vinblastine sulfate

Chemical name: Vinblastine sulfate. Molecular weight: 909.06. This product is a white or off-white loose or amorphous solid, which is hygroscopic and will turn yellow when exposed to light or heat.

On October 27, 2017, the list of carcinogens published by the International Agency for Research on Cancer of the World Health Organization was preliminarily compiled for reference. Vinblastine sulfate is in the list of three carcinogens (the carcinogenicity of humans has not yet been classified [1] ). [2]

CAS No. 143-67-9

Structural formula

EINECS: 205-606-0 [3]

Molecular formula C46H58N4O9·H2SO4

Molecular weight 909.06

Specification 10mg

Melting point: 267°C

Specific optical rotation: -21.7°(c=2, CH3OH 21°C)

Water solubility:>=1 g/100 mL at 24.5℃

Content: 99%

Packing: 25kg cardboard drum

Properties: White or almost white crystalline powder, odorless, hygroscopic, turns yellow when exposed to light or heat, and is easily soluble in water.

Uses: Anti-tumor drugs, used in the treatment of Hodgkin's disease and choriocarcinoma, and also have a certain effect on lymphosarcoma, acute leukemia, breast cancer, etc.

Drug Analysis Editor Voice

Method name: Vinblastine sulfate-Determination of vinblastine sulfate-spectrophotometric method

Scope of application: This method uses spectrophotometry to determine the content of vinblastine sulfate.

This method is suitable for the determination of vinblastine sulfate.

Method principle: Precisely weigh this product into a measuring bottle. After adding water to dissolve, add absolute ethanol to the mark while shaking. Shake well, accurately measure an appropriate amount and place an absolute ethanol in another measuring bottle. Ultraviolet-visible spectrophotometry, at the wavelength of 264nm, respectively measure the absorbance, and calculate according to the absorption coefficient (E1 m) of 179, which is obtained.

Reagent: absolute ethanol

Equipment: Visible spectrophotometer

Sample preparation: 1. Preparation of test solution

Accurately weigh about 5mg of this product, accurately weigh it, and place it in a 50mL measuring bottle. After adding 5mL of water to dissolve it, add absolute ethanol to the mark while shaking. Shake well, accurately measure 10mL, and place it in another 50mL measuring bottle. , And then add absolute ethanol to dilute to the mark, shake well, as the test solution.

Note: "Precision weighing" means that the weighing should be accurate to one thousandth of the weighed weight. "Precision measuring" means that the accuracy of measuring the volume should meet the accuracy requirements of the volume pipette in the national standard.

Note: Drying method is used for "moisture determination". Take 2-5g of the test product, spread it flat in a flat weighing bottle that is dry to constant weight, with a thickness of no more than 5mm, and a loose sample no more than 10mm, accurately weighed, open the bottle cap and dry at 100-105°C for 5 hours. Cap the bottle, move it to a desiccator, cool for 30 minutes, accurately weigh it, and then dry at the above temperature for 1 hour, cool, and weigh until the difference between two consecutive weighings does not exceed 5 mg. According to the lost weight, calculate the percentage of water contained in the test product.

Operation steps: 1. Determination of the test product

Take the above-mentioned test product solution, according to ultraviolet-visible spectrophotometry, at 264nm wavelength, measure the absorbance according to law, and calculate the content of each bottle according to the absorption coefficient (E1 m) of 179.

References: Pharmacopoeia of the People's Republic of China, edited by the National Pharmacopoeia Commission, Chemical Industry Press, 2005 edition, Part Two, p.722.

Drug properties editing voice

Drug name

Vinblastine Sulfate [base]

Drug alias

Vinblastine

Formulation specifications

Powder injection: 10mg.

Pharmacology and Toxicology

Vinblastine is an alkaloid with anticancer activity extracted from Catharanthus roseus. Mainly inhibit the polymerization of tubulin, and hinder the formation of spindle microtubules, so that mitosis stops in the metaphase. It can also act on the cell membrane, interfere with the transport of amino acids in the cell membrane, inhibit protein synthesis, and inhibit RNA synthesis. Vinblastine has a broad anti-tumor spectrum. It has obvious anti-tumor activity against mouse L1210 leukemia, Ehrlich ascites carcinoma, S180, C3H mouse spontaneous and metastatic breast cancer, etc. at a dose of 0.05 to 0.1 mg/kg. The growth of choriocarcinoma cells in the hamster cheek pouch also has an inhibitory effect.

Pharmacokinetics

Oral absorption is poor, and intravenous administration is required. After intravenous injection of vinblastine, it quickly distributes in various tissues, rarely penetrates the blood-brain barrier, and the protein binding rate is 75%. The blood removes the drug in a two-way type, with t1/2α for 4.5 minutes, t1/2β for 190 minutes, and peripheral elimination phase t1/2γ for about 24 hours. It is metabolized in the liver, and most of it is excreted in bile, and 33% is excreted in feces within 3 days after medication, of which mainly metabolites, 21% is excreted in urine as a prototype.

Adaptation certificate

Mainly used for the treatment of solid tumors. It has good curative effect on malignant lymphoma, testicular tumor and choriocarcinoma. It also has certain curative effect on lung cancer, breast cancer, ovarian cancer, skin cancer, Wilms tumor and monocytic leukemia.

Hodgkin's disease and malignant lymphoma can also be used to treat chorioepithelial carcinoma and breast cancer.

Adverse reactions

1. Hematological toxicity: It is a dose-limiting toxicity. The bone marrow suppression effect is stronger than that of vincristine, and it recovers quickly after stopping the drug.

2. Gastrointestinal reactions: decreased appetite, nausea, vomiting, diarrhea, abdominal pain, stomatitis, etc.

3. Peripheral nerve toxicity: numbness of the finger (toe) tip, pain in the limbs, muscle tremor, loss of tendon reflexes, etc.

4. Local irritation: Thrombophlebitis can occur in the injected blood vessel, and leakage outside the blood vessel can cause local tissue necrosis.

5. Others: A small number of patients may have orthostatic hypotension, hair loss, insomnia, headaches, etc.

interaction

If there are other white blood cell lowering drugs in the combined chemotherapy regimen, the dose should be reduced. When the liver is insufficiency, if other anticancer drugs excreted by bile (such as doxorubicin) are used together, the dose should be reduced. Combined with allopurinol, colchicine or probenecid, vinblastine can increase blood uric acid concentration.

Dosage

Intravenous injection, adult 10mg (or 6mg/m2)/time, dissolved in normal saline, once/week, a total of 60mg～80mg (or 10mg/m2) for a course of treatment. Children are 0.1mg～0.15mg/kg each time according to their body weight, once a week.

Precautions

Pregnancy category D, it is forbidden for pregnant women and breastfeeding women. Patients with bone marrow suppression, a history of gout, liver damage, infection, tumor has invaded the bone marrow, a history of urate kidney stones, and patients who have undergone radiotherapy or anticancer drug therapy should be used with caution. During intravenous injection, the liquid leaks to the outside of the blood vessel, and the injection should be stopped immediately and sealed locally. After skin ulcer occurs, treat it as an ulcer. It cannot be injected intramuscularly, subcutaneously or intrathecally.

2010 edition of the Chinese Pharmacopoeia revised and updated content editing Voice

Vinblastine Sulfate

Liusuan Changchunjian

Vinblastine Sulfate

Page Number: 2005 Edition Two-722

[Revision]

[Check] Acidity Take 15mg of this product, add 10ml of water to dissolve it, and measure it according to the law (Appendix VI H). The pH should be 3.5～5.0.

The clarity and color of the solution: Take 50mg of this product and add 10ml of water to dissolve. The solution should be clear and colorless. If the color develops, it should not be deeper than the yellow standard colorimetric solution No. 1 (Appendix ⅨA Method 1).

Take an appropriate amount of this product, dissolve it with water and dilute it to make a solution containing 0.4mg per 1ml, as the test solution (1); accurately measure 1ml into a 25ml measuring flask, dilute to the mark with water, shake well, as Test solution (2). Separately take appropriate amounts of vinblastine sulfate and vincristine sulfate, dissolve and dilute with water to prepare a mixed solution containing 0.4 mg per 1 ml, as a system suitability test solution. According to high performance liquid chromatography (Appendix V D) determination. Use octadecylsilane bonded silica gel (particle size 5μm) as filler; detection wavelength 262nm; use diethylamine solution (take 14ml diethylamine, add 986ml water, mix well, adjust pH 7.5 with phosphoric acid)-200ml acetonitrile and A mixture of 800ml methanol (32:68) is the mobile phase; the column temperature is 30°C. Measure 200μl each of the system suitability test solution and the test solution (1) and (2) into the liquid chromatograph, and record the chromatogram until the retention time of the main peak is 3 times. In the chromatogram recorded by the system suitability test solution, the resolution of the vinblastine sulfate peak and the peak of vincristine sulfate should be greater than 4.0; in the chromatogram recorded by the test solution, measure the peak area and calculate according to the following formula.

(1) A single impurity shall not exceed 1.0%.

(2) The total amount of impurities shall not exceed 3.0%.

In the formula: ri is the peak area of a single impurity in the test solution (1) except for the solvent peak;

rt is the sum of impurity peak areas in the test solution (1) except for the solvent peak;

rv is the peak area of the vinblastine sulfate peak in the test solution (2). [4]

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