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甲基丙烯酰胺接枝结冷胶作为缓释片剂基质的合成、表征及评价

Synthesis, characterization and evaluation of methacrylamide grafted gellan as sustained release tablet matrix.

作者信息

Nandi Gouranga, Patra Poushali, Priyadarshini Rosy, Kaity Santanu, Ghosh Lakshmi Kanta

出版信息

Int J Biol Macromol. 2015 Jan;72:965-74. doi: 10.1016/j.ijbiomac.2014.09.052.

DOI:10.1016/j.ijbiomac.2014.09.052
PMID:25316428
Abstract

In the present study, the microwave induced synthesis of polymethacrylamide-grafted-gellan gum (PMaa-g-GG) was carried out by free radical initiation using cerric (IV) ammonium nitrate (CAN) as redox initiator. Concentrations of methacrylamide (Maa), CAN and microwave irradiation time were taken as variable synthetic parameters. The modified polysaccharide obtained from different synthetic conditions was then characterized by FTIR, CHN analysis, DSC and powder X-ray diffraction. The yield and extent of grafting were assessed by determining percentage grafting, percentage grafting efficiency, percentage conversion and these were correlated with elemental analysis. The acute oral toxicity study of modified polysaccharide was performed as per OECD guideline. Histological comparison of different organs between control and test animal showed no significant difference. Sustained release tablets of diclofenac sodium (DS) were prepared with modified gellan. In vitro dissolution study showed the tablets were capable of releasing the drug over a period of 8 h.

摘要

在本研究中,以硝酸铈(IV)铵(CAN)作为氧化还原引发剂,通过自由基引发进行微波诱导合成聚甲基丙烯酰胺接枝结冷胶(PMaa-g-GG)。将甲基丙烯酰胺(Maa)、CAN的浓度以及微波辐照时间作为可变合成参数。然后,通过傅里叶变换红外光谱(FTIR)、CHN分析、差示扫描量热法(DSC)和粉末X射线衍射对不同合成条件下得到的改性多糖进行表征。通过测定接枝率、接枝效率百分比、转化率来评估接枝产率和接枝程度,并将这些与元素分析相关联。按照经合组织(OECD)指南进行改性多糖的急性口服毒性研究。对照动物和受试动物不同器官的组织学比较显示无显著差异。用改性结冷胶制备双氯芬酸钠(DS)缓释片。体外溶出度研究表明该片剂能够在8小时内释放药物。

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