The objective of this study was to evaluate the pharmacokinetics of oral cyclosporin A (CsA) when co-administered to enhance the oral absorption of paclitaxel. Patients received oral paclitaxel in doses of 60-360 mg/m(2) in combination with a dose of oral CsA of 15 mg/kg. Dose escalation of paclitaxel from 60 to 300 mg/m(2) resulted in a significant decrease in the area under the concentration-time curve (AUC) of CsA from 24.4+/-9.9 to 17.6+/-2.8 mg/l.h (p=0.03) (n=28). In conclusion, increases in the paclitaxel dose resulted in a decrease in the AUC of CsA. This observation may be explained by the increase in the co-solvent Cremophor EL of paclitaxel causing reduced absorption of CsA.
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http://dx.doi.org/10.1097/00001813-200108000-00005 | DOI Listing |
Sci Rep
January 2025
Division of Human Nutrition and Health, Wageningen University, Stippeneng 4, 6708 WE, Wageningen, The Netherlands.
Cannabidiol (CBD), a specialized metabolite (phytocannabinoid) abundant in Cannabis sativa, is attracting increasing attention for its alleged health-promoting properties. The present study aimed to investigate the pharmacokinetics of CBD and its primary metabolite, 7-hydroxy-cannabidiol (7-OH-CBD), following a single oral dose of a CBD-rich Cannabis sativa extract, equivalent to 70 mg CBD, in healthy male (n=5) and female (n=6) participants. Using a randomized crossover design, the study evaluated the impact of a standardized high-fat meal compared to fasting on the oral bioavailability of CBD.
View Article and Find Full Text PDFExpert Opin Pharmacother
January 2025
Mediprobe Research Inc, London, ON, Canada.
Introduction: Alopecia affects many individuals, with androgenetic alopecia (AGA) being the most common form in both men and women. The exact etiology of AGA is unclear. The systemic treatments of AGA include 5-alpha reductase inhibitors (finasteride, dutasteride), low-dose oral minoxidil.
View Article and Find Full Text PDFJ Med Chem
January 2025
College of Chemistry, Zhengzhou University, Zhengzhou 450001, China.
The P2YR is activated by UDP and UDP glucose and is involved in many human inflammatory diseases. Based on the molecular docking analysis of currently reported P2YR antagonists and the crystallographic overlap study between PPTN and compound , a series of 3-substituted 5-amidobenzoate derivatives were designed, synthesized, and identified as promising P2YR antagonists. The optimal compound (methyl 3-(1-benzo[]imidazol-2-yl)-5-(2-(-tolyl) acetamido)benzoate, IC = 0.
View Article and Find Full Text PDFBiomater Sci
January 2025
School of Chemistry, Chemical Engineering and Life Science, Hubei Key Laboratory of Nanomedicine for Neurodegenerative Diseases, Wuhan University of Technology, 122 Luoshi Road, Wuhan 430070, China.
To enhance the antibacterial efficacy of tildipirosin against (S.A.) infections, optimized solid lipid nanoparticles loaded with tildipirosin (SLN-TD) were developed, using docosanoic acid (DA), octadecanoic acid (OA), hexadecanoic acid (HA), and tetradecanoic acid (TA) as lipid components.
View Article and Find Full Text PDFRSC Adv
January 2025
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University P.O. Box 80260 Jeddah 21589 Saudi Arabia +966 553399718.
A mutual prodrug of sertraline-methylpropyphenazone (SER-MP) was prepared and characterized using a spectral method. The yield of the prepared SER-MP was 90%, and its purity reached 98.8%.
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