Tips for: Solid Oral Dosage Forms

Achieving the desired drug release profile in hard gelatin capsules is a significant challenge in pharmaceutical formulation development. The release profile of a drug is crucial to its therapeutic effectiveness, and it must be tailored to meet specific patient needs. Targeted release profiles are often required for drugs that need to be delivered at particular sites in the gastrointestinal tract or at a specific time after administration. However, formulating hard gelatin capsules with precise and predictable release profiles can be difficult due to various factors such as API solubility, excipient interactions, and the capsule shell’s dissolution characteristics.
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Drug-excipient interactions can significantly impact the stability, solubility, bioavailability, and release profile of a pharmaceutical product. However, inadequate studies on these interactions during the drug development phase can lead to formulation failures, delayed product approval, or safety issues. It is essential to conduct comprehensive studies to assess the compatibility between the active pharmaceutical ingredient (API) and the excipients used in the formulation to avoid unforeseen issues during manufacturing or after the product reaches the market. Incomplete or insufficient evaluation of these interactions can lead to suboptimal drug performance or stability problems, compromising therapeutic outcomes and regulatory approval.
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Polymorphism in pharmaceuticals refers to the ability of a compound to exist in different crystalline forms, known as polymorphs. The polymorphic form of an active pharmaceutical ingredient (API) can significantly impact its solubility, stability, dissolution rate, and bioavailability. In the development of capsule formulations, polymorphic changes can lead to formulation instability, where different polymorphs of the API may exhibit varying degrees of solubility, leading to inconsistent drug release and therapeutic efficacy. Managing polymorphic transitions is essential to ensure that the drug maintains its desired performance throughout its shelf life.
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Lipid-based formulations have gained popularity for improving the bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs). However, achieving the desired bioavailability in these formulations can be challenging. Lipid-based systems, such as soft gelatin capsules containing oils, lipid emulsions, and solid lipid nanoparticles, offer a promising strategy for enhancing drug solubility and absorption. Despite their potential, there are several challenges in ensuring that the drug is effectively released, absorbed, and reaches the systemic circulation in the desired therapeutic amounts. These challenges include variability in drug release, poor stability of lipid excipients, and limitations in drug absorption due to physiological factors.
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The use of plasticizers in soft gelatin capsules is essential to enhance the flexibility and mechanical properties of the capsule shell. However, the incompatibility of the active pharmaceutical ingredient (API) with the plasticizers can lead to various issues, including drug degradation, altered release profiles, and poor bioavailability. This issue arises when the plasticizer interacts with the API, leading to physical or chemical changes in the drug that can compromise its stability and therapeutic efficacy. Understanding and addressing these incompatibilities is critical to ensuring the stability and performance of the soft gelatin capsule formulation.
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The quality and consistency of excipients play a crucial role in the development of pharmaceutical products, particularly in capsule formulations. The lack of standardization in excipient grades can lead to variability in product performance, including poor reproducibility in terms of fill weight, dissolution rates, and stability. Such variability can result in batch-to-batch differences, affecting the overall quality of the final product. Inconsistent excipient quality not only hinders reproducibility but also raises concerns regarding regulatory compliance, particularly in ensuring that the finished product meets the required specifications.
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Capsule content leakage during product development trials is a significant issue that can compromise the stability, efficacy, and safety of pharmaceutical products. This problem typically arises when the soft gelatin capsule shell is unable to effectively contain the fill material, leading to leakage of the active pharmaceutical ingredient (API) or excipients. Leaking capsules can result in product contamination, loss of API, incorrect dosing, and difficulty in achieving the desired therapeutic effect. Identifying and addressing the root causes of leakage is essential to ensuring the integrity of the capsule and the success of the formulation.
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