01. December 2017
The low aqueous solubility of celecoxib (CCB) hampers its oral bioavailability and permeation from aqueous environment through biological membranes. The aim of this study was to enhance the aqueous solubility of CCB by complexation with cyclodextrin (CD) in the presence of water-soluble polymer. The effects of different CDs (αCD, βCD, γCD, 2-hydroxypropyl-β-cyclodextrin and randomly methylated β-cyclodextrin (RMβCD)) and mucoadhesive, water-soluble polymers (hydroxypropyl methylcellulose (HPMC),
30. November 2017
Instacoat 4G wins in the category Excellence in R&D - Development of new product / techology.
29. November 2017
Purpose Characterisation of powder flow is important for pharmaceutical processing and manufacturing. This work aims at a better understanding of how fractal particle and bulk properties affect the static and dynamic flow of excipients. Methods Traditional methods of flowability testing, e.g. the angle of repose or the flow through an orifice, were complemented by avalanching in a rotational drum. Dynamic image analysis provided a fractal contour line dimension of the powder bulk in the drum...
29. November 2017
The methacrylate-copolymer Eudragit® EPO (EPO) has previously shown to greatly enhance solubilization of acidic drugs via ionic interactions and by multiple hydrophobic contacts with polymeric side chains. The latter type of interaction could also play a role for solubilization of other compounds than acids. The aim of this study was therefore to investigate the solubility of six poorly soluble bases in presence and absence of EPO by quantitative ultra-pressure liquid chromatography with...
29. November 2017
Meloxicam (MLX) is a non-steroidal anti-inflammatory cyclooxygenase (COX) inhibitor that is used to relieve inflammation and pain. MLX has a preferential affinity for COX-2, which is associated with a lower incidence of gastrointestinal side effects. The drug belongs to Class II of the Biopharmaceutical Classification System (BCS) in which dissolution is the limiting step of its bioavailability. In view of this classification, carrying out further studies regarding the compatibility of MLX with...
28. November 2017
Particle design via spherical agglomeration is a size enlargement technique used in various bulk and fine chemical industries, with recent interest extending into pharmaceuticals, in which an immiscible bridging liquid is added to agglomerate crystals prior to deliquoring. Spherical agglomeration has the potential to dramatically simplify downstream processing, and improves the handling of difficult, needle-shaped crystals. This review consolidates the understanding of the controlling process...
28. November 2017
Recent work has established polymer strip films as a robust platform for delivery of poorly water-soluble drugs via slurry casting, in particular using stable drug nanosuspensions. Here, a simpler, robust method to directly incorporate dry micronized poorly water-soluble drug, fenofibrate (FNB), is introduced. As a major novelty, simultaneous surface modification using hydrophilic silica along with micronization was done using fluid energy mill (FEM) in order to reduce FNB hydrophobicity and...
27. November 2017
Drug solubility can pose a great challenge for the development of novel formulations and impacts a wide spectrum of drugs with poor solubilities. Drug efficacy is known to be proportionally related to the solubility of a drug. Poor solubility of a drug leads to low dissolution rate and in turn to low absorption in the gastrointestinal tract following oral administration. Pharmaceutical particle technology is often used to improve poor aqueous solubility of drug compounds that limits in vivo bioa
26. November 2017
Many physical responses of powders, granules, and compacts such as powder flow and tensile strength are determined largely by their absolute and relative densities (1–8). Although measuring these properties is a simple task, a review of the literature reveals that a combined source of density data that formulation scientists can refer to does not exist.
26. November 2017
The objective of this study was the development of retarded release pellets using vegetable calcium stearate (CaSt) as a thermoplastic excipient. The matrix carrier was hot melt extruded and pelletized with a hot-strand cutter in a one step continuous process. Vegetable CaSt was extruded at temperatures between 100 and 130 °C, since at these temperatures cutable extrudates with a suitable melt viscosity may be obtained. Pellets with a drug loading of 20% paracetamol released 11.54% of the drug a