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建立活血止痛膏中有效成分丹皮酚、丁香酚、胡椒碱微透析体内外回收率校正方法,为其经皮药动学研究提供依据。利用高效液相色谱法测定透析液中丹皮酚、丁香酚、胡椒碱的浓度,并计算微透析探针回收率;研究浓度、校正方法对3种成分微透析探针回收率的影响,并考察探针吸附性、体内外回收率的稳定性和重复性。结果表明,以30%乙醇生理盐水作为灌流液时,探针对3种成分均无明显的吸附,短时间内即可从探针上被完全洗脱下来;在8 h内,3种成分体内外回收率均能保持稳定;交替用含药溶液和空白灌流液灌流探针3次,3种成分体内外回收率基本不变。不同质量浓度丹皮酚(2.46~53.64 mg·L~(-1))、丁香酚(4.26~32.15 mg·L~(-1))和胡椒碱(5.75~45.87 mg·L~(-1))体外回收率分别为(45.7±4.66)%,(41.3±3.96)%,(27.82±2.95)%,即3种成分的探针回收率对浓度没有依赖性;在相同条件下,零净通量法、透析法和反透析法所测得的探针体外回收率几乎相等。因此,采集部位药物的浓度可用体外测得的回收率或在体回收率进行校正。同时也证明了该研究建立的微透析方法可用于活血止痛膏的经皮药动学研究。
To establish a method for the recovery of paeonol, eugenol and piperine microdialysis, which is the active ingredient in Huoxuezhitong cream, to provide the basis for its percutaneous pharmacokinetic study. The concentrations of paeonol, eugenol and piperine in the dialysate were determined by high performance liquid chromatography, and the recoveries of microdialysis probes were calculated. The effects of concentration and calibration methods on the recoveries of microdialysis probes were studied. Probe probe adsorption, stability and repeatability of in vitro and in vivo recovery. The results showed that when 30% ethanol normal saline was used as the perfusate, the probe had no obvious adsorption on the three components and could be completely eluted from the probe in a short time. Within 8 h, the three components The internal and external recoveries could be kept stable. The drug solution and blank perfusate were alternately used to perfuse the probe three times. The recovery rates of the three components in vitro and in vivo were basically unchanged. Paeonol (2.46 ~ 53.64 mg · L ~ (-1)), eugenol (4.26 ~ 32.15 mg · L ~ (-1)) and piperine (5.75 ~ 45.87 mg · L ~ ) In vitro were (45.7 ± 4.66)%, (41.3 ± 3.96)% and (27.82 ± 2.95)%, respectively. The recovery rate of the three components was independent of concentration. Under the same conditions, Quantitative, dialysis and reverse dialysis measured probe recovery rate in vitro is almost equal. Therefore, the concentration of drug at the collection site can be measured in vitro or in vivo recovery rate of recovery. At the same time, it also proves that the microdialysis method established in this study can be applied to the percutaneous pharmacokinetic study of Huoxuezhitong cream.