a Drug Discovery, Delivery and Patient Care (DDDPC), School of Life Sciences, Pharmacy and Chemistry , Kingston University London , Kingston-upon-Thames , UK.
b Aston Pharmacy School , Aston University , Birmingham , UK.
Pharm Dev Technol. 2018 Jun;23(5):442-453. doi: 10.1080/10837450.2017.1363775. Epub 2017 Aug 18.
The fast development in materials science has resulted in the emergence of new pharmaceutical materials with superior physical and mechanical properties. Low-substituted hydroxypropyl cellulose is an ether derivative of cellulose and is praised for its multi-functionality as a binder, disintegrant, film coating agent and as a suitable material for medical dressings. Nevertheless, very little is known about the compaction behaviour of this polymer. The aim of the current study was to evaluate the compaction and disintegration behaviour of four grades of L-HPC namely; LH32, LH21, LH11, and LHB1. The macrometric properties of the four powders were studied and the compaction behaviour was evaluated using the out-of-die method. LH11 and LH22 showed poor flow properties as the powders were dominated by fibrous particles with high aspect ratios, which reduced the powder flow. LH32 showed a weak compressibility profile and demonstrated a large elastic region, making it harder for this polymer to deform plastically. These findings are supported by AFM which revealed the high roughness of LH32 powder (100.09 ± 18.84 nm), resulting in small area of contact, but promoting mechanical interlocking. On the contrary, LH21 and LH11 powders had smooth surfaces which enabled larger contact area and higher adhesion forces of 21.01 ± 11.35 nN and 9.50 ± 5.78 nN, respectively. This promoted bond formation during compression as LH21 and LH11 powders had low strength yield.
材料科学的快速发展导致了具有优越物理和机械性能的新型药物材料的出现。低取代羟丙基纤维素是纤维素的醚衍生物，因其多功能性而备受赞誉，可用作粘合剂、崩解剂、薄膜包衣剂以及适合医用敷料的材料。然而，人们对这种聚合物的压缩行为知之甚少。本研究旨在评估四种等级的 L-HPC（即 LH32、LH21、LH11 和 LHB1）的压缩和崩解行为。研究了四种粉末的宏观性质，并采用模外法评估了其压缩行为。LH11 和 LH22 的流动性能较差，因为这些粉末主要由具有高纵横比的纤维状颗粒组成，这降低了粉末的流动性。LH32 的可压缩性较差，表现出较大的弹性区域，使得这种聚合物更难以塑性变形。这些发现得到了 AFM 的支持，AFM 显示 LH32 粉末的高粗糙度（100.09±18.84nm），导致接触面积小，但促进了机械互锁。相反，LH21 和 LH11 粉末具有光滑的表面，能够实现更大的接触面积和更高的粘附力，分别为 21.01±11.35nN 和 9.50±5.78nN。这促进了 LH21 和 LH11 粉末在压缩过程中形成键合，因为它们的屈服强度较低。
