八粉末直接压片处方设计及影响因素考察.docVIP

LABORATORY 8: Design of tablet formulations for direct compression and investigation of the influencing factors LABORATORY OBJECTIVES a) To learn the test methods of powder flowability and compressibility, and diluent potential of excipients used for direct compression. b) To learn the significance of various compression pressure parameters in the tabletting process and the methods of measurement. c) To understand the formulation design of tablet formulations for direct compression and the quality characteristics of tablets made by direct compression. INTRODUCTION Direct compression is a method for preparing tablets. In this process, the drug and suitable excipients are mixed to form a uniform powder mixture which is compressed directly into tablets without the granulation process. The flowability and compressibility of most active ingredients are often unsuitable for direct compression, therefore, direct compression is only applicable to materials possessing good flowability and compressibility. It is known that the granulation process is used to improve the micromeritic properties of a tablet formulation. However, for products containing lower level of active drug ( 50 mg), a direct compression formulation can be developed by mixing the drug with excipients with good flowability and compressibility. Therefore, the selection of proper excipients and formulation optimization are the key tasks for successful tablet preparation by direct compression. Besides the two requirements mentioned above, excipients for direct compression need to have a high dilution potential which is defined as the ability to impart adequate flowability, compressibility, and lubrication to the a powder mixture containing different percentage of the active drug for direct compression. Microcrystalline cellulose (Avicel 101, Avicel 102), spray dried lactose, calcium monobasic phosphate hydrate (Ca(H2PO4)2) are commonly used excipients for direct compression abroad, while microcrystalline cell