Kollitab DC 87 L – the all-in-one tableting solution

Traditionally, an active pharmaceutical ingredient (API) is formulated as an immediate release tablet by combining various excipients. Each individual excipient addresses a specific need in the overall formulation concept. Typical requirements are:

• increasing the tablet volume with a filler

• improving tablet strength with a binder

• adjusting the disintegration features by employing a disintegrant

• lowering the ejection force by selecting an effective lubricant.

Further formulation components might also be required such as wetting agents or glidants to improve the powder flow of the tableting blend.

There is a huge selection of excipients available to formulators. All these ingredients need to be evaluated, cleverly combined and their synergies considered. The relevant ratios must also be examined to build up the required target product profile. Having such options is generally a desired feature and key for optimising formulations of demanding APIs. Though, in the field of low-to-mid dose APIs, which do not require any special attention when being formulated as immediate release tablets, the situation is very different. Options ask for experience, knowledge, a huge stock of excipients, multiple trials, financial resources and substantial time investments. Time, being the most precious aspect of all, could be spend in other projects.

Consistently, formulators must balance their efforts. Time can either be invested in the development of a standard tablet or put into challenging, yet commercially more interesting projects, respectively. This is the area of conflict where both an all-in-one tableting aid and a virtual pharma assistant come in handy. Holistically, these two tools simplify formulation development and free up time and resources greatly re-quired.

The all-in-one tableting aid

Co-processed excipients are well established in the pharmaceutical community. Uniting the performances and synergies of cleverly combined excipients and the benefits of a dedicated manufacturing process, co-processed excipients provide performances that single components are uncapable to deliver. All-in-one excipients evolutionarily developed from this concept (see Table 1). By adding missing attributes, they are transformed to offer fully fetched formulation concepts, satisfying all the needs of an immediate release target product profile.

All-in-one components combine the functionalities required to formulate an immediate-release tablet, with the application ease of a ready-to-use component and the robustness and processing reliability of a customised formulation.

Is an all-in-one excipient specifically optimised to support customised formulation concepts of a dedicated API? No, surely not. That is not the claim. All-in-one excipients are optimised to simplify development, increase processing robustness and reduce the overall cost of tablet manufacturing. Indeed, following the concept and utilising all its overarching benefits provides various advantages throughout the entire business, such as:

• purchasing benefits by reducing the number of vendors which reduces complexities

• quality and regulatory benefits by minimising testing efforts and expenses, which reduces paperwork

• warehousing benefits by minimising the number of excipients, freeing up expensive storage area

• research and development benefits by simplifying formulation development and shortening time-to-market, freeing up precious resources.

• production benefits by allowing for direct compression and streamlining of processes, hereby decreasing manufacturing complexity and risk of failure.

Formulation development is much more straight forward with Kollitab DC 87 L

Reduce components with Kollitab DC 87 L

An evaluation of marketed drug products reveals that a huge variety of excipients are used in pharma manufacturing. To formulate four drug products, today’s formulation concepts easily require 15+ ingredients (four APIs and 11+ excipients). Utilising the capabilities of an all-in-one component reduces the number of ingredients to five. There are still four APIs, but just one excipient: Kollitab DC 87 L.

Kollitab DC 87 L can substitute 11+ excipients in the warehouse and it substitutes an even larger number of excipients on the list of components screened during drug product development.

Instead of testing various fillers, binders, disintegrants and lubricants, altering their ratio and still compromising on the overall performance of a physical powder blend, formulation development is much more straight forward with Kollitab DC 87 L.

The only variable is the mixing ratio of the API and the all-in-one tableting aid. However, even this ratio can be predicted using ZoomLab, a virtual pharma assistant.

The virtual pharma assistant

ZoomLab is part of a series of BASF’s web-based assistance supporting the pharma industry with expertise. Alongside RegXcellence (providing documents and information for mainly regulatory purposes) and MyProductWorld (supporting with information on products and allowing for sample requests), ZoomLab has been tailored to simplify formulators’ lives. The algorithms and modules provided by ZoomLab range from topical applications to coated oral solid dosage forms providing modified drug release, additionally considering solubility and bioavailability of the API.

ZoomLab underpins the profound formulation expertise of BASF’s application experts and is the outcome of decades of scientific formulation work. The heart of ZoomLab is a formulation wizard. This unique tool calculates the most promising formulation concept based on very simple tests to characterise the API (e.g. particle size distribution, flowability, tablet-ability) and some general information on its chemical nature. Thus, suitable excipients are selected according to the specific needs of the API and based on their chemical compatibility. Additionally, there is an API database within ZoomLab which holds information on the chemical nature and physical behaviour of generic APIs. If listed, a first virtual prototype of a drug product can be generated within minutes, even without having ever touched the API.

A holistic approach

Leveraging the capabilities of ZoomLab leads to a robust and reliable formulation concept without the need of conducting a single trial.

Combining the advantages of the virtual pharma assistant with the performance of Kollitab DC 87 L provides a vast set of advantages, resulting in a major simplification in the development of immediate release tablets. The time that is liberated can be invested in more relevant projects.

The combination of both tools provides maximum flexibility and spontaneity, relevant for tender business. If an API has been characterised previously or is even listed among the generic APIs in the ZoomLab database, one can check a Kollitab DC 87 L based formulation concept even without having any of the formulation components. If the ZoomLab check is successful, the next simple steps are ordering the two components (API and Kollitab DC 87 L) and following the manufacturing instructions provided by ZoomLab. The result is the first prototypes will be ready in no time. •