The global population is increasingly busy, and getting older every day. With the number of patients on the go, facing their senior years, dealing with problems swallowing, orally disintegrating tablets are increasingly popular, with patients and pharma developers alike. Outsourcing-Pharma discussed ODT trends and challenges with Nasser Syed, head of global marketing for GBU Pharma at Roquette, and selecting the right excipients.
OSP: Could you please share some of the reasons why the market is seeing an increased demand for oral disintegrating tablets (ODTs)?
NS: Oral disintegrating tablets (ODTs) are becoming a popular delivery system across both the pharmaceutical and nutraceutical fields, with new innovations being explored in the prescription (Rx), over-the-counter (OTC), and nutraceutical markets. A patient-centric drug delivery system, they are designed to increase compliance across several patient populations, especially geriatrics and pediatrics who are most likely to suffer from dysphagia – i.e. swallowing difficulties. This is particularly significant as the world’s population continues to grow and people are living longer (geriatric as well as pediatric patients are increasing).
Meanwhile, ODTs are considered easier to administer compared to classic dosage forms, like swallowable tablets and capsules, since there is no need for water. When disintegrated in the mouth (with just saliva), they offer faster onset of action, better absorption, and improved bioavailability. This makes them attractive dosage formats for patients and manufacturers alike.
OSP: What are some of the key challenges and considerations regarding the design and formulation of such tablets?
NS: The ideal ODT should be both physically and chemically stable, and not too large (<500mg). The tablet should disintegrate completely within the mouth in no more than 30 seconds, and give no unpleasant sensations, including bad taste, gritty texture, or burning sensation. For these desired attributes, formulators must select suitable excipients for creating compressed or lyophilized ODTs, with direct compression being the preferred mode.
Key considerations regarding the design and formulation of ODTs include:
- Class of active pharmaceutical ingredient (API) – BCS Class 1 and 3 are most suitable as they are highly soluble.
- API bitterness – this affects taste experience in the patient.
- Choice of excipients – they give the finished tablet the hardness without compromising oral disintegration properties.
- Manufacturing process – in most cases, direct compression is the most preferred.
OSP: Can you please share some of the advantages of ODTs, when it comes to patient adherence and convenience?
NS: When it comes to geriatric and pediatric patients, tablets and capsules can have certain limitations, such as bitter taste and swallowing discomfort due to large pill sizes. Patients with specific requirements, like those with a learning disability, can also find it challenging to consume classic oral dosage forms, potentially affecting adherence to medications and compromising patient outcomes.
ODTs help to overcome these challenges because they are designed to disintegrate easily when placed on the tongue – simplifying the process of taking medication and making them a more convenient option. In addition, they have a pleasant taste and mouthfeel and are therefore considered an efficient alternative to traditional oral delivery dosage forms.
After disintegration, the API is then absorbed via mucous membranes of the oral cavity, pharynx, and esophagus (also known as pregastric absorption), in addition to the gastrointestinal tract. This provides rapid relief and enhances drug bioavailability. For these reasons, ODTs help to improve patient adherence and are inspiring significant innovations across the pharmaceutical space.
OSP: Are there advantages we see with clinical trial teams, hospitals, and caregivers administering such drugs?
NS: For medical professionals and caregivers, the successful and efficient administration of medication is key to ensuring the best patient compliance, and therefore outcomes. ODTs offer peace of mind, as they are much simpler to administer compared to traditional tablets and capsules – there is no need for water to initiate dissolution, and as a result, no challenges associated with swallowing. For clinical research teams, ODTs provide better patient adherence to the investigational drug clinical protocol.
OSP: What types of drugs are best suited for the ODT format? And, conversely, which drugs might not be optimal in ODTs?
NS: Due to ODTs' ability to provide rapid onset of action, they are particularly suited to therapeutic categories where fast relief is desired, such as painkillers and analgesics, anti-allergy medications, and treatments for gastrointestinal discomfort. Additional drugs commonly available in an ODT format include:
- Nonsteroidal anti-inflammatory drugs (NSAIDs)
- Blood pressure management
Drugs that are considered not optimal for ODTs include:
- Low potency drugs with a high proportion of APIs
- APIs that exhibit bitterness
- Controlled-/sustained-release medications
- Combination drugs.
OSP: Can you please share some of the notable excipients Roquette offers that are suited for ODTs?
NS: Roquette has extensive experience in the development of excipients suitable for ODTs, including those that can support the development of technologically challenging formulations. Our notable excipients suited for ODTs are PEARLITOL Flash, PEARLITOL Mannitol pharma range, GLYCOLYS, and SOLUTAB.
PEARLITOL Flash is a mannitol and starch co-processed excipient that enables robustness with rapid disintegration. It enables the simple production of high-quality pharmaceutical and nutraceutical ODTs formulations by direct compression. Other benefits include:
- A uniquely pleasant taste experience
- Superior wettability properties compared with other platforms, resulting in fast self-disintegration
- Less lubricant is required thanks to its inherent self-lubricating properties.
Our PEARLITOL Mannitol pharma range, available in various grades, is used as fillers and/or binders, as well as bulk sweeteners. The range offers exceptional physical and chemical stability and extremely low hygroscopicity. Importantly though, excipients from this range need to be combined with a suitable disintegrant.
In addition, Roquette offers a range of super-disintegrants:
- GLYCOLYS - Sodium Starch Glycolate, available in three grades
- SOLUTAB - Croscarmellose Sodium, available in three grades.
OSP: Do you have anything you’d like to add about ODTs—challenges, benefits, advice for developers considering the format for their therapies?
NS: Roquette has been present in the pharma market for more than 40 years, becoming a trusted partner for the exploration of new possibilities using high-quality excipients across the industry. Our commitment, dedication, and passion for a healthier world are unwavering – and providing patient-friendly dosage forms is a critical part of ensuring patient compliance.
As well as supporting our partners in creating life-saving medicines, we must also support them in producing solutions that are convenient for patients to consume and for healthcare professionals to administer. Through our in-depth understanding of pharmaceutical products, alongside our wider portfolio of high-quality excipients, we can do just that.