Overview[1][3]
Naphthoquine phosphate is a heterocyclic organic compound that has a killing effect on various Plasmodium schizonts and some strains of Plasmodium gametocytes and tissue-stage protozoa, and has a good curative effect on drug-resistant Plasmodium. ; Has a long-term preventive effect on Plasmodium. Naphtholquin phosphate is a tetrahydronaphthol antimalarial compound that has not been widely used in the field of antimalarial drugs. It is a new structural type of killer of Plasmodium blood schizonts (asexuals).
Preparation[4]
Preparation of compound naphthoquin phosphate pellets
Add 125g of artemisinin, 78.3g of naphthoquine phosphate, 60g of microcrystalline cellulose, 35g of mannitol, 17.5g of sodium carboxymethyl starch and 15g of cross-linked polyvinylpyrrolidone into a wet mixer and mix evenly. Stir and mix 130g of 50% ethanol to prepare a soft material. Add the soft material to an extruder with an orifice plate with a hole diameter of 0.7mm to extrude a strip. Add the strip to a spheronizing machine and spheronize at 600 rpm to prepare wet pills. Add the wet pellets to the fluidized bed, control the inlet air temperature to 70°C and the material temperature to 50°C, and dry to obtain the pellet core. The pellet core is coated using the bottom spray method in the fluidized bed. The coating agent is 23.5g polyvinyl alcohol and 3.5g polyethylene glycol. The inlet air temperature is controlled to 60°C, the material temperature is 35°C, and the air volume is 0.3m3/ min, coat layer by layer until completely wrapped, and the coating weight increases by 8%.
Pharmaceutical Rohm and Haas resin metabolism[1]
Naphtholquine phosphate is absorbed quickly and completely after oral administration, with a peak time of 2 to 4 hours. The relative bioavailability is 96.4%. It is widely distributed, with the highest concentration in the liver, followed by the kidneys, spleen, and lungs. The concentration in blood cells is higher than that in plasma. ; Excretion is mainly urine, followed by feces.
Apply[2]
The antibacterial spectrum of naphthoquine phosphate:
Note: “+” in the table indicates the growth of indicator bacteria and no antibacterial effect; “—”waterproofing agent” indicates that it has not been used; “w” indicates that the antibacterial effect is weak; “▲” indicates that the indicator bacteria do not grow; ” ☆” means suppress first and then grow; “⑴” means “Sabourourary dextrose agar medium”; “⑵” means “nutritional agar medium”.
Minimum inhibitory concentration:
Note: “⑴” in the table means “Sabourourard dextrose agar medium”; “⑵” means “nutrient agar medium”.
It can be seen from the experimental results that, except for Candida albicans, naphthoquine phosphate has an inhibitory effect on all selected strains and has a broad antibacterial spectrum.
Main reference materials
[1] National Essential Medicines Manual
[2] [Chinese invention, Chinese invention authorization] CN201410316092.4 A new use of naphtholquin phosphate [disclosed]/A use of naphtholquin phosphate [authorized]
[3] [Invented in China, Authorized by China Invention] CN97111840.X Preparation method of synergistic antimalarial drug naphtholquin phosphate
[4] [Invented in China, China��Invention authorization] CN201110072303.0 A compound naphthoquine phosphate pellet and its preparation method
