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Oral bioavailability
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The use of natural-origin active compounds in disease treatment is currently a prevailing trend. Mangiferin, a major component found in mangoes, is present in relatively high proportions. To develop a formulation and process for producing nano mangiferin using the selfassembly method with phosphatidylcholine and chitosan.
10p
vikoch
27-06-2024
2
1
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Egypt is the world's largest date producing country. Different functional foods pertaining to date seeds were attempted before. Phenolic phytochemicals are not well absorbed in gastrointestinal tract, which results in lower bioactivity. Nanotechnology helps to resolve poor oral bioavailability. Aim was to evaluate the in-vivo anti-inflammatory properties of date seed powder (DSP) nanoparticles (NPs) and infusion in rats fed a high fat diet (HFD).
10p
viisac
23-09-2023
5
1
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The recent pharmaceutical interest toward confinement effects on the physical state, solubility and release of drugs has paved the way to new material designs for drug delivery. Deeper understanding on how the pore size or the additional functionalities of the nanocarriers can influence the bioavailability of the cargo is nonetheless needed to explore further the potential of nanocarriers in this area.
8p
vironald
15-12-2022
11
2
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Oral semaglutide is the only orally available GLP-1 receptor agonist. To achieve adequate bioavailability after oral administration, co-formulation with an absorption enhancer is needed.
5p
viporsche
28-10-2022
11
2
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In silico studies reports that their physicochemical, ADMET and druglikeness properties were found to be in standard limit, which infers that, these compounds may not have problems with oral bioavailability. Molecular docking studies showed that the pyrimidines have better enzyme inhibitory activity onTMPKmt.
4p
mudbound
10-12-2021
7
1
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In the present experiment the depletion profile study of Albendazole and its metabolites (ABZSO and ABZSO2) were carried out in the plasma of Pangasianodon hypophthalmus. The experiment consists of three treatment groups and control. A 20mg/kg body weight dose of ABZ was given through intraperitoneal, intramuscular and orally respectively to the three treatment groups while no drug was given to control group.
9p
nguathienthan8
20-10-2020
12
1
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Poor initial response to tamoxifen due to CYP2D6 polymorphism and adverse side effects are two clinical challenges in tamoxifen therapy. We report the development and preclinical testing of a boronic prodrug to orally deliver 4-OHT at therapeutically effective concentrations but at a fraction of the standard tamoxifen dose.
9p
viamsterdam
18-09-2020
10
0
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Venetoclax (ABT-199), a first-in-class orally bioavailable BCL-2-selective inhibitor, was recently approved by the FDA for use in patients with 17p-deleted chronic lymphocytic leukemia who have received prior therapy. It is also being evaluated in numerous clinical trials for treating patients with various hematologic malignancies.
10p
vidhaka2711
31-07-2020
11
1
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Doxorubicin hydrochloride (DOX·HCl), an anthracycline glycoside antibiotic, exhibits low oral bioavailability due to active efflux from intestinal P-glycoprotein receptors. The oral administration of DOX remains a challenge hence; no oral formulation for DOX is marketed, till date.
14p
vijiraiya2711
27-05-2020
14
1
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A sensitive, specific, reproducible and optimized high performance liquid chromatography with fluorescence detection (HPLC-FLD) method for the determination of bergapten in rat plasma was established and applied to the pharmacokinetic and bioavailability study in rat after oral and intravenous administration of bergapten.
8p
vijiraiya2711
27-05-2020
10
0
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Capsaicin has multiple pharmacological activities including antioxidant, anticancer, and antiinflammatory activities. However, its clinical application is limited due to its poor aqueous solubility, gastric irritation, and low oral bioavailability. This research was aimed at preparing sustained-release matrix pellets of capsaicin to enhance its oral bioavailability.
11p
caothientrangnguyen
09-05-2020
7
0
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This work aimed at improving the solubility of curcumin by the preparation of spray-dried ternary solid dispersions containing Gelucire®50/13-Aerosil® and quantifying the resulting in vivo oral bioavailability and anti-inflammatory activity. The solid dispersion containing 40% of curcumin was characterised by calorimetry, infrared spectroscopy and X-ray powder diffraction. The solubility and dissolution rate of curcumin in aqueous HCl or phosphate buffer improved up to 3600- and 7.3-fold, respectively.
10p
caothientrangnguyen
09-05-2020
14
2
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Chemotherapy via oral route of anticancer drugs offers much convenience and compliance to patients. However, oral chemotherapy has been challenged by limited absorption due to poor drug solubility and intestinal efflux. In this study, we aimed to develop a nanosuspension formulation of oridonin (Odn) using its cyclodextrin inclusion complexes to enhance oral bioavailability. Nanosuspensions containing Odn/2 hydroxypropyl-β-cyclodextrin inclusion complexes (Odn-CICs) were prepared by a solvent evaporation followed by wet media milling technique.
9p
caothientrangnguyen
09-05-2020
14
1
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To improve the solubility and oral bioavailability of erlotinib, a poorly water-soluble anticancer drug, solid self-emulsifying drug delivery system (SEDDS) was developed using solid inert carriers such as dextran 40 and Aerosil® 200 (colloidal silica). The preliminary solubility of erlotinib in various oils, surfactants, and co-surfactants was determined. Labrafil M2125CS, Labrasol, and Transcutol HP were chosen as the oil, surfactant, and co-surfactant, respectively, for preparation of the SEDDS formulations. The ternary phase diagram was evaluated to show the self-emulsifying area.
8p
caothientrangnguyen
09-05-2020
13
1
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The administration of ketones to induce a mild ketosis is of interest for the alleviation of symptoms associated with various neurological disorders. This study aimed to understand the pharmacokinetics (PK) of D-β-hydroxybutyrate (BHB) and quantify the sources of variability following a dose of (R)-3-hydroxybutyl (R)-3-hydroxybutyrate (ketone monoester). Healthy volunteers (n = 37) were given a single drink of the ketone monoester, following which, 833 blood BHB concentrations were measured. Two formulations and five dose levels of ketone monoester were used.
11p
caothientrangnguyen
09-05-2020
14
1
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AR-42, a new orally bioavailable, potent, hydroxamate-tethered phenylbutyrate class I/IIB histone deacetylase inhibitor currently is under evaluation in phase 1 and 2 clinical trials and has demonstrated activity in both hematologic and solid tumor malignancies. This report focuses on the preclinical characterization of the pharmacokinetics of AR-42 in mice and rats.
9p
caothientrangnguyen
09-05-2020
17
2
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Quantifying the multiple processes which control and modulate the extent of oral bioavailability for drug candidates is critical to accurate projection of human pharmacokinetics (PK). Understanding how gut wall metabolism and hepatic elimination factor into first-pass clearance of drugs has improved enormously. Typically, the cytochrome P450s, uridine 5′- diphosphate-glucuronosyltransferases and sulfotransferases, are the main enzyme classes responsible for drug metabolism. Knowledge of the isoforms functionally expressed within organs of first-pass clearance, their anatomical topology (e.
16p
caothientrangnguyen
09-05-2020
18
0
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Instantly dissolving buccal films have gained attention owing to their easy administration and capability to surmount the hepatic first pass effect of drugs. Dapoxetine hydrochloride (DPX) has a low oral bioavailability due to significant hepatic first pass metabolism. In addition, DPX is a weakly basic drug with a pH dependent solubility that could limit its dissolution in the body neutral fluids.
10p
partimesinhvien
08-05-2020
15
1
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Pueraria candollei var. mirifica is a medicinal plant that is promoted as a “Champion Product” by the Government of Thailand. This plant has been reported to relieve postmenopausal symptoms, prevent and reverse bone loss, inhibit the growth of breast cancer, and alleviate cardiovascular diseases in preclinical and clinical studies.
9p
vimax2711
30-03-2020
11
1
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Quercetin (QT) as a bioactive flavonoid has a potential therapeutic activity for numerous neuronal injuries and neurodegenerative diseases. However, the low absorption rate of QT, especially through the bloodbrain barrier, restricts its bioactivity in the body.
12p
vimax2711
30-03-2020
9
1
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