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选择少量的助流剂可提高布洛芬片剂的拉伸强度。

Selection of Small Amounts of Glidant Capable of Improving the Tensile Strength of Ibuprofen Tablets.

机构信息

Department of Physical Chemistry, Hoshi University.

Research & Development Headquarters Self-Medication, Taisho Pharmaceutical Co., Ltd.

出版信息

Chem Pharm Bull (Tokyo). 2021;69(4):374-382. doi: 10.1248/cpb.c20-00924.

Abstract

This study examined the selection of small amounts of excipients capable of improving the compactability of ibuprofen, thereby enabling the miniaturization of ibuprofen tablets. Various glidants in amounts of 1% of the total volume were added to dry surface-modified ibuprofen, and the tensile strengths of the resulting tablets were evaluated. The characteristics of the excipients that affected the tensile strengths of the tablets were then extracted using a tensile strength prediction model. We confirmed that the effective angle of the internal friction of the mixed powder, the coating form of the glidant, the packing fraction of the raw material, and the mixed powder affect the tensile strength of the tablet. A smooth particle layer was formed on the surface of the ibuprofen particles when a glidant with a packing fraction of <0.05 was used. In the sample with a smooth particle layer, the angle of the critical state line increased significantly and the tensile strength improved. We inferred that the smoothness of the particle layer allowed the ibuprofen particles to come into close contact with each other. Consequently, the number of junctions increased, and the frictional force between the particles improved, resulting in tablets with improved tensile strengths. In conclusion, the compactability of ibuprofen was improved by adding 1% glidant with a packing fraction of <0.05. The reduction in excipients will allow the creation of smaller tablets, making them easier to swallow. Therefore, the medication adherence of customers will be improved.

摘要

本研究考察了选择少量赋形剂来改善布洛芬可压缩性的方法,从而实现布洛芬片剂的微型化。向干燥的表面改性布洛芬中添加了 1%总用量的各种助流剂,并评估了所得片剂的拉伸强度。然后使用拉伸强度预测模型提取影响片剂拉伸强度的赋形剂特性。我们证实,混合粉末的有效内摩擦角、助流剂的涂覆形式、原料的堆积分数以及混合粉末会影响片剂的拉伸强度。当使用堆积分数<0.05 的助流剂时,布洛芬颗粒的表面会形成光滑的颗粒层。在具有光滑颗粒层的样品中,临界状态线的角度显著增加,拉伸强度得到改善。我们推断,颗粒层的光滑度使得布洛芬颗粒能够紧密接触。因此,增加了颗粒之间的连接数量,改善了颗粒之间的摩擦力,从而提高了片剂的拉伸强度。总之,通过添加堆积分数<0.05 的 1%助流剂可以提高布洛芬的可压缩性。减少赋形剂的用量可以使片剂更小,更容易吞咽。因此,可以提高客户的用药依从性。

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