Nottingham Digestive Diseases Centre and National Institute for Health Research (NIHR) Nottingham Biomedical Research Centre, Nottingham University Hospitals NHS Trust and University of Nottingham, Nottingham NG7 2UH, U.K.
School of Pharmacy, University of Nottingham, Nottingham NG7 2RD, U.K.
Mol Pharm. 2024 Apr 1;21(4):1553-1562. doi: 10.1021/acs.molpharmaceut.3c01123. Epub 2024 Mar 5.
Oral dosage forms are the most widely and frequently used formulations to deliver active pharmaceutical ingredients (APIs), due to their ease of administration and noninvasiveness. Knowledge of intragastric release rates and gastric mixing is crucial for predicting the API release profile, especially for immediate release formulations. However, knowledge of the intragastric fate of oral dosage forms to date is limited, particularly for dosage forms administered when the stomach is in the fed state. An improved understanding of gastric food processing, dosage form location, disintegration times, and food effects is essential for greater understanding for effective API formulation design. standard and controlled modeling has played a significant role in predicting the behavior of dosage forms . However, discrepancies are reported between and disintegration times, with these discrepancies being greatest in the fed state. Studying the fate of a dosage form is a challenging process, usually requiring the use of invasive methods, such as intubation. Noninvasive, whole body imaging techniques can however provide unique insights into this process. A scoping review was performed systematically to identify and critically appraise published studies using MRI to visualize oral solid dosage forms in healthy human subjects. The review identifies that so far, an all-purpose robust contrast agent or dosage form type has not been established for dosage form visualization and disintegration studies in the gastrointestinal system. Opportunities have been identified for future studies, with particular focus on characterizing dosage form disintegration for development after the consumption food, as exemplified by the standard Food and Drug Administration (FDA) high fat meal.
口服剂型是最广泛和常用的制剂，用于输送活性药物成分（APIs），因为它们易于给药且无创伤。了解胃内释放率和胃混合对于预测 API 释放曲线至关重要，特别是对于即时释放制剂。然而，迄今为止，对于口服剂型在胃处于进食状态下的胃内命运的了解有限，特别是对于处于进食状态下给予的剂型。为了更好地理解有效 API 制剂设计，需要更好地了解胃中食物处理、剂型位置、崩解时间和食物效应。标准和受控建模在预测剂型行为方面发挥了重要作用。然而， 和 崩解时间之间存在差异，在进食状态下这些差异最大。研究剂型的命运是一个具有挑战性的过程，通常需要使用侵入性方法，如插管。然而，非侵入性的全身成像技术可以提供对此过程的独特见解。本文进行了系统的范围审查，以确定和批判性评价使用 MRI 可视化健康人体口服固体制剂的已发表研究。该综述确定，到目前为止，尚未为胃肠道中的剂型可视化和崩解研究建立通用的稳健对比剂或剂型类型。已经确定了未来研究的机会，特别是侧重于描述剂型崩解，以在进食后进行开发，例如标准的食品和药物管理局（FDA）高脂肪餐。
