Physical mechanical and tablet formation properties of hydroxypropylcellulose: In pure form and in mixtures

Abstract

The aim of the study was to analyze hydroxypropylcellulose (HPC) in pure form and in excipient mixtures and to relate its physical and chemical properties to tablet binder functionality. The materials used were Klucel hydroxypropylcellulose grades ranging from low to high molecular weight (80-1000 kDa) of regular particle size (250 μm mean size) and fine particle size (80 μm mean size). These were compared with microcrystalline cellulose, spray-dried lactose, and dicalcium phosphate dihydrate. Thermal behavior of HPC was analyzed by modulated temperature differential scanning calorimetry (MTDSC). Tablets of the pure materials and of dry blends with 4% low viscosity, fine particle HPC and 30% high viscosity, fine particle HPC were produced on an instrumented eccentric tableting machine at 3 relative humidities. The 3-dimensional (3-D) model with the parameters time plasticity d, pressure plasticity e, and the twisting angle ω, the inverse of fast elastic decompression was compared with the Heckel method for characterization of compaction. Elastic recovery and compactibility were also studied. The results show that HPC tablet formation is characterized by high plastic deformation. The d, e, and ω values were markedly higher as compared with the reference materials. Plasticity was highest for the fine particle size HPC types. Maximum compactibility was observed for low molecular weight, fine particle size HPC. Tableting of the mixtures showed deformation, which was strongly influenced by HPC. Plasticity and crushing force of formed tablets was increased. In conclusion, HPC is characterized by strong plastic deformation properties, which are molecular weight and particle size dependent.

The DSC approach to study non-freezing water contents of hydrated hydroxypropylcellulose (HPC)

“…It is a semi-crystalline polymer with relatively low T g and a high degree of amorphous content, which causes high molecular mobility and plasticity [1]. Similarly to other structural analogs of cellulose, HPC can be treated as a natural material, that is biocompatible with human tissues (including blood), nontoxic and relatively low cost [2].…”

Quality-by-Design II: Application of Quantitative Risk Analysis to the Formulation of Ciprofloxacin Tablets

“…For the formulation variables, we have identified the binder level and source, disintegrant level, and Mg stearate type as the highest risk variables that should be examined when developing the design space. For this formulation, the binder was HPC; our previous results (4) and the literature have shown that physical-chemical properties of HPC (25) and the level in a roller compaction granulation formulation (26) can affect the mechanical properties of a tablet and the drug release rate. Based upon this information, we studied the source and level of HPC; because different sources of HPC are made from different feed stocks, different manufacturing methods and different processing conditions can affect the physical-chemical properties of HPC and hence product quality.…”

Eudragit E100 and Polysaccharide Polymer Blends as Matrices for Modified-Release Drug Delivery I: Physicomechanical Properties

“…Their rigidity may have been enhanced by the intramolecular hydrogen bonding [11] that may have been strengthened in the presence of bound-water before drying. Furthermore, hardness of a tablet is dependent on its ability to undergo plastic deformation [19,20]. Lyophilization may have improved their plastic deformation thereby increasing the cohesive forces between the polymer particles which led to harder tablets.…”