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Melt Dispersion Adsorbed onto Porous Carriers: An Effective Method to Enhance the Dissolution and Flow Properties of Raloxifene Hydrochloride.
ASSAY and Drug Development Technologies ( IF 1.8 ) Pub Date : 2020-09-16 , DOI: 10.1089/adt.2020.990
Ashok Neelkanth Mahajan 1 , Naazneen Surti 1 , Priyal Patel 1 , Ashwini Patel 1 , Dimal Shah 1 , Vandana Patel 1
Affiliation  

The objective of the present investigation is to enhance the dissolution and flow properties of raloxifene hydrochloride (RXH), a biopharmaceutical classification system class II drug. Melt dispersion of RXH with polyethylene glycol (PEG) 6000 was prepared by the fusion method. The melt dispersion was then adsorbed onto a porous adsorbent, Neusilin, by the melt adsorption method. Response surface methodology was employed to establish the design space for formulation variables such as the ratio of RXH to PEG 6000 in melt dispersion and amount of porous adsorbent to melt dispersion. Differential scanning calorimetry, scanning electron microscopy, X-ray diffraction, Fourier-transform infrared spectroscopy, and accelerated stability techniques were utilized to characterize formulations. Negative Gibbs free energy values indicated spontaneous solubilization of RXH in PEG 6000. The time required for 80% of drug release from optimized formulation was <20 min compared with plain RXH. Accelerated stability studies confirmed the stabilization of amorphous melt dispersion in nanopores (nanoconfinement) of inorganic silicate Neusilin. Melt dispersion, adsorbed on porous carriers, is a promising technique to improve the dissolution characteristic as well as flow properties of drug molecules.

中文翻译:

吸附在多孔载体上的熔体分散体:一种提高盐酸雷洛昔芬溶解和流动性能的有效方法。

本研究的目的是提高雷洛昔芬盐酸盐 (RXH) 的溶出度和流动性,这是一种生物制药分类系统 II 类药物。RXH 与聚乙二醇 (PEG) 6000 的熔融分散体是通过熔融法制备的。然后通过熔体吸附法将熔体分散体吸附到多孔吸附剂 Neusilin 上。响应面方法用于建立配方变量的设计空间,例如熔体分散体中 RXH 与 PEG 6000 的比率以及多孔吸附剂与熔体分散体的量。差示扫描量热法、扫描电子显微镜、X 射线衍射、傅里叶变换红外光谱和加速稳定性技术被用来表征配方。负吉布斯自由能值表明 RXH 在 PEG 6000 中自发溶解。与普通 RXH 相比,从优化配方中释放 80% 的药物所需的时间 <20 分钟。加速稳定性研究证实了无定形熔体分散在无机硅酸盐 Neusilin 的纳米孔(纳米限制)中的稳定性。吸附在多孔载体上的熔体分散是一种很有前途的技术,可以改善药物分子的溶出特性和流动特性。
更新日期:2020-09-17
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