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用于提高盐酸曲马多生物利用度的牙龈-藻酸盐聚合物微球:制剂与评价

Gum-Alginate Polymeric Microspheres to Enhance the Bioavailability of Tramadol Hydrochloride: Formulation and Evaluation.

作者信息

Noureen Shazia, Noreen Sobia, Ghumman Shazia Akram, Batool Fozia, Hameed Huma, Hasan Sara, Noreen Fozia, Elsherif Mervat A, Bukhari Syed Nasir Abbas

机构信息

Institute of Chemistry, University of Sargodha, Sargodha 40100, Pakistan.

College of Pharmacy, University of Sargodha, Sargodha 40100, Pakistan.

出版信息

Pharmaceutics. 2022 Apr 22;14(5):916. doi: 10.3390/pharmaceutics14050916.

Abstract

Combinations of polymers can improve the functional properties of microspheres to achieve desired therapeutic goals. Hence, the present study aimed to formulate gum (PAG) and sodium alginate microsphere for sustained drug release. Blended and coated microspheres were prepared using the ionotropic gelation technique. The effect of polymer concentration variation was studied on the structural and functional properties of formulated microspheres. FTIR, XRD, and thermal analysis were performed to characterize the microspheres. All the formulations were well-formed spherical beads having an average diameter from 579.23 ± 07.09 to 657.67 ± 08.74 μm. Microspheres entrapped drugs within the range 65.86 ± 0.26-83.74 ± 0.79%. The pH-dependent swelling index of coated formulations was higher than blended. FTIR spectra confirmed the presence of characteristic peaks of entrapped Tramadol hydrochloride showing no drug-polymer interaction. In vitro drug release profile showed sustained release following the Korsmeyer-Peppas kinetic model with an R value of 0.9803-0.9966. An acute toxicology study employing the oral route in Swiss albino mice showed no signs of toxicity. It can be inferred from these results that blending PAG with sodium alginate can enhance the stability of alginate microspheres and improve its drug release profile by prolonging the release time.

摘要

聚合物组合可以改善微球的功能特性,以实现预期的治疗目标。因此,本研究旨在制备用于药物缓释的果胶(PAG)和海藻酸钠微球。采用离子凝胶法制备了混合和包衣微球。研究了聚合物浓度变化对所制备微球的结构和功能特性的影响。通过傅里叶变换红外光谱(FTIR)、X射线衍射(XRD)和热分析对微球进行了表征。所有制剂均为形状良好的球形微珠,平均直径在579.23±07.09至657.67±08.74μm之间。微球包封药物的范围在65.86±0.26 - 83.74±0.79%之间。包衣制剂的pH依赖性溶胀指数高于混合制剂。傅里叶变换红外光谱证实了包封的盐酸曲马多特征峰的存在,表明不存在药物 - 聚合物相互作用。体外药物释放曲线显示,遵循Korsmeyer - Peppas动力学模型的缓释,R值为0.9803 - 0.9966。在瑞士白化小鼠中采用口服途径进行的急性毒理学研究未显示出毒性迹象。从这些结果可以推断,将PAG与海藻酸钠混合可以提高海藻酸钠微球的稳定性,并通过延长释放时间改善其药物释放曲线。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d63/9144292/2d84de64edf7/pharmaceutics-14-00916-g001.jpg

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