Abstract
Oral solid dosage forms that contain APIs in the amorphous state have become commonplace because of many drug substances exhibiting poor water solubility, which negatively impacts their absorption in the human GI tract. While micronization, solvent spray-drying, and hot-melt extrusion can address solubility issues, spray coating of the APIs onto beads and tablets offers another option for producing amorphous drug products. High-level comparisons between bead and tablet coating technologies have the potential for simpler equipment and operation that can reduce the cost of development and manufacturing. However, spray coating directly onto tablets is not without challenges, especially with respect to meeting uniformity acceptance value (AV) criteria, comprising accuracy (mean) and precision (variance) objectives. The feasibility of meeting AV criteria is examined, based on mathematical models for accuracy and precision. The results indicate that the main difficulty in manufacturing satisfactory drug-layered tablets by spray coating is caused by the practical limitations of achieving the necessary coating precision. Despite this limitation, it is shown that AV criteria can be consistently met by appropriate materials monitoring and control as well as processing equipment setup, operation, and maintenance.
Highlights
Jaehwi LeeThe main advantage of creating oral solid dosage forms containing an amorphous active pharmaceutical ingredient (API) is the improved drug solubility in the human GI tract that leads to higher bioavailability
The methods used to derive the relationship between the acceptance value criteria, accuracy, and precision parameters are provided
This relationship indicates that coefficient of variation (CV) values must be less than s to satisfy the Equation (8)
Summary
Jaehwi LeeThe main advantage of creating oral solid dosage forms containing an amorphous active pharmaceutical ingredient (API) is the improved drug solubility in the human GI tract that leads to higher bioavailability. Drug products with drug-layered pellets have a historical significance [2] and, as shown, the manufacturing process requires fewer steps compared to those for typical solid-dosage forms prepared, for example, when using amorphous APIs obtained using the classic techniques. This table indicates the potential reduction in the number of manufacturing unit operations required to produce the final dosage form, which can be of considerable benefit for development cost and time-to-market and for commercial manufacturing when considering the capital and operating costs of multiple unit operations
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