Accelerated reactive dissolution model of drug release from long-acting injectable formulations.

Long-acting injectable formulations represent a rapidly emerging category of drug delivery systems that offer several advantages compared to orally administered medicines. Rather than having to frequently swallow tablets, the medication is administered to the patient by intramuscular or subcutaneous injection of a nanoparticle suspension that forms a local depot from which the drug is steadily released over a period of several weeks or months. The benefits of this approach include improved medication compliance, reduced fluctuations of drug plasma level, or the suppression of gastrointestinal tract irritation.

Occurrence and prevention of Pickering foams in pharmaceutical nano-milling.

Particle size reduction to sub-micrometer dimensions in stirred media mills is an increasingly common formulation strategy used for improving the bioavailability of poorly aqueous soluble active pharmaceutical ingredients (APIs). Due to their hydrophobic character, the API particles need to be stabilised by a surfactant in order to form a stable nano-suspension. This work is concerned with the understanding of an undesired phenomenon often encountered during the development and scale-up of wet nano-milling processes for hydrophobic APIs - the formation of foams.

Scale-up from batch to flow-through wet milling process for injectable depot formulation.

Injectable depot formulations are aimed at providing long-term sustained release of a drug into systemic circulation, thus reducing plasma level fluctuations and improving patient compliance. The particle size distribution of the formulation in the form of suspension is a key parameter that controls the release rate. In this work, the process of wet stirred media milling (ball milling) of a poorly water-soluble substance has been investigated with two main aims: (i) to determine the parametric sensitivity of milling kinetics; and (ii) to develop scale-up methodology for process transfer from batch to flow-through arrangement.

Preparation of feed premix for veterinary purposes.

This experimental study describes the preparation of a veterinary medicated premix containing tetracycline hydrochloride for oral administration to aquatic animals. For the manufacture of the premix, commercially produced animal feed is used, which is intended for consumption in the form of pellets that were coated with a mixture of chlortetracycline hydrochloride and other excipients. Feed pellets were combined with a mixture of an active substance and excipients with a large specific surface (colloidal silica - Aerosil® 200) allowing an easy adhesion to the surface of the pellets, and a solid polymer with a low glass transition point (Eudragit® E) which ensures the formation of a hard coat.