The Current Trends and Challenges Influencing the Oral Solid Dose Market
Dr. Uwe Hanenberg, Head of Product Development, Oral Solid Dose and Dr. Maria Lundin-Johnson, Head of Formulation Development, at Recipharm, explore the current trends influencing the oral solid dose (OSD) market and the significant challenges they present to the advancement of medicines.
As the OSD market continues to grow, drug product developers and manufacturers face new challenges. Driven by increased demand for more patient-centric formulations, these challenges include improving ease of administration, finding solutions for the individual challenges of the active molecule(s), overcoming formulation issues for OSD biologics and adapting drug products to maintain their competitive edge in the market.
Constant innovation is crucial to ensure OSD drug products provide the best experience for patients and stand out from others in the market. The use of new excipients plays a vital role in delivering the necessary innovation for OSD products to succeed. These excipients add essential characteristics to drug formulations to help companies meet ever-evolving consumer needs.
Recent excipient advancements present pharmaceutical companies with an opportunity to better address patient needs and optimise the performance of their drug products. But how can they effectively harness the benefits of these excipients to overcome their most pressing challenges?
The Evolving OSD Landscape
Across the OSD market, there are significant developments that are impacting both prescription drugs and over-the-counter (OTC) medications.
● Enhancing the patient experience
Patients expect more than just the efficacy of medication; they also demand a convenient experience that encompasses texture, shape and taste. Advancements in science have meant that these once difficult-to-control factors can be more readily adapted to the palatability needs of patients, such as improved mouthfeel (i.e. improving the texture and sensation of a substance when orally ingested), taste and swallowability.
By adapting and optimising these characteristics, pharmaceutical companies can improve patient adherence to medication regimens, which is crucial for successful treatment outcomes.
Enhancing these factors is particularly relevant for vulnerable patient populations, such as children and the elderly. In paediatric patients, having a reasonably palatable flavour is important, as it encourages adherence to OSD medications. Sweeteners and flavours can help mask the naturally bitter taste of many active pharmaceutical ingredients (APIs), making them more appealing to children, in line with paediatric guidelines.
Similarly, the geriatric population faces swallowing difficulties, such as dysphagia, which can make it challenging to take medications. Therefore, the need for smaller and easier-to-swallow pills demands formulation adjustments and the use of appropriate excipients to ensure comfortable administration for older patients.
● Streamlining decision-making for general practitioners
This consideration of patient experience extends to general practitioners, who need to assess if a medication’s convenience might affect a patient’s willingness to adhere to the prescribed course of treatment. Therefore, ease of administration should be a central focus during the design and development of OTC and prescription medications.
● The emergence of OSD biologics
In recent years, significant advancements have made OSD biologics increasingly viable. Traditionally, the delivery of biologics necessitated parenteral administration; however, the ability to administer these biologics orally has opened up a plethora of possibilities for self-administration by patients. This reduces the need for in-clinic visits and provides a more convenient option for patients while alleviating the burden on healthcare providers.
Nevertheless, biologics pose unique challenges when it comes to oral administration, primarily due to their extreme sensitivity to environmental conditions such as temperature, pH levels and shear stress. In the harsh environment of the stomach, biologics tend to degrade before reaching the site of absorption. Moreover, due to their large molecular size, orally administered biologics also face challenges in absorption through the intestinal mucosa.
Considering these factors, the development of OSD forms for biologics necessitates novel formulations, different production processes, solutions to absorption challenges and a paradigm shift in terms of storage. Selecting the optimal excipients is crucial to making oral delivery a viable alternative to injection for biopharmaceutical treatments.
● Facing the upcoming “patent cliff”
As a wide range of originator drug products face an imminent patent cliff, a new wave of generics is set to flood the market. To thrive and differentiate themselves from competitors in the market, pharmaceutical companies must explore alternative administration routes.
By pivoting dosage forms to more patient-centric administration routes, such as OSD, companies can retain their competitive edge by meeting current market demands. The key to achieving this is by exploring the optimal excipients to make these new formulations viable.
Harnessing the Right Excipients
In recent years, significant advancements have been made in excipient development that offer various benefits to manufacturers, including:
● Improving mouthfeel and flavour: The right excipients can be used to enhance the palatability of OTC medicines by effectively masking the bitter taste of APIs.
● Extending stability and shelf life: Excipients play a crucial role in enhancing the stability and shelf life of the active pharmaceutical ingredient (API) while improving its therapeutic performance.
● Enabling OSD biologic formulations: Excipients can be used to help enhance the potential for successful oral delivery of biologic molecules.
● Facilitating controlled release: Excipients can be used to develop OSD products that control the rate of API release to provide sustained therapeutic effects over an extended time.
● Increasing Bioavailability: Excipients can be used to help enhance solubility or absorption of the API in the human body.
● Enabling fixed-dose combinations: By combining multiple active ingredients into a single dosage form, excipients can be harnessed to create fixed-dose combinations that simplify medication regimens for patients with multiple conditions.
● Providing healthier options: By substituting conventional excipients with healthier alternatives that have a lower potential for harm, such as replacing titanium dioxide, whitening agents or sugar-based taste modifiers, pharmaceutical companies can appeal to a wider market.
Considerations for Incorporating New Excipients into a Formulation
When it comes to incorporating new excipients into a formulation, pharmaceutical companies can face various challenges. Whether they are reformulating an existing drug product or developing a new one, several factors must be taken into account to ensure successful formulation development. Here are some key considerations:
● Compatibility with the API: It is crucial to assess whether the excipient is compatible with the API and other ingredients. Care must be taken to avoid any negative impact on the API’s therapeutic effect, stability or shelf life.
● Processability: The formulation process should be robust, and the organisation should have the capability to manufacture the formulation at a cost-effective scale. It is also important to ensure that the new excipient can be sourced reliably and at a large scale to meet the demand for the reformulated product.
● Compatibility with the current primary packaging: The excipient should not compromise the safety or performance of the drug formulation by interacting with compounds in the primary packaging material. It is also crucial to assess and mitigate the risk of extractables and leachables, where substances from the packaging materials could impact the product’s quality and safety.
● Thorough assessment: The new excipient should perform its intended function without any surprises. For example, if a pleasant flavour inadvertently causes tooth decay or a slight colour change makes the product toxic, these issues need to be identified and addressed. Additionally, the excipient should be approved for use in its target markets, and any potential legal or regulatory issues must be thoroughly considered.
● Cost-effectiveness: Reformulation can be expensive and carries inherent risks. It is essential to evaluate whether the investment of time and resources in the reformulation will truly enhance the patient experience and justify the costs involved.
The Importance of Expert Support
For any organisation that works to bring a drug to market, having access to a talent pool of sector knowledge, policy expertise and scientific competence is invaluable.
Contract development and manufacturing organisations (CDMOs) specialising in formulation development and with a finger on the pulse of each new generation of excipients can offer the required support to navigate the complex excipient market.
By selecting the right partner with the right expertise and capabilities, pharmaceutical companies are better equipped to find the right ingredients that allow them to successfully reformulate their OSD products and adapt to patient demands to keep pace with the evolving market.