目的 通过制备快速凝胶化的西帕依溃结安灌肠液(简称溃结安)壳聚糖(CS)/β-甘油磷酸钠(β-GP)温敏凝胶,减少药物的损失,明确其释药能力的变化。方法 以温敏凝胶为载体,以胶凝时间为指标,通过单因素实验考察β-GP质量浓度、pH值、温度对温敏凝胶的影响。采用扫描电镜(SEM)表征凝胶的形状和表面形态,采用红外光谱仪(FTIR)表征凝胶胶凝前后的结构变化。通过载药温敏凝胶体外释放实验,评估凝胶释药能力。结果 溃结安温敏凝胶的胶凝温度为(37.0±4.5)℃,(6.00±0.82)min由液态转变成半固态,对药物的释放速度明显减慢,24 h时累积释放率仅为(67.78±0.35)%(n=3),而等量原料药24 h累积释放率为(90.43±0.62)%(n=3),释药行为接近Weibull模型,释药机制为药物扩散与凝胶溶蚀的双重机制。结论 在37.0 ℃时可实现溃结安溶胶到半固体凝胶的转变,CS/β-GP凝胶体系对溃结安的释放具有缓释性。

Objective By developing a rapid gelation chitosan (CS)/β-glycerophosphate (β-GP) thermosensitive hydrogel containing Kuijiean, to decrease the loss of drug and confirm the capabilities of the drug delivery. Methods Thermosensitive hydrogel was a carrier, gel time was chosen in this study as the index to investigate the effect of β-GP concentration, pH value, and temperature on the thermosensitive hydrogel by single factor experiments. The properties of the hydrogel were characterized regarding shape and surface morphology by using scaning electron microscopy (SEM); The chemical structure diversification of hydrogels upon gelation was charactered by FTIR spectrometer. By the experiments of the drug loaded thermosensitive hydrogel to deliver drug in vitro, the diversification of the capabilities of the drug delivery was evaluated. Results The temperature of Kuijiean thermosensitive hydrogel was (37.0 ± 4.5) ℃, by which the sol gel could transform into semi-solid gel at (6.00 ± 0.82) min, the drug release rate slowed down obviously, and the cumulative release rate was only (67.78 ± 0.35)% (n = 3) by 24 h, while the cumulative release rate of the equal quantity of raw material drug was (90.43 ± 0.62)% (n = 3) by 24 h. The release behavior was close to the Weibull model, the drug release mechanism was a double mechanism combining drug diffusion and gel erosion. Conclusion It is true that achieves the transformation of Kuijiean from sol to semi-solid gel at 37.0 ℃. The CS/β-GP gel system allows the sustained release of the Kuijiean.

国家自然科学基金资助项目(81160395)