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氨酚待因2号片是一改进的解热镇痛复方药,其中含扑热息痛300 mg/片,磷酸可待因15 mg/片。作为新的复方药,有必要对其药代动力学进行研究。本文用原料药配成水剂与片剂对比,计算相对生物利用度。用HPLC和GC-MS法分别检测了8位正常健康志愿者一次po氨酚待因2号片剂或水剂(30 mg磷酸可待因和600mg扑热息痛)后血浆中可待因和扑热息痛的含量。结果如下:po两片氨酚待因2号片后,扑热息痛的药代动力学符合二室模型;t_(peak)=0.74 h±s 0.43 h,C_(max)=8.04 mg·L~(-1)±s 3.96 mg·L~(-1),t_(1/2)=2.81 h±s1.09 h,Clr=0.39 L·h~(-1)±s 0.12 L·h~(-1),Cls=30.77 L·h~(-1)±s 9.02 L·h~(-1)。氨酚待因片中的可待因的药代动力学符合二室模型;t_(peak)=0.87 h±s 0.15 h,C_(max)=50.65μg·L~(-1)±s10.17μg·L~(-1),t_(1/2)=3.11h±s 0.49h,Clr=16.12L·h~(-1)±s 2.02L·h~(-1),Cls=173L·h~(-1)±s 11.40 L·h~(-1);po水剂对照药后,扑热息痛和可待因的药代动力学房室模型均与po片剂的药代规律相似,统计学上无显著差异(P>0.05)。扑热息痛和可待因的相对生物度分别为99.97％±s 10.55％,100.73％±s 7.85％。
Paracetamol tablets no. 2 is an improved antipyretic and analgesic compound drugs, including paracetamol 300 mg / tablet, codeine phosphate 15 mg / tablet. As a new compound, it is necessary to study its pharmacokinetics. In this paper, raw materials dubbed agent and tablet contrast, calculate the relative bioavailability. The levels of codeine and paracetamol in plasma were determined by HPLC and GC-MS after a single oral dose of po, paracetamol, or hydrocortisone (30 mg codeine phosphate and 600 mg paracetamol) in eight normal healthy volunteers . The results were as follows: po Pharmacokinetics of paracetamol after two tablets of paracetamol was in line with the two-compartment model; t peak value = 0.74 h ± s 0.43 h, C max = 8.04 mg · L ~ 1) ± s 3.96 mg · L -1, t 1/2 = 2.81 h ± s 1.09 h, Clr = 0.39 L · h -1 ± s 0.12 L · h -1 ), Cls = 30.77 L · h -1 ± s 9.02 L · h -1. Pharmacokinetics of codeine in paracetamol was in compliance with the two-compartment model; t peak = 0.87 h ± s 0.15 h, C max = 50.65 μg · L -1 ± s 10.17 μg · L -1, t 1/2 = 3.11h ± s 0.49h, Clr = 16.12L · h -1 ± s 2.02L · h -1, Cls = 173L · h ~ (-1) ± s 11.40 L · h ~ (-1); pharmacokinetic model of acetaminophen and codeine pharmacokinetics were similar to po drugs, There was no significant difference (P> 0.05). The relative bioavailability of paracetamol and codeine were 99.97% ± s 10.55% and 100.73% ± s 7.85%, respectively.