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基于壳聚糖的原位形成聚电解质复合物:一种用于高剂量药物的潜在持续给药聚合物载体。

Chitosan based in situ forming polyelectrolyte complexes: A potential sustained drug delivery polymeric carrier for high dose drugs.

作者信息

Lal Niharika, Dubey Juhi, Gaur Praveen, Verma Navneet, Verma Anurag

机构信息

Department of Pharmaceutics, School of Pharmaceutical Sciences, IFTM University, Moradabad, Uttar Pradesh, 244001, India.

Department of Pharmaceutics, School of Pharmaceutical Sciences, IFTM University, Moradabad, Uttar Pradesh, 244001, India.

出版信息

Mater Sci Eng C Mater Biol Appl. 2017 Oct 1;79:491-498. doi: 10.1016/j.msec.2017.05.051. Epub 2017 May 10.

Abstract

The present study investigated the feasibility of using combination of Cationic and anionic polymers as sustained release carrier for the delivery of high dose gastric acid soluble model drug Paracetamol. Various formulations were prepared using wet granulation technique. Briefly a cooled (4°C) neutral solution of chitosan (CH) was combined with cooled aqueous solution (4°C) of anionic polymer such as Gum Ghatti (GG) and Xanthan gum (XG). This polyelectrolyte solution was then used to granulate the model drug Paracetamol. The prepared tablets were evaluated for various pharmacopoeial and non pharmacopoeial parameters viz. Thickness, Hardness, Friability, Weight Variation, Content uniformity and Drug Content. The drug release study carried out in 0.1M HCl revealed in situ Polyelectrolyte complex formation (PEC) between CH and anionic biopolymers. This in situ PEC formation resulted in sustained delivery of high dose gastric fluid soluble drug Paracetamol. Further, effect of incorporation starch and lactose as tablet diluents on release rate was also studied. It was observed that paracetamol release from lactose granulation was faster than tablets prepared with starch as diluents. From the data generated it was concluded that In situ PEC formation approach has sufficient potential to sustain the release of drugs like paracetamol.

摘要

本研究考察了使用阳离子聚合物与阴离子聚合物的组合作为高剂量胃酸溶性模型药物对乙酰氨基酚缓释载体的可行性。采用湿法制粒技术制备了各种制剂。简要来说,将壳聚糖(CH)的冷却(4°C)中性溶液与阴离子聚合物如阿拉伯胶(GG)和黄原胶(XG)的冷却水溶液(4°C)混合。然后用这种聚电解质溶液对模型药物对乙酰氨基酚进行制粒。对制备的片剂进行了各种药典和非药典参数的评估,即厚度、硬度、脆碎度、重量差异、含量均匀度和药物含量。在0.1M盐酸中进行的药物释放研究表明,CH与阴离子生物聚合物之间形成了原位聚电解质复合物(PEC)。这种原位PEC的形成导致了高剂量胃酸溶性药物对乙酰氨基酚的持续释放。此外,还研究了加入淀粉和乳糖作为片剂稀释剂对释放速率的影响。观察到对乙酰氨基酚从乳糖制粒中的释放比以淀粉作为稀释剂制备的片剂更快。根据所获得的数据得出结论,原位PEC形成方法具有足够的潜力来维持对乙酰氨基酚等药物的释放。

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