By David Calvert, August 2024
We always state that formulation plays a key role in almost every product and that a different format can lead to different applications and opportunities. Recently I came across a couple of examples where different formulation formats have been instrumental in the success of the same active and where different formats have been used for different applications.
So, I am a Type 2 diabetic and have been so for over 10 years now. At the start of the year, I was invited to take part in a clinical trial for a drug to control blood glucose levels where they wished to make an additional claim that it also reduced the risk of a heart attack or stroke. The trial involved taking a drug called “Semiglutide” in tablet format over a period of five years and then answering a series of questionnaires. Now some of you may recognise that active but until a friend said to me “Oh, that’s Ozempic®” I had not made the link to the weight loss drug which has been in the media a lot recently. Ozempic® and Wegovy® are both in injectable format that are injected weekly. There is a tablet version of semiglutide called Rybelsus®.
So why the different formats? Well, I guess one reason may be intellectual property and another will undoubtedly be the regulatory approval for the formats. Another could be the consumer needs and preference, which in drug use plays a large part in conformance. Tablets do not require the use of needles but can have side effects such as nausea and abdominal pain and often need to be taken on an empty stomach, or with food. Tablets also need to be able to withstand the acid environment of the stomach to get into the blood stream. Needles can have similar side effects but in the case of Ozempic® and Wegovy® only need to be administered once a week and have no issues regarding timing of food and drink. Formulators need to take all of these factors into consideration right at the start of the formulation design and we have written a number of articles on this design for formulation approach.
My experience with semiglutide got me thinking further about my medication for diabetes and then I discovered that a drug I had taken for a while called Gliclazide was described as a sulfonylurea. iFormulate carry out many projects in agrochemicals and sulfonylureas are a prominently used herbicide. Although sulfonylureas are water soluble, they are not hydrolytically stable. This has led to the development of the Oil Dispersion (OD) format, where particles are suspended in an oil, thus eliminating water until the product is mixed in the spray tank. So, a family of actives which require different formulations in order to be acceptable in the application.
These two simple examples demonstrate to me the value of formulation, and the formulator and show how a well-designed formulation can bring significant commercial success.
