurately weighed, water was added to dissolve and quantitatively diluted to prepare a solution containing about 100ug(75mg specification) or 50ug( 37.5mg specification) per 1 ml, which was determined by the same method. The dissolution amount of each tablet at different times was calculated separately. The dissolution amount of each tablet in 2 hours, 4 hours, 6 hours, 8 hours and 12 hours should be less than 25%, 25% to 50%, 40% to 65%, respectively, 55% to 80% and more than 75%, shall comply 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 octanosilane bonded silica gel as filler; Acetonitrile -0. The mobile phase was 1 mol/ L potassium dihydrogen phosphate solution (25:75); The detection wavelength was 225nm; The number of theoretical plates was not less than 2000 according to the peak of venlafaxine hydrochloride.
- determination of 20 tablets of this product, remove the coating, precision weighing, fine grinding, precision weighing fine powder (about 5mg equivalent to venlafaxine hydrochloride), put in 50ml measuring flask, add the appropriate amount of mobile phase, shake to dissolve venlafaxine hydrochloride, dilute to scale with mobile phase, shake well, filter, take filtrate as test solution, take 10u1 injection of human liquid chromatograph with precision, record chromatogram; in addition, an appropriate amount of venlafaxine hydrochloride reference substance was accurately weighed, dissolved and quantitatively diluted with mobile phase to make about 0 per 1 ml. lmg solution, the same method for determination. According to the external standard method to calculate the peak area, that is.
category
Same as venlafaxine hydrochloride.
specification
(1)37.5mg (2)75mg
storage
sealed and stored in a dry place.
Last Update：2022-01-01 14:20:44
AKOS 92111 - Reference Information
| EPA chemical substance information | information provided by: ofmpeb.epa.gov (external link) |
| Introduction | venlafaxine is a serotonin and norepinephrine reuptake inhibitor (SNRI) class of antidepressants. The drug is approved for the treatment of major depressive disorder (MDD), generalized Anxiety disorder (GAD) and concomitant Anxiety depression. It is commonly used in its hydrochloride salt form, namely venlafaxine hydrochloride. |
| clinical effect | venlafaxine, as a novel antidepressant, is clinically effective in the treatment of depression and anxiety spectrum disorders, and chronic pain, has been widely used in depression, anxiety, obsessive-compulsive disorder, ADHD, alcohol dependence, somatoform disorders, schizophrenia, adult panic disorder after depression, sexual dysfunction and so on. The drug is safe and effective in the treatment of depression, and the compliance of patients is good, which is beneficial to the long-term maintenance treatment of patients with depression. Although a small number of patients can occur Sleep Initiation and Maintenance Disorders, but the addition of small doses of sedative hypnotics, generally can be significantly improved. Compared with other antidepressants, the drug has obvious advantages, especially for the more severe depression and Anxiety symptoms, and has a better effect, and has a faster effect, has become the first-line drug for the treatment of depression. |
| adverse reactions | venlafaxine has little affinity for adrenergic, M1 cholinergic and histamine H1 receptors, thus, the adverse reactions caused by similar tricyclic antidepressants (TCAs) are avoided, and there are almost no adverse reactions such as anticholinergic, orthostatic hypotension and sedation. However, about Nausea of the response occurs in l/3 users, especially in the first few weeks. An analysis of 3000 cases collected in a database showed that dizziness, Head Pain, sleep disturbances, dry mouth and nervousness were also common, with incidences of Nausea and 17% respectively, somnolence 15%, Sleep Initiation and Maintenance Disorders 10%, dry mouth 12%, the clinical manifestations of adverse reactions are mostly mild, moderate, patients can tolerate. The adverse reactions occurred in the treatment of 2 weeks, and drug dose, with the extension of treatment time, adverse reactions gradually reduced. Sudden withdrawal of visible withdrawal syndrome such as Sleep Initiation and Maintenance Disorders, Anxiety, Nausea, sweating, tremor, dizziness or paresthesia, etc., 1 weeks after the withdrawal of visible symptoms disappeared. |
| pharmacokinetics | venlafaxine is mainly absorbed from the gastrointestinal tract after oral administration, and the absorption is rapid and good. A single oral dose can be absorbed by 92%, and the oral bioavailability is 40% ~ 45%, suggesting that venlafaxine has a significant first-pass effect after oral administration. In the body mainly through the liver cytochrome P450 enzyme metabolism, the original drug and its metabolite O-Desmethylvenlafaxine mainly through the kidney excretion, about 92% by the urine, 1.9% by the feces. The apparent elimination half-lives of venlafaxine and O-desmethyl-venlafaxine were 5±2 and 11±2h, and the apparent volumes of distribution were 7.5±3.7 and 5.7±1.8L/kg, respectively. The steady-state blood drug concentration can be reached within 3d after multiple administration. Eating does not affect the absorption of the drug. The binding rates of venlafaxine and O-Desmethylvenlafaxine to plasma proteins were small, 27% and 30%, respectively. In the creatinine clearance rate <30mL/min in patients with kidney disease, the use of this product should be noted to adjust the dose of moderate renal insufficiency, the dose should be reduced by 50%; Mild to moderate renal insufficiency, the dose should be reduced by 25%. It is also necessary to reduce the dose or to carry out individualized dose administration in patients with hepatic impairment. |
| biological activity | Venlafaxine HCl is a serotonin-norepinephrine reuptake inhibitor (SNRI), it is used to treat major depressive disorder, generalized anxiety disorder, acute anxiety disorder and social phobia. |
| Target | Value |
Last Update：2024-04-09 21:32:08
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Product Name: Venlafaxine Hydrochloride Request for quotation
CAS: 99300-78-4
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: 99300-78-4
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
Multiple SpecificationsSpot supply
Product Name: Venlafaxine Hydrochloride Visit Supplier Webpage Request for quotationCAS: 99300-78-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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