Tips for: Solid Oral Dosage Forms

Solubility is a critical factor in the development of soft gelatin capsules, as the active pharmaceutical ingredient (API) must be readily available for absorption in the gastrointestinal tract. Many poorly soluble drugs require the use of solubilizers to enhance their bioavailability. However, finding solubilizers that are compatible with the gelatin shell used in soft gelatin capsules presents challenges. Gelatin is sensitive to various solvents and solubilizers, and some of these substances can affect the stability, dissolution, and release characteristics of the capsule. Therefore, the selection of appropriate solubilizers that do not interfere with the soft gelatin shell and ensure optimal drug solubility is essential.
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Powder flowability is a crucial factor in the encapsulation process, especially for hard gelatin capsules. Poor flow properties can lead to significant challenges in manufacturing, including inconsistent fill weights, dosage variations, and even production delays. Inconsistent powder flow can result from a variety of factors, such as particle size distribution, moisture content, or the inherent characteristics of the active pharmaceutical ingredient (API). These flow issues are particularly problematic in formulations containing fine powders, hygroscopic materials, or APIs that tend to clump together, all of which can complicate the capsule filling process.
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Achieving consistent fill weight in hard gelatin capsules is a critical aspect of capsule manufacturing. Inconsistent fill weight can lead to variations in drug dosage, affecting the therapeutic efficacy of the medication. This issue is especially problematic for drugs with a narrow therapeutic index, where even slight variations in dosage can lead to ineffective treatment or toxicity. Ensuring uniformity in capsule fill weight requires precise control over the formulation process, accurate dosing of the active pharmaceutical ingredient (API), and careful management of excipient properties.
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Thermolabile active pharmaceutical ingredients (APIs) are sensitive to heat and may degrade or lose their potency when exposed to high temperatures during manufacturing or storage. Incorporating these sensitive APIs into soft gelatin capsules presents a significant challenge, as the encapsulation process typically involves heating the gelatin and the encapsulation mass. For APIs that degrade at relatively low temperatures, it is essential to develop formulation strategies that protect the drug from thermal degradation while ensuring efficient capsule formation and drug release.
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Enteric-coated capsules are designed to protect the active pharmaceutical ingredient (API) from the acidic environment of the stomach and ensure that it is released in the more neutral pH of the small intestine. This type of formulation is essential for drugs that are unstable in gastric conditions or that need to be absorbed in the intestines to achieve optimal bioavailability. However, creating enteric-coated capsule formulations presents challenges in terms of coating consistency, stability, and controlled release. Ensuring that the coating does not break down prematurely and that it is applied uniformly can be complex and requires careful formulation and manufacturing processes.
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Developing modified-release capsules presents significant challenges in pharmaceutical formulation due to the need for precise control over the release rate of the active pharmaceutical ingredient (API). Modified-release capsules are designed to release their contents in a controlled, delayed, or sustained manner, rather than all at once. This allows for the drug to be released over time, maintaining therapeutic levels in the bloodstream for longer periods. However, achieving the desired release profile while ensuring the drug’s stability, bioavailability, and patient compliance can be complex. The development process involves balancing the interactions between the capsule material, excipients, and the API, as well as meeting stringent regulatory guidelines.
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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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