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Amorphous solid dispersions (ASDs) are used as bioavailability enhancing formulations on the premise of the increased solubility of the amorphous form over its crystalline counterpart. Recent studies have shown that ASDs can, during dissolution, generate amorphous nanoparticles that were initially postulated to serve as a source of rapidly dissolving compound during absorption. Researchers have proposed that nanoparticles, including crystalline nanoparticles, may provide additional benefits to absorption such as drifting in the mucous layer. However, there are limited published data on the impact of nanoparticle size on bioavailability in vivo and, to our knowledge, there have been no published examples looking at the impact of differential size of in situ generated nanoparticles from an ASD. Anacetrapib, a highly lipophilic, Biopharmaceutics Classification System IV compound, formulated as an ASD that generates nanoparticles upon dissolution, was used in the studies described in this manuscript. A differential response in bioavailability was observed with ∼100 nm or smaller particles resulting in higher average exposure compared to ∼200 nm or larger particles. This increase in bioavailability could not be fully accounted for by the improvement in dissolution rate and was not as pronounced as that achieved by improving solubilization by co-administration with a high fat meal.
This article was published in the following journal.
Name: Journal of pharmaceutical sciences
Magnetic Fe-B, Fe-Ni-B, and Co-B nanoparticles were successfully synthesized and introduced to water to prepare aqueous ferrofluids. The Fe-B, Fe-Ni-B, and Co-B particles are homogeneous amorphous nan...
Increases in food portion sizes have been identified as a possible contributor to the increased prevalence of obesity in humans. However, little is known about the origin of behavioural tendencies to ...
More than 40% of newly developed drug molecules are highly hydrophobic and, thus, suffer from low bioavailability. Kinetically trapping the drug as a nanoparticle in an amorphous state enhances solubi...
Strain variation within nanoparticles plays a crucial role in defining important properties related to their applications. Transmission electron microscopy (TEM) based imaging techniques are mostly us...
Polymorphism of pharmaceutical substances has a significant impact on their physicochemical properties, durability, bioavailability and consequently on their pharmacological activity. Solid dosage for...
This study will evaluate the effects of 2 different dose levels of anacetrapib on low-density lipoprotein-cholesterol (LDL-C) and high-density lipoprotein cholesterol (HDL-C) in participan...
This study is to investigate the bioavailability of a hot-melt extruded amorphous solid dispersion formulation of Efavirenz compared to a marketed formulation(Stocrin®).
There are currently no studies evaluating the effect of anacetrapib on blood vessel function and stiffness of the arteries. The REVEAL-Vasc trial will assess whether anacetrapib, in additi...
For persons with impairments and certain illnesses the use of service dogs may have positive effect. The effects of using these dogs to assist in every day life need to be studied further....
This study will evaluate the Area Under the Curve (AUC(0 to infinity)) of anacetrapib in subjects with impaired renal function and healthy matched control subjects.
Congenital vascular anomalies in the brain characterized by direct communication between an artery and a vein without passing through the CAPILLARIES. The locations and size of the shunts determine the symptoms including HEADACHES; SEIZURES; STROKE; INTRACRANIAL HEMORRHAGES; mass effect; and vascular steal effect.
An effect usually, but not necessarily, beneficial that is attributable to an expectation that the regimen will have an effect, i.e., the effect is due to the power of suggestion.
A family of terrestrial carnivores with long snouts and non-retractable claws. Members include COYOTES; DOGS; FOXES; JACKALS; RACCOON DOGS; and WOLVES.
A species of gram-positive bacteria in the family STAPHYLOCOCCACEAE. It is a zoonotic organism and common commensal in dogs, but can cause disease in dogs and other animals. It also can be associated with human disease.
A synthetic PGE2 analog that has an inhibitory effect on gastric acid secretion, a mucoprotective effect, and a postprandial lowering effect on gastrin. It has been shown to be efficient and safe in the treatment of gastroduodenal ulcers.