Tips for: Solid Oral Dosage Forms

Bitter-tasting active pharmaceutical ingredients (APIs) present a significant challenge in capsule formulation, especially for oral dosage forms. Many patients, particularly pediatric or geriatric populations, struggle with swallowing pills that have an unpleasant taste. Masking the bitter taste of drugs is critical for improving patient compliance and ensuring the success of oral drug therapies. While tablets and oral solutions also face this challenge, soft gelatin capsules, which are often preferred for their ease of swallowing and precise dosing, can provide unique opportunities for taste masking solutions.
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Water-sensitive active pharmaceutical ingredients (APIs) pose significant challenges in soft gelatin capsule formulations. The hydrophilic nature of gelatin capsules makes them inherently sensitive to moisture, which can interact with water-sensitive APIs, leading to degradation, loss of potency, or altered bioavailability. Formulating soft gelatin capsules with these types of APIs requires innovative strategies to protect the drug from moisture-induced instability while ensuring that the capsule performs as intended during storage and administration.
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Cross-linking reactions between gelatin and aldehyde-containing drugs present a significant challenge in soft gelatin capsule formulations. Gelatin, as a natural polymer, contains amino acids with functional groups that can react with aldehydes, leading to the formation of cross-linked structures. These reactions can affect the stability, bioavailability, and release profile of the drug, as well as the mechanical properties of the capsule shell. Aldehyde-containing drugs, such as certain antibiotics, anticancer agents, and some steroids, are particularly susceptible to such reactions, requiring careful formulation strategies to avoid degradation or undesirable interactions.
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Some drugs are susceptible to degradation in the acidic environment of the stomach, which can result in reduced efficacy or harmful byproducts. To prevent gastric degradation, specialized coatings are required for the active pharmaceutical ingredient (API) in capsule formulations. These coatings ensure that the API remains intact until it reaches the more neutral or alkaline conditions of the small intestine, where it can be effectively absorbed. Designing a coating system that provides adequate protection from gastric degradation, while ensuring proper drug release at the target site, is crucial for maintaining drug stability and therapeutic efficacy.
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Uneven distribution of low-dose drugs in powder blends is a common challenge faced during the formulation of capsule dosage forms. Achieving a uniform blend of the active pharmaceutical ingredient (API) with excipients is critical to ensuring consistent dosing in each capsule. For low-dose drugs, where small amounts of the API are required, even slight variations in the powder blend can lead to significant dose discrepancies. This can result in issues such as poor bioavailability, ineffective therapeutic outcomes, or potential safety risks due to inconsistent dosing.
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Fixed-dose combination (FDC) products are commonly used in pharmaceutical formulations to improve patient adherence and optimize therapeutic outcomes. However, developing these products, especially in capsule form, presents unique challenges. FDCs involve combining two or more active pharmaceutical ingredients (APIs) into a single dosage form, which can result in compatibility, stability, and manufacturing issues. Ensuring uniformity of dose, compatibility of the APIs, and maintaining stability throughout the shelf life are essential to the success of FDC capsule formulations.
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