Özalp Yıldız, Chunu Joseph Turemi, Jiwa Nailla
Near East University Faculty of Pharmacy, Department of Pharmaceutical Technology, Nicosia, Cypus.
Turk J Pharm Sci. 2020 Jun;17(3):249-253. doi: 10.4274/tjps.galenos.2019.38278. Epub 2020 Jun 22.
This study was performed to understand the behavior of poorly compressible paracetamol powder using a compaction simulator (CS), equipment that records data during the compaction process. The aim was to investigate the compressibility of paracetamol tablets using a dry granulation (slugging) process, with different formulation compositions.
Formulations were prepared to observe the effect on compressibility with two different lactose-based fillers, Flowlac100 and Granulac70, and a binder, Kollidon K90. In each combination, a total of four formulations were prepared with paracetamol to filler ratios of 1:1 and 0.8:1. Tablets were produced by single punch (11.28 mm) CS at six different pressures (152, 210, 263, 316, 400, and 452 MPa). During compression, upper punch displacement and force data were produced by the CS equipment. The compressed tablets were tested for hardness, thickness, and weight variation and compared with each other.
All formulations reached maximum tensile strength at compaction pressures between 263 and 316 MPa. In the formulations without binder, those containing Granulac70 had higher tensile strength than those containing Flowlac100 at both filler ratios. The results obtained indicated that the addition of binder to the formulations (F-45-1, F-45-2, F-50-3, and F-50-4) improved the compressibility of paracetamol. Formulation F-45-2, containing Flowlac100 and binder, showed better compressibility at 2.9 MPa tensile strength. Data from the CS were used to compare Young's modulus and work of compaction on selected formulations (F-45-1 and F-45-2).
The proposed lactose-based filler, Flowlac100, with low pressure can be successfully applied for improving the compressibility of paracetamol. An optimum formulation can be designed with smaller amounts of materials using a compaction simulator.
本研究旨在使用压片模拟器（CS）来了解难压缩的对乙酰氨基酚粉末的行为，该设备可在压片过程中记录数据。目的是研究采用干法制粒（制粒压片）工艺、不同配方组成的对乙酰氨基酚片剂的可压缩性。
制备配方以观察两种不同的乳糖基填充剂（Flowlac100和Granulac70）以及粘合剂（聚乙烯吡咯烷酮K90）对可压缩性的影响。在每种组合中，总共制备了四种配方，对乙酰氨基酚与填充剂的比例为1:1和0.8:1。通过单冲压片机（11.28毫米）CS在六种不同压力（152、210、263、316、400和452兆帕）下生产片剂。在压缩过程中，CS设备生成上冲头位移和力的数据。对压制的片剂进行硬度、厚度和重量差异测试，并相互比较。
所有配方在263至316兆帕之间达到最大抗张强度。在不含粘合剂的配方中，在两种填充剂比例下，含有Granulac70的配方比含有Flowlac100的配方具有更高的抗张强度。所得结果表明，向配方（F - 45 - 1、F - 45 - 2、F - 50 - 3和F - 50 - 4）中添加粘合剂可提高对乙酰氨基酚的可压缩性。含有Flowlac100和粘合剂的配方F - 45 - 2在抗张强度为2.9兆帕时显示出更好的可压缩性。CS的数据用于比较所选配方（F - 45 - 1和F - 45 - 2）的杨氏模量和压实功。
所提出的低压乳糖基填充剂Flowlac100可成功用于提高对乙酰氨基酚的可压缩性。使用压片模拟器可以用较少量的材料设计出最佳配方。
