Progesterone was administered to postmenopausal women in a form of vaginal suppositories containing 100 and 200 mg active substance in Butyrum cacao (BC) and Massa estarinum (ME), a base with emulsifying properties. In the case of single doses, blood samples were taken at 2, 4, 6, 24, 48 and 72 h. Another group of patients received vaginal suppositories (100 mg progesterone) once a day for a 6 day period, with blood samples taken 12 h after each administration. The plasma levels of progesterone were evaluated by radioimmunoassay. The time of maximum concentration (tmax) was 4 h in most cases, and 6 h in the others. The plasma levels were not dose-proportional. Peak plasma concentrations were in the range of 10-15 ng/ml with a mean of 10.5 ng/ml for the 100 mg and 12 ng/ml for the 200 mg doses. The ratio of the mean area under the curve (AUC) for 200 mg and the mean AUC for the 100 mg dose was found to be 1.37. Replacing BC with ME resulted in the lowering of cmax and AUC, and an increase in tmax following a reducing in the rate and extent of adsorption. In the case of ME suppositories, the variability in AUC, cmax and tmax was greater compared to that observed with the BC suppositories. Elimination half-time was in the range of 9-10 h for BC and 14 h for ME suppositories. In vitro assessment of the release kinetics from a hydrophobic and an emulsion type base confirmed previous findings: the latter base assured better pharmaceutical availability. The repeated doses did not seem to produce an accumulation of progesterone in the plasma. On the contrary, a small decrease in plasma levels over time appeared during the 6 day period. Numerical analysis revealed an excellent goodness of fit for the in vivo experimental data via biexponential curves, i.e. a pseudomonocompartmental model.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1007/BF03192299 | DOI Listing |
Int Urol Nephrol
January 2025
Department of Urology, Hualien Tzu Chi Hospital, Buddhist Tzu Chi Medical Foundation, Tzu Chi University, Hualien, Taiwan.
Purpose: Urinary cytokine changes may serve as biomarkers to assess treatment outcomes for interstitial cystitis/bladder pain syndrome (IC/BPS). This study analyzed the changes in urinary cytokines following various bladder therapies and explored their clinical significance in therapeutic mechanisms.
Methods: A total of 122 patients with IC/BPS treated with platelet-rich plasma (PRP), botulinum toxin-A (BoTN-A), hyaluronic acid (HA), or low-energy shock wave (LESW) were evaluated.
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Center of Studies and Research Toxic-Pharmacological, School of Pharmacy, Federal University of Goias, Leste Universitario, 240th Street, Corner of 5th Avenue, Goiania, GO, 74605-170, Brazil.
The CCl-induced hepatotoxicity model is a traditional preclinical assay applied to evaluate potential hepatoprotective compounds. However, several studies have used it with inappropriate dose and exposure time, generating both weak response or irreversible liver injury, as well as lack of representative liver and plasma biomarkers. Therefore, this study aims to determine the best dose and exposure time of CCl in Wistar rats, permitting a proper evaluation of potential hepatoprotective effect.
View Article and Find Full Text PDFAnalyst
January 2025
School of Chemistry, Institute of Science, Suranaree University of Technology, 111 University Avenue, Muang District, Nakhon Ratchasima 30000, Thailand.
Nicotinamide adenine dinucleotide is a crucial coenzyme in cellular metabolism and is implicated in various diseases. This work introduces an electrochemical bioanalytical method utilizing solution-phase formate dehydrogenase (CbFDH) for detecting its oxidized form (NAD) in human blood plasma samples. The detection mechanism involves the catalytic conversion of NAD to NADH, facilitated by CbFDH in the presence of formate.
View Article and Find Full Text PDFJ Cell Sci
January 2025
Department of Molecular Biosciences, Northwestern University, Evanston, IL 60208, USA.
Cells form multiple, molecularly distinct membrane contact sites (MCSs) between organelles. Despite knowing the molecular identity of several of these complexes, little is known about how MCSs are coordinately regulated in space and time to promote organelle function. Here, we examined two well-characterized mitochondria-ER MCSs - the ER-Mitochondria encounter structure (ERMES) and the mitochondria-ER-cortex anchor (MECA).
View Article and Find Full Text PDFAnesthesiology
January 2025
Department of Anesthesiology, Sunnybrook Health Sciences Centre, Toronto, ON, Canada.
Background: Tranexamic acid is an anti-fibrinolytic agent routinely used during hip and knee joint replacement surgery to minimize bleeding. Chronic kidney disease is a common chronic health problem seen among adults requiring major arthroplasty surgery. Tranexamic acid is renally cleared and may accumulate in chronic kidney disease.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!