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目的研究复方樟柳碱(CA)在家兔体内的药代动力学及组织分布特征。方法家兔颞浅动脉旁皮下注射0.7 mL·kg~(-1)复方樟柳碱注射液,用LC-MS/MS法测定氢溴酸樟柳碱及盐酸普鲁卡因在家兔血浆及组织中的浓度,用Win Nonlin 6.2软件计算药代动力学参数。结果氢溴酸樟柳碱和盐酸普鲁卡因的主要药代动力学参数如下:C_(max)分别为(12.93±1.90),(895.47±213.99)ng·mL~(-1);t_(max)分别为(0.35±0.18),(0.24±0.15)h;t_(1/2)分别为(0.82±0.22),(0.49±0.11)h;AUC_(0-t)分别为(19.20±5.71),(706.59±121.90)ng·mL~(-1)·h。氢溴酸樟柳碱在视网膜、脉络膜,肾及肺中分布较高,盐酸普鲁卡因在视网膜、脉络膜、脾及肾中分布较高。结论复方樟柳碱注射液颞浅动脉旁皮下注射给药后吸收快,消除半衰期短,组织分布广泛。
Objective To study the pharmacokinetics and tissue distribution characteristics of compound anisodine (CA) in rabbits. Methods The compound anisodine injection (0.7 mL · kg -1) was injected subcutaneously into the superficial temporal artery of rabbits. The contents of anisodine hydrobromide and procaine hydrochloride in rabbits plasma and Tissue concentrations were calculated using the Win Nonlin 6.2 software to calculate pharmacokinetic parameters. Results The main pharmacokinetic parameters of anisodine hydrobromide and procaine hydrochloride were as follows: C max (12.93 ± 1.90), (895.47 ± 213.99) ng · mL -1; t_ ( max were (0.35 ± 0.18) and (0.24 ± 0.15) h respectively; t 1/2 was 0.82 ± 0.22 and 0.49 ± 0.11 h, respectively; AUC 0 t was 19.20 ± 5.71 ), (706.59 ± 121.90) ng · mL -1 (-1) h. Anisodizine hydrobromide in the retina, choroid, kidney and lung distribution is high, procaine hydrochloride in the retina, choroid, spleen and kidney distribution is high. Conclusion Compound anisodine injection subcutaneous injection of superficial temporal artery after subcutaneous injection fast absorption, elimination of short half-life, extensive tissue distribution.