The present study aimed to develop nanocrystal formulations of meloxicam (MEL) in order to enhance its biopharmaceutical properties and provide a rapid onset of action. Nanocrystal formulations were...
Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies
We designed and synthesized of 1,3,5-trioxazatriquinanes with o- or p-hydroxyphenyl rings as analogs of the κ opioid receptor agonist SYK-146 with m-hydroxyphenyl groups.
Biopharmaceutical profiling of new antitumor pyrazole derivatives
Several new pyrazole derivatives have demonstrated promising antiproliferative and cytotoxic effects, but their poor solubility raised concerns over possible biopharmaceutical limitations.
Pazopanib as third line therapy for metastatic renal cell carcinoma: clinical efficacy and temporal analysis of cytokine profile
Purpose: Pazopanib has been assessed primarily in cytokine refractory or treatment naïve patients with metastatic renal cell carcinoma. Outcomes have been associated...
Model-Based Bioequivalence assessment of a commercial Azithromycin Capsule against Pfizer Zithromax® Tablet marketed in Jamaica
Clinical evidence indicated that effective substitution of azithromycin capsule with a tablet dosage form should be based on evidence of providing equivalent in vivo AUC/MIC ratio at the site of infection.
Isoxazolotacrines as non-toxic and selective butyrylcholinesterase inhibitors for Alzheimer’s disease
Owing to the complex nature of Alzheimer's disease, there is a renewed and growing search for multitarget non-toxictacrines as simple, easily available drugs in order to stop the progress and development of the disease.
PEGylated cyclodextrins as novel siRNA nanosystems: Correlations between polyethylene glycol length and nanoparticle stability
Silencing disease-related genes in the central nervous system (CNS) using short interfering RNA (siRNA) holds great promise for treating neurological disorders.
In vitro – in silico – in vivo drug absorption model development based on mechanistic gastrointestinal simulation and artificial neural networks: Nifedipine osmotic release tablets case study
In vitro--in vivo correlations (IVIVC) are generally accepted as a valuable tool in modified release formulation development aimed at (i) quantifying the in vivo drug delivery profile and...
The acute effects of daily nicotine intake on heart rate – A toxicokinetic and toxicodynamic modelling study
Joint physiologically-based toxicokinetic and toxicodynamic (PBTK/TD) modelling was applied to simulate concentration-time profiles of nicotine, a well-known stimulant, in the human body following single and repeated dosing.
Pharmacokinetics of Paracetamol in Göttingen Minipigs: In Vivo Studies and Modeling to Elucidate Physiological Determinants of Absorption
Onset and rate of gastric emptying are important determinants of drug absorption after oral dosing.
Viscosity-mediated negative food effect on oral absorption of poorly-permeable drugs with an absorption window in the proximal intestine: In vitro experimental simulation and computational verification
Concomitant food intake can diminish oral absorption of drugs with limited permeability and an absorption window in the proximal intestine, due to viscosity-mediated decrease in dosage form disintegration time and drug dissolution rate.
Detection and phenotyping of circulating tumor cells in high-risk localized prostate cancer
Background: In this study, we aimed to determine the feasibility of identifying CTCs in patients with HRLPC, using a modified isolation procedure using the CellSearch...
Eslicarbazepine and the enhancement of slow inactivation of voltage-gated sodium channels: A comparison with carbamazepine, oxcarbazepine and lacosamide
This study aimed at evaluating the effects of eslicarbazepine, carbamazepine (CBZ), oxcarbazepine (OXC) and lacosamide (LCM) on the fast and slow inactivated states of voltage-gated sodium channels (VGSC).
Computational Predictions of Glass-Forming Ability and Crystallization Tendency of Drug Molecules
Amorphization is an attractive formulation technique for drugs suffering from poor aqueous solubility as a result of their high lattice energy.
RNA-seq reveals aurora kinase-driven mTOR pathway activation in patients with sarcomatoid metastatic renal cell carcinoma
Sarcomatoid metastatic renal cell carcinoma (mRCC) is associated with a poor prognosis, and the biology of the disease has been inadequately characterized.
Physiologically Based Absorption Modelling to Predict the Impact of Drug Properties on Pharmacokinetics of Bitopertin
Bitopertin (RG1678) is a glycine reuptake inhibitor in phase 3 trials for treatment of schizophrenia. Its clinical oral pharmacokinetics is sensitive to changes in drug substance particle size and dosage form.
Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists
Furan-2-carbohydrazides were found as orally active glucagon receptor antagonists. Starting from the hit compound 5, we successfully determined the structure activity relationships of a series...
Network representations and methods for the analysis of chemical and biochemical pathways
Systems biologists increasingly use network representations to investigate biochemical pathways and their dynamic behaviours.
In Silico Prediction of Major Drug Clearance Pathways by Support Vector Machines with Feature-Selected Descriptors
We have previously established an in silico classification method ("CPathPred") to predict the major clearance pathways of drugs based on an empirical decision with only four physicochemical...
Dissolution testing combined with computer simulation technology to evaluate the bioequivalence of domestic amoxicillin capsule
Re-evaluation of bioequivalence of generic drugs is one of the key research focus currently. As a means to ensure consistency of the therapeutic effectiveness of drug products, clinical bioequivalence...