一般論文
創薬段階における微量粉体試料による打錠特性の予測とその検証
キーワード:
tablets,
formability,
adhesive property,
tableting problems,
tensile strength,
pre-formulation
2011 年 71 巻 4 号 p. 237-244
詳細
2011 年 71 巻 4 号 p. 237-244
This report aimed to predict the tableting problems such as sticking and capping in the production scale of manufacturing tablets with only a small quantity of drug substances in an early stage of drug development. First, the tableting properties of drug substances which included formability and adhesive property were evaluated by using a Micro Powder Characterizer (MPC) and tableting problems were predicted. Next, continuous tableting was performed using a rotary tableting machine used in production, and the relation between the properties of obtained tablets and the predicted tableting problems was studied. Aspirin and ascorbic acid were used as the drug substances. Testing of compression and ejection was conducted using MPC with a sample of about 10 mg which consisted of the drug substance and excipients. The formability was evaluated from the total energy and the tensile strength of tablets, and the adhesive property was evaluated from the ejection energy and the tensile strength of tablets. The prediction of incidence of tableting problems based on the evaluation of formability and adhesive property corresponded well with the actual incidence of tableting problems at continuous tableting by a rotary tableting machine.
From these results, it was inferred that the tablet formulation without tableting problems at continuous tableting was enabled in an early stage of drug development, in the so-called pre-formulation by the evaluation of formability and adhesive property with an infinitesimal quantity of samples by using MPC.
