What Is Artesunate?

Artesunate is a class of antimalarial drugs that control the symptoms of malaria.

Artesunate

Artesunate is a class of antimalarial drugs that control the symptoms of malaria.

Chinese name

Artesunate

Foreign name

Artesunate

Molecular formula

C19H28O8

Different name

Artesunate

CAS number:

88495-63-0

Artesunate

Pharmacodynamics

The mechanism of action is the same as that of berberine.

Pharmacokinetics

After intravenous injection, the blood concentration decreased quickly, and T1 / 2 was about 30 minutes. Widely distributed in the body, higher intestine, liver, kidney. It is mainly metabolized in the body. Only a small amount is excreted by urine and feces.

It is suitable for the rescue of cerebral malaria and various critical malaria.

1. The first oral dose of 100mg, 50mg twice a day, for 5 days.

2. Before the intravenous injection, add the attached 5%

Animal tests have shown significant embryo toxicity and should be used with caution in pregnant women.

This product should be injected in time after dissolution, if cloudy, it can not be used; For extremely severe patients, the first dose can be doubled; After malaria control, other should be used

No adverse effects were observed at the recommended dose. If used in excess (greater than 2.75 mg / kg), a transient reduction in peripheral reticulocytes may occur.

The excessive use (greater than 2.75 mg / kg) may cause a transient decrease in peripheral reticulocytes.

Artesunate

Qinghaohuzhi

Artesunate

C19H28O8 384.43

This product is dihydroartemisinin-10--succinate monoester. Calculated as anhydrous, C19H28O8 should be 98.0% to 102.0%.

[Properties] This product is a white crystalline powder; odorless and almost tasteless.

This product is easily soluble in ethanol, acetone or chloroform, and very slightly soluble in water.

Melting point The melting point of this product (Appendix VI C) is 131 to 136 ° C (oral) or 132 to 137 ° C (for injection).

The specific rotation is taken from this product, accurately weighed, dissolved in dichloromethane and quantitatively diluted to make a solution containing 25mg per 1ml, and determined according to law (Appendix VI E). The specific rotation is + 4.5 ° to + 6.5 °.

[Identification] (1) Take about 50mg of this product, add 1ml of chloroform to dissolve, and then put 3 ~ 4 drops on the white porcelain plate. After the chloroform evaporates, add 1 drop of 2% vanillin sulfuric acid solution, showing red .

(2) Take about 50mg of this product, add 1ml of ethanol solution (80 100) containing 7% hydroxylamine hydrochloride, and then add 3ml of potassium hydroxide test solution made of ethanol, heat in a water bath to boil, let cool, and add dilute hydrochloric acid to It was acidic, and added 1 drop of ferric chloride test solution, which was purple.

(3) In the chromatogram 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 reference solution.

(4) The infrared light absorption spectrum of this product should be consistent with the control spectrum (spectrum set 221).

[Check] The acidity of this product is 0.20g, add 20ml of water and shake, determine according to law (Appendix VI H), the pH value should be 3.5 ~ 5.0.

Clarity and color of solution (for injection) Take 0.60g of this product and add 6ml of 5% sodium bicarbonate solution to dissolve. The solution should be clear and colorless; if it is turbid, compare with turbidity standard solution No. 1 (Appendix B) Must not be thicker.

Take 0.25g of chloride, shake with 25ml of water, filter, and check the filtrate according to law (Appendix A). If turbidity occurs, it must not be more concentrated (0.02%) than the control solution made of 5.0ml of standard sodium chloride ).

Relevant substances: Take 40mg of this product, place it in a 10ml volumetric flask, add acetonitrile to dissolve and dilute to the mark as the test solution; precisely measure 1ml of test solution, place it in a 100ml volumetric flask, dilute to the mark with acetonitrile, shake As the control solution (1), take 1ml of the control solution (1) precisely, place it in a 10ml volumetric flask, dilute to the mark with acetonitrile, and shake it as the control solution (2). According to the chromatographic conditions under the content determination item, after the elution of the artesunate peak was completed, the linear gradient elution was performed according to the following table. Take 40 l of the control solution (2) and inject it into the liquid chromatograph. The signal-to-noise ratio of the artesunate peak should be greater than 3. Take 40 l of the control solution (1) and inject it into the liquid chromatograph, adjust the detection sensitivity so that the peak height of the main component chromatographic peak is 10% to 20% of the full range; and then accurately measure each of the test solution and the control solution (1). 40 l were injected into the liquid chromatograph and the chromatogram was recorded. If there are impurity peaks in the chromatogram of the test solution, the peak area of a single impurity peak should not be larger than the control solution (1) except the solvent peak and the gradient elution peak (1%), and the peak area is larger than the control solution (1 ) The impurity peaks with an area of 1/2 of the main peak must not exceed one (0.5%), and the sum of the area of each impurity peak must not be greater than 2 times (2.0%) the area of the main peak of the control solution (1).

Time (minutes)	Acetonitrile (%)	Phosphate buffer (%)
0	42	58
20	75	25
30	42	58
40	42	58

Moisture is taken from 0.5g of this product and measured according to the moisture determination method (Appendix M, first method A). The moisture content must not exceed 0.5%.

Take 1.0g of this product and check it according to law (Appendix N). The remaining residue should not exceed 0.1%.

The heavy metal shall be taken as the residue left under the burning residue, and shall be inspected in accordance with the law (Appendix H Second Law). The content of heavy metal shall not exceed 20 parts per million.

[Content determination] Determination according to high performance liquid chromatography (Appendix VD).

Chromatographic conditions and system suitability test using octadecylsilane bonded silica as a filler; acetonitrile-phosphate buffer solution (take 1.36 g of potassium dihydrogen phosphate, add 1000 ml of water to dissolve, and adjust the pH to 3.0 with phosphoric acid) ( 42:58) is the mobile phase; the column temperature is 30 ° C; the detection wavelength is 210nm. Take 4mg dihydroartemisinin reference substance and place it in a 10ml volumetric flask, add methanol to dissolve and dilute to the mark, and use it as a dihydroartemisinin reference substance solution. 1ml of artemisinin reference solution, add an appropriate amount of methanol to dissolve and dilute to the mark, take 40l into the liquid chromatograph, dihydroartemisinin presents two chromatographic peaks, the artesunate peak and adjacent dihydroartemisinin The resolution of the peaks should meet the requirements.

About 25mg of this product is determined by measurement. Weigh accurately, place it in a 25ml measuring flask, add methanol to dissolve and dilute to the mark, shake well, take 20l accurately, inject into the liquid chromatograph, and record the chromatogram. About 10 mg of artesunate reference was weighed accurately, placed in a 10 ml volumetric flask, and measured in the same way. Calculate the peak area according to the external standard method.

[Category] Antimalarial drugs.

[Storage] shading, sealed, and stored in a cool place.

[Preparation] (1) Artesunate tablets (2) Artesunate for injection