What is GLP-1, and why is it important in formulation development? Glucagon-like peptide-1, or GLP-1, is a hormone that helps regulate blood sugar, manage appetite, and support digestion. Certain medications, known as GLP-1 agonists, mimic these functions and are especially helpful for people with type 2 diabetes or obesity.
How can pharmaceutical companies ensure they are developing these drugs effectively? This guide explains important factors in the formulation development of GLP-1 dosage forms.
How GLP-1 Agonists Work
GLP-1 is a natural hormone produced by the small intestine in response to eating. It supports metabolic balance by suppressing the release of glucagon and helping the body produce more insulin when blood sugar rises after food intake. The hormone also slows down gastric emptying, which contributes to feelings of fullness and reduced appetite.
GLP-1 agonists or drugs can mimic these natural functions in people with insulin resistance. They stimulate the release of insulin and suppress glucagon, which helps to regulate blood sugar levels. Since GLP-1 agonists slow digestion and reduce appetite, they may also help with weight management.
Formulation Development of GLP-1 Dosage Forms
For many years, people with type 2 diabetes have used GLP-1 drugs as part of their treatment plans. In more recent years, the FDA approved certain GLP-1 receptor agonists for weight loss in people with obesity, regardless of whether they have diabetes.
However, the effectiveness of GLP-1 drugs depends on how they are formulated. These medications are made from peptides, which are fragile molecules that can break down easily in the body. Pharmaceutical companies need to develop formulations that keep the drug stable and help it work as intended.
To achieve this, pharma companies have developed different dosage forms that help deliver the medication more effectively and improve patient outcomes. These include:
Injectable Formulations
Currently, most GLP-1 agonists come as injectable formulations that are taken either daily or weekly. These injections deliver the drug directly into the bloodstream, bypassing the digestive system, where peptides would normally break down. Advances in peptide formulation development have made it possible to extend the drug’s effects, so it is now common to have longer gaps between doses.
Oral GLP-1 Dosage Forms
While injections work well and are the most common dosage form, not everyone likes needles. That is why researchers are working on other options, like oral solid dose formulations. The problem with oral GLP-1 drugs is that they tend to break down in stomach acid and enzymes before the body absorbs them.
Drug developers use special coatings and absorption enhancers to improve bioavailability, helping the medication survive the digestive system and reach the bloodstream.
Sublingual Tablets
Another option is sublingual tablets, which dissolve under the tongue. This method allows the drug to be absorbed directly into the bloodstream, bypassing the digestive system altogether. Usually, specialized compounding pharmacies prepare these customized formulations.
However, while sublingual tablets are a promising alternative for patients looking for a needle-free option, the FDA warns about the potential dangers of unapproved compounded GLP-1 agonists.
Pharma companies must, therefore, carefully consider the legal and regulatory status of these formulations. Partnering with a full-service CDMO like Vici Health Sciences, which has extensive experience in regulatory strategy and filing services, can help avoid costly mistakes.
The Role of Analytical Testing and Compounding in GLP-1 Formulations
GLP-1 drugs require rigorous quality control to work effectively. This is why analytical testing of GLP-1 products is crucial to ensureAdvanced that each batch is pure, potent, and stable. In addition to detecting degradation, advanced testing methods are also important for detecting degradation and refining formulations to make them more effective.
In some cases, a compounding pharmacy may create custom GLP-1 formulations. The process combines different ingredients with FDA-approved drugs. This can be useful for people who need a specific dosage or are allergic to certain ingredients in existing formulations. Custom GLP-1 formulations may also offer patients an alternative form of the medication not yet available commercially.
However, it is important to note that these compounded medications are not FDA-approved and should be used with caution. Pharmacies must follow current FDA policies to ensure that compounders stay compliant.
Develop Effective GLP-1 Therapies: Let Vici Health Sciences Guide You
Drug developers must go beyond standard formulations to make GLP-1 agonists work effectively. These therapies need to be stable, bioavailable, and compliant with strict regulatory standards. Every decision in the development process impacts how well these drugs perform for patients.
At Vici Health Sciences, we provide the expertise pharmaceutical companies need to meet these challenges. With a strong track record in regulatory strategy and filing services, we help efficiently bring innovative, patient-friendly GLP-1 therapies to market. Contact us today to get started.
