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Development of metformin hydrochloride loaded dissolving tablets with novel carboxymethylcellulose/poly-l-lysine/TPP complex.
International Journal of Biological Macromolecules ( IF 7.7 ) Pub Date : 2020-03-26 , DOI: 10.1016/j.ijbiomac.2020.03.191
Qing-Xi Wu 1 , Zi-Dan Wang 2 , Meng-Fei Zheng 3 , Ting Su 3 , Xiao-Hui Wang 3 , Yi-Xin Guan 4 , Yan Chen 1
Affiliation  

Natural polymers like polysaccharides, polypeptides and their derivatives are broadly applied in drug delivery due to excellent biocompatibility and biodegradability. In this study, the dissolving tablets, formed with carboxymethylcellulose/poly-l-lysine/tripolyphosphate (CMC/PLL/TPP) complex, were prepared using metformin hydrochloride (MetHCl) as model drug. Confocal laser scanning microscopy observation manifested that FITC-labeled PLL interacted with CMC and formed a uniform interior microstructure. Scanning electron microscope images showed the drug-loaded tablets had well-formed shapes with smooth surfaces. MetHCl embedded interior the microstructures of the tablets and represented in a crystal form. Thermo-gravimetric analysis and differential scanning calorimetry indicated that the drug-loaded tablets had stable thermal properties with less moisture content (3.52%). Fourier transform infrared spectrometer confirmed that the CMC/PLL/TPP complex was fabricated via the electrostatic interactions between -NH3+, -COO- and -[P2O54-]- groups. The drug-loaded tablets had a high drug loading efficiency of 85.76% and drug encapsulation efficiency of 81.47%, and a shorter wetting time of 2.16 min in SSF (pH 6.8) and lower swelling ratio of 233.34%. The drug loaded in the samples could be released completely within 10 min in simulated saliva fluid (SSF pH 6.8), indicating a rapid drug release and dissolving profile in the environment, which could be developed for dissolving tablets.

中文翻译:

用新型羧甲基纤维素/聚-1-赖氨酸/ TPP复合物开发盐酸二甲双胍溶出片。

天然聚合物(如多糖,多肽及其衍生物)具有出色的生物相容性和生物降解性,因此广泛用于药物输送。在这项研究中,使用盐酸二甲双胍(MetHCl)作为模型药物,制备了由羧甲基纤维素/聚-1-赖氨酸/三聚磷酸盐(CMC / PLL / TPP)复合物形成的溶解片剂。共聚焦激光扫描显微镜观察表明,FITC标记的PLL与CMC相互作用并形成均匀的内部微观结构。扫描电子显微镜图像显示载药的片剂具有良好的形状,具有光滑的表面。MetHCl嵌入片剂的微结构内部,并以晶体形式表示。热重分析和差示扫描量热法表明,载药片剂具有稳定的热性能,且水分含量较低(3.52%)。傅里叶变换红外光谱仪证实,CMC / PLL / TPP络合物是通过-NH3 +,-COO-和-[P2O54-]-基团之间的静电相互作用制备的。载药片剂的载药率高,达85.76%,包封率达81.47%,在SSF(pH 6.8)中的润湿时间较短,为2.16min,溶胀率较低,为233.34%。样品中加载的药物可以在10分钟内在模拟唾液(SSF pH 6.8)中完全释放,这表明药物在环境中的释放和溶解特性迅速,可以开发用于溶解片剂的药物。傅里叶变换红外光谱仪证实,CMC / PLL / TPP络合物是通过-NH3 +,-COO-和-[P2O54-]-基团之间的静电相互作用制备的。载药片剂的载药率高,达85.76%,包封率达81.47%,在SSF(pH 6.8)中的润湿时间较短,为2.16min,溶胀率较低,为233.34%。样品中加载的药物可以在10分钟内在模拟唾液(SSF pH 6.8)中完全释放,这表明药物在环境中的释放和溶解特性迅速,可以开发用于溶解片剂的药物。傅里叶变换红外光谱仪证实,CMC / PLL / TPP络合物是通过-NH3 +,-COO-和-[P2O54-]-基团之间的静电相互作用制备的。载药片剂的载药率高,达85.76%,包封率达81.47%,在SSF(pH 6.8)中的润湿时间较短,为2.16min,溶胀率较低,为233.34%。样品中加载的药物可以在10分钟内在模拟唾液(SSF pH 6.8)中完全释放,这表明药物在环境中的释放和溶解特性迅速,可以开发用于溶解片剂的药物。在SSF(pH 6.8)中润湿时间缩短了2.16分钟,溶胀率降低了233.34%。样品中加载的药物可以在10分钟内在模拟唾液(SSF pH 6.8)中完全释放,这表明药物在环境中的释放和溶解特性迅速,可以开发用于溶解片剂的药物。在SSF(pH 6.8)中润湿时间缩短了2.16分钟,溶胀率降低了233.34%。样品中加载的药物可以在10分钟内在模拟唾液(SSF pH 6.8)中完全释放,这表明药物在环境中的释放和溶解特性迅速,可以开发用于溶解片剂的药物。
更新日期:2020-03-27
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