水溶性聚合物对含二甲双胍的漂浮型黏膜黏附片体外性能的影响

Influence of water-soluble polymers on the in vitro performance of floating mucoadhesive tablets containing metformin.

作者信息

Rajab Mazen, Jouma Muhidien, Neubert Reinhard H H, Dittgen Michael

机构信息

Faculty of Pharmacy, Arab International University , Ghabaghib/Daraa, Damascus , Syrian Arab Republic and.

出版信息

Drug Dev Ind Pharm. 2014 Jul;40(7):879-85. doi: 10.3109/03639045.2013.789052. Epub 2013 Apr 22.

Abstract

CONTEXT

The in vitro performance of floating mucoadhesive metformin tablets was optimized using different polymer ratios of polyvinylpyrrolidone (PVP) tamarind seed gum (TSG) and hydroxypropylmethylcellulose (HPMC).

OBJECTIVE

The objectives of this investigation were to investigate the combinatorial effects of PVP, TSG and HPMC; to study the work of adhesion measured on stainless steel (Wss) and on rabbit gastric mucosa (Wgm); and a comparison of hydrophilic and more hydrophobic tablets.

MATERIAL AND METHODS

In vitro performance was measured as tablet hardness (H), tablet floating lag time (FLT), time needed to release 60% of drug content (t60%), swelling thickness (S), Wss and Wgm. To compare the effects, a simplex lattice mixture design was used.

RESULTS AND DISCUSSION

H, FLT, Wss and Wgm were found dependent on polymer ratio. H was increased when PVP ratio was increased. FLT, Wss and Wgm were increased when HPMC ratio was increased. The p value for the lack of fit for all models were greater than 0.05. An approximate linear correlation between Wgm and Wss was established (R(2) = 0.71). The tablets containing PVP resulted in larger H, shorter FLT and t60%, whereas Wss and Wgm were enhanced.

CONCLUSION

The different in vitro performance of tablets containing different water-soluble polymers could be explained partially by the differences in the hydrophilic properties of the polymers and the ability of PVP to interact with HPMC or TSG. An equation established is used to conclude mucoadhesion based on adhesion measurements on stainless steel.

摘要

背景

使用不同比例的聚乙烯吡咯烷酮(PVP)、罗望子胶(TSG)和羟丙基甲基纤维素(HPMC)对漂浮型黏附性二甲双胍片的体外性能进行了优化。

目的

本研究的目的是研究PVP、TSG和HPMC的组合效应;研究在不锈钢上(Wss)和兔胃黏膜上(Wgm)测量的黏附功;以及比较亲水性和疏水性更强的片剂。

材料与方法

通过片剂硬度(H)、片剂漂浮滞后时间(FLT)、释放60%药物含量所需时间(t60%)、溶胀厚度(S)、Wss和Wgm来测定体外性能。为了比较效果,采用了单纯形格子混合设计。

结果与讨论

发现H、FLT、Wss和Wgm取决于聚合物比例。当PVP比例增加时,H增加。当HPMC比例增加时,FLT、Wss和Wgm增加。所有模型失拟的p值均大于0.05。建立了Wgm和Wss之间的近似线性相关性(R(2) = 0.71)。含有PVP的片剂导致更大的H、更短的FLT和t60%,而Wss和Wgm增强。

结论

含有不同水溶性聚合物的片剂不同的体外性能可以部分地通过聚合物亲水性的差异以及PVP与HPMC或TSG相互作用的能力来解释。基于在不锈钢上的黏附测量建立的一个方程用于推断黏附性。

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