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评价改性薯蓣淀粉的材料和片剂成型性能。

Evaluation of the material and tablet formation properties of modified forms of Dioscorea starches.

机构信息

Department of Pharmaceutics and Biopharmaceutics, Institute of Pharmacy, Martin-Luther-University Halle-Wittenberg, Halle/Saale, Germany.

出版信息

Drug Dev Ind Pharm. 2009 Nov;35(11):1389-406. doi: 10.3109/03639040902960185.

Abstract

Starches obtained from four different Dioscorea species-namely, White yam (Dioscorea rotundata), Bitter yam (Dioscorea dumetorum), Chinese yam (Dioscorea oppositifolia), and Water yam (Dioscorea alata)-were modified by cross-linking, hydroxypropylation, and dual modification-cross-linking followed by hydroxypropylation. The physicochemical, material, and tablet properties of the modified starches were investigated with the aim of understanding their properties to determine their potential use for different applications. The tablet formation properties were assessed using 3D modeling, the Heckel equation, and force-displacement profiles. The analyzed tablet properties were elastic recovery, compactibility, and disintegration. The result indicates that the modifications generally increased the swelling power for all the starches in the rank order hydroxypropyl > hydroxypropylated cross-linked > cross-linked (CL) while the solubility did not show a clear-cut pattern. This indicates that hydroxypropylation generally showed the strongest effects on swelling. Furthermore, hydroxypropylation improved the hot water swelling of the CL starches. The modifications did not cause any detectable morphological change in the starch granules shape or size although slight rupture was observed in some granules. CL starch had the lowest water sorption capacity and hydroxypropylation increased the sorption capacity of the CL starches. The material property results indicate that hydroxypropylation and cross-linking did not significantly improve the flowability and compressibility but improved bonding, which resulted in an increased compaction and higher tablet crushing force even though they all disintegrated rapidly. Thus, the modified Dioscorea starches showed potentials for development as new excipients in solid dosage form design, and they could be useful as disintegrants or for Soft tableting.

摘要

从四种不同的薯蓣属植物中提取的淀粉,即白山药(薯蓣属圆山药)、苦山药(薯蓣属块茎)、山药(薯蓣属对叶)和水山药(薯蓣属),通过交联、羟丙基化和双改性-交联后羟丙基化进行改性。通过对改性淀粉的物理化学、材料和片剂性质进行研究,旨在了解其性质,确定其在不同应用中的潜在用途。通过 3D 建模、Heckel 方程和力-位移曲线来评估片剂的形成特性。分析的片剂性质包括弹性恢复、可压缩性和崩解性。结果表明,改性通常会按羟丙基化>羟丙基交联>交联(CL)的顺序增加所有淀粉的溶胀能力,而溶解度没有明显的规律。这表明羟丙基化通常对溶胀有最强的影响。此外,羟丙基化提高了 CL 淀粉的热水溶胀能力。尽管在一些颗粒中观察到轻微的破裂,但改性并没有导致淀粉颗粒形状或大小的任何可检测到的形态变化。CL 淀粉的吸水性最低,羟丙基化增加了 CL 淀粉的吸水性。材料性能结果表明,羟丙基化和交联并没有显著改善流动性和可压缩性,但改善了粘结性,从而导致压实度增加,片剂破碎力增加,尽管它们都迅速崩解。因此,改性薯蓣淀粉具有作为固体剂型设计中新型赋形剂的发展潜力,它们可用作崩解剂或用于软压片。

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