Aims: The aims of the study were to: (1) evaluate the gastrointestinal transit, release and absorption of budesonide from tablets with a new multimatrix formulation (MMX) designed to release the drug throughout the whole colon, and (2) assess the influence of food on budesonide bioavailability.
Methods: Two phase I studies, each comprising 12 healthy males, were performed. Gastrointestinal transit of (153)Sm-labelled tablets containing 9 mg budesonide was evaluated by means of pharmaco-scintigraphy. The effect of food was tested by comparing plasma pharmacokinetics after intake of a high fat and high calorie breakfast with fasting controls.
Results: (153)Sm-labelled tablets reached the ascending colon after a mean +/- SD 9.8 +/- 6.9 h. Initial tablet disintegration was observed in the ileum in 42% and the ascending and transverse colon in 33% of subjects. Ninety-six per cent of the dose was absorbed into the systemic circulation during passage through the whole colon including the sigmoid. Food significantly decreased C(max) values from 1429 +/- 1014 to 1040 +/- 601 pg mL(-1) (P = 0.028) and AUC values from 14 814 +/- 11 254 to 13 486 +/- 9369 pg h(-1) mL(-1) (P = 0.008). Mean residence time and t(max) increased by 12-29%. There was no drug accumulation after 1 week of once daily oral administration of budesomide.
Conclusions: MMX-budesonide tablets appear suitable for targeted colonic drug delivery. Transit parameters and low systemic bioavailability warrant further studies with the new formulation.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1884991 | PMC |
| http://dx.doi.org/10.1111/j.1365-2125.2005.02517.x | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Gene therapy ameliorates bowel dysmotility and enteric neuron degeneration and extends survival in lysosomal storage disorder mouse models.
Sci Transl Med
January 2025
Department of Pediatrics, Washington University in St. Louis, School of Medicine, St. Louis, MO 63110, USA.
Children with neurodegenerative disease often have debilitating gastrointestinal symptoms. We hypothesized that this may be due at least in part to underappreciated degeneration of neurons in the enteric nervous system (ENS), the master regulator of bowel function. To test this hypothesis, we evaluated mouse models of neuronal ceroid lipofuscinosis type 1 and 2 (CLN1 and CLN2 disease, respectively), neurodegenerative lysosomal storage disorders caused by deficiencies in palmitoyl protein thioesterase-1 and tripeptidyl peptidase-1, respectively.
View Article and Find Full Text PDFAdvanced polymeric systems for colon drug delivery: from experimental models to market applications.
Soft Matter
January 2025
Department of Chemical Materials and Industrial Production (DICMaPI), University of Naples Federico II, P.le Tecchio 80, Naples 80125, Italy.
In recent years, nano and micro drug delivery systems targeting the colon have gained more attention due to increasing interest in treating colon diseases such as colorectal cancer and inflammatory bowel disease, , Crohn's disease and ulcerative colitis. Usually, nanocarriers are exploited for their enhanced permeability properties, allowing higher penetration effects and bioavailability, while microcarriers are primarily used for localized and sustained release. In bowel diseases, carriers must go into a delicate environment with a strict balance of gut bacteria (, colon), and natural or biodegradable polymers capable of ensuring lower toxicity are preferred.
View Article and Find Full Text PDFPolysaccharide-based drug delivery targeted approach for colon cancer treatment: A comprehensive review.
Int J Biol Macromol
January 2025
Department of Gastroenterology, Shengjing Hospital of China Medical University, Shenyang, Liaoning, China. Electronic address:
Colon cancer is a leading cause of cancer-related morbidity and mortality worldwide, necessitating advancements in therapeutic strategies to improve outcomes. Current treatment modalities, including surgery, chemotherapy, and radiation, are limited by systemic toxicity, low drug utilization rates, and off-target effects. Colon-targeted drug delivery systems (CDDS) offer a promising alternative by leveraging the colon's unique physiology, such as near-neutral pH and extended transit time, to achieve localized and controlled drug release.
View Article and Find Full Text PDFAssociation of Mucin-Degrading Gut Microbiota and Dietary Patterns with Colonic Transit Time in Constipation: A Secondary Analysis of a Randomized Clinical Trial.
Nutrients
December 2024
Department of Bioconvergence, Hoseo University, 165 Sechul-Ri, BaeBang-Yup, Asan 31499, ChungNam-do, Republic of Korea.
Background: The relationship between gut microbiota composition, lifestyles, and colonic transit time (CTT) remains poorly understood. This study investigated associations among gut microbiota profiles, diet, lifestyles, and CTT in individuals with subjective constipation.
Methods: We conducted a secondary analysis of data from our randomized clinical trial, examining gut microbiota composition, CTT, and dietary intake in baseline and final assessments of 94 participants with subjective constipation.
Feasibility and complications of videocapsule endoscopy in dogs weighing 7 kg or less.
J Vet Intern Med
January 2025
Department of Clinical Studies, Ontario Veterinary College, University of Guelph, Guelph, Ontario, Canada.
Background: Videocapsule endoscopy (VCE) is a valuable tool for investigating gastrointestinal (GI) diseases in dogs. Its use is not recommended in dogs ≤4.3 kg, because of risks of GI endoscopic capsule (EC) retention and bowel obstruction.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!