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目的:采用高水溶性β-环糊精衍生物磺丙基醚-β-环糊精(SPE7-β-CD)制备尼美舒利(Nim)包合物,并确定其两组分物质的量之比。方法:采用等摩尔系列法,在保持总物质的量一致的情况下,配置不同比例(1:3、1:2、2:3、1:1、3:2、2:1、3:1)的SPE7-β-CD与Nim的系列溶液,对系列溶液的吸光度与同浓度Nim的吸光度之差(ΔA)进行分析;另配制pH分别为5.45、6.82、7.68的含不同浓度(0.2×10-4、0.4×10-4、0.6×10-4、0.8×10-4、1×10-4mol/L)SPE7-β-CD的Nim包合物,对其进行相溶解度曲线分析,并进行紫外扫描,在393nm波长处计算相邻曲线间的吸光度差值,以此确定两组分物质的量之比。结果:ΔA最大处SPE7-β-CD与Nim的物质的量之比为1:1;不同pH下Nim随SPE7-β-CD浓度增加相溶解度呈梯度增加,相溶解度曲线呈AL型,表示SPE7-β-CD与Nim的物质的量之比为1:1;紫外扫描结果表明,相邻曲线间Nim在393nm波长处吸光度差值相等,表示SPE7-β-CD与Nim的物质的量之比为1:1。结论:SPE7-β-CD与Nim在溶液中可形成物质的量之比为1:1的可溶性包合物。
OBJECTIVE: To prepare nimesulide (Nim) inclusion complex using sulfopropyl β -cyclodextrin (SPE7-β-CD), a highly water-soluble β- The ratio of volume. Methods: Using the equimolar series of methods, with the same total amount of material, different ratios (1: 3,1: 2,2: 3,1: 1,3: 2,2: 1,3: 1 ) Solution of SPE7-β-CD and Nim were used to analyze the difference (ΔA) between the absorbance of the series of solutions and the absorbance of the same concentration of Nim. The other solutions were prepared with different concentrations (0.2 × 10 -4, 0.4 × 10 -4, 0.6 × 10 -4, 0.8 × 10 -4, 1 × 10 -4 mol / L) Nim inclusion complex of SPE7-β-CD was subjected to phase solubility curve analysis and subjected to UV scanning, in the 393nm wavelength calculation of the absorbance difference between adjacent curves, in order to determine the amount of two components of the ratio. Results: The ratio of the amount of SPE7-β-CD to Nim was 1: 1 at the maximum ΔA. The solubility of Nim increased with the increase of SPE7-β-CD concentration at different pH. The phase solubility curve showed AL-type, indicating that SPE7 The ratio of the amount of substance of β7-β-CD to Nim was 1: 1. The results of UV-scan showed that the difference of absorbance between adjacent curves was equal at 393nm, 1: 1. CONCLUSIONS: SPE7-β-CD and Nim form soluble clathrates with a 1: 1 ratio of substances in solution.