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西米淀粉衍生的羟丙基淀粉钠:一种增强制剂性能的有效超级崩解剂。

Sago-Starch-Derived Sodium Starch Glycolate: An Effective Superdisintegrant to Enhance Formulation Performance.

作者信息

Putra Okta Nama, Musfiroh Ida, Paramitasari Derina, Pudjianto Karjawan, Ikram Emmy Hainida Khairul, Chaidir Chaidir, Muchtaridi Muchtaridi

机构信息

Doctoral Program of Pharmacy, Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Jatinangor 45363, Indonesia.

Research Center for Agroindustry, Research Organization for Agriculture and Food, National Research and Innovation Agency (BRIN), Tangerang 15314, Indonesia.

出版信息

Polymers (Basel). 2025 Apr 28;17(9):1208. doi: 10.3390/polym17091208.

Abstract

This study focused on optimizing sago-starch-derived sodium starch glycolate (SSG) as a superdisintegrant using a Response Surface Methodology (RSM). The aim was to enhance the formulation performance by achieving an optimal degree of substitution (DS) in the synthesis of SSG from sago starch and evaluating its performance in mefenamic acid tablet formulation. The SSG was synthesized using an organic solvent slurry method, which involves crosslinking starch with sodium trimetaphosphate (STMP) and substituting it with sodium monochloroacetate (SMCA). The reaction conditions, including the temperature, SMCA ratio, and reaction time, were optimized using the RSM. The optimal conditions were identified as a temperature range of 45-55 °C, an SMCA ratio of 0.75-1.5, and a reaction time of 120-240 min. The maximum predicted DS value was 0.24, with a validated DS value of 0.246 ± 0.021. The SSG-containing mefenamic acid formulation met USP standards and showed a superior disintegration time compared to the existing SSG. The optimized SSG derived from sago starch can be effectively used as a superdisintegrant in pharmaceutical formulations, offering a sustainable and economically viable alternative source of SSG. This contributes to the development of more effective drug delivery systems and promotes sustainable agriculture in Indonesia.

摘要

本研究聚焦于使用响应面法(RSM)优化西米淀粉衍生的羟丙基二淀粉磷酸酯(SSG)作为超级崩解剂。目的是通过在由西米淀粉合成SSG的过程中实现最佳取代度(DS)并评估其在甲芬那酸片剂配方中的性能,来提高配方性能。SSG采用有机溶剂淤浆法合成,该方法涉及用偏磷酸钠(STMP)使淀粉交联并用一氯乙酸钠(SMCA)进行取代。使用RSM对反应条件,包括温度、SMCA比例和反应时间进行了优化。确定的最佳条件为温度范围45 - 55°C、SMCA比例0.75 - 1.5以及反应时间120 - 240分钟。预测的最大DS值为0.24,验证后的DS值为0.246±0.021。含SSG的甲芬那酸配方符合美国药典标准,与现有的SSG相比崩解时间更短。源自西米淀粉的优化SSG可有效地用作药物制剂中的超级崩解剂,提供了一种可持续且经济可行的SSG替代来源。这有助于开发更有效的药物递送系统,并促进印度尼西亚的可持续农业发展。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d0b9/12073232/94276d0e47f4/polymers-17-01208-g001.jpg

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