Artesunate preparation for injection, and application thereof

Abstract

The invention discloses an artesunate preparation for injection. The artesunate preparation for injection includes sterile artesunate powder and an auxiliary material pH regulator powder for injection. The pH regulator for injection is one of disodium hydrogen phosphate, dipotassium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, sodium hydroxide and potassium hydroxide, or a mixture containing more of above substances according to an arbitrary ratio, and preferably one of the disodium hydrogen phosphate and dipotassium hydrogen phosphate or a mixture containing the disodium hydrogen phosphate and dipotassium hydrogen phosphate according to an arbitrary ratio. A molar ratio of the sterile artesunate to the pH regulator is 1:1 to 1:6, and preferably 1:1.0 to1:4.0. The above composition has obviously better solubility, solution stability and solid preparation stability than commercially available artesunate for injection, and is suitable for being clinically used.

Description

technical field

[0001] The invention relates to an artesunate preparation for injection, its preparation and application, and belongs to the technical field of medicine preparation. Background technique

[0002] Artemisinin, also known as artemisinin, is a sesquiterpene lactone drug with peroxy groups extracted from the stems and leaves of the plant Artemisia annua. It is widely used as a drug for treating malaria, mainly for vivax malaria and falciparum malaria. Symptom control, and treatment of chloroquine-resistant strains. Artemisinin-based combination therapy has been widely used in the treatment of malaria for nearly half a century, and has played a huge role in the human war against malaria. Artemisinin has disadvantages such as high dosage, high recurrence rate, and low solubility in water and oil. Scientists and pharmaceutical companies have discovered artemisinin derivatives (dihydroartemisinin, artemether, artemisinin, etc.) in the structural modification of arte...

Examples

Embodiment 1

[0029] Prescription: Artesunate 1000 parts, disodium hydrogen phosphate 554 parts (weight)

[0030] Preparation method: take sterile artesunate for injection and disodium hydrogen phosphate for injection out of the outer packaging, remove dust and clean, wipe and sterilize, and transfer them to a sterile room for standby; After the disodium hydrogen phosphate is separately pulverized, 100-mesh sieve is used; the sieved artesunate and disodium hydrogen phosphate are mixed evenly according to the prescription ratio, and after passing the full inspection, they are divided into vials according to the clinically required dose, and the stoppers are pressed. , capping, light inspection, qualified inspection, labeling, and packaging to obtain artesunate for injection.

Embodiment 2

[0032] Prescription: 1000 parts of artesunate, 738 parts of disodium hydrogen phosphate (by weight)

[0033] Preparation method: take sterile artesunate for injection and disodium hydrogen phosphate for injection out of the outer packaging, remove dust and clean, wipe and sterilize, and transfer them to a sterile room for standby; After the disodium hydrogen phosphate is separately pulverized, 100-mesh sieve is used; the sieved artesunate and disodium hydrogen phosphate are mixed evenly according to the prescription ratio, and after passing the full inspection, they are divided into vials according to the clinically required dose, and the stoppers are pressed. , capping, light inspection, qualified inspection, labeling, and packaging to obtain artesunate for injection.

Embodiment 3

[0035] Prescription: Artesunate 1000 parts, disodium hydrogen phosphate 1477 parts (weight)

[0036]Preparation method: take sterile artesunate for injection and disodium hydrogen phosphate for injection out of the outer packaging, remove dust and clean, wipe and sterilize, and transfer them to a sterile room for standby; After the disodium hydrogen phosphate is separately pulverized, 100-mesh sieve is used; the sieved artesunate and disodium hydrogen phosphate are mixed evenly according to the prescription ratio, and after passing the full inspection, they are divided into vials according to the clinically required dose, and the stoppers are pressed. , capping, light inspection, qualified inspection, labeling, and packaging to obtain artesunate for injection.

technical field

[0001] The invention relates to an artesunate preparation for injection, its preparation and application, and belongs to the technical field of medicine preparation. Background technique

[0002] Artemisinin, also known as artemisinin, is a sesquiterpene lactone drug with peroxy groups extracted from the stems and leaves of the plant Artemisia annua. It is widely used as a drug for treating malaria, mainly for vivax malaria and falciparum malaria. Symptom control, and treatment of chloroquine-resistant strains. Artemisinin-based combination therapy has been widely used in the treatment of malaria for nearly half a century, and has played a huge role in the human war against malaria. Artemisinin has disadvantages such as high dosage, high recurrence rate, and low solubility in water and oil. Scientists and pharmaceutical companies have discovered artemisinin derivatives (dihydroartemisinin, artemether, artemisinin, etc.) in the structural modification of arte...

Examples

Embodiment 1

[0029] Prescription: Artesunate 1000 parts, disodium hydrogen phosphate 554 parts (weight)

[0030] Preparation method: take sterile artesunate for injection and disodium hydrogen phosphate for injection out of the outer packaging, remove dust and clean, wipe and sterilize, and transfer them to a sterile room for standby; After the disodium hydrogen phosphate is separately pulverized, 100-mesh sieve is used; the sieved artesunate and disodium hydrogen phosphate are mixed evenly according to the prescription ratio, and after passing the full inspection, they are divided into vials according to the clinically required dose, and the stoppers are pressed. , capping, light inspection, qualified inspection, labeling, and packaging to obtain artesunate for injection.

Embodiment 2

[0032] Prescription: 1000 parts of artesunate, 738 parts of disodium hydrogen phosphate (by weight)

[0033] Preparation method: take sterile artesunate for injection and disodium hydrogen phosphate for injection out of the outer packaging, remove dust and clean, wipe and sterilize, and transfer them to a sterile room for standby; After the disodium hydrogen phosphate is separately pulverized, 100-mesh sieve is used; the sieved artesunate and disodium hydrogen phosphate are mixed evenly according to the prescription ratio, and after passing the full inspection, they are divided into vials according to the clinically required dose, and the stoppers are pressed. , capping, light inspection, qualified inspection, labeling, and packaging to obtain artesunate for injection.

Embodiment 3

[0035] Prescription: Artesunate 1000 parts, disodium hydrogen phosphate 1477 parts (weight)

[0036]Preparation method: take sterile artesunate for injection and disodium hydrogen phosphate for injection out of the outer packaging, remove dust and clean, wipe and sterilize, and transfer them to a sterile room for standby; After the disodium hydrogen phosphate is separately pulverized, 100-mesh sieve is used; the sieved artesunate and disodium hydrogen phosphate are mixed evenly according to the prescription ratio, and after passing the full inspection, they are divided into vials according to the clinically required dose, and the stoppers are pressed. , capping, light inspection, qualified inspection, labeling, and packaging to obtain artesunate for injection.

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