Picker K M
Martin-Luther-University Halle-Wittenberg, Institute of Pharmaceutical Technology and Biopharmacy, Halle/Saale, Germany.
Eur J Pharm Biopharm. 1999 Jul;48(1):27-36. doi: 10.1016/s0939-6411(99)00009-0.
The modulation of tableting and release behavior of combinations of kappa-carrageenan Gelcarin((R)) GP 911 NF and microcrystalline cellulose (MCC) Avicel((R)) PH 101 has been evaluated. Graded binary mixtures were tableted to a maximum relative density of 0.850 at the maximum displacement of the upper punch. Additionally, ternary mixtures with the same ratios of kappa-carrageenan and MCC and a constant percentage of theophylline monohydrate (20% (v/v)) were tested for their release behavior. Tablets produced from pure kappa-carrageenan deformed more elastically than pure MCC, the tablets produced were stable but not at the same degree as those made from MCC. Scanning electron microscopy (SEM) pictures showed that for MCC a smooth surface of the tablets resulted, tablets made from kappa-carrageenan showed less 'fusion' and thus more mechanical interlocking is responsible for their stability. Binary mixtures showed a continuous change in compaction properties from plastic to elastic deformation. All ternary mixtures with theophylline deformed more plastically than the binary mixtures, the change in deformation properties remained the same. Theophylline reduced the crushing strength due to its different fracture properties. The ternary mixtures showed different release mechanisms: Fast release up to 20% (v/v) kappa-carrageenan, slower release starting from 30% (v/v). The kinetics of release tended at 70% (v/v) more clearly towards zero-order kinetics. This change in release is in accordance with a change in swelling of tablets made of the binary mixtures.
已对κ-卡拉胶Gelcarin((R)) GP 911 NF与微晶纤维素(MCC)Avicel((R)) PH 101组合的压片和释放行为进行了调制评估。将分级二元混合物在上冲头的最大位移下压片至最大相对密度0.850。此外,还测试了具有相同κ-卡拉胶和MCC比例以及恒定百分比一水合茶碱(20%(v/v))的三元混合物的释放行为。由纯κ-卡拉胶制成的片剂比纯MCC更具弹性变形,所生产的片剂是稳定的,但程度不如由MCC制成的片剂。扫描电子显微镜(SEM)图片显示,对于MCC,片剂表面光滑,由κ-卡拉胶制成的片剂显示出较少的“融合”,因此更多的机械互锁是其稳定性的原因。二元混合物的压实性能从塑性变形到弹性变形呈现连续变化。所有含茶碱的三元混合物比二元混合物更具塑性变形,变形性能的变化保持不变。由于其不同的断裂特性,茶碱降低了抗压强度。三元混合物表现出不同的释放机制:κ-卡拉胶含量高达20%(v/v)时快速释放,从30%(v/v)开始释放较慢。在70%(v/v)时,释放动力学更明显地趋向于零级动力学。这种释放变化与二元混合物制成的片剂的溶胀变化一致。