Nano-Artesunate capsule and preparation process thereof

Abstract

The invention relates to a nano-Artesunate capsule and a preparation process thereof. A capsule heart is Artesunate, a capsule film is gelatin, a capsule shape is in a ball shape or an ellipsoid shape, and the diameter of the capsule is 30 nm. The invention adopts the following preparation process: swelling the gelatin by distilled water to form colloid, dissolving powdered Artesunate in ethanol at the room temperature, dissolving glacial acetic acid in the distilled water, taking gelatin solution, slowly dropping the Artesunate ethanol solution under the stirring in a water bath with the constant temperature of 40 DEG C, adjusting pH value with glacial acetic acid solution, slowly dropping formaldehyde under the condition of ice bath, solidifying to form the capsule, and freezing and drying to obtain powder of the nano-Artesunate capsule. The capsule prepared by the invention can be taken orally as well as injected by injection, the dosage is small, and no toxic or side effect occursby taking orally; and the injection cannot cause thrombus, and the like in blood vessels, can support sustained release of medicine delivery, and the injection has high efficiency and long effective period. The grain size of the capsule is uniform, the covering state is good, and the covering rate is 50%; the addition of emulsifier and coagulant aid is not needed during preparation, the process issimple, and the operation is convenient.

Description

technical field [0001] The invention relates to a nano artesunate capsule and a preparation process thereof. Background technique [0002] Artesunate (Artesunate) is a derivative of the semiterpene lactone compound artemisinin, the chemical name is dihydroartemisinin-1,2-a-succinic acid monoester, and the molecular formula is C 19 o 8 h 28 , molecular weight 384.43, white powder, odorless, almost tasteless, easily soluble in acetone, chloroform, soluble in ethanol or ethyl acetate, almost insoluble in water, melting point 130---137. Artesunate mainly acts on the erythrocytic clones of Plasmodium, and is currently the only effective derivative of artemisinin that can be made into water-soluble preparations. It is used for the treatment of various malaria, especially multidrug-resistant falciparum malaria. It also has anti-pregnancy, anti-fibrosis, anti-schistosome, anti-toxoplasma, anti-arrhythmia and tumor cytotoxic effects. [0003] The main problems of artemisinin and ...

AI Technical Summary

Problems solved by technology

Although both dragon's blood and artesunate are powdery solids, they are easily soluble in organic solvents such as ethanol, but artesunate has a peroxide bridge ring structure, which is unstable, easy to break the ring when heated, and easily reacts with hydroxyl groups to lose Active, dragon's blood is not easy to react with hydroxyl; dragon's blood is slightly soluble in water, artesunate is insoluble in water

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