製剤学的特徴に着目したレボドパ/カルビドパ配合製剤における一包化調剤の適否

抄録

Indexes to evaluate the propriety of one-dose package dispensing from the side of pharmaceutics include hardness and friability. However, the number of pharmaceuticals disclosing the details of these data is very restricted. Therefore we have investigated the propriety of one-dose package dispensing in levodopa/carbidopa preparations by measuring the change over time in hardness and friability of the pharmaceuticals for which it was thought that there were many opportunities to perform one-dose package dispensing. As a result, the propriety of one-dose package dispensing depends on brand and content in spite of the use of the same component pharmaceuticals, and the evaluation of two pharmaceuticals has shown that one-dose package dispensing was inappropriate. As a result of measuring the change over time in hygroscopicity, because hygroscopicity correlated extremely strongly with the ratio of decrease in hardness and the ratio of increase in friability, it was suggested that differences in the hygroscopicity of each drug influenced strongly the propriety of one-dose package dispensing. In addition, a possibility that the mass ratio of levodopa/carbidopa in a tablet and the initial mass of the tablet had also influenced the change was shown. Secondly, when we investigated the additives used, it was found that the inclusion of talc and the exclusion of microcrystalline cellulose caused inappropriate hardness in one of the drugs.

In order to perform a more detailed examination, it is necessary to have information about the amount of the additive, but this is not currently disclosed. Disclosure as soon as possible is desirable in order to achieve the proper use of pharmaceuticals.