76494-51-4
Ligustrazine hydrochloride
CAS: 76494-51-4
Molecular Formula: C8H12N2.ClH
76494-51-4 - Names and Identifiers
| Name | Ligustrazine hydrochloride |
| Synonyms | Tetrapyrazine HCl Tetramethylpyrazine HCl LigustrazineHydrochloride Ligustrazine hydrochloride LIGUSTRAZOINEHYDROCHLORIDE Ligustrazine Hydrochloride Chuanxiongzine Hydrochlorid Pyrazine, tetramethyl-, hydrochloride 2,3,5,6-tetramethylpyraine hydrochloride 2,3,5,6-Tetramethylpyrazine hydrochloride Chuanxiongzine Hydrochloride, TetraMethylpyrazine hydrochloride |
| CAS | 76494-51-4 |
| EINECS | 1592732-453-0 |
| InChI | InChI=1/C8H12N2.ClH/c1-5-6(2)10-8(4)7(3)9-5;/h1-4H3;1H |
76494-51-4 - Physico-chemical Properties
| Molecular Formula | C8H12N2.ClH |
| Molar Mass | 172.658 |
| Boling Point | 192.7°C at 760 mmHg |
| Flash Point | 71.6°C |
| Solubility | DMSO : ≥ 300 mg/mL |
| Vapor Presure | 0.671mmHg at 25°C |
| Appearance | White crystalline powder |
| Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
| Sensitive | Easily absorbing moisture |
| MDL | MFCD01109103 |
| Physical and Chemical Properties | White crystalline powder, soluble in methanol, ethanol, DMSO and other organic solvents, derived from the dry root of Ligusticum chuanxiong. |
| Use | With anti-platelet coagulation, expansion of small arteries, for the treatment of occlusive cerebrovascular disease |
76494-51-4 - Reference
| Reference Show more | 1. Liu zejuan Wu Yue Jiang Xuehua Liu Xiaojuan Wang LingZhang Rongyang Li. Effect of Danshen Chuanxiongqin Zhusheye danshensu on the pharmacokinetics of ligustrazine hydrochloride in rats [J]. West China Journal of Pharmacy, 2017, 32(02):182-185. 2. Yuan Rong, Chen Min, Xin Qi, etc. Effect of ligustrazine on angiogenesis in atherosclerotic mice [J]. Chinese Journal of Traditional Chinese Medicine, 2019, 034(005):2250-2254. 3. Hao Jing, Wang Xiaoning, Yan Mengru, et al. Optimization of formulation and in vitro release behavior of ligustrazine hydrochloride nasal gel by Central composite design-response surface methodology [J]. Chemistry and bonding, 2020, v.42;No.189(01):17-19 39. 4. [IF = 3] Qu Lala et al."Phenotypic assessment and ligand screening of ETA/ETB receptors with label-free dynamic mass redistribution assay." N-S. 2020 Jun;393(6):937-950 |
76494-51-4 - Standard
Authoritative Data Verified Data
This product is 2,3,5, 6-tetramethylpyrazine hydrochloride dihydrate. The content of C8H12N2 • HC1 shall not be less than 99.0% calculated as anhydrous.
Last Update：2024-01-02 23:10:35
76494-51-4 - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline powder.
- This product is soluble in water, dissolved in ethanol and chloroform.
melting point
take this product, without drying, according to the determination (General 0612), the melting point is 86.5~90°C.
Last Update：2022-01-01 14:20:32
76494-51-4 - Differential diagnosis
Authoritative Data Verified Data
- take about 10mg of this product, add 5ml of water to dissolve, and add 2 drops of bismuth potassium chloride solution to generate orange-red precipitate.
- take this product, add water to make a solution containing about 12ug per 1 ml, according to ultraviolet-visible spectrophotometry (General 0401), there is a maximum absorption at the wavelength of 295nm.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 1098).
- the aqueous solution of this product can identify the reaction of (1) (General rule 0301).
Last Update：2022-01-01 14:20:33
76494-51-4 - Exam
Authoritative Data Verified Data
chloride
take 0.15g of this product, precision weighing, add 25ml of water to dissolve, add 5 drops of bromophenol blue indicator solution, and use silver nitrate titration solution (0.1 mol/L) titration, to the solution gray purple. Each 1 ml of silver nitrate titration solution (0.1 mol/L) is equivalent to 3.545mg of C1, containing chloride should be 16.5% ~ 17.5%.
Related substances
take an appropriate amount of this product, add water to dissolve and dilute to make a solution containing 0.5mg per lml as a test solution; Take 1ml for precision measurement and put it in a 200ml measuring flask, water was added to dilute to the scale, shake, as a control solution. According to the high performance liquid chromatography (General rule 0512) test, silica gel bonded with eighteen alkyl silane was used as the filler, methanol-water (45:55) was used as the mobile phase, and the detection wavelength was 295nm. Take 2mg of ligustrazine hydrochloride and 12mg of dimethyl phthalate (impurity I) respectively, put them in a-100ml measuring flask, add 2ml of methanol to dissolve, dilute with water to the scale, shake well, and inject 20u1 into the liquid chromatograph, record the chromatogram, the number of theoretical plate according to the calculation of ligustrazine peak is not less than 2000, the separation degree of ligustrazine peak and impurity I peak should be greater than 4.0. 20 u1 of the test solution and the control solution were respectively injected into the human liquid chromatograph, and the chromatogram was 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 sum of each impurity peak area shall not be greater than the main peak area of the control solution (0.5%).
residual solvent
take about 0.5g of this product, weigh it accurately, place it in the top empty bottle, add 5ml of water accurately to dissolve it, seal it, and use it as a test solution. Take about 50mg of acetone, weigh it accurately, put it in a 100ml measuring flask, dilute it to scale with water, shake it well, take 5ml of acetone and place it in the top empty bottle, seal it, as a reference solution ^ According to the determination of residual solvent (General 0861 second method), the capillary column with polyethylene glycol as stationary liquid is used as the chromatographic column; The starting temperature is 50°C, and the maintenance time is 5 minutes, the temperature was then increased to 180°C at a rate of 50°C per minute for 2 minutes; The inlet temperature was 200°C; And the detector temperature was 250°C. The Headspace bottle had an equilibration temperature of 80°C and an equilibration time of 30 minutes. The number of theoretical plates shall not be less than 1000 based on the acetone peak. The test solution and the reference solution were sampled by Headspace injection, and the chromatograms were recorded. According to the external standard method to calculate the peak area, the residual amount of acetone should comply with the provisions.
moisture
take this product, according to the moisture determination method (General 0832 first method 1), the moisture should be 16.5% ~ 18.5%.
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 14:20:34
76494-51-4 - Content determination
Authoritative Data Verified Data
take this product about 0.15g, precision weighing, add acetic anhydride 40ml, according to the potential titration method (General 0701), with perchloric acid titration solution (0.1 mol/L) titration and titration results were corrected with a blank test. Each 1 ml of perchloric acid titration solution (0.1 mol/L) corresponds to 17.27mg of C8H12N2-HCL.
Last Update：2022-01-01 14:20:34
76494-51-4 - Category
Authoritative Data Verified Data
vasodilators.
Last Update：2022-01-01 14:20:35
76494-51-4 - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 14:20:35
76494-51-4 - Ligustrazine hydrochloride injection
Authoritative Data Verified Data
This product is a sterile aqueous solution of ligustrazine hydrochloride. The content of ligustrazine hydrochloride (C8H12N2 • HCI • 2H20) shall be between 90.0% and 110.0% of the labeled amount.
trait
This product is a clear colorless liquid.
identification
- take about 10ml of this product and add 2 drops of bismuth potassium iodide solution to generate orange-red precipitate.
- take this product and dilute with water to make a solution containing about 0401 mg of ligustrazine hydrochloride in each lml, and measure it by UV-visible spectrophotometry (general rule), there is a maximum absorption at a wavelength of 295nm.
- This product chloride identification (1) of the reaction (General 0301).
examination
- the pH value should be 2.0 to 3.0 (General 0631).
- Related substances take this product and dilute it with water to make a solution containing 0.5m g of ligustrazine hydrochloride per 1ml as a test solution; Take 1ml for precision measurement and put it in a 200ml measuring flask, as a control solution, it was diluted to the scale with water and shaken. According to the chromatographic condition test under the content determination item, 20 u1 of the test solution and the control solution are respectively injected into the liquid chromatograph, 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 sum of each impurity peak area shall not be greater than the main peak area of the control solution (0.5%).
- bacterial endotoxin this product, according to the law to check (General 1143), each 1 mg of ligustrazine hydrochloride containing endotoxin should be less than 3.75EU.
- 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; Methanol-water (45:55) as mobile phase; The detection wavelength was 295nm. Weigh 2mg of ligustrazine hydrochloride and 12mg of reference product of impurity I respectively, put them in the same 100ml measuring flask, add 2ml of methanol to dissolve, dilute with water to scale, shake well, and inject 20u1 into human liquid chromatograph, record the chromatogram, the separation degree of ligustrazine peak and impurity I peak should be greater than 4.0, and the number of theoretical plates should not be less than 2000 according to the calculation of ligustrazine peak.
- precision measurement: take an appropriate amount of this product (about 10 mg of ligustrazine hydrochloride), put it in a 100ml measuring flask, dilute it with water until it is calibrated, shake well, and inject 20ul into the liquid chromatograph, record the chromatogram; Accurately weigh appropriate amount of ligustrazine hydrochloride reference substance, add water to dissolve and quantitatively dilute to make 0 in each lml. lmg solution, the same method for determination. According to the external standard method to calculate the peak area, that is.
category
with ligustrazine hydrochloride.
specification
(l)2ml:40mg (2)10ml:40mg
storage
shade, close, and store in a cool place.
Last Update：2022-01-01 14:20:36
76494-51-4 - Reference Information
| introduction | ligustrazine hydrochloride, its function is to inhibit platelet aggregation and prevent thrombosis. At the same time, it can resist vascular damage caused by serotonin and bradykinin, increase capillary resistance, reduce capillary permeability, and prevent edema caused by increased vascular permeability. Clinically, it is mainly used for occlusion syndrome, thrombophlebitis, capillary bleeding, etc. The market demand for this product is large. |
| clinical application | ligustrazine hydrochloride can be used to treat cerebral insufficiency, cerebral thrombosis, cerebral embolism and other ischemic vascular diseases, such as coronary atherosclerotic heart disease, vasculitis, etc. When the patient is in the acute phase of the disease, intravenous drip is usually used. |
| usage and dosage | intravenous drip of acute ischemic cerebrovascular disease and other ischemic vascular diseases, intravenous drip is generally used. With this product injection 40~80mg(1~2), diluted in 5% glucose injection or sodium chloride injection 250~500ml intravenous drip. The speed should not be too fast, once a day, 10 days as a course of treatment, generally use 1~2 courses. Acupoint injection of ischemic cerebrovascular disease convalescence and sequelae general acupoint injection. Choose 3-4 acupoints each time, inject 10-20mg(1/4-1/2) into each acupoint, once every other day, 15 times as a course of treatment, generally use 1-2 courses of treatment, in the interval day of administration Can be combined with scalp acupuncture treatment. |
| incompatibility | ligustrazine hydrochloride for injection has incompatibility with ceftriaxone sodium, azlocillin sodium, fusidate sodium, cefoperazone sodium, salvia miltiorrhiza injection, qingkailing, yanhuning, methylprednisolone sodium succinate, pantoprazole sodium and other drugs. The reason is that ligustrazine is acidic, and when used in combination with other drugs (especially alkaline drugs), it is easy to produce turbidity or precipitation due to pH changes. Therefore, when multiple drugs must be used in combination in clinical practice, when there is no sufficient evidence to prove that they can be used at the same time, they should be injected intravenously alone, and 0.9% sodium chloride injection or 5% glucose injection should be used between the two drugs. After the drug in the original infusion tube is washed, the second liquid medicine is changed to avoid turbidity or precipitation caused by direct contact between the two drugs, and reduce adverse drug reactions caused by improper use of the drug. |
| adverse reactions & taboos | this product is acidic and irritating by acupoint injection. Patients with cerebral hemorrhage and bleeding tendency should not be used, and those who are allergic to this product should not be used. |
| precautions | is not suitable for intramuscular injection. The speed of intravenous drip should not be too fast. Children and elderly patients should be used according to children and elderly doses. |
| chemical properties | white crystalline powder, soluble in methanol, ethanol, DMSO and other organic solvents, derived from dried roots of Ligusticum wallichii. |
| use | used for content determination/identification/pharmacological experiments, etc. Pharmacological effects: suitable for occlusive vascular disease, cerebral thrombosis, vasculitis, coronary heart disease, angina pectoris, etc. It has a good effect on the acute phase, recovery phase and sequelae of ischemic cerebrovascular disease, such as insufficient blood supply to the brain, cerebral thrombosis, cerebral embolism, cerebral arteriosclerosis, etc., and can improve hemiplegia and aphasia caused by these diseases, Dysphagia, numbness, weakness, headache, dizziness, insomnia, tinnitus, unstable walking, memory loss and other symptoms. anti-platelet coagulation, expansion of small arteries, treatment of occlusive cerebrovascular disease. |
Last Update：2024-04-09 15:16:35
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