What Is Clemastine Fumarate?

Clomustine fumarate is a white or almost white crystalline powder, odorless and slightly bitter. Clemastine Fumarate is a successful antihistamine developed by Sandoz in the 1960s. Since then, it has been launched in the United States, Japan, and Germany. This product is a typical, representative second-generation H1 receptor antagonist. It is clinically used to treat various allergic diseases caused by histamine. It is currently recognized as the best antihistamine in the world. one.

Clomustine fumarate

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Clomustine fumarate is a white or almost white crystalline powder, odorless and slightly bitter. Clemastine Fumarate is a successful antihistamine developed by Sandoz in the 1960s. Since then, it has been launched in the United States, Japan, and Germany. This product is a typical, representative second-generation H1 receptor antagonist. It is clinically used to treat various allergic diseases caused by histamine. It is currently recognized as the best antihistamine in the world. one.

Drug Name

Clomustine fumarate

Alias

Snowpin

Foreign name

Clemastine Fumarate

Whether prescription drugs

Non-prescription drugs

Dosage

One piece at a time

Adverse reactions

No

Whether to include health insurance

Incorporate

Hanyu Pinyin

Fumasuan Lumasiting

Chinese alias (R- (R *, R *))-1-methyl-2- (2- (1- (4-chlorophenyl) -1-phenethoxy) ethyl) -pyrrolidine (E ) -2-butenoate

English alias clemastine hydrogen fumarate; (2R) -2- {2-[(1R) -1- (4-chlorophenyl) -1-phenylethoxy] ethyl} -1-methylpyrrolidine; (2R) -2- {2-[( 1R) -1- (4-chlorophenyl) -1-phenylethoxy] ethyl} -1-methylpyrrolidine (2E) -but-2-enedioate

EINECS 239-055-2

Molecular formula C21H26CLNOC4H4O4

Molecular weight 459.97

This product is slightly soluble in methanol and very slightly soluble in water or chloroform. Specific rotation is taken from this product, accurately weighed, dissolved in methanol and quantitatively diluted to make a solution containing about 10 mg per 1 ml, and measured according to law (Appendix VI E). The specific rotation is + 15 ° to + 18 °.

(1) Take this product, add lukewarm ethanol solution (8 10) to make a solution containing about 20mg per 1ml, as the test solution; take a reference of clomustine fumarate, and make it into each 1ml in the same way It contains about 5 mg of the solution as a reference solution. According to the thin layer chromatography (Appendix V B) test, draw 5 l of each of the two solutions, point them on the same silica gel GF254 thin layer plate, and use isopropyl ether-formic acid-water (70: 25: 5) as the developing agent. Expand, dry, heat at 100 ° C for 30 minutes, remove, let cool, and inspect under UV light (254nm). The main spot of the test solution should be the same as the main spot of the reference solution. (2) The infrared light absorption spectrum of this product should be consistent with the control spectrum (spectrum set 514).

Clarity and color of methanol solution: Take 100mg of this product, add 10.0ml of methanol to dissolve, the solution should be clear and colorless; if it is turbid, compare with control solution (take 0.00002mol / L sodium chloride solution 2.5ml, water 2.5ml, 2.5 5.0ml mol / L nitric acid solution and 1.0ml 0.1mol / L silver nitrate solution, mix well and use within 5 minutes), it must not be more concentrated; if color is developed, compare with colorimetric solution (take 1 volume colorimetric trichloro Ferric solution-copper sulfate solution-cobalt chloride solution-water (6: 1: 1: 42) and 3 volumes of water are mixed uniformly], it must not be deeper.

The acidity is 1.0g of this product, and 10ml of water is added to make a suspension, which is determined according to law (Appendix VI H). The pH value should be 3.2-4.2.

Loss on drying: Take this product and dry to constant weight at 105 ° C. Lose weight should not exceed 0.5% (Appendix L).

Take 1.0g of this product for heavy metal and check it according to law (Appendix H second method). The content of heavy metal must not exceed 20 parts per million. Relevant substances: Take 100mg of this product, add 5.0ml of chloroform-methanol (1: 1) to dissolve, and use it as the test solution; take an appropriate amount of the precise amount, add chloroform-methanol (1: 1) and dilute to 1ml. The solutions of 0.10mg, 0.06mg and 0.02mg were used as control solutions (1), (2) and (3). According to the thin layer chromatography (Appendix V B) test, draw 5 l of each of the above four solutions, point them on the same silica gel G thin layer plate, and expand with chloroform-methanol-concentrated ammonia solution (90: 10: 1). Agent, unfolded, dried at room temperature, sprayed with dilute potassium iodide test solution, and then sprayed with hydrogen peroxide test solution, inspect after color development. If the test solution exhibits impurity spots, compared with the control solution, the total amount of impurities shall not be greater than 1.0%, and any one of the impurity spots shall not be greater than 0.5%.

Take about 0.35g of this product, accurately weigh, add 60ml of glacial acetic acid to dissolve, titrate by potentiometric method (Appendix A), titrate with perchloric acid titrant (0.1mol / L), and use the blank test Correction. Each 1ml of high-acid titrant (0.1mol / L) is equivalent to 46.00mg of C21H26ClNO · C4H404.

test methods

Method name:

Clomustine fumarate-determination of clomustine fumarate-potentiometric titration

Application:

This method uses potentiometric titration to determine the content of clomustine fumarate (C21H26ClNO · C4H4O4).

This method is applicable to the determination of clomustine fumarate.

Method principle:

After the test product was dissolved by shaking with glacial acetic acid, the titration method (Appendix A) was used to titrate with a perchloric acid titrant (0.1 mol / L), and the results of the titration were corrected by a blank test. Each 1mL of perchloric acid titration solution (0.1mol / L) is equivalent to 46.00mg of C21H26ClNO · C4H4O4.

Reagent:

1. Water (newly boiled to room temperature)

Glacial acetic acid

3. Perchloric acid titrant (0.1mol / L)

4. Reference potassium hydrogen phthalate

5. Anhydrous glacial acetic acid

6. Crystal violet indicator liquid

equipment:

Sample preparation:

1. Perchloric acid titrant (0.1mol / L)

Preparation: Take 750mL of anhydrous glacial acetic acid (calculated with water content, add 5.22mL of acetic anhydride per 1g of water), add 8.5mL of perchloric acid (70 ~ 72%), shake well, let cool, add an appropriate amount of anhydrous glacial acetic acid 1000mL, shake well and leave for 24 hours. If the test sample is easily acetylated, the water content of the solution must be determined by the moisture measurement method, and then the water content of the solution is adjusted to 0.01% ~ 0.2% with water and acetic anhydride.

Calibration: Take about 0.16g of standard potassium hydrogen phthalate dried to constant weight at 105 , accurately weigh, add 20mL of anhydrous glacial acetic acid to dissolve, add 1 drop of crystal violet indicator solution, and slowly titrate with this solution to Blue, and the titration results are corrected with a blank test. Each 1mL of perchloric acid titration solution (0.1mol / L) is equivalent to 20.42mg of potassium hydrogen phthalate. Calculate the concentration of this solution based on the consumption of this solution and the amount of potassium hydrogen phthalate taken.

Crystal violet indicator liquid

Take 0.5 g of crystal violet and add 100 mL of glacial acetic acid to dissolve.

Storage: Place in a brown glass bottle and keep tightly closed.

Steps:

Take about 0.35g of this product, accurately weigh, add 60mL of glacial acetic acid to dissolve, titrate by potentiometric method (Appendix A), titrate with perchloric acid titrant (0.1mol / L), and use the blank test Correction. Each 1mL of perchloric acid titration solution (0.1mol / L) is equivalent to 46.00mg of C21H26ClNO · C4H4O4.

Note 1: "Precision weighing" means that the weighed weight should be accurate to one thousandth of the weight. Precision requirements.

Note 2: "Determination of moisture" uses the drying method, taking 2 to 5 g of the test sample, and spreading it in a flat weighing bottle that is dry to constant weight, the thickness does not exceed 5 mm, and the loose test sample does not exceed 10 mm. Open the bottle cap and dry at 100 ~ 105 ° C for 5 hours. Place the cap on the dryer, cool it for 30 minutes, and weigh it precisely. Then dry it at the above temperature for 1 hour, cool, and weigh until two times in a row. The difference in weighing does not exceed 5 mg. Calculate the moisture content (%) in the test product based on the weight lost. ^[1]

Shaded and sealed.

Western medicine (including chemical drugs, biochemical drugs, antibiotics, radiopharmaceuticals, pharmaceutical excipients))

This product is [R- (R *, R *)]-1-methylpicroline-2- [2- [1- (4-chlorophenyl) -1-phenethoxy] ethyl] -pyrrolidine ( E) -2-Butenedioate. Calculated based on dry products, C21H26ClNO · C4H4O4 should be 98.0% -102.0%.

Antihistamine

Mastin fumarate tablets are the first four new drugs developed by Shandong Institute of Pharmaceutical Industry in China, and have obtained a new drug certificate. At the same time, they have received three years of administrative protection.

After more than 40 years of clinical practice summary abroad and domestic clinical verification, clomustine fumarate is a fast-acting, long-acting, highly effective, safe and reliable antihistamine. The pharmacokinetics of clomustine fumarate tablets show that the product is absorbed quickly after oral administration, and takes effect after 30 minutes, and quickly relieves the symptoms. After 1 hour, the blood concentration reaches the highest value, and it is similar to similar antihistamines such as zismin and chlorine. In contrast to Lei He, this product is the fastest. Its antihistamine effect lasts for 12 hours, its antihistamine effect is 10 times stronger than that of chlorpheniramine, and its side effects (central effects) of sleepiness are slight. The total effective rate for treating allergic rhinitis is 98%, and the cure rate for chronic urticaria is 61.3%. Clomustine not only has an anti-histochemical effect on histamine released by basophils and lung tissues, but also has a certain anti-cytotoxic effect on cytotoxins at high concentrations. It is mainly used clinically for allergic rhinitis, urticaria, eczema and other allergic dermatitis.