壳聚糖类型和浓度对离子凝胶-冷冻干燥法制备穿心莲内酯-壳聚糖微粒物理特性和释药行为的影响

R. Sari, M. Sugiarto, W. Amirah, H. Yusuf
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引用次数: 1

摘要

穿心莲内酯溶解度低,生物利用度低,半衰期短(t1/2 = 1.5-2小时),壳聚糖微颗粒有望改善其溶出度。因此,本研究以三聚磷酸钠(TPP)为交联剂,考察壳聚糖浓度对离子凝胶法制备的穿心莲内酯微颗粒体外释放的影响。此外,用19 cPs和50 cPs两种不同浓度的壳聚糖制备了微颗粒。结果表明,制备的微颗粒呈球形,大小呈非均相,红外光谱表明壳聚糖与TPP之间存在离子键。DTA热像图和XRD衍射图显示了晶体结构向非晶态转变。微颗粒中穿心花内酯的包封率(EE)约为78%,对壳聚糖浓度(19 cPs和50 cPs)没有影响。释放动力学遵循Higuchi模型,pH比穿心莲内酯物质高7±0.05。研究了穿心莲内酯壳聚糖微颗粒对其溶出率的提高作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
The Effect of Chitosan Type and Concentration on Physical Characteristics and Drug Release Behavior of Andrographolide-Chitosan Microparticles Prepared by Ionic Gelation – Freeze Drying
Andrographolide is low in solubility and bioavailability, with short half-life (t1/2 = 1.5-2 hours), with chitosan micro-particles expected to improve its dissolution. Therefore, the objective of this research was to investigate the effect of chitosan concentration and the in vitro release of andrographolide from micro-particles prepared by ionic gelation using sodium tripolyphosphate (TPP) as cross-linker. Furthermore, the micro-particles used were prepared with two different concentration of chitosan namely 19 cPs and 50 cPs. The result showed that the micro-particles obtained were spherical in shape and heterogeneous in size, with Infrared spectra indicating ionic bonding between chitosan and TPP. The DTA thermogram and XRD diffractogram exhibited a change in crystal structure to a more amorphous form. The entrapment efficiency (EE) of andrographolide in micro-particles was about 78%, with no impact on the chitosan concentrations (19 cPs and 50 cPs) affected by EE. The kinetics released was followed by the Higuchi model in phosphate buffer, with pH 7 ± 0,05 higher than the andrographolide substance. It was investigated that andrographolide-chitosan micro-particles had the ability to enhance its dissolution rate.
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