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 |
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 |
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 |
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.
take this product, without drying, according to the determination (General 0612), the melting point is 86.5~90°C.
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%.
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%).
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.
take this product, according to the moisture determination method (General 0832 first method 1), the moisture should be 16.5% ~ 18.5%.
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
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).
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.
vasodilators.
light shielding, sealed storage.
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.
This product is a clear colorless liquid.
with ligustrazine hydrochloride.
(l)2ml:40mg (2)10ml:40mg
shade, close, and store in a cool place.
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. |