In the rapidly growing and evolving cannabinoid space, crafting more patient-centric pharmaceuticals that meet therapeutic needs and convenience is at the forefront of drug developers’ minds. Yet, manufacturers continue to face challenges in this realm, due to the lipophilic nature of cannabinoid molecules and their limited solubility.
This is particularly relevant when formulating cannabinoids into solid oral medications, like tablets, capsules, or oral disintegrating tablets (ODTs) – the preferred administration route for most patients, but also the most complex in the cannabinoid field. With this in mind, there is a unique opportunity to spearhead innovation in this space and pioneer the creation of appealing solid oral dosage formats with optimal bioavailability and patient experience. Read on to dive deeper into the latest advancements in cannabinoid solid oral drug development – including groundbreaking insights from Alexandru Zabara PhD, Innovation Manager at dsm-firmenich.
Solid Oral Dosage formats: The Cornerstone of Patient-centric Care in the Cannabinoid Arena
Improving a patient’s experience of taking a medication starts with the drug format, and for many, tablets and capsules are the most convenient option. However, in the cannabinoid space, this can be rather complicated.
Currently cannabinoids, like cannabidiol (CBD) active pharmaceutical ingredient (API), require a dose above 300–400 mg per day to have any real therapeutic effect.1 As a result, patients must administer high volumes of cannabinoid[1]based medications – which are usually in liquid form – to achieve a beneficial outcome. This is an unpleasant experience for the individual and can increase the risk of unwanted adverse effects, fueling demand for more patient[1]focused solutions within the cannabinoid category, like solid oral dosage forms.
Not only are solid oral dosage forms more convenient for patients, but they also offer superior safety (due to accurate dosing and ease of administration), good patient compliance and an overall superior experience compared to liquid drugs. Solid oral dosage formats are also better for the rapid treatment of acute conditions because liquid solutions require longer periods of time before the active ingredient can reach its maximum concentration within the systemic circulation.
Furthermore, solid oral forms remove the complications associated with the administration of some liquid (oil-based) products – which are usually delivered via a syringe or dropper, presenting multiple challenges for patients, including inaccurate dosing and sensory hurdles. So, why aren’t drug developers creating more solid dosage formats?
The Bioavailability Opportunity: Unlocking Cannabinoid Efficacy
Developing patient-centric cannabinoid[1]based drugs means making solid oral dosage forms a reality. However, to guarantee successful solid oral cannabinoid formulation, drug manufactures need to overcome one critical barrier – low and variable bioavailability of the active. Why? Because the bioavailability of cannabinoid molecules, like CBD, is linked to their efficacy and the dose required to achieve a positive therapeutic outcome.
The poor oral bioavailability of cannabinoid molecules is a result of several factors – namely incomplete absorption and substantial pre-systemic elimination in the liver. Cannabinoids, specifically CBD, have extremely low solubility in water and high lipophilicity, which means that a significant fraction of the orally ingested dose is not absorbed by the gut.
