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用兔/体外法测定了抗疟药咯萘啶(PND)对恶性疟原虫FCC_1株的最低有效浓度(MEC),并结合已取得的人体内药物动力学研究结果初步探讨了PND的剂量方案。给药后兔血清中PND的MEC为4.7±1.2ng/ml,正常兔血清加PND的MEC为5.2±2.0ng/ml,两者无显著性差异(P>0.05)。根据推算而建议的剂量方案:d_(1)4mg/kg,d_(2)2mg/kg,im;或胶囊(或肠溶片)d_(1)10mg/kg,d_(2)5mg/kg,po。按此方案可使im后1min～72h,po后1(或3)～72h体内保持至少约2倍于MEC的全血药浓度。此方案尚待作临床研究,以评价其疗效和副反应。
The minimum effective concentration (MEC) of anti-malarial drug pyronaridine (PND) against Plasmodium falciparum FCC_1 was determined by rabbit / in vitro method and the dosage regimen of PND was preliminarily discussed in combination with the pharmacokinetic results obtained in human. The MEC of rabbit PND after administration was 4.7 ± 1.2ng / ml and that of normal rabbits plus PND was 5.2 ± 2.0ng / ml. There was no significant difference between the two groups (P> 0.05). The dosage regimen suggested on the basis of estimation: d 1 mg / kg, d 2 mg / kg, im 2; or capsule d) (mg / kg) po. According to this program can be im 1min ~ 72h, po 1 (or 3) ~ 72h in vivo to maintain at least about 2 times the whole blood of MEC plasma concentration. This program remains to be clinical studies to evaluate its efficacy and side effects.