Rebranding Lipophilic Excipients

Solubilizers play an important role in dissolving poorly soluble molecules. As the number of poorly soluble lipophilic and/or hydrophobic molecules increases—whether as "brick dusts" or waxy substances—the industry is struggling to identify the appropriate lipophilic excipients (surfactants, solubilizers, solvents or polymers) that can be used to develop such poorly soluble formulations into solid dosages and other forms of pharmaceutical products. Furthermore, the complexity of such formulations is increasing and often two or more solubilizers and/or cosolvents are required to develop stable and efficacious formulations with enhanced bioavailability (1).

Table I: Kolliphor® grades.

As pharmaceutical manufacturers develop generic and new molecules that require high-quality, functional excipients, they seek support from excipient manufacturers. Indeed, the pharmaceutical industry relies on excipient manufacturers to design and produce excipients that are appropriate to the envisaged dosage form and API. This is a complex undertaking made all the more difficult because of the number of different names that manufacturers use for their excipients. However, several excipient manufacturers are now streamlining the structure, nomenclature and functionality of their excipients, including solubilizers.

Table II: Kollisov® grades.

Such rebranding has been used in other industries to reduce complexity and to promote products on the merits of their performances and qualities, ideally without undermining the old brands. This is now occurring among excipient manufacturers, particularly those that carry lipophilic excipients, including BASF, as well as other companies. Many companies have used branding and rebranding to either introduce new products or reintroduce an old product under a single 'prefix' to simplify identification. In the case of BASF, Cremophor®, Solutol®, Lutrol® and other solubilizers will become part of the Kolliphor® brand family.

Table III: Kolliwax® grades.

The basis for rebranding with the same prefix is to identify molecules by structures, functions and the applications of choice; enable the company's brand products to be recognized; and to differentiate pharmaceutical excipients from other grades. Rebranding is a tedious and time-consuming process, and in some instances adds complexity if the functionality of the molecule is not well defined.

Table IV: Kollicream® grades.

Here, we provide a synopsis of how we have undertaken the process of rebranding our solubilizers for pharmaceutical applications. With a few exceptions, we have tried to preserve some of the characters from the old product brand name to avoid confusion and to allow scientists to easily recognize them. The surfactants and solubilizers, as well as related products, have been categorized under four umbrella rebranding subgroups:

• Kolliphor: For amphiphilic substances such as ionic and non-ionic surfactants, solubilizers and emulsifying agents, as shown in Table I.

• Kollisolv: For solvents such as mediumchain triglycerides, propylene glycol, liquid polyethylene glycols and liquid poloxamers, as shown in Table II.

• Kolliwax: This name was coined to represent consistency factors, such as those in fatty acids, alcohols and glycerides, as shown in Table III.

• Kollicream: The name was chosen to represent emollients such as fatty acid esters and special fatty alcohols, as shown in Table IV.

Conclusion

Rebranding gives us the opportunity to include other solubilizers and related excipients based on their chemistry and functionalities in our four umbrella subgroups. With continuing interest to increase drug solubilization, it is our understanding that this rebranding will reduce the complexity involved in selecting pharmaceuticalgrade excipients in formulation development. Thus, this will encourage excipients manufacturers to adopt a norm to simplify complex product portfolios.

Reference

1. C.J.H. Porter, C.W. Pouton, J.F. Cuine and W.N. Charman, Adv. Drug Delivery Rev. 60 (6), 673–691 (2008).

Download your free copy of BASF's solubility enhancement compendium at: www.innovate-excipients.basf.com