Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Santiago de Compostela, Santiago de Compostela, Spain.
Drug Dev Ind Pharm. 2013 Jul;39(7):1107-12. doi: 10.3109/03639045.2012.713363. Epub 2012 Aug 31.
Particles composed of 90:10 or 80:20 mixtures of the hyperbranched poly(esteramide) Hybrane S1200 and the poorly water-soluble drug hydrochlorothiazide were produced by hot melt extrusion at maximum temperatures of 90°C without any need for addition of a plasticizer. In dissolution rate assays in USP 29 apparatus II, particles of the smallest size category (<250 µm) containing 10% of hydrochlorothiazide released 95% of their load within 5 min. This fast release is attributed to the combination of the high solubility of Hybrane S1200, the dispersion of the drug in non-crystalline form in the polymer matrix (attested to by the results of powder X-ray diffractometry, and scanning electron microscopy), and to the fact that the main interaction between drug and polymer is through hydrogen bonds (attested to by ATR-IR difference spectra).
采用热熔挤出法，在最高温度为 90°C 的条件下，无需添加增塑剂，即可将 90:10 或 80:20 的超支化聚酯酰胺 Hybrane S1200 与难溶性药物氢氯噻嗪组成的颗粒制备出来。在 USP 29 仪器 II 中的溶出速率试验中，载药量为 10%的最小粒径 (<250 µm) 的颗粒在 5 min 内释放了 95%的药物。这种快速释放归因于 Hybrane S1200 的高溶解度、药物以无定形形式分散在聚合物基质中的特性（粉末 X 射线衍射和扫描电子显微镜的结果可以证明），以及药物和聚合物之间的主要相互作用是通过氢键（ATR-IR 差谱可以证明）。
