Solid formulation is well-established in the pharmaceutical industry and there are many standard processes and methods, as well as a variety of formulations and dosage types. Challenges such as poor solubility remain, however, and necessitate innovative problem-solving strategies.
This page provides an overview of common challenges in solid formulation of small molecules, highlighting effective and tailor-made solutions specifically developed to overcome critical obstacles in drug development.
Solubility enhancement is a key challenge in pharmaceutical formulation development, as an increasing number of APIs in the development pipeline are poorly water-soluble. A range of approaches are available to enhance solubility which have to be evaluated depending on the API and specific formulation requirements as there is no one-size-fits-all solution for poorly water-soluble APIs. Strategies for solubility enhancement are typically based on the classification of the API according to the Biopharmaceutics Classification System (BCS), or the more recent Developability Classification System (DCS), resulting in a tailored approach for the individual API.
Pharmaceutical development and manufacturing is moving away from the concept of “blockbuster drugs” and toward addressing the needs of very defined patient populations. At the same time, process efficiency and process economics are now more important than ever. New technologies are on the rise and offer new opportunities and the potential to disrupt traditional pharmaceutical manufacturing concepts.
Tablet coatings play an important role in solid dose formulation as they offer numerous benefits. They improve appearance, mask unpleasant colors or tastes, differentiate from other drug products, protect the tablet core from moisture, modify the release behavior, and improve swallowability. The development of a coating formulation and a process to ensure optimal performance requires substantial expertise. Also, the selection of the coating components is a critical step and material-specific properties have to be taken into consideration, as well as recent regulatory developments.
Despite being one of the most widely used oral solid dosage forms, formulation of compressed tablets can be challenging, and several manufacturing approaches can be used. Formulators benefit from greater flexibility when selecting the best technology during formulation development for their specific API and final formulation requirements. Learn about the common techniques for tablet manufacturing direct compression, wet granulation, and dry granulation, and their respective benefits and drawbacks.
Many factors in a drug formulation can have a negative effect on the stability of the API. Reduced API stability can result in reduced shelf life, reduced efficacy, or in the worst-case scenario, cause harm to a patient. There are several considerations that must be taken into account when developing a formulation or when dealing with instabilities: Is the API sensitive to environmental factors such as light, heat, or humidity? Is the API prone to instabilities induced by common excipient impurities such as peroxides or reducing sugars? Is the API incompatible with selected formulation methods?
Pleasant taste and palatability influence patient acceptance of a final formulation and can have a significant impact on patient compliance. These factors are particularly relevant for oral administration routes, liquid formulations, orally disintegrating tablets (ODTs), and certain patient groups (pediatric, geriatric).
Controlled release of oral solid formulations ensures alignment of drug performance and therapeutic need. The benefits of sustained release include reduced dose frequency, greater patient convenience, and increased compliance. In many cases, long-acting efficacy of the API is required. When selecting excipients for sustained-release formulations, drug manufacturers require options that deliver superior reliability and consistency with release kinetics unaffected by outer conditions such as pH value.
Orally disintegrating tablets (ODT) offer convenience and speed. These tablets are designed to dissolve quickly in the mouth before being swallowed, without the need for water.
Inhalation drug delivery is an attractive, noninvasive route of administration when rapid onset of action, minimal side effects and excellent bioavailability are desired. Accurate dosing of the dry powder inhalation (DPI) formulation can be challenging, however, due to the small amount of dosage and fine particle size required.
Formulating solid dosage forms can be quite challenging and complex. On the way to the final formulation, there are many obstacles to overcome, whether it is API stability, bioavailability, or release kinetics that have to be optimized, just to name a few. Finding a trusted partner with application and regulatory expertise that supports you in identifying the best approach for your specific API can make a difference – helping you to reduce efforts, accelerate development time, and ultimately, bring your drug development project to success.
Contact our technical experts to learn more about our extensive application services.
This white paper examines the potential impact of poor API stability in solid dose drug development, explores the causes of insta bility and explains how excipients can help in creating stable formulations. Finally, it also presents some case studies to illustrate their potential effectiveness.
Achieving the appropriate release kinetics for an active pharmaceutical ingredient (API) is essential to ensure success of the therapeutic. For example, for sustained release formulations, a consistent API dose over a prolonged period ensures that levels in the blood plasma remain within the therapeutic window.
Inhalation drug delivery methods are attractive, noninvasive routes when rapid onset of action, minimal side effects and excellent bioavailability are desired. However, not many drugs are administered this way and accurate dosing can be a challenge.
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