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基于黄原胶和丙烯酸树脂的聚电解质复合物缓释片的体外-体内评价

In vitro-in vivo evaluation of xanthan gum and eudragit inter polyelectrolyte complex based sustained release tablets.

作者信息

Deb Tamal Krishna, Ramireddy B, Moin Afrasim, Shivakumar H G

机构信息

Department of Pharmaceutics, JSS College of Pharmacy, JSS University, Mysore, Karnataka, India.

出版信息

Int J Pharm Investig. 2015 Jan-Mar;5(1):65-72. doi: 10.4103/2230-973X.147236.

DOI:10.4103/2230-973X.147236
PMID:25599035
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4286837/
Abstract

INTRODUCTION

Polyelectrolyte complexes (PECs) are the association complexes formed between oppositely charged particles (e.g., polymer-polymer, polymer-drug and polymer-drug-polymer). These are formed due to electrostatic interaction between oppositely charged polyions. Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) advocated in use of painful and inflammatory rheumatic and certain non-rheumatic conditions. The drug has a relatively short elimination half-life, which limits the potential for drug accumulation. As an analgesic, it has a fast onset and long duration of action.

AIM

invitro-invivo evaluation of Xanthan gum and Eudragit E100 inter polyelectrolyte complex based sustained release tablet.

MATERIALS AND METHOD

Xanthan gum and Eudragit E100 were used as PEC and were prepared using different proportions i.e. in 1:1 to 1:6 ratio. The optimum ratio of E100 and XG was 1:6 used to characterize the IPC and the formulation of tablet. The tablets were prepared by wet granulation using PVP K30 as binder.

RESULTS AND DISCUSSION

FT-IR and DSC studies confirmed the formation of IPC. Scanning Electron Microscopy (SEM) studies showed highly porous tablet surface. The tablets were evaluated for hardness, weight variation, and drug content, found to be within limits. In vitro and in vivo studies concluded that tablets showed sustained release profile. The short term stability study of the optimized formulation indicated that the formulation was stable.

CONCLUSION

Since the Poly Electrolyte Complex delay the release of the drug, it can be employed in formulating sustained release matrix tablets.

摘要

引言

聚电解质复合物(PEC)是由带相反电荷的粒子(如聚合物-聚合物、聚合物-药物和聚合物-药物-聚合物)形成的缔合复合物。它们是由于带相反电荷的聚离子之间的静电相互作用而形成的。双氯芬酸是一种非甾体抗炎药(NSAID),常用于治疗疼痛性和炎症性风湿性疾病以及某些非风湿性疾病。该药物的消除半衰期相对较短,这限制了药物积累的可能性。作为一种镇痛药,它起效快且作用持续时间长。

目的

对基于黄原胶和丙烯酸树脂E100的聚电解质复合物缓释片进行体外-体内评价。

材料与方法

使用黄原胶和丙烯酸树脂E100作为PEC,并以不同比例(即1:1至1:6)制备。E100和XG的最佳比例为1:6,用于表征离子对复合物和片剂的配方。片剂通过湿法制粒制备,并使用PVP K30作为粘合剂。

结果与讨论

傅里叶变换红外光谱(FT-IR)和差示扫描量热法(DSC)研究证实了离子对复合物的形成。扫描电子显微镜(SEM)研究显示片剂表面具有高度多孔性。对片剂进行了硬度检测、重量差异检测和药物含量检测,结果均在规定范围内。体外和体内研究得出结论,片剂呈现缓释特性。对优化配方的短期稳定性研究表明该配方是稳定的。

结论

由于聚电解质复合物可延迟药物释放,因此可用于制备缓释基质片剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec4d/4286837/8510021eb8be/IJPI-5-65-g015.jpg
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