A significant number of challenges await OSD product developers and manufacturers as 2023 approaches; it’s a mature market segment that faces competition from a host of other delivery routes. Considerable — and ongoing — innovation is necessary to ensure that OSD drug products continue to offer the best possible experience for patients and stand out from rival delivery routes in the market.
A new generation of excipients has a key role to play in delivering the innovation required to ensure the enduring success of the OSD sector. The right excipients can impart vital characteristics to their drug formulations to meet ever-evolving consumer needs.
Pharmaceutical companies now have an opportunity to address the customer needs that are driving industry trends and challenges, make revisions and incorporate them into their drug products. But how can they ensure that they’re able to harness the benefits of new excipients to meet future trends? And how can they achieve this while also optimising the performance of their products
The trends and challenges facing the OSD market
Several key trends are affecting not just prescription OSD drugs, but also those available over-the-counter (OTC). Some of the most noteworthy trends include the following.
The growing importance of the patient experience and changing patient demands: The need to carefully consider the patient experience is as important as ever. The texture, shape and scale of the OSD, as well as its taste, can be adapted and optimised to address a major issue: patient adherence.
With prescribed drugs in particular, this consideration also plays into the thinking of general practitioners: “If this course of medication is in any way an inconvenience, is this person likely to stick to it?”
In terms of OTC and prescription medications, ease of administration is especially pertinent and should be considered throughout the design and development stage. This is paramount for paediatric and geriatric patients, for whom the administration of treatments needs to be as comfortable as possible.
As there is a growing number of clinically relevant swallowing issues (such as dysphagia) in older patient populations, this group often requires smaller, easier-to-swallow pills.1 With children, having a reasonably palatable flavour is preferable whenever possible (according to paediatric guidelines).
For example, sweeteners and flavours help to mask the naturally bitter taste of many active pharmaceutical ingredients (APIs) and encourage children to adhere to OSD medications.
The rise of OSD biologics: Developments in recent years have made OSD biologics increasingly viable. Traditionally, biologics have had to be delivered parenterally. Being able to administer biologics orally can potentially make a wide range of treatments available for self-administration by the patient, rather than having to visit a clinic.
This makes them more convenient for the patient while reducing the burden on healthcare providers.
That said, biologics are often sensitive to conditions such as temperature, pH and shear stress; they will generally degrade in the harsh conditions of the stomach long before they reach the site of absorption. Orally administered biologics also have, owing to their large molecular size, typical challenges in terms of absorption through the intestinal mucosa.
With this in mind, biologic OSD forms will require new formulations, different production processes, solutions for absorption challenges and a whole new mode of thinking regarding storage to make oral delivery a viable alternative to injection for biopharma treatments.
Small-scale batches and 3D printing: A significant development is a move towards small-scale batches for more specialised, targeted medicines. In this realm — production-wise — 3D printing is playing an increasingly significant role, providing a malleable solution to a range of manufacturing problems. The benefits of 3D printing include
- cost-effectiveness: the technology provides a cost-efficient solution to manufacturing small quantities of a drug product
- flexibility: 3D printing can easily be adapted to produce different products quickly (unlike a large-scale production line)
- speed: effectively, a manufacturer can produce Drug A on Monday morning, clean the machine and then produce Drug B on the same apparatus on Monday afternoon with no significant changes apart from the feedstock of raw materials
- finesse and precision: should a product require a more robust molecular structure to achieve a particular objective, then 3D printing provides a pivotal role in achieving this.
How to address these changes with the right excipients
Meeting these trends is crucial if pharma companies are to continue to thrive and stand out against the competition within the OSD space … and against products using rival administration routes.
The key to addressing the challenges posed by these changes in the OSD landscape lies in the choice of excipients in the drug formulation. Excipients can impart vital attributes to a formulation — not just to extend the stability and shelf-life of the API but to complement and enhance its therapeutic performance as well.
Considerable innovation has taken place in recent years in the field of excipient development, not only to support the stability and enhance the shelf-life of APIs. Examples of this innovation include
- ingredients to enhance mouthfeel and support the incorporation of pleasant flavours in OTC medicines and mask the bitter taste of many APIs
- excipients to support enhanced controlled release, enabling more effective fixed-dose combination and long-acting OSD products; this is in addition to enhancing the effective oral delivery of biologic molecules
- the need to replace previously common excipients — such as whitening agents (titanium dioxide) or sugar-based taste modifiers — with more health conscious or less potentially damaging fill material.
Similar challenges and areas for development face the industry as an ongoing endeavour, and it’s certainly something that warrants constant vigilance.
Things to consider when incorporating new excipients into a formulation
Whether reformulating an existing drug product or developing a new one, incorporating this new generation of excipients can be a challenge for pharmaceutical companies. Several factors need to be considered to ensure successful formulation development.
Compatibility with the API: Does the excipient need to be tailored to be more compatible with the API and other ingredients? Have you done everything possible to avoid undermining the API's therapeutic effect and ensure there are no adverse effects on stability or shelf-life?
Processability: Is the process robust and can your organisation support the manufacturing of the formulation at a cost-effective scale? Have you looked into the possibility of 3D printing as a potential alternative?
Compatibility with the current primary packaging: Does encouraging the leaching of compounds from the primary packaging material affect the safety or performance of the drug formulation?
Does it do the job it’s meant to do, with no unexpected surprises? Have you added a pleasant flavour that accidentally causes tooth decay? Have you made something toxic by slightly changing its colour? In short, have you assessed your changes thoroughly?
Is it easy to source at scale? Does your revised product have a robust and reliable supply chain?
Is it legal and approved for use in target markets? Have you paid enough attention to any potential problems?
Is your project cost-effective to reformulate? No one wants to reformulate unless they absolutely must, as it's expensive and always carries an element of risk. Is the investment of time and energy into the reformulation really going to transform the experience of end patients for the better?
Provided organisations equip themselves with formulation development expertise and continue to be mindful of the changing OSD landscape, they can be confident that they have the tools needed to adapt and thrive in 2023 and beyond.
The need for expert support
For any drug-producing organisation, the benefits of being able to call on a talent pool that’s rich in sector knowledge, policy know-how and scientific competence are invaluable as a means of helping them to stay up to speed with the latest trends.
There are contract development and manufacturing organisations (CDMOs) with dedicated formulation development experience and specialist expertise in the new generation of excipients.
These partners can help pharma companies to navigate the complex excipient market to find the ingredients they need to successfully reformulate their OSD products and keep up with a fast-changing market.
Reference
- N. Drumond and S. Stegemann, “Better Medicines for Older Patients: Considerations between Patient Characteristics and Solid Oral Dosage Form Designs to Improve Swallowing Experience,” Pharmaceutics 13(1), 32 (2021).
