Because of the specific thermodynamic properties of active pharmaceutical ingredients, the process of crystallization often meets implementation challenges in the pharmaceutical industry. Therefore, it is essential to select the appropriate method and system for the crystallization of a drug. Ceritinib, an active ingredient in the treatment of lung cancer, was formed as a result of pH modification during the cooling crystallization of ceritinib dihydrochloride solution. By carrying out processes in various solvent systems, several polymorphs were produced. A combination of forms B and C was generated in the ethanol–water system, resulting in smaller crystals. The acetone–water system produced pure form A, which has larger crystals and is more applicable for forthcoming studies. To additionally enhance granulometric properties, ceritinib form A was recrystallized in tetrahydrofuran at different temperatures using antisolvent crystallization. Crystallization at a higher saturation temperature results in larger and more compact crystals, which enhances filtration and drying.

The formulation process for some drugs can be challenging, due to their unfavorable physical and mechanical properties and poor water solubility. Powder technology has made a significant impact in regard to the modification of the particles in active pharmaceutical ingredients (APIs) to produce high-quality granules. Spherical particles are preferred over other shapes, due to their high tap and bulk density, reduced dustiness, better flowability, strong anti-caking properties, and better mechanical performance during tableting. The present study investigates the possibility of obtaining spherical crystals of ceritinib, a drug used for the treatment of anaplastic lymphoma kinase (ALK)-positive advanced non-small cell lung cancer, which belongs to BCS class IV drugs and has a platy crystal shape. Ceritinib spheres were prepared by spherical agglomeration, in a ternary system, and quasi-emulsion solvent diffusion, with the addition of polyvinylpyrrolidone, as well as a combination of these two methods. With the combined method of spherical crystallization, crystals with the most favorable morphology and the narrowest distribution of particle sizes were obtained, which was the reason for further optimization. The influence of different impeller geometries and mixing rates on the morphology of the obtained crystals was examined and the optimal conditions for the process were selected. Using empirical correlations and a visual criterion, the process was scaled up from a 0.1 L to a 1 L batch crystallizer. The obtained crystals were characterized by light and scanning electron microscopy. The addition of a bridging liquid and/or a polymer additive did not change the internal structure of the ceritinib crystals, which was confirmed by X-ray powder diffraction.

In the pharmaceutical industry, deep eutectic solvents can be used to enhance the solubility, permeability, and absorption of active pharmaceutical ingredients. In this paper, deep eutectic solvents were prepared by combining the active pharmaceutical ingredient fosamprenavir calcium with lactic acid in certain molar ratios. The aim of this study was to create a therapeutic deep eutectic solvent with the same therapeutic effect as the active pharmaceutical ingredient, but with enhanced properties. ¹H NMR and FTIR spectroscopy were used to identify and characterize the chemical composition and structural changes of the prepared THEDES. Maximum solubility, the release of the active pharmaceutical ingredient from the therapeutic deep eutectic solvent, and permeability were tested. Different mathematical models were chosen to describe the kinetic behavior of the drug release.

One of the main challenges facing the pharmaceutical industry today is the low solubility of active pharmaceutical ingredients (APIs), which leads to low bioavailability, reduced therapeutic efficacy, and the need for higher drug doses. Eutectic solvents (ES) offer a promising solution by effectively dissolving APIs, creating API-ES systems that can significantly improve drug solubility and delivery. In this study, three distinct ESs were prepared by combining various components, with their successful formation confirmed through Fourier Transform Infrared Spectroscopy. Key physicochemical properties, including the density, viscosity, and pH of the prepared solvents, were subsequently determined. Ceritinib (CRT), an API utilized in the treatment of non-small cell lung cancer, was then incorporated into the prepared ESs to yield the API-ES systems. A comparative analysis was conducted to assess the release profiles of pure CRT versus CRT within the API-ES systems. Furthermore, the permeability and diffusion coefficient of the drug within these systems were also determined. The results conclusively demonstrated that the formation of the API-ES system increased the solubility of CRT in water. This achievement represents a vital initial step toward optimizing the delivery of this drug and highlights the significant potential for developing a novel, improved pharmaceutical formulation.