04. September 2018
A decrease in the release rate over time is typically encountered when dealing with hydrophilic matrix systems for oral prolonged release due to progressive increase of the distance the drugmolecules have to cover to diffuse outwards and reduction of the area of the glassy matrix at the swelling front. In order to solve this issue, a novel formulation approach based on non-uniformdistribution of the active ingredient throughout the swellable polymer matrix was proposed and evaluated. Various...
25. April 2018
Parenteral sustained release systems for proteins which provide therapeutic levels over a longer period avoiding frequent administration, which preserve protein stability during manufacturing, storage and application and which are biodegradable and highly biocompatible in the body are intensively sought after. The aim of this study was to generate and study mannitol core microparticles loaded with a monoclonal antibody IgG1 and coated with lipid either hard fat or glyceryl stearate at different...
01. March 2018
Form changes during drug product processing can be a risk to the final product quality in terms of chemical stability and bioavailability. In this study, online Raman spectroscopy was used to monitor the form changes in real time during high shear wet granulation of Compound A, a highly soluble drug present at a high drug load in an extended release formulation. The effect of water content, temperature, wet massing time and drying technique on the degree of drug transformation were examined.
06. November 2017
The aim of this study was to improve the pharmaceutical properties of theobromine (TB), particularly its flowability and dissolution rate, by preparing solid dispersions using different technologies (hot melt extrusion—HME, freeze-drying—FD, and supercritical fluid—SF) as well as testing different hydrophilic polymeric matrixes (Eudragit™ E, Plasdone™ S and Soluplus™)
11. August 2017
The goal of this study was to test the feasibility to load non-ordered, non-spherical mesoporous silica with the model drug paracetamol, and subsequently coat the loaded particles using one single pilot scale fluid bed system equipped with a Wurster insert. Mesoporous silica particles (Davisil®) with a size ranging from 310 to 500 μm and an average pore diameter of 15 nm were loaded with paracetamol to 18.8% drug content. Subsequently, loaded cores were coated with ethylcellulose to obtain...
07. February 2017
Abstract Enteric-coated fixed-dose combinations of ezetimibe and lovastatin were prepared by fluid bed coating aiming to avoid the acidic conversion of lovastatin to its hydroxyacid derivative. In a two-step process, sucrose beads were layered with a glass solution of ezetimibe, lovastatin and Soluplus®, top-coated with an enteric layer. The impact of different bead size, enteric polymers (Eudragit L100® and Eudragit L100-55®) and coating time was investigated. Samples were evaluated by...
17. November 2016
Abstract This study aimed to apply quality risk management based on the The International Conference on Harmonisation guideline Q9 for the early development stage of hot melt coated multiparticulate systems for oral administration. N-acetylcysteine crystals were coated with a formulation composing tripalmitin and polysorbate 65. The critical quality attributes (CQAs) were initially prioritized using failure mode and effects analysis. The CQAs of the coated material were defined as particle...
30. October 2016
Abstract Diclofenac topical formulations are often preferred for drug administration to patients who experience serious GIT problems. Absorption of the drug through the skin, however, can be challenging due to the natural protective feature of the stratum corneum (SC). In this article, fluid gels prepared from gellan gum were explored as a topical drug delivery vehicle. Rheological analysis of the formulations showed that it was possible to produce a topical gel with a viscosity and the...
26. October 2016
Abstract The multiparticulate drug product concept covering micropellets, pellets, and mini-tablets is presented as a highly feasible approach to present convenient and patient friendly medication for the geriatric population. Improved swallowability and optimized administration regimen going along with defined drug dosage are achievable. Extemporaneous preparation of medicines from standard medication can be avoided going along with improved patient safety. With one multiparticulate pellet,...
09. August 2016
Abstract This work aimed at developing enalapril maleate granules in order to improve its stability in solid dosage form. Granules were prepared by hot melt granulation using a fluidized bed apparatus. Gelucire 50/13®, polyethylene glycol 6000 e Poloxamer 407® were studied and compared as binders in 2 × 2 factorial designs where the proportions of enalapril maleate, binders and spray dried lactose were varied. The granulation process resulted in high yields and granule sizes that...