Sowunmi A
Department of Pharmacology and Therapeutics, University of Ibadan, Nigeria.
East Afr Med J. 1996 Feb;73(2):111-4.
The pharmacokinetics of quinine were assessed in healthy adult Africans after a single oral dose of 500 mg quinine base (n = 11) and after a single intramuscular injection of 500 mg quinine base (n = 7). Quinine was assayed in plasma by high performance liquid chromatographic method (HPLC). Quinine was rapidly absorbed reaching a mean peak concentrations of 2.9 (sd 0.5) and 4.5 (1.3) mg L-1 respectively in a median time of 3.0 (range 2.0-4.0) and 1.5 (range 0.5 4.0) h respectively after oral and intramuscular administration. The peak concentration (Cmax) was significantly higher after intramuscular than after oral administration [Cmax = 4.5 (1.3) versus 2.9 (0.5) mg L-1, p < 0.01]. The mean half-life [t1/2z = 11.7 (2.9) versus 10.7 (3.5) h, P > 0.2] respectively, volume of distribution (Vz = 2.5 (0.7) versus 2.2 (0.99) L Kg-1, P > 0.2) respectively and estimated plasma clearance [CLp = 0.15 (0.04) versus 0.15 (0.09) L h-1 Kg-1, P > 0.2] respectively were not significantly different after oral and intramuscular administration. The mean AUCo-oo was higher after intramuscular than after oral administration [71.8 (29.4) versus 54.9 (19.2) mg.h.L, P > 0.1] respectively but this was not significant. The pharmacokinetic parameters after intramuscular dose were similar to those obtained in seven healthy subjects given quinine by slow intravenous infections over four hours. The dose was well tolerated.
对11名健康成年非洲人单次口服500毫克奎宁碱(n = 11)以及7名健康成年非洲人单次肌肉注射500毫克奎宁碱(n = 7)后,评估了奎宁的药代动力学。采用高效液相色谱法(HPLC)测定血浆中的奎宁。口服和肌肉注射后,奎宁均迅速吸收,口服给药后中位时间3.0小时(范围2.0 - 4.0小时)达到平均峰值浓度2.9(标准差0.5)毫克/升,肌肉注射后中位时间1.5小时(范围0.5 - 4.0小时)达到平均峰值浓度4.5(1.3)毫克/升。肌肉注射后的峰值浓度(Cmax)显著高于口服给药后的峰值浓度[Cmax = 4.5(1.3)对2.9(0.5)毫克/升,p < 0.01]。平均半衰期[t1/2z = 11.7(2.9)对10.7(3.5)小时,P > 0.2]、分布容积(Vz = 2.5(0.7)对2.2(0.99)升/千克,P > 0.2)以及估计的血浆清除率[CLp = 0.15(0.04)对0.15(0.09)升/小时/千克,P > 0.2]在口服和肌肉注射给药后均无显著差异。肌肉注射后的平均AUCo-oo高于口服给药后的平均AUCo-oo[71.8(29.4)对54.9(19.2)毫克·小时·升,P > 0.1],但差异不显著。肌肉注射剂量后的药代动力学参数与7名健康受试者在4小时内缓慢静脉输注奎宁后获得的参数相似。该剂量耐受性良好。