STUDY OF PHARMACOKINETICS OF LIVER TARGETING ANTIMALARIAL AGENT NEOGLYCOALBUMIN-PRIMAQUINE CONJUGATE(NGA-PQ)AND PRIMAQUINE PHOSPHATE IN MOUSE

A normal phase high-performance liquid chromatography process was used to separate and detect primaquine in blood and liver after a single intravenous dose of the hepatictargeting agent neoglycoalbumine-primaquine conjugate(NGA-PQ)and primaquine phosphate (PQP)in mice.6-Methoxy-8-(4-amino- butyrylamino ) quinoline synthesized and identified by us was usedas an internal standard to be added to biologic samples obtained from mice at different times after givenNGA-PQ or PQP.The mixture was extracted with ether after alkalinization in the PQP group. In theNGA- PQ group ,the biological samples must be hydrolized by heating under nitrogen and acidcondition in a domestic pressure cooker before extraction. The extracts were evaporated to drynessunder nitrogen ,then dissolved in the mobile phase(chloroform-methanol-amonium hydroxide=86.8:12.5:0.7).The results showed that the hepatic PQ collecting ratio and the retention time ofPQ in liver in the NGA-PQ group were higher and longer than those in the PQP group. The resultsalso point out that NGA-PQ has liver targeting property.