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首页> 外文期刊>Journal of Ocean University of China >Preparation and in vitro Release Performance of Sustained-release Captopril/Chitosan-gelatin Net-polymer Microspheres
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Preparation and in vitro Release Performance of Sustained-release Captopril/Chitosan-gelatin Net-polymer Microspheres

机译:卡托普利/壳聚糖-明胶净聚合物微球缓释制剂的制备及体外释放性能

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摘要

The captopril/Chitosan-gelatin net-polymer microspheres (CTP/CGNPMs) were prepared using Chitosan (CTS) and gelatin (GT) by the methods of emulsification, cross-linked reagent alone or in combination and microcrystalline cellulose (MCC) added in the process of preparation of microspheres, which aimed to eliminate dose dumping and burst phenomenon of microspheres for the improvement of the therapeutic efficiency and the decrease of the side effects of captopril (CTP). The results indicated that CTP/CGNPMs had a spherical shape, smooth surface and integral structure inside but no adhesive phenomena in the preparation. The size distribution ranged from 220 μm to 280 μm. The CTP release test in vitro demonstrated that CTP/CGNPMs played the role of retarding the release of CTP compared with ordinary CTP tablets. The release behaviors of CGNPMS were influenced by preparation conditions such as experimental material ratio (EMR) and composition of cross linking reagents. Among these factors, the EMR (1/4), CLR (FA+SPP) and 0.75% microcrystalline cellulose (MCC) added to the microspheres constituted the optimal scheme for the preparation of CTP/CGNPMs. The ER, DL and SR of CTP/CGNPMs prepared according to the optimal scheme were 46.23 + 4.51%, 9.95 ± 0.77% and 261 ± 42%, respectively. The CTP/CGNPMs had the good characteristics of sustained release of drug and the process of emulsification and cross-linking were simple and stable. The CGNPMs are likely to be an ideal sustained release formulation for water-soluble drugs.
机译:卡托普利/壳聚糖明胶网状聚合物微球(CTP / CGNPMs)是通过乳化方法,壳聚糖(CTS)和明胶(GT)制备的,单独或结合使用交联试剂,并在其中加入微晶纤维素(MCC)。微球的制备方法,旨在消除微球的剂量倾倒和破裂现象,从而提高治疗效率并降低卡托普利(CTP)的副作用。结果表明,CTP / CGNPMs具有球形,光滑的表面和内部完整的结构,但在制备过程中没有粘附现象。尺寸分布在220μm至280μm的范围内。体外CTP释放测试表明,与普通CTP片剂相比,CTP / CGNPM起到了延缓CTP释放的作用。 CGNPMS的释放行为受制备条件的影响,例如实验材料比(EMR)和交联剂的组成。在这些因素中,添加到微球中的EMR(1/4),CLR(FA + SPP)和0.75%微晶纤维素(MCC)构成了制备CTP / CGNPM的最佳方案。根据最佳方案制备的CTP / CGNPM的ER,DL和SR分别为46.23 + 4.51%,9.95±0.77%和261±42%。 CTP / CGNPM具有良好的药物缓释特性,其乳化和交联过程简单,稳定。 CGNPM可能是水溶性药物的理想缓释制剂。

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