The development of new direct compression excipients should include a comprehensive and rapid determination of deformation properties. The aim of this study was to characterize StarLac, a new coprocessed compound for direct compression based on lactose and maize starch. For this purpose, the effects of the base materials (maize starch and spraydried lactose) were considered and the influence of the spraydrying process was investigated. This was performed by comparing the physical mixture of starch and spray-dried lactose at the same ratio as for StarLac. For analysis of the deformation behavior, the 3-D model and the Walker equation were applied; for verification, the Heckel equation and the pressure time function (a modified Weibull equation) were used. The advantages of StarLac are its good flowability depending on the spray-drying process, an acceptable crushing force due to its lactose content, its rapid disintegration depending on starch, and a brilliant fast release of an active ingredient, such as theophylline monohydrate. The volume-pressure deformation properties of StarLac were dependent on the lactose properties. Only at high maximum relative density (ρ rel, max ) did the influence of starch cause a change in these properties. A network-like structure can be observed using scanning electron microscopy pictures. Overall, StarLac deformed plastically with a low portion of elasticity. The physical mixture exhibited a more elastic behavior than StarLac. However, the part of the powder that was irreversibly compressed was much lower than was observed for the single substances. This behavior is caused by an interaction between the components, which in StarLac is prevented by spray drying.
The purpose of this study was to complete information on elastic recovery during a compression cycle by measuring the expansion of the tablet after ejection, and thus, to measure the whole recovery process, which means the time dependency of elastic recovery. Two methods were applied: manual measurement by a micrometer screw, and a continuous measurement by thermomechanical analysis, always at a constant temperature and humidity. Elastic recovery of the tablet continued after ejection from the die, and the amount of expansion was different for the tableting materials used. The results showed that expansion continued for most of the materials over several days, until a steady state of the tablet and its physical properties was reached. The extent and the profiles of the elastic recovery curves were different for the tableting materials dicalcium phosphate dihydrate, carrageenan, microcrystalline cellulose, cellulose acetate, hydroxypropyl methylcellulose and theophylline monohydrate. There were slight differences between both the methods used. The profiles of the materials could be related to some properties of the materials.
Carrageenans are hydrocolloids in the rubbery state at standard conditions. They are useful excipients for controlled-release tablets. Three carrageenans, two kappa-carrageenans (Gelcarin GP-812 NF and GP-911 NF) and one iota-carrageenan (Gelcarin GP-379 NF), are analyzed regarding their release behavior in combination with sorption, swelling, and rheology. The iota-carrageenan has a higher substitution by sulfate groups. The kappa-carrageenan Gelcarin GP-812 NF contains a small amount of potassium chloride left over from processing. Water sorption of the pure materials was studied gravimetrically, and the rheology of different solutions (2% and 5% w/w) was studied by cup-cylinder rotation viscosimetry. Swelling was determined as the vertical expansion of the tablets with a specially designed swelling apparatus. Drug release from the tablets was performed by the USP paddle method for 8 hr. The data indicate that drug release increases when water sorption and swelling extent decrease and as viscosity increases. The order of release is nearly zero-order kinetics for theophylline monohydrate, a nonionic drug. Diffusion of the anionic drug diclofenac sodium is anomalous. In addition, the influence of the added salts potassium and calcium chloride on swelling and release was studied. Before tableting, physical mixtures of these salts with and without theophylline monohydrate were prepared. Swelling and release change in the same order, but this is only valid when the ionic interactions responsible for this are strong enough. Besides this, physical mixing of salts with the carrageenans can result in an increased release of drug caused by decreased cohesion of the matrix during drug release, mainly for calcium chloride.
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