Table 1 Characteristics of artemisinin and its derivatives

Artemisinin

C₁₅H₂₂O₅

-

Poorly soluble in water and oil;

Melting point 156–157℃;

Molecular weight 282.35

Powder;

Micronized powder;

Tablet;

Capsule;

Suppository

Oral

Intramuscular injection

Rectal

T_max 1–3 h

Volume of distribution 1420–1560L

Clearance 445–479L/h

T_1/2 2.27–2.29 h

T_max 3.4 h

T_max 5.6 h

Antimalaria; Antivirus;

Antihelminth;

Anticancer;

Antiinflammation;

[24,25,26, 31, 32]

DHA

C₁₅H₂₄O₅

Modifying carbonyl groups into

hydroxyl groups;

The active metabolite of all artemisinins

Molecular weight 284.4

Powder;

Tablet;

Oral

Intramuscular injection

Rectal

T_max 0.9–1.6 h

–

T_max 4 h

Antimalaria;

Anticancer;

[24, 26, 28, 29, 32]

ART

C₁₉H₂₈O₈

Hemisuccinate derivative of DHA

Water-soluble;

Molecular weight

384.4

Powder

Suppository

Tablet

Injection

Oral

Intramuscular injection

Rectal

Intravenous administration

Bioavailability 61%-88%

T_max 15–39 min

Volume of distribution 14.8L/kg

Clearance 20.6L/kg/hr

T_1/2 0.36–1.2 h

Bioavailability 86.4–88%

T_max 7.2–12 min

T_1/2 25.2–48.2 h

Clearance 2.4–3.48L/kg/hr

Volume of distribution 1.09–3.98L/kg

Bioavailability 54.9%

T_max 0.58–1.43 h

T_1/2 0.9–0.95 h

Clearance 2–3L/kg/hr

Volume of distribution 0.1–0.3L/kg

Antimalaria;

Antiparasite;

Antitumor;

Antivirus;

Antiinflammation;

Antibacterial

[24, 27, 30,31,32]

ARM

C₁₆H₂₆O₅

Production methyl ether from DHA

Oil-soluble;

Molecular weight

298.4

Powder

Injection

Capsule

Oral

Intramuscular injection

Rectal

T_max 1.7–6 h

T_max 1.3–8.7 h

T_max 3.1 h

Antimalaria

[24, 31, 32]

ARE

C₁₇H₂₈O₅

Production β-ethyl ether from DHA

Oil-soluble;

Practically insoluble in water;

Molecular weight

312.4

Powder

Injection

Oral

Intramuscular injection

Rectal

–

T_max 4.8–7 h

–

Antimalaria

[24, 31, 32]