[Correlations between micromeritic properties of mixing powders of danshen extract and formability of their pellets].

It was difficult to prepare traditional Chinese medicine pellets due to the adverse characteristics of the herbal extract. In this study, Danshen extract (DS) powder mixed with different proportions of microcrystalline cellulose (MCC), lactose and starch were made into pellets by extrusion-spheronization. Particle size, span, bulk density, tapping density, compressibility, Hausner ratio and angle of repose were used to evaluate the micromeritic properties of mixing powders. Feret diameter, aspect ratio, yield, density and friability were used to evaluate the properties of the pellets. The correlations between micromeritic properties of raw material powders and the formability of their pellets were analyzed by cluster analysis, principal component analysis and partial least squares regression analysis. As a result, the particle size of the powders was negatively correlated with the size, density, yield, and was positively correlated with the friability of their pellets. The span, density, compressibility and angle of repose of the powders were positively correlated with the size, density, yield, and were negatively correlated with the friability of their pellets. So there were certain correlations between the micromeritic properties of raw material powders and the properties of their pellets prepared by extrusion-spheronization. This research provided a foundation for the technology and method of traditional Chinese medicine extract pellets.

Improvement of the bioavailability of curcumin by a supersaturatable self nanoemulsifying drug delivery system with incorporation of a hydrophilic polymer: in vitro and in vivo characterisation.

OBJECTIVES: The current study was focused on preparing curcumin (CUR) supersaturated self-nano-emulsion (PI-CUR-SNEDDS) using hydrophilic polymer and to study the influence of polymer precipitation inhibitor on the physicochemical and biopharmaceutical properties of the PI-CUR-SNEDDS. METHODS: PI-CUR-SNEDDS were prepared using hydrophilic polymer in order to maintain the supersaturation of CUR in nano-emulsion solution, artificial gastrointestinal fluid (AGF), and the precipitates formed, and characterised by in vitro dispersion tests, in vitro intestinal absorption and in vivo pharmacokinetic and compared with CUR-SNEDDS. KEY FINDINGS: PI-CUR-SNEDDS prepared with 2% hydroxypropyl methylcellulose 55-60 (HPMC55-60) as precipitation inhibitor (PI) significantly improved the viscosity, physical stability and CUR's equilibrium solubility of nanoemulsion. HPMC55-60 and CUR interact in AGF through intermolecular interactions, form hydrogen bonds, and produce amorphous precipitates. Compared with CUR-SNEDDS, the proportion of CUR in the hydrophilic phase increased by about 3-fold, and apparent permeability coefficient (Papp) in duodenum, jejunum, ileum, and colon increased by 2.30, 3.65, 1.54 and 2.08-fold, respectively, and the area under the plasma concentration-time curve0-12h of PI-CUR-SNEDDS also increased by 3.50-fold. CONCLUSIONS: Our results suggested that HPMC55-60 maintained the CUR supersaturation state by forming hydrogen bonds with CUR, increasing the solution's viscosity and drug solubilisation, thus improving the absorption and bioavailability of CUR.