Droplet‐Templated Antisolvent Spherical Crystallization of Hydrophilic and Hydrophobic Drugs with an in situ Formed Binder,Advanced Healthcare Materials

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Droplet‐Templated Antisolvent Spherical Crystallization of Hydrophilic and Hydrophobic Drugs with an in situ Formed Binder
Advanced Healthcare Materials ( IF 10.0 ) Pub Date : 2017-09-29 , DOI: 10.1002/adhm.201700797
Tonghan Gu ₁ , Eunice W. Q. Yeap ₂ , Zheng Cao ₁ , Denise Z. L. Ng ₂ , Yinying Ren ₁ , Ran Chen ₁ , Saif A. Khan ₂ , T. Alan Hatton ₁

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This study presents a novel droplet‐templated antisolvent spherical crystallization method applicable to both hydrophilic and hydrophobic drugs. In both cases, an alginate hydrogel binder forms in situ, concurrently with the crystallization process, effectively binding the drug crystals into monodisperse spheres. This study presents a detailed process description with mass transfer modeling, and with characterization of the obtained alginate/drug spheres in terms of morphology, composition, and drug loading. Although glycine and carbamazepine are used as model hydrophilic and hydrophobic drugs, this method is easily generalized to other drugs, and offers several benefits such as minimal thermal impact, fast crystallization rates, high drug–binder loading ratios, and high selectivity toward metastable polymorphs.

中文翻译：

具有原位形成的粘合剂的亲水性和疏水性药物的液滴模板反溶剂球形结晶

这项研究提出了一种适用于亲水性和疏水性药物的新型液滴模板抗溶剂球形结晶方法。在两种情况下，藻酸盐水凝胶粘合剂都与结晶过程同时形成，从而有效地将药物晶体结合到单分散球体中。这项研究通过传质建模以及获得的藻酸盐/药物球的形态，组成和载药量表征，对过程进行了详细描述。尽管甘氨酸和卡马西平被用作亲水性和疏水性药物的模型，但该方法易于推广到其他药物，并具有多种优势，例如最小的热影响，快速的结晶速率，高的药物结合剂负载率以及对亚稳多晶型物的高选择性。

更新日期：2017-09-29

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