von Eggelkraut-Gottanka Stephan G, Abed Salah Abu, Müller Wolfgang, Schmidt Peter C
Department of Pharmaceutical Technology, Auf der Morgenstelle 8, D-72076 Tübingen, Germany.
Pharm Dev Technol. 2002 Nov;7(4):433-45. doi: 10.1081/pdt-120015046.
The purpose of this study was to investigate the influence of roller compaction parameters on granule and tablet quality of a dry herbal extract from St. John's wort (Hypericum perforatum L.), which is widely used in the treatment of mild to moderate depressive disorders. Eight different extract batches were blended with 0.5, 2, and 5% of magnesium stearate and were compacted at different compaction forces using a gap width and force controlled roller compactor. The ribbon formed was milled into granules having mean particle sizes up to 700 microns. The roller compaction of the extracts decreased significantly the angle of repose from about 45 to 32 degrees and the Hausner ratio from about 1.2 to 1.1. Tabletting of granulated extract instead of extract powder effectively reduced not only dust and feeding problems during the tabletting process but also prevented capping. The incorporation of 2 and 5% of magnesium stearate into the roller compacted extract reduced significantly the sticking of the dry herbal extracts to the punch faces without affecting the crushing strength of the tablets. Tablets containing granulated extracts exhibited a 3-fold lower disintegration time of about 12 min compared to tablets containing extract powder. Dissolution studies revealed that hyperforin, hypericin, and rutin were more rapidly released from tablets containing granulated extract. Therefore, roller compaction leveled out the differences in technological properties between the eight dry herbal extracts and compression of granulated extract significantly improved tablet quality.
本研究的目的是调查滚压参数对贯叶连翘(Hypericum perforatum L.)干燥草药提取物颗粒和片剂质量的影响,贯叶连翘广泛用于治疗轻至中度抑郁症。将八个不同的提取物批次与0.5%、2%和5%的硬脂酸镁混合,并使用间隙宽度和压力控制的滚压机在不同的压力下进行压实。形成的条带被研磨成平均粒径达700微米的颗粒。提取物的滚压显著降低了休止角,从约45度降至32度,哈斯纳比从约1.2降至1.1。用颗粒提取物而非提取物粉末压片不仅有效减少了压片过程中的粉尘和进料问题,还防止了裂片。在滚压提取物中加入2%和5%的硬脂酸镁可显著降低干燥草药提取物与冲头表面的粘连,且不影响片剂的抗压强度。与含有提取物粉末的片剂相比,含有颗粒提取物的片剂崩解时间约为12分钟,降低了三倍。溶出度研究表明,金丝桃素、金丝桃苷和芦丁从含有颗粒提取物的片剂中释放得更快。因此,滚压消除了八种干燥草药提取物在工艺性能上的差异,颗粒提取物的压片显著提高了片剂质量。