脑心通胶囊对缬沙坦在大鼠体内药动学的影响

目的 研究脑心通胶囊对缬沙坦在大鼠体内药动学的影响。方法 建立液相色谱-串联质谱（LC-MS/MS）法检测缬沙坦血药浓度，并进行专属性考察、回收率试验、基质效应、稳定性试验等方法学验证；24只SD雄性大鼠，随机均分为3组，每组8只，分别为缬沙坦组（A组），缬沙坦和脑心通胶囊单次给药组（B组），脑心通胶囊给药7 d后，第8天ig给予缬沙坦和脑心通胶囊组（C组），于给药前及给药后不同时间点由大鼠眼眶静脉丛采血，采用液相色谱-串联质谱（LC-MS/MS）法测定血浆中缬沙坦的质量浓度，DAS2.0软件统计分析，得到缬沙坦的药动学参数。结果 成功建立LC-MS/MS法检测缬沙坦血药浓度方法，方法学验证符合药动学相关规范要求。口服缬沙坦在大鼠体内的药动学属于一室模型。B组C_max明显低于A组，但差异无统计学差异；B组t_1/2显著高于A组（P<0.05）；C组t_max、t_1/2、AUC_0-tn、AUC_0-∞均显著高于A组（P<0.05、0.01），K_e显著低于A组（P<0.05）；C组AUC_0-tn、AUC_0-∞显著高于B组（P<0.05）。结论 大鼠经连续ig给药脑心通胶囊后，可显著延缓缬沙坦在大鼠体内的达峰时间，并使缬沙坦在大鼠体内的生物利用度升高。

Effect of Naoxintong Capsules on pharmacokinetics of valsartan in rats

Objective To study the effect of Naoxintong Capsules on pharmacokinetics of valsartan in rats. Methods 24 SD rats were randomly divided into three groups:valsartan group (group A), valsartan group (group B) and Naoxintong Capsules group (group B), each group had 8 rats. On the 8th day, valsartan and Naoxintong Capsules were given by gavage (group C). Plasma samples were collected at different times after the drug administrationfrom the orbital veins of the rats. The concentrations of valsartan in plasma were determined by LC-MS/MS, and the pharmacokinetic parameters of valsartan were obtained in rats by the statistical analysis of DAS 2.0 Software. Results Combined with the valsartan single administration group (group C), t_max, t_1/2, and AUC were significantly increased (P<0.05 or P<0.01), and Ke was significant decreased (P<0.05) in the Naoxintong and valsartan combined administration group. Conclusion The rats significantly delayed the peak time of valsartan, and the bioavailability of valsartan in rats after continuous administration of Naoxintong was increased. It is instructive to study the combined use of valsartan and Naoxintong capsule.