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使用单冲压片机和旋转压片机对包有尤特奇NE的胃滞留微丸进行可压性研究。

Compressibility of gastroretentive pellets coated with Eudragit NE using a single-stroke and a rotary tablet press.

作者信息

Łunio Rafał, Sawicki Wieslaw, Skoczeń Przemysław, Walentynowicz Olga, Kubasik-Juraniec Jolanta

机构信息

Department of Pharmaceutical Technology, Medical University of Gdańsk, Gdańsk, Poland.

出版信息

Pharm Dev Technol. 2008;13(4):323-31. doi: 10.1080/10837450802089206.

Abstract

In this study, 15 kinds of powders with different compression mechanisms were used in the process of filling-binding substances in tablets with pellets. Applied substances possessed dominant brittle time-independent mechanism or time-dependent viscoplastic, viscoelastic mechanism of compression. Using 6 kN compression force in a single-stroke tablet press during 150 ms of compression, damage to the polymer film and pellet core was found in all formulations. As a result, the authors observed an increase of releasing rate of verapamil hydrochloride (VH). A larger contact area between powders and pellets and connected with this better protective properties were ensured by powders with time-independent compression mechanism (eg, D-sorbitol or D-mannitol). Unsymmetrically applied compression force was a reason for inconsistent densification and insufficient protection of the pellets. Taking into consideration the low rotation speed of the turret (10 rpm) in the rotary tablet press, the total compaction time was much longer than in the single-stroke tablet press. The compression time in the case of the rotary tablet press should be considered as the sum of the precompression (about 130 ms) and main compression (about 280 ms) phase times. Compression force applied by upper and lower punch in the precompression and main compression phase was affected uniformly on the pellets' surface, and when protected against fragmentation, allowed only some slight deformation. The powders in tablet formulation were fragmentized and rearranged independent of their compression mechanisms. It was found that the releasing rate of VH from pellets compressed by rotary tablet press with 6, 12, and 18 kN of compression force was similar to the releasing rate from uncompressed pellets.

摘要

在本研究中,15种具有不同压缩机制的粉末被用于含微丸片剂的填充-黏合物质过程。所应用的物质具有占主导地位的脆性时间无关机制或时间相关的黏塑性、黏弹性压缩机制。在单冲压片机中使用6 kN的压缩力,压缩150 ms,发现在所有配方中聚合物膜和微丸核心均受到损伤。结果,作者观察到盐酸维拉帕米(VH)释放速率增加。具有时间无关压缩机制的粉末(如D-山梨醇或D-甘露糖醇)确保了粉末与微丸之间更大的接触面积,并因此具有更好的保护性能。不对称施加的压缩力是微丸致密化不一致和保护不足的原因。考虑到旋转压片机中转盘的低转速(10 rpm),总压实时间比单冲压片机长得多。旋转压片机的压缩时间应视为预压缩(约130 ms)和主压缩(约280 ms)阶段时间之和。上下冲头在预压缩和主压缩阶段施加的压缩力均匀地作用于微丸表面,在防止破碎的情况下,仅允许一些轻微变形。片剂配方中的粉末破碎并重新排列,与它们的压缩机制无关。发现用6、12和18 kN压缩力的旋转压片机压缩的微丸中VH的释放速率与未压缩微丸的释放速率相似。

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