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目的:本研究对制备的环维黄杨星D羟丙基-β-环糊精包合物(D hydroxypropyl-β-cyclodextrin complex,CBHD)理化性质进行表征,并考察其在大鼠体内的药动学特征。方法:采用红外光谱法、差示扫描量热法对CBHD物进行表征。大鼠灌胃给予CBHD和环维黄杨星D(CB)混悬液后,于不同时间点大鼠眼底静脉丛取血。采用HPLC/FLD测定血浆中CB的浓度。结果:CBHD的理化性质与CB和物理混合物明显不同,差示扫描量热法测定结果显示形成包合物后一种新物相峰出现;CBHD和CB的主要药动学参数如下:Cmax为(76.83±6.73)μg/L和(69.27±8.66)μg/L;Tmax为(6.00±0.00)h和(4.33±0.00)h;AUC0~t为(1 541.04±178.61)μg/(L·h)和(619.93±75.67)μg/(L·h)。结论:CBHD的相对生物利用度为248.58%,CBHD明显提高了CB在大鼠体内的生物利用度。
OBJECTIVE: In this study, the physicochemical properties of the prepared D-hydroxypropyl-β-cyclodextrin complex (CBHD) were characterized and its pharmacokinetics in rats Learn characteristics. Methods: Infrared spectroscopy and differential scanning calorimetry were used to characterize CBHD. After intragastric administration of CBHD and cyclophosphamide D (CB) suspension in rats, blood was collected from the venous plexus of rats at different time points. The concentration of CB in plasma was determined by HPLC / FLD. Results: The physical and chemical properties of CBHD were significantly different from that of CB and physical mixtures. The results of differential scanning calorimetry showed that a new phase peak appeared after the formation of inclusion complex. The main pharmacokinetic parameters of CBHD and CB were as follows: Cmax was ( 76.83 ± 6.73) μg / L and (69.27 ± 8.66) μg / L; Tmax was (6.00 ± 0.00) h and (4.33 ± 0.00) h respectively; AUC0 ~ t was (1 541.04 ± 178.61) μg / (L · h) And (619.93 ± 75.67) μg / (L · h), respectively. Conclusion: The relative bioavailability of CBHD is 248.58%. CBHD significantly improves the bioavailability of CB in rats.