Frederick D. Sancilio's research while affiliated with Sancilio & Company, Inc. and other places

Publications (8)

Article
Full-text available
Despite recent advances, the drug development process continues to face significant challenges to efficiently improve the poor solubility of active pharmaceutical ingredients (API) in aqueous media or to improve the bioavailability of lipid-based formulations. The inherent high intra- and interindividual variability of absorption of oral lipophilic...
Article
The US Food and Drug Administration (FDA) draft guidance for establishing bioequivalence (BE) of ω-3 acid ethyl esters (containing both eicosapentaenoic acid [EPA] and docosahexaenoic acid [DHA] as ethyl esters), used to treat severe hypertriglyceridemia, recommends the conduct of 2 studies: one with participants in the fasting state and one with p...
Article
Background The absorption of eicosapentaenoic acid (EPA; 20:5n-3) and docosahexaenoic acid (DHA; 22:6n-3) omega-3–acid ethyl esters (EEs) is influenced by food. There is a need for a formulation of EE that is less impacted by food effect. SC401 is a novel Advanced Lipid Technologies–based formulation of EPA-EE and DHA-EE. In the presence of an aque...
Article
Purpose: The US Food and Drug Administration has approved several highly purified ω-3 fatty acid prescription drugs for the treatment of severe hypertriglyceridemia. These differ in the amounts and forms of docosahexaenoic acid (DHA) and/or eicosapentaenoic acid (EPA). This study compared the bioavailability of SC401 (1530 mg EPA-ethyl esters [EEs...
Article
Full-text available
Gout is one of the most common forms of inflammatory arthritis, affecting over 8 million adults in the US. Individuals with gout are advised to avoid the habitual intake of purine-rich foods such as meats, seafood, purine-rich vegetables, and animal protein. An increased risk of developing or having subsequent attacks of gout is particularly associ...

Citations

... Classical ways to increase drugs' water solubility are well known and include strategies related to the modification of the chemical entity itself or strategies dependent on formulation excipients. Modification of the drug molecule itself includes salt formation (which can be useful when the chemical entity has an ionizable moiety) and hydrophilic prodrug development (molecule with an additional moiety that has to be metabolized in order to exhibit pharmacological activity), both of which can result in not only higher aqueous solubility but also increased chemical stability [30]. As for strategies concerning formulation excipients, these include pH control (useful with weak acidic or basic drugs), the use of organic solvents (either the change of the solvent to an oil or, preferentially, the use of water-miscible organic solvents in mixture with water), the use of hydrophilic surfactants (above the critical micellar concentration), and the preparation of soluble complexes. ...
... These formulations help to reduce triglyceride and very-low-density lipoprotein levels ( Figure 15). The mechanism underlying these effects is not very well understood, but the potential mechanisms proposed to date include the inhibition of diacylglycerol acyltransferase, increased activity of plasma lipoprotein lipase, a decrease in lipogenesis, and an increase in β-oxidation in the liver ( Figure 15) [218,223]. ...
... From the perspective of dosage and administration, absorption of this type is poor in the fasting state. But it improves if taken after a high-fat meal (13)(14)(15)(16); therefore, patients are instructed to take it orally after meals. DHA/TG and EPA/TG have also been reported to be affected by the diet (16); however, because the timing of intake is not specified for supplements like it is for pharmaceuticals, it would be helpful to modify the formulation to lessen the impact of factors such as whether it is taken with food and the amount of fat intake. ...
... Self-emulsifying drug delivery systems (SEDDSs) are lipid-based formulations composed of a mixture of oil and surfactants, and optionally cosurfactants and cosolvents, that in contact with an aqueous phase, such as a digestive liquid, and under mild agitation simulating the movements of the gastrointestinal tract, will form a fine and stable emulsion (17,18). Improved absorbability of DHA/EE and EPA/EE through the use of SEDDS has been reported (19)(20)(21)(22)(23). In contrast, research on improving absorption with emulsified DHA/TG and EPA/TG has mainly focused on comparing gelled or emulsified-gelled foods with non-emulsified soft capsules (24)(25)(26). ...
... Currently, a variety of methods have been established for the determination of purines in foods, including ion chromatography [15], capillary electrophoresis [16], enzymeassisted electrochemical detection [17], and high-performance liquid chromatography (HPLC) [18,19]. Among these methods, HPLC is the mainstream detection method. ...