Okor R S, Nwankwo M U
Department of Pharmaceutics, University of Benin, Nigeria.
J Clin Pharm Ther. 1988 Jun;13(3):219-23. doi: 10.1111/j.1365-2710.1988.tb00184.x.
Chloroquine phosphate (CP) has been formulated in a suppository base consisting of polyethylene glycol, PEG 1000 and PEG 6000 (7:3) with 0.5% polysorbate 80 included as an absorption promoter. Peak chloroquine blood levels in children (mean body weight 10 kg, age 21 months) were 0.67 +/- 0.08 micrograms/ml (after 200 mg CP) and 1.06 +/- 0.23 micrograms/ml (after 300 mg CP) following rectal administration of the suppositories. Prior to drug administration, the base level chloroquine was 0.30 +/- 0.02 micrograms/ml. Elimination half lives calculated from the rapid phase of log concentration-time curves were 3.3 h (after 200 mg CP) and 2.7 h (after 300 mg CP), respectively. Based on literature evidence the blood levels obtained with the 300 mg CP suppositories would be therapeutic in the management of malaria and rheumatoid disease.
磷酸氯喹（CP）已被制成栓剂，其基质由聚乙二醇、聚乙二醇1000和聚乙二醇6000（7:3）组成，并含有0.5%的聚山梨酯80作为吸收促进剂。对儿童（平均体重10千克，年龄21个月）直肠给药该栓剂后，氯喹血药峰浓度在给予200毫克CP后为0.67±0.08微克/毫升，给予300毫克CP后为1.06±0.23微克/毫升。给药前，基础氯喹水平为0.30±0.02微克/毫升。根据对数浓度-时间曲线的快速相计算出的消除半衰期分别为3.3小时（给予200毫克CP后）和2.7小时（给予300毫克CP后）。基于文献证据，300毫克CP栓剂所获得的血药水平对疟疾和类风湿疾病的治疗具有疗效。
