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研究将果胶和壳聚糖用作丸剂配方中的天然赋形剂。

Investigation of using pectin and chitosan as natural excipients in pellet formulation.

机构信息

Department of Pharmaceutics, School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.

Department of Pharmaceutics, School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran; Nanotechnology Research Center, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.

出版信息

Int J Biol Macromol. 2018 Dec;120(Pt A):1208-1215. doi: 10.1016/j.ijbiomac.2018.08.129. Epub 2018 Aug 27.

Abstract

This study aimed to evaluate the potential of applying pectin and chitosan polysaccharides in pellet formulation. These biopolymers have advantages such as biocompatibility, low toxicity, low price and easy processing which make them interesting candidates for drug delivery purposes. Careful control of pellet porosity is essential to achieve an appropriate drug release profile. Replacing microcrystalline cellulose (MCC) with polysaccharides, especially pectin, leads to increased pellet porosity. Theophylline, dimenhydrinate and ibuprofen were chosen as model drugs. Investigation of possible ionic interactions between drugs and excipients is crucial to optimize the formulation of pellets with acceptable drug release. Differential scanning calorimetry of chitosan showed an endothermic peak; however, this peak was not observed in thermograms of the pectin, implying the lack of interaction between polysaccharides. Fourier transform infrared analysis did not indicate any interaction between drugs and polymers. Incorporation of MCC into the pellet formulation significantly increased the mean dissolution time while substitution of MCC with polysaccharides led to a faster release for each of the three drugs - that were different in their net charges - in both acidic and buffer media. These results highlight the potential value of polysaccharides in improving drug delivery characteristics of pharmaceutical pellets.

摘要

本研究旨在评估将果胶和壳聚糖多糖应用于微丸制剂的潜力。这些生物聚合物具有生物相容性、低毒性、低价格和易于加工等优点,使其成为药物传递目的的有趣候选物。仔细控制微丸的孔隙率对于实现适当的药物释放曲线至关重要。用多糖代替微晶纤维素(MCC),特别是果胶,会导致微丸的孔隙率增加。茶碱、茶苯海明和布洛芬被选为模型药物。研究药物和赋形剂之间可能存在的离子相互作用对于优化具有可接受药物释放的微丸制剂至关重要。壳聚糖的差示扫描量热法显示出吸热峰;然而,在果胶的热谱中没有观察到这个峰,这表明多糖之间没有相互作用。傅里叶变换红外分析也没有表明药物和聚合物之间存在任何相互作用。将 MCC 掺入微丸制剂中显著增加了平均溶出时间,而用多糖替代 MCC 则导致三种药物(净电荷不同)在酸性和缓冲介质中的释放速度更快。这些结果突出了多糖在改善药物传递特性方面的潜在价值。

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