Itraconazole (ITZ) is an antifungal drug commercially available as an oral solution or more commonly as 100 mg capsules. It has been reported that the bioavailability of the oral solution is only 55% [1]. One of the strategies to improve its solubility, and therefore its bioavailability, is to produce amorphous solid dispersions (ASDs) using the hot melt extrusion (HME) process. To produce tablets of these ITZ ASDs, with ITZ dose of 100 mg, it is necessary to increase the tablet weight to accommodate for other excipients which can facilitate disintegration and improve the bioavailability. Therefore, during formulation development it is important to consider quality attributes such as tablet size and shape as these would ease swallowing for patients along with acceptability of the product overall.

A large international pharmaceutical manufacturer approached Quadro with an application to reduce the size of a small percentage of over-sized particles contained within a dry granulation formulation. 

This paper covers a brief overview of the steps for pharmaceutical product development under the quality by design (QbD) framework; introduces design of experiments (DoE) applied to formulation of tablets and gives an example of how to design piroxicam amorphous solid dispersions (ASD) tablets using DoE.

Pharmaceutical companies worldwide have been using the Comil® for removing lumps from pharmaceutical wet masses prior to the drying process. When blending active ingredients, binders and water or solvent in a high shear mixer/granulator it forms irregularly sized lumps which, if not de-agglomerated, results in long drying times and poorer particle size distributions.

Amorphous solid dispersions (ASDs) have been widely used to improve the bioavailability of poorly water-soluble drugs [1]. They are comprised of high molar mass polymer carriers that stabilise the active pharmaceutical ingredients (APIs) in their amorphous state. 

The aim of this study was to optimize the tablet compression process of an immediate-release analgesic formulation and to resolve the tableting challenges that appeared during the process development.

Poor compliance with a medication regimen reduces treatment effectiveness for the patient and has a significant impact on overall healthcare costs. Some of the common factors influencing compliance are the disease being treated, patient age and the therapy regimen itself. Therefore, when developing dosage forms, it is important to consider specific patient challenges for different diseases. This article explores the needs of different patient groups, identifies frequent issues leading to non-compliance, looks at the role of orally disintegrating tablets (ODTs) in helping improve patient compliance and provides examples of improving the delivery profile of the drug.

Although probiotics are mostly administered in the form of capsules, there are some advantages of tablets in terms of production effort, cost efficiency and stability of the probiotic bacteria. As probiotics are sensitive to high pressure and temperature, it is essential to select appropriate excipients for direct compression to ensure sufficient viability of the bacteria cells during production and storage. The aim of this study was to investigate the performance of the high functional excipient PROSOLV® EASYtab Nutra for direct compression of probiotic tablets. As PROSOLV® EASYtab Nutra is an all-in-one composite, only one mixing step is required before the compaction which makes the tableting process easy and comfortable. In order to evaluate the performance of PROSOLV® EASYtab Nutra, the survival rate of the bacteria and functional tablet properties were determined and compared to a lactose-based formulation. The study showed that PROSOLV® EASYtab Nutra is considerably better suited for direct compression of probiotic tablets because of the remarkable survival rate of 91.5 % of the bacteria cells as well as the quick disintegration within 18 seconds, which is almost 10 times faster compared to the lactose formulation. Furthermore PROSOLV® EASYtab Nutra is characterized by excellent compactability and an extremely low friability.

In the present study, the performance of PROSOLV EASYtab SP was tested in four DC formulations with different model APIs. Each of selected APIs presented a particular challenge in terms of producing tablets with suitable hardness, weight uniformity, content uniformity and/or reliable dissolution profiles. PROSOLV EASYtab SP was shown to perform considerably better than the corresponding physical mixture of its components for all formulations tested.

Compaction simulators are a key technology allowing scientists to develop formulations and troubleshoot tablet defects. It means that formulation scientists or tech transfer engineers can assess the influence of process parameters on tablet properties to preempt risk during scale-up or to solve production issues with minimal powder consumption and avoiding unnecessary use of production assets. 

The goal of this bulletin is to generate tablet defects such as capping and use precompression to lessen this phenomenon without modifying the formulation. This will demonstrate that such tablet defects can be foreseen on compaction simulators right from the development stage to reduce cost and save time during scale-up and production.