3D Raman mapping as an analytical tool for investigating the coatings of coated drug particles.

The properties of dry-coated paracetamol particles (fast-dissolving model drug) with carnauba wax particles as the coating agent (dissolution retardant) were investigated. Raman mapping technique was used to non-destructively examine the thickness and homogeneity of coated particles. The results showed that the wax existed in two forms on the surface of the paracetamol particles, forming a porous coating layer: i) whole wax particles on the surface of paracetamol and glued together with other wax surface particles, and ii) deformed wax particles spread on the surface. Regardless of the final particle size fraction (between 100 and 800 µm), the coating thickness had high variability, with average thickness of 5.9 ± 4.2 µm. The ability of carnauba wax to decrease the dissolution rate of paracetamol was confirmed by dissolution of powder and tablet formulations. The dissolution was slower for larger coated particles. Tableting further reduced the dissolution rate, clearly indicating the impact of subsequent formulation processes on the final quality of the product.

3D Raman mapping as an analytical tool for investigating the coatings of coated drug particles / 药物分析学报

The properties of dry-coated paracetamol particles(fast-dissolving model drug)with carnauba wax particles as the coating agent(dissolution retardant)were investigated.Raman mapping technique was used to non-destructively examine the thickness and homogeneity of coated particles.The results showed that the wax existed in two forms on the surface of the paracetamol particles,forming a porous coating layer:i)whole wax particles on the surface of paracetamol and glued together with other wax surface particles,and ii)deformed wax particles spread on the surface.Regardless of the final particle size fraction(between 100 and 800 μm),the coating thickness had high variability,with average thickness of 5.9±4.2 μm.The ability of carnauba wax to decrease the dissolution rate of paracetamol was confirmed by dissolution of powder and tablet formulations.The dissolution was slower for larger coated particles.Tableting further reduced the dissolution rate,clearly indicating the impact of subsequent formulation processes on the final quality of the product.

Pharmaceutical Product Characterization and Manufacturability of Surfactant-Enriched Oil Marbles with Abiraterone Acetate.

The present study investigates the physicochemical properties and stability of a novel lipid-based formulation-surfactant-enriched oil marbles containing abiraterone acetate. While the biopharmaceutical performance of this formulation has been reported recently, this study aims to fill the gap between a promising in vivo performance and industrial applicability. A series of techniques were employed to assess the solid-state characteristics of oil marble cores along with their physicochemical properties upon stability testing. The chemical stability of abiraterone acetate in the formulation was also investigated. The core of the formulation was found to be stable both physically and chemically over 12 months of storage. The in vitro performance of stressed samples was evaluated using a dissolution experiment. The formulation has successfully self-emulsified upon incubation in bio-relevant media, resulting in a fast and complete API release. An important issue connected with the excipient used as a covering material of oil marbles has been identified. The seemingly insignificant water sorption caused agglomeration of the oil marbles and consequently compromised the dissolution rate in some of the stressed samples. Replacing HPMC with lactose as a covering material resulted in more favorable properties upon storage. Overall, it has been shown that oil marbles are an industrially applicable concept of the solidified lipid-based formulation.

Monitoring of particle sizes distribution during Valsartan precipitation in the presence of nonionic surfactant.

Particle size is a key parameter when dealing with drug particle formation, delivery or dissolution. The correct measurement of particle size depends on various factors, such as sample preparation or dilution, but also on the choice of method for its characterization. In this work, we study the process of precipitation of poorly water-soluble drug Valsartan from supersaturated solution in the presence of nonionic surfactant Tween 20. Several techniques including dynamic light scattering (DLS) operated in several measuring modes, optical microscope (OM) and static light scattering (SLS) were used to analyze the kinetics of particle formation. As concluded by the results, the increase in turbidity of the solution seriously limits the application of classical DLS to properly measure the particle size and polydispersity. One way to get around this restriction is by dilution, which however results in a decrease in the size of Valsartan particles in the studied population. In contrast, here we present for a first time technique based on modulated 3D cross correlation DLS equipped with the sample goniometer to determine size of submicron particles of the drug in highly turbid solutions. Additionally, a modified OM was used to measure micron-sized particles for samples without any dilution in a continuous mode. Measured particle sizes combined with measured Valsartan concentration allowed us to identify mechanism responsible for the particle formation from supersaturated solutions. The main mechanism, as it is shown in this work, is covering surface of precipitate particles by the amount of used Tween 20.