The dynamic interaction between variables within the gastrointestinal tract and the physiochemical properties of a drug in a delivery system determine the rate and extent of absorption of that drug. Among the major physiologic variables are pH, gastric emptying time, and intestinal transit time. Some physicochemical properties of interest include solubility, particle size, and chemical form of the drug. Attributes of the formulation such as controlled-release mechanism, pH sensitivity, and size, shape, and density of the product can also affect absorption. Food has also been reported to influence the absorption from some but not all controlled-release products. As a more thorough understanding of the many factors involved in drug absorption is developed, the formulation of more sophisticated oral drug delivery systems will be possible.
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http://dx.doi.org/10.1016/0091-6749(86)90047-3 | DOI Listing |
Med Chem
January 2025
Laboratory of Biotechnology and Natural Resources Valorization, Faculty of Sciences of Agadir, Ibn Zohr University, Agadir, Morocco.
Background: We continue to struggle with the prevention and treatment of the influenza virus. The 2009 swine flu pandemic, caused by the H1N1 strain of influenza A, resulted in numerous fatalities. The threat of influenza remains a significant concern for global health, and the development of novel drugs targeting these viruses is highly desirable.
View Article and Find Full Text PDFProkinetic agents are drugs used to enhance gastrointestinal motility and treat disorders such as Gastroesophageal Reflux Disease (GERD) and gastroparesis. pH-dependent release systems offer targeted drug delivery, allowing prokinetic agents to be released specifically in desired regions of the gastrointestinal tract. This optimizes drug efficacy and minimizes systemic side effects.
View Article and Find Full Text PDFSmall
January 2025
DWI-Leibniz Institute for Interactive Materials e.V., RWTH Aachen University, Forckenbeckstr. 50, 52074, Aachen, Germany.
Compartmentalization is crucial for control over complex biological cascade reactions. In microgels, the formation of discrete compartments allows for simultaneous uptake and orthogonal release of physicochemically distinct drugs, among others. However, many state-of-the-art approaches yielding compartmentalized microgels require the use of specific, though not always biocompatible, components and temperatures well above the physiological range, which may damage possible biological cargo.
View Article and Find Full Text PDFMol Pharm
January 2025
Department of Pharmacy, National and Kapodistrian University of Athens, Zografou 15771, Greece.
The simulation of antral conditions for estimating drug apparent equilibrium solubility after a high-calorie, high-fat meal is challenging. In this study, (1) we measured the apparent equilibrium solubility of two model lipophilic drugs, ketoconazole and danazol, in antral aspirates collected at various time points after a minced high-calorie, high-fat meal and a glass of water 30 min after initiation of meal administration, and we designated one point estimate for ketoconazole and one point estimate for danazol; (2) we evaluated the usefulness of FeSSGF-V2 and FEDGAS pH = 3 in reproducing the two point estimates; (3) we evaluated potential compositions of FeSSGF-V3 that simulate the pH, the buffer capacity toward both less acidic and more acidic values, and the antral lipid and protein contents with easily accessible, commercially available products, and (4) we identified the most useful composition of FeSSGF-V3 for reproducing the two point estimates. For both model drugs, apparent solubility in FeSSGF-V2 and in FEDGAS pH 3 deviated substantially from the corresponding point estimate.
View Article and Find Full Text PDFInt J Pharm X
June 2025
Technology of Radiology and Medical Imaging Department, Faculty of Applied Health Science Technology, October 6 University, Egypt.
Objectives: Colorectal cancer is the third most common cancer worldwide, accounting for approximately 10 % of all cancer cases. It is also the second leading cause of cancer-related deaths globally. Phloretin is a natural compound found in apples and other fruits.
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