Previous attempts to improve the dissolution and absorption properties of itraconazole (ITZ) through advanced formulation design have focused only on release in acidic media; however, recent reports indicate that absorption occurs primarily in the proximal small intestine. This suggests that enhancing supersaturation of ITZ in neutral aqueous environments is essential for improving absorption. The aim of this study was to evaluate different polymeric stabilizers with either immediate release (IR) (Methocel™ E5, Methocel™ E50, Kollidon® 12, and Kollidon® 90) or enteric release (EUDRAGIT® L 100-55, HP-55, and HP-55S) properties to determine the chemical and physical attributes of the polymeric stabilizers that promote supersaturation of ITZ in neutral media. Each amorphous composition was produced by hot-melt extrusion and characterized by differential scanning calorimetry. Dissolution testing by a supersaturated acidic-to-neutral pH change method was conducted on each composition. Testing of IR composition...

Enhanced in vivo absorption of itraconazole via stabilization of supersaturation following acidic-to-neutral pH transition.

Microencapsulation has been developed by the pharmaceutical industry as a means to control or modify the release of drug substances from drug delivery systems. In drug delivery systems microencapsulation is used to improve the bioavailability of drugs, control drug release kinetics, minimize drug side effects, and mask the bitter taste of drug substances. The application of microencapsulation has been extended to the food industry, typically for controlling the release of flavorings and the production of foods containing functional ingredients (e.g. probiotics and bioactive ingredients). Compared to the pharmaceutical industry, the food industry has lower profit margins and therefore the criteria in selecting a suitable microencapsulation technology are more stringent. The type of microcapsule (reservoir and matrix systems) produced and its resultant release properties are dependent on the microencapsulation technology, in addition to the physicochemical properties of the core and the shell materials. This review discusses the factors that affect the release of bioactive ingredients from microcapsules produced by different microencapsulation technologies. The key criteria in selecting a suitable microencapsulation technology are also discussed. Two of the most common physical microencapsulation technologies used in pharmaceutical processing, fluidized-bed coating, and extrusion-spheronization are explained to highlight how they might be adapted to the microencapsulation of functional bioactive ingredients in the food industry.

Microencapsulation as a Tool for Incorporating Bioactive Ingredients into Food

Statistical optimisation of diclofenac sustained release pellets coated with polymethacrylic films.

Quinine sulphate pellets for flexible pediatric drug dosing: formulation development and evaluation of taste-masking efficiency using the electronic tongue.

Os polimeros representam uma das classes de materiais mais versateis disponiveis para aplicacoes em diversas areas, inclusive a farmaceutica. Polimeros naturais, naturais modificados e sinteticos sao empregados como excipientes farmaceuticos para a formulacao de cosmeticos e medicamentos de liberacao convencional e de liberacao modificada. Nos dias atuais, polimeros sao desenvolvidos para atuarem como moduladores e direcionadores da liberacao de farmacos em sitios especificos no organismo. Polimeros biodegradaveis, bioadesivos, biomimeticos e hidrogeis responsivos tem sido amplamente incluidos em formulacoes farmaceuticas. Os avancos na idealizacao de novos Sistemas de Liberacao de Farmacos somente sao e serao permitidos a partir do desenvolvimento de polimeros projetados especificamente para a area farmaceutica. Neste sentido, o presente artigo visa a revisar e apresentar informacoes sobre o uso de polimeros em aplicacoes farmaceuticas que poderao ser uteis no planejamento de novos sistemas com desempenhos superiores.

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Aplicações farmacêuticas de polímeros

Formulation and process considerations affecting the stability of solid dosage forms formulated with methacrylate copolymers.

Poly(meth)acrylates were introduced to the pharmaceutical market in 1954 for the use in oral dosage forms in order to replace time-consuming sugar coatings on tablets in the beginning, closely followed by more functional versions in order to create taste masked and protective coatings or enteric-coated as well as extended release-coated particles, but also for the creation of extended release matrix structures.

Wolfgang Weisbrod

Papers

Formulation and process considerations affecting the stability of solid dosage forms formulated with methacrylate copolymers.

Application of Poly(meth)acrylate Copolymers for Oral Multiparticulate Drug Delivery Systems