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目的建立灵敏、简便的HPLC-UV法测定大鼠血浆中坎地沙坦的质量浓度,用于研究坎地沙坦酯固体脂质纳米粒在大鼠胃肠道的吸收情况。方法采用Eclipse XCB-C18色谱柱(150 mm×4.6 mm,5μm),流动相为水(体积分数0.1%磷酸,体积分数0.1%三乙胺,pH值2.7)-乙腈(体积比42∶58),流速为1.0 mL·min-1,检测波长为254 nm。结果测定坎地沙坦的线性范围在0.01～1 mg·L-1时,回归方程为A=7.028ρ+4.200×10-2(r=0.999 8);线性范围在0.3～30 mg·L-1时,回归方程为A=0.237ρ+1.00×10-3(r=0.999 2),定量下限达到10μg.L-1。日内、日间RSD值均小于10.0%,提取回收率大于75%。该方法用于评价坎地沙坦酯固体脂质纳米粒及原料药在大鼠胃肠道的吸收。结论该方法灵敏、简单、可靠,可用于测定血浆中坎地沙坦的质量浓度。与原料药相比,坎地沙坦酯固体脂质纳米粒在胃和小肠部位的吸收均有显著提高。
Objective To establish a sensitive and simple HPLC-UV method for the determination of the concentration of candesartan in rat plasma and to study the absorption of candesartan cilexetil solid lipid nanoparticles in the gastrointestinal tract of rats. Methods Eclipse XCB-C18 column (150 mm × 4.6 mm, 5 μm) was used. The mobile phase was water (volume fraction 0.1% phosphoric acid, volume fraction 0.1% triethylamine, pH 2.7) , The flow rate was 1.0 mL · min-1, the detection wavelength was 254 nm. Results The linear regression equation of candesartan was 0.01 ~ 1 mg · L-1, A = 7.028ρ + 4.200 × 10-2 (r = 0.999 8), linear range was 0.3-30 mg · L- 1, the regression equation was A = 0.237ρ + 1.00 × 10-3 (r = 0.999 2), and the lower limit of quantification was 10μg.L-1. The daily and daily RSD values were less than 10.0%, extraction recovery rate was greater than 75%. The method was used to evaluate the absorption of candesartan cilexetil solid lipid nanoparticles and drug substance in the gastrointestinal tract of rats. Conclusion The method is sensitive, simple and reliable and can be used to determine the concentration of candesartan in plasma. Compared with API, candesartan cilexetil solid lipid nanoparticles in the stomach and small intestine absorption were significantly increased.