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目的研究复方磺胺甲(口恶)唑(SMZco)对环孢素A(CsA)在兔体内药动学特征的影响。方法 6只(?)性日本大耳白兔,采用自身对照法,予CsA 9 mg·kg~(-1),ig,bid,连续灌胃给药7 d,于第8天应用LC-MS方法测定兔体内CsA浓度,DAS软件分析其药动学特征。完成CsA浓度检测后,即联用SMZco,37 mg·kg~(-1),ig,bid,1周后再次测定CsA的药动学特征,获得主要药动学参数,统计分析。结果联用SMZco前后CsA在兔体内的主要药动学参数分别是AUC_(0→∞)(9 262.764±3 060.376)、(5 729.079±343.687)μg·h·L~(-1);MRT_(0→∞)(14.669±6.487)、(5.973±1.409)h;t_(1/2)(8.791±4.321)、(3.14±1.356)h;ρ_(max)(784.4±392.59)、(1 066.833±279.593)μg·L~(-1)。联用SMZco后CsA的AUC_(0→∞),MRT和t_(1/2)均缩短,且差异均有统计学意义(P<0.05)。结论 SMZco与CsA联合给药时,可促进CsA的体内代谢,缩短体内滞留时间。
Objective To study the effects of SMZco on cyclosporine A (CsA) in rabbits. Methods Six Japanese white rabbits were administrated with CsA 9 mg · kg -1, ig, bid for 7 days by self-control method, and were administered with LC-MS Methods CsA concentration was measured in rabbits and the pharmacokinetic characteristics were analyzed by DAS software. After CsA concentration test, the pharmacokinetic characteristics of CsA were determined again after SMZco, 37 mg · kg -1, ig, bid for one week, and the main pharmacokinetic parameters were obtained and statistically analyzed. Results The main pharmacokinetic parameters of CsA before and after administration of SMZco in rabbits were AUC 0 ~ ∞ (9 262.764 ± 3 060.376), (5 729.079 ± 343.687) μg · h · L -1, MRT_ ( 0 → ∞) (14.669 ± 6.487), (5.973 ± 1.409) h; t 1/2 (8.791 ± 4.321), (3.14 ± 1.356) h; ρ max (784.4 ± 392.59), (1 066.833 ± 279.593) μg · L -1. The AUC_ (0 → ∞), MRT and t_ (1/2) of CsA after SMZco administration were shortened, and the difference was statistically significant (P <0.05). Conclusion SMZco combined with CsA can promote the in vivo metabolism of CsA and shorten the residence time in vivo.