Desai R P, Neau S H, Pather S I, Johnston T P
Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, 64110-2499, USA.
Drug Dev Ind Pharm. 2001 Aug;27(7):633-41. doi: 10.1081/ddc-100107319.
Ethylcellullose has traditionally been used in tablets as a binder in an alcohol solution form. In the present study, fine-particle ethylcellulose (FPEC) was used as a binder to manufacture immediate-release tablets by the direct compression technique. The binding potential of FPEC is compared to that of commercially available coarse-particle ethylcellulose at the same viscosity grade and to that of hydrophilic binders. The compression force setting was kept constant for all batches. The concentration of the binder was varied from 5% to 25%. Acetaminophen was used as a model drug because capping is a problem frequently observed during high-speed compaction and further processing of acetaminophen tablets. In this study, there would be an increase in the contact area with FPEC and hence greater bond formation. This greater bond formation should be able to reduce the problem of capping in tablets containing highly elastic materials such as acetaminophen. Tablets were evaluated based on the following tests: weight variation, extent of capping, hardness, friability, disintegration, and dissolution. Based on the results of these tests, FPEC proved to be an effective binder for directly compressed acetaminophen tablets. The 10% and 15% formulations of FPEC passed all the tests and also produced the hardest tablets.
乙基纤维素传统上在片剂中用作醇溶液形式的粘合剂。在本研究中，细颗粒乙基纤维素（FPEC）被用作粘合剂，通过直接压片技术制备速释片剂。将FPEC的粘合潜力与相同粘度等级的市售粗颗粒乙基纤维素以及亲水性粘合剂的粘合潜力进行比较。所有批次的压片力设定保持恒定。粘合剂的浓度从5%变化到25%。对乙酰氨基酚用作模型药物，因为在对乙酰氨基酚片剂进行高速压片和进一步加工过程中经常会出现裂片问题。在本研究中，与FPEC的接触面积会增加，因此会形成更强的结合。这种更强的结合应该能够减少含有高弹性材料（如对乙酰氨基酚）的片剂中的裂片问题。基于以下测试对片剂进行评估：重量差异、裂片程度、硬度、脆碎度、崩解和溶出度。基于这些测试的结果，FPEC被证明是直接压片的对乙酰氨基酚片剂的有效粘合剂。FPEC的10%和15%配方通过了所有测试，并且还生产出了最硬的片剂。
