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基于反离子诱导聚集的盐酸齐多夫定复合藻酸盐水凝胶微粒给药系统

Composite alginate hydrogel microparticulate delivery system of zidovudine hydrochloride based on counter ion induced aggregation.

作者信息

Roy Harekrishna, Rao P Venkateswar, Panda Sanjay Kumar, Biswal Asim Kumar, Parida Kirti Ranjan, Dash Jharana

机构信息

Department of Pharmatechnology, Vikas College of Pharmaceutical Sciences, Suryapet, Nalgonda, Andhra Pradesh, India.

Department of Biosciences and Technology , VIT University, Vellore, Tamil Nadu, India.

出版信息

Int J Appl Basic Med Res. 2014 Sep;4(Suppl 1):S31-6. doi: 10.4103/2229-516X.140728.

Abstract

AIM

The present study deals with preparation of zidovudine loaded microparticle by counter ion induced aggregation method. During this study effect of polyacrylates and hypromellose polymers on release study were investigated.

MATERIALS AND METHODS

The ion induced aggregated alginate based microparticles were characterized for surface morphology, particle size analysis, drug entrapment study, in-vitro study, Fourier-transform infrared (FTIR) spectroscopy, and differential scanning calorimetry (DSC) study.

RESULTS AND DISCUSSION

The result showed Eudragit RL-100 (ERL) based formulations had smoother surface as well as their mean particle sizes were found greater compared with Eudragit RS-100 (ERS) microparticles. Furthermore, drug entrapments were found to be more in ERL formulae as compared with ERS. RL3 released 101.05% drug over a period of 8(th) h and followed Higuchi profile and Fickian diffusion. Moreover, data obtained illustrated that, higher amount of quaternary ammonium group, alkali value, and glass transition temperature may be possible reason for improving permeability of ERL based formulations. It was also noticed, hyroxypropyl methylcellulose (HPMC) K4M premium grade polymer sustained drug release more than HPMC K15M. In addition, drug-excipient interaction study was carried out by FTIR and DSC study.

摘要

目的

本研究采用反离子诱导聚集法制备齐多夫定载药微粒。在此研究过程中,考察了聚丙烯酸酯和羟丙甲纤维素聚合物对释放研究的影响。

材料与方法

对离子诱导聚集的海藻酸盐基微粒进行表面形态、粒度分析、药物包封研究、体外研究、傅里叶变换红外(FTIR)光谱和差示扫描量热法(DSC)研究。

结果与讨论

结果表明,与尤特奇RS - 100(ERS)微粒相比,基于尤特奇RL - 100(ERL)的制剂表面更光滑,平均粒径更大。此外,与ERS相比,ERL配方中的药物包封率更高。RL3在第8小时内释放了101.05%的药物,遵循 Higuchi 模型和菲克扩散。此外,获得的数据表明,较高的季铵基团含量、碱值和玻璃化转变温度可能是提高基于ERL的制剂渗透性的原因。还注意到,羟丙基甲基纤维素(HPMC)K4M高级聚合物的药物缓释效果比HPMC K15M更好。此外,通过FTIR和DSC研究进行了药物 - 辅料相互作用研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ecc1/4181129/2bac6e55953c/IJABMR-4-31-g002.jpg

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