Abstract
We previously reported a novel method for the precise prediction of tablet properties (e.g., tensile strength (TS)) using a small number of experimental data. The key technique of this method is to compensate for the lack of experimental data by using data of placebo tablets collected in a database. This study provides further technical knowledge to discuss the usefulness of this prediction method. Placebo tablets consisting of microcrystalline cellulose, lactose, and cornstarch were prepared using the design of an experimental method, and their TS and disintegration time (DT) were measured. The response surfaces representing the relationship between the formulation and the tablet properties were then created. This study investigated tablets containing four different active pharmaceutical ingredients (APIs) with a drug load ranging from 20–60%. Overall, the TS of API-containing tablets could be precisely predicted by this method, while the prediction accuracy of the DT was much lower than that of the TS. These results suggested that the mode of action of APIs on the DT was more complicated than that on the TS. Our prediction method could be valuable for the development of tablet formulations.
Highlights
Tablet properties are affected substantially by the physicochemical properties of the loaded active pharmaceutical ingredients (APIs) as well as by formulation factors and process parameters [1,2]
This study investigated the mode of action of the formulation factors on the tablet properties of different API-containing tablets using response surface method (RSM)
The absolute values of the API-containing tablets decreased steadily with an increase in drug load; for instance, ACE-containing tablets in Rp. 5 had a tensile strength (TS) of 2.45 MPa at a drug load of 20%, while at a 60% load the TS was decreased by 0.82 MPa
Summary
Tablet properties are affected substantially by the physicochemical properties of the loaded active pharmaceutical ingredients (APIs) as well as by formulation factors and process parameters [1,2]. It is difficult to predict them depending on these factors quantitatively in pharmaceutical development because the mode of action of APIs on a tablet’s properties is complicated and is substantially influenced by the drug loading. A better understanding of the mode of action of these factors on the pharmaceutical characteristics of the tablets became more important after the introduction of the “quality by design (QbD)” concept at the International Conference on Harmonization Q8 guideline in 2008 [3]. According to the QbD concept, quality must be built into the product; pharmaceutical researchers are required to perform formulation design based on a systematic, scientific, risk-based, holistic, and proactive approach. RSM can visualize the causal relationships between the factors and the pharmaceutical characteristics, which were used to identify crucial formulation factors from numerous potential factors [5,6,7,8,9], to optimize formulation [10,11] or process parameters [11,12,13], and to construct design spaces [14,15,16,17,18]
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