银锻苷磷脂复合物的研制及其理化溶解性质测定
首发时间:2020-04-07
摘要:目的:制备银锻苷磷脂复合物,对其理化性质进行研究。方法:采用溶剂挥法制备银锻苷磷脂复合物,以复合率作为评价指标,利用单因素分析和正交实验,考察银锻苷与磷脂在不同反应溶剂、反应比例、反应时间、反应温度等因素对复合率的影响,确定银锻苷磷脂复合物的最佳制备工艺。通过UV、FT-IR、DSC、XRD测定银锻苷磷脂复合物的理化性质,推测复合物的形成机理。结果:最佳制备工艺为银锻苷与磷脂按1比2 (w/w),反应溶剂为无水乙醇,药物浓度为4 mg/mL,在反应温度为50 ℃下加热搅拌3 h。结论:磷脂复合物溶解度和油水分配系数显著提高。通过分析FT-IR,DSC,XRD结果,发现银锻苷磷脂复合物中没有新的化学键生成,而具有完全不同于物理混合物的理化特征,推测可能是与磷脂之间的氢键或范德华力形成稳定的复合结构,复合物中的银锻苷以无定型的状态存在于磷脂中。
关键词: 药物分析 银锻苷磷脂复合物 理化性质 油水分配系数
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Research on the Preparation and Physicochemical Solubility Determination of Tiliroside Phospholipid Complex
Abstract:Objective: To prepare tiliroside phospholipid complex and investigate its physical and chemical properties. Methods: The solvent evaporation method was adopted to make the tiliroside-phospholipid complex and the complex rate as the evaluation index. This study investigated a series of experiments, including a single factor and orthogonal analysis. Then the responses kind of the solvent, the feed ratio of tiliroside and phospholipid, reactant concentration, reaction time, and reaction temperature were examined, and the preparation process was validated. The physicochemical properties of tiliroside phospholipid complex were measured by UV, FT-IR, DSC, and XRD, and the formation mechanism of the complex was speculated. Results: The feed ratio of phospholipid and tiliroside was the crucial factor, and the best manufacture conditions were obtained as follows: the weight ratio of phospholipid and tiliroside was 2:1, reacted in the ethyl alcohol for three h at 50 ℃, the concentration of TIL was 4 mg/ml. Conclusion: Study on preparation and physicochemical properties of tiliroside phospholipid complex. The results showed that there was no new chemical bond formation between drug and phospholipid in the tiliroside phospholipid complex, but it was entirely different from the physical mixture. A stable composite structure was formed between tiliroside and phospholipid by hydrogen bond or van der Waals force, and the complex exists in phospholipid with the amorphous state.
Keywords: Pharmaceutical analysis Tiliroside phospholipid complex physicochemical properties Oil-water partition coefficients
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