Pharmacology

Studies on pharmacokinetics and bioavailability of aminophylline in partridge chickens
Veterinary medicine plays a significant role in the development of animal husbandry. Drugs residual in food would follow the food-chain coming into human body, which might bring hidden dangers to people. Chicken is the prime source of meat food, whose quality is important for our life and health. Therefore, it is necessary to realize the withdrawal period and establish an efficient, sensitive a...


Metabolic pathway profiling of the derivative of important herbal component noscapine
The present study aims to investigate the influence of metabolic behavior by the introduction of bromo atom into the structure of noscapine. Oral gavage of 50 mg/kg bromo-noscapine for 6- to 8-week-old male mice with C57BL/6 background resulted in the detection of the metabolite undergoing cleavage of methylenedioxy group (II), demethylated bromo-noscapine (III, IV), meconine (V), bromo-cotarn...
Emerging Technologies to Increase Ligand Binding Assay Sensitivity
Ligand binding assays (LBAs) have been the method of choice for protein analyte measurements for more than four decades. Over the years, LBA methods have improved in sensitivity and achieved larger dynamic ranges by using alternative detection systems and new technologies. As a consequence, the landscape and application of immunoassay platforms has changed dramatically. The introduction of bead...


Comparative Pharmacology and Toxicology of Pharmaceuticals in the Environment: Diphenhydramine Protection of Diazinon Toxicity in Danio rerio but Not Daphnia magna
Pharmaceuticals and other contaminants of emerging concern present unique challenges to environmental risk assessment and management. Fortunately, mammalian pharmacology and toxicology safety data are more readily available for pharmaceuticals than other environmental contaminants. Identifying approaches to read-across such pharmaceutical safety information to non-target species represents a ma...
Biodegradable Microparticles Loaded with Doxorubicin and CpG ODN for In Situ Immunization Against Cancer
In situ immunization is based on the concept that it is possible to break immune tolerance by inducing tumor cell death in situ in a manner that provides antigen-presenting cells such as dendritic cells (DCs) with a wide selection of tumor antigens that can then be presented to the immune system and result in a therapeutic anticancer immune response. We designed a comprehensive approach to in s...


Molecular Interaction Studies of Amorphous Solid Dispersions of the Antimelanoma Agent Betulinic Acid
Betulinic acid (BA), a novel natural product with antimelanoma activity, has poor aqueous solubility (...
Determining the Polymer Threshold Amount for Achieving Robust Drug Release from HPMC and HPC Matrix Tablets Containing a High-Dose BCS Class I Model Drug: In Vitro and In Vivo Studies
It is challenging to achieve mechanically robust drug-release profiles from hydrophilic matrices containing a high dose of a drug with good solubility. However, a mechanically robust drug release over prolonged period of time can be achieved, especially if the viscosity and amount of the polymer is sufficiently high, above the “threshold values.” The goal of this research was to determine t...

Effects of opioids on human serotonin transporters
The serotonin (5-hydroxtryptamine, 5-HT) system plays a role in analgesia and emesis. The aim of this study was to test whether opioids or ketamine inhibit the human 5-HT transporter and whether this increases free plasma 5-HT concentrations. HEK293 cells, stably transfected with the human 5-HT transporter cDNA, were incubated with morphine, hydromorphone, fentanyl, alfentanil, pethidine (meper...
Paraplegia after epidural-general anesthesia in a Morquio patient with moderate thoracic spinal stenosis
We describe an instance in which complete paraplegia was evident immediately postoperatively after apparently uneventful lumbar epidural-general anesthesia in a patient with Morquio Type A syndrome (Morquio A) with moderate thoracic spinal stenosis. A 16-yr-old male with Morquio A received lumbar epidural-general anesthesia for bilateral distal femoral osteotomies. Preoperative imaging had reve...

Ultrasound-guided saphenous nerve block – within versus distal to the adductor canal: a proof-of-principle randomized trial
Reliable saphenous nerve blockade is a desirable complement to popliteal sciatic nerve blockade for foot and ankle surgery. We compared two promising ultrasound-guided techniques, the supine adductor canal (AC) technique and the prone peri-saphenous branch of the descending genicular artery (Peri-SBDGA) technique, using 8 mL of 2% lidocaine with epinephrine 1:400,000. Following Research Ethic...
Simultaneous active intracellular delivery of doxorubicin and C6-ceramide shifts the additive/antagonistic drug interaction of non-encapsulated combination
Drug resistance remains the Achilles tendon undermining the success of chemotherapy. It has been recognized that success requires the identification of compounds that, when combined, lead to synergistic tumor inhibition while simultaneously minimizing systemic toxicity. However, in vivo application of such protocols is dependent on the ability to deliver the appropriate drug ratio at the tumor ...

Liposomal carfilzomib nanoparticles effectively target multiple myeloma cells and demonstrate enhanced efficacy in vivo
Carfilzomib, a recently FDA-approved proteasome inhibitor, has remarkable anti-myeloma (MM) activity. However, its effectiveness is limited by associated severe side-effects, short circulation half-life, and limited solubility. Here, we report the engineering of liposomal carfilzomib nanoparticles to overcome these problems and enhance the therapeutic efficacy of carfilzomib by increasing tumor...
Sedative Agents and Prophylaxis in ICU Delirium
Delirium is a form of acute brain dysfunction in the critically ill that is associated with significant morbidity and mortality in addition to increases in healthcare costs. Important risk factors for delirium include a patient’s underlying illness, metabolic disturbances, sedative and psychoactive medications, and underlying cognitive impairment. Vigilant monitoring and recognition are the f...
A New Reversible and Potent P2Y 12 Receptor Antagonist (ACT-246475): Tolerability, Pharmacokinetics, and Pharmacodynamics in a First-in-Man Trial
ACT-246475 is a new reversible, selective, and potent antagonist of the platelet P2Y12 receptor. This study was a first-in-man trial investigating the tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of ACT-246475 and its di-ester prodrug (ACT-281959) in healthy males. The study had a double-blind, randomized, ascending single-dose design with an oral formulation F1 (i....
Add-On Treatment with Pregabalin for Patients with Uncontrolled Neuropathic Pain Who Have Been Referred to Pain Clinics
The aim of this study was to investigate the impact of pregabalin on pain, other symptoms, and patient-reported outcomes for patients with uncontrolled pain who have been referred to pain clinics. Adult patients with uncontrolled pain who had a score of ≥4 in the DN4 questionnaire were evaluated at baseline, month 3, and month 6. Evaluations included pain levels using a visual analog (VAS) sc...