Li Wenyan, Huo Mengmeng, Sen Chaudhuri Arka, Yang Chen, Cao Dazhong, Wu Zhenghong, Qi Xiaole
Key Laboratory of Modern Chinese Medicines, China Pharmaceutical University, Nanjing, 210009, People's Republic of China.
J Mater Sci Mater Med. 2017 May;28(5):67. doi: 10.1007/s10856-017-5886-7. Epub 2017 Mar 23.
Currently, polysaccharide-based hydrogels are widely studied macromolecular networks to modify drug dissolution from controlled-releasing matrix tablets. Among them, polyelectrolyte complexes (PEC) films consisted of chitosan (CS) and sodium alginate (SA) could be obtained via spontaneously assembling under physiological gastrointestinal environment. Here, we utilized these self-assembled PEC films as an efficient coating materials to develop controlled-released matrix tablets through compression coating process, with paracetamol (APAP) as model drug. The constitutive and morphology characteristic studies on these PEC films illustrated that the mixture of CS and SA with the weight ratio of 1:1 would be an promising outer layer for compression-coating tablets. In addition, the in vitro drug releasing behavior experiments demonstrated that the optimized compression coating tablets displayed satisfied zero-order drug releasing profits. Furthermore, the in vivo pharmacokinetic studies of these APAP loaded compression-coated tablets in New Zealand rabbits gave that the T (12.32 ± 1.05 h) was significantly prolonged (p < 0.01), compared to that (0.89 ± 0.26 h) of common APAP tablets (Jinfuning) after oral administration. These studies suggest that the compression-coated tablets with self-assembled PEC film as coating outer layer may be a promising strategy for peroral controlled release delivery system of water soluble drugs.
目前，基于多糖的水凝胶是用于改变控释基质片剂中药物溶出度的广泛研究的大分子网络。其中，由壳聚糖（CS）和海藻酸钠（SA）组成的聚电解质复合物（PEC）薄膜可在生理胃肠道环境下通过自发组装获得。在此，我们利用这些自组装的PEC薄膜作为高效包衣材料，通过压制包衣工艺开发控释基质片剂，以对乙酰氨基酚（APAP）作为模型药物。对这些PEC薄膜的组成和形态特征研究表明，重量比为1:1的CS和SA混合物将是压制包衣片剂的有前景的外层。此外，体外药物释放行为实验表明，优化后的压制包衣片剂显示出令人满意的零级药物释放效果。此外，这些载有APAP的压制包衣片剂在新西兰兔体内的药代动力学研究表明，与口服普通APAP片剂（金芙宁）后的T（0.89±0.26小时）相比，T（12.32±1.05小时）显著延长（p＜0.01）。这些研究表明，以自组装PEC薄膜作为包衣外层的压制包衣片剂可能是水溶性药物口服控释给药系统的一种有前景的策略。
