Orally disintegrating tablets (ODTs) provide both convenience and comfort for a wide range of patient populations, but currently available disintegrants can only dissolve within 30 seconds. A faster disintegrant that can be used for direct compression of ODTs that disintegrate in under 10 seconds yet still have excellent hardness and a pleasant mouthfeel would create new formulating opportunities. SPI Pharma has bridged that gap with its new UltraBurst™ excipient platform.
Why Orally Disintegrating Tablets?
Orally disintegrating tablets (ODTs) disintegrate in the mouth, releasing the active pharmaceutical ingredient (API) for delivery to the stomach. As such, they provide both convenience and comfort to patients. This dosage form is particularly attractive for people who have difficulty taking conventional tablets or capsules, such as children, the elderly, who often have problems swallowing, and psychiatric patients. Since water is not required to take ODTs, they are also beneficial for people who are traveling and in areas of the world where access to fresh water is limited.
Consequently, ODT formulations find use with pediatric, geriatric, and psychiatric medicines. They are also ideal for drugs that treat conditions where rapid absorption and onset are important, such as pain relievers for headaches and migraines, antiemetics for nausea, and anti-hypertensives for lowering blood pressure.
The interest in ODT products is driving interest in superdisintegrants — excipients that enable rapid disintegration of tablets in the mouth. In fact, the global superdisintegrants market is projected to expand at a compound annual growth rate of 7.9% from $366.4 million in 2018 to $536.5 million by 2023.1
UltraBurst from SPI Pharma is the first new preformulated product that releases APIs in under 10 seconds in vivo while maintaining best-in-class compactability, hardness, and friability across a wide range of API loadings and tablet weights.
The Need for Speed, Low Friability, and Mouthfeel
Current superdisintegrants on the market today, including SPI Pharma’s preformulated Pharmaburst® product, enable disintegration within the mouth in under 30 seconds. The challenge with ODTs is to produce tablets that disintegrate more rapidly in the mouth but are highly stable during production, packaging, storage, and shipment. That requires robust hardness and minimal friability (the U.S. Pharmacopeia limit is 1%) to prevent breakage of the tablets. An attractive mouthfeel is also essential.
Until recently, the primary way to achieve super-fast disintegration in under 10 seconds while still maintaining tablet durability has been to produce ODTs via freeze drying, which is a specialized and expensive process. Freeze drying is also the only manufacturing method that enables the production of low-tablet-weight ODTs.
Therefore, there has been an unmet need for a new excipient technology that allows flash disintegration and the formulation of ODTs over a wide range of dosage levels and tablet weights while maintaining physical robustness. Such a solution would enable the creation of new, cost-effective, rapidly disintegrating ODTs and thus increase access to this patient-centric dosage form to many new parts of the world, as well as new patient populations.
Disintegration Under Ten Seconds
UltraBurst from SPI Pharma bridges that gap. This innovative excipient platform for direct compression of ODTs is the first new preformulated product that releases APIs in under 10 seconds in vivo while maintaining best-in-class compactability, hardness, and friability across a wide range of API loadings and tablet weights.
This new technology was developed by adopting the mindset and point of view of our pharmaceutical industry customers from the outset. Specific effort was made to address areas of concern and expectations of formulation development experts. Our focus was to improve not only the disintegration time, but the friability and packaging performance, and to achieve all of that via a cost-effective solution.
Accelerating Novel ODT Formulation Development
Our UltraBurst platform is evolutionary and revolutionary. With its combination of properties and suitability for cost-effective direct compression, UltraBurst is opening up a really exciting space for ODTs that had not previously been served by practical preformulation technology.
In addition to its flash disintegration capability, UltraBurst has very low friability when compared with other platforms. It is also highly stable, with very low moisture uptake, both during compression (which avoids issues with sticking) and during storage. No special precautions must be taken during production (e.g., low humidity), and no specialized packaging (e.g., blister packs) is required.
The mouthfeel of ODTs formulated with UltraBurst is pleasant and smooth, with no grittiness or texture-related issues due to the narrow particle size and weight ranges of the product.
As a preformulated excipient platform, UltraBurst also simplifies the formulation process. For APIs that do not require taste masking, only a small quantity of lubricant must be added before direct compression. The addition of sweeteners and flavorants, if necessary, has no impact on the performance of the UltraBurst platform, which maintains blend and content uniformity, even for large taste-masked actives, across relevant production scales.
The broad range of API loadings and tablet weights that are possible with the UltraBurst platform also affords new ODT formulating opportunities. Using this technology, it is possible to create low-dose, 100-mg tablets with a 5-second disintegration time or improve the disintegration time of a 700-mg ODT tablet by 35% without any loss of hardness or friability performance.
Very thin tablets can be produced, which are often preferred by patients, while maintaining all of the important tablet properties. In addition, tablet weights can be reduced when using the UltraBurst excipient platform. For instance, the weight of 300-mg loratadine tablets formulated with conventional excipients can be reduced to 100 mg using UltraBurst yet still provide the same dose. This reduction in excipient use enables smaller tablets and reduces costs.
Importantly, UltraBurst comprises excipients used in current oral dose forms and thus complies with pharma-level quality and regulatory expectations. Overall, this new ODT excipient platform bridges the gap to extremely fast disintegration and for the first time brings to market a flash ODT preformulation for direct compression that is ready to use and cost-effective.
SPI Pharma understands that it isn’t good enough to just make another effective product; we need to elevate the performance of the industry, and we believe we have done that with UltraBurst.
Innovation Based on Decades of ODT Experience
The development of UltraBurst was achieved by leveraging SPI Pharma’s extensive base of formulation and materials science expertise and knowledge gained over nearly two decades in the ODT space. This new technology extends our existing portfolio of products, including our Pharmaburst ODT solution, mannitol-based offerings, and our range of taste-masking systems.
With these capabilities, SPI Pharma’s value proposition focuses on the development of patient-centric dosage forms. Pharmaburst and UltraBurst emerged as part of our strategy to build a performance advantage using our high-performing mannitol in state-of-the-art, patient-centric ODT formulations and platforms. We believe that ODTs address a very practical element of patient-centric drug development with respect to patient experiences and preferences and how those preferences vary around the world.
With our insight and expertise, SPI Pharma is able to create new platforms such as UltraBurst, opening doors that were previously closed to some formulators because of needs like disintegration time or drug load (tablet size). Our technical experts are also available to help with the rapid design and optimization of custom formulations, including challenging ODT applications, and to meet aggressive timelines.
Supporting the Entire ODT Space
SPI Pharma brings to the table a unique combination of products (e.g., Pharmaburst, UltraBurst, Advantol® for Nutraceutical ODTs, Mannogem® Mannitol for chewables) and knowledge, making us the ideal partner for the formulation of not only low-dose, low-weight, fast-disintegrating ODTs, but all orally disintegrating dosage forms.
In the ODT space, we are committed to ongoing improvement of our products and opening new avenues for drug development. By doing so, our customers can continue to improve their products and expand their offerings, ultimately benefitting patients.
Reference
- Superdisintegrants Market by Product (Modified Starch, Modified Cellulose, Crospovidone, Ion Exchange Resin), Formulation (Tablet, Capsules), Therapeutic Area (Gastrointestinal, Cardiovascular, Neurology, Oncology, Hematology) - Global Forecast to 2023. MarketsandMarkets. 2017.