The quest to develop of oral insulin for diabetes
Taking a pill is the most common form of drug administration, but despite numerous attempts over the past 9 decades to develop an oral insulin pill, there is no commercially available insulin for oral delivery.
Why is it so desirable to develop insulin tablets? Unlike injections, oral insulin therapy would not be associated with pain or fear of pain. Furthermore, it would be a more discrete way to take the necessary treatment. Availability of oral insulin would therefore very likely increase patient compliance with therapeutic instructions.
In addition, oral insulin delivery also holds the promise of a better risk to benefit profile: the oral route with insulin passing through the gastrointestinal tract before entering the circulation has unique pharmacodynamic advantages. The insulin reaches the circulation via the hepatic portal vein in a manner similar to endogenous insulin whereas subcutaneous injections induce high systemic levels of insulin and thus carry a greater risk of hypoglycemia, weight gain and other effects.
Profil has conducted clinical pharmacology investigations with various oral insulin formulations. From these clinical trials we know that an oral insulin tablet can be absorbed via the intestine and can lower blood glucose. These trials have also shown that high insulin doses are needed because the bioavailability and biopotency are low. Furthermore, the absorption rates and effects are highly variable and food intake can severely hamper the efficacy of oral insulin medications.
Improved insulin structure and tablet formulations are needed to accelerate insulin absorption, allowing the medicine to be taken shortly before a meal, and to produce a consistent glucose-lowering effect. These are the obstacles standing in the way of the commercialization of the long-sought oral insulin.