Lunio R, Sawicki W
Department of Pharmaceutical Technology, Medical University of Gdansk, Poland.
Pharmazie. 2008 Oct;63(10):731-5.
The influence of pellet core ingredients on pellet behaviour, e.g. during compression, is well known. In this study the influence of components of a Kollicoat SR polymer film on mechanical properties was investigated. The aim of this study was to evaluate the influence of polymer film components on the mechanical properties of the pellet as a whole, from the point of view of tableting. Tablets should disintegrate into undeformed pellets floating in this environment for 5-6 h, releasing the model drug--verapamil hydrochloride--if possible in a controlled way. The usefulness of texture analysis and work of compression measurement was also evaluated. Kollicoat SR in the form of a 30D aqueous dispersion was chosen as the main component of the polymer film. Polyvinyl pyrrolidone K-30 as a pore former, and propylene glycol, triethyl citrate and dibutyl sebacate plasticisers were selected as typical additives. The influence of different thickness of polymer film on behaviour during stress was also evaluated. After coating the cores with a 20 microm Kollicoat SR dispersion film, an increase in mechanical strength, in comparison to the pellet core, was observed (2.74 to 3.34 mJ). Addition of porophor increased the work of compression by 50% to 5.1 mJ. The investigation of the influence of plasticiser on film properties proved that the kind of plasticiser used in the polymer film had no effect on the mechanical properties of the film or pellets. Only in the case of the film with triethyl citrate was no distinct of the pellet core found. Pellets coated both with films with triethyl citrate and with dibutyl sebacate, in contrast to pellets with a film coating with propylene glycol, showed a significant decrease of the dissolution rate of verapamil hydrochloride (20, 10 and 40% at 6 hours, respectively). It is possible to compress pellets with a 50 microm polymer film without affecting the dissolution rate, as was confirmed during release studies. When using Kollicoat SR the most appropriate plasticizer seems to be triethyl citrate, and in this case a change of behavior during compression analysis by texture analyzer was observed. But so relationship was found between the type of plasticizer and the work needed to obtain a given deformation.
丸芯成分对丸剂行为的影响，例如在压制过程中的影响，是众所周知的。在本研究中，考察了Kollicoat SR聚合物薄膜成分对机械性能的影响。本研究的目的是从压片的角度评估聚合物薄膜成分对整个丸剂机械性能的影响。片剂应崩解成未变形的丸剂，在这种环境中漂浮5 - 6小时，尽可能以可控的方式释放模型药物——盐酸维拉帕米。还评估了质地分析和压缩功测量的实用性。选择30D水分散体形式的Kollicoat SR作为聚合物薄膜的主要成分。选择聚乙烯吡咯烷酮K - 30作为致孔剂，丙二醇、柠檬酸三乙酯和癸二酸二丁酯作为典型的增塑剂。还评估了不同厚度的聚合物薄膜对应力作用下行为的影响。用20微米的Kollicoat SR分散薄膜包衣丸芯后，观察到与丸芯相比机械强度有所增加（从2.74毫焦增加到3.34毫焦）。添加致孔剂使压缩功增加了50%，达到5.1毫焦。对增塑剂对薄膜性能影响的研究证明，聚合物薄膜中使用的增塑剂种类对薄膜或丸剂的机械性能没有影响。仅在含有柠檬酸三乙酯的薄膜的情况下，未发现丸芯有明显变化。与用丙二醇薄膜包衣的丸剂相比，用柠檬酸三乙酯和癸二酸二丁酯薄膜包衣的丸剂显示盐酸维拉帕米的溶出速率显著降低（6小时时分别为20%、10%和40%）。在释放研究中证实，可以压制具有50微米聚合物薄膜的丸剂而不影响溶出速率。使用Kollicoat SR时，最合适的增塑剂似乎是柠檬酸三乙酯，在这种情况下，通过质地分析仪观察到压缩分析过程中的行为变化。但是在增塑剂类型与获得给定变形所需的功之间未发现这种关系。
