低熔点药物在芝麻胶共磨混合物中的固态和溶解行为

Seham Shaboun, E. Nep, N. Ngwuluka, A. Adebisi, B. Conway, Alan M. Smith, K. Asare-Addo
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引用次数: 1

摘要

寻找无毒和成本有效的固体分散制剂载体增加了研究人员对可再生资源的关注。本研究从芝麻叶(Sesamum radiatum, SRG)中提取树胶,并研究其在布洛芬(Ibuprofen, IBU)固体分散制剂中的作用。采用IBU与SRG的不同配比(4:1、1:1、1:4),磨矿时间分别为1 min、5 min和10 min进行物理混合和研磨。采用DSC、FT-IR和XRPD对其进行了固态表征。研究了共磨比和共磨时间对药物溶出度的影响。固态表征表明,在固体分散配方中,SRG不与IBU相互作用。然而,SRG延缓了所有配方中IBU的释放。虽然共磨固体分散体的溶解率高于物理混合体(PM),但随着SRG比例的降低,溶解率也在增加,但该技术并未显著改善IBU的溶解率。配方周围的凝胶层表明,SRG可能被证明是一种有用的亲水载体,可以作为基质的缓释载体,也许胶的一种改性形式可以用于固体分散体。
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Solid state and dissolution behaviour of a low melting point drug in co-milled mixtures of Sesamum radiatum gum
The search for non-toxic and cost effective carriers for solid dispersion formulations has increased the focus of researchers on renewable resources. In this study, gum was extracted from the leaves of Sesamum radiatum (SRG) and its role in solid dispersion formulations of Ibuprofen (IBU) investigated. Physical mixing and comilling using different ratios of IBU to SRG (4:1, 1:1, 1:4) and milling times of 1 min, 5 min, and 10 min was employed. Solid state of these formulations was characterized using DSC, FT-IR and XRPD. The effect of the co-milling ratio and time on drug dissolution was also studied. Solid state characterization showed that SRG does not interact with IBU in the solid dispersion formulations. However, SRG retarded the release of IBU from all the formulations. Although the co-milled solid dispersions gave a higher dissolution than the physical mixes (PM), with the dissolution rate increasing as the ratio of SRG decreases, the technique did not result in appreciable improvement in the dissolution of IBU. The gel layer that surrounded the formulations suggest SRG may prove useful as a hydrophilic carrier in matrices for extended release and perhaps a modified form of the gum could be used in solid dispersions.
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