Solidification of hesperidin nanosuspension by spray drying optimized by design of experiment (DoE).

Objective: To accelerate the determination of optimal spray drying parameters, a "Design of Experiment" (DoE) software was applied to produce well redispersible hesperidin nanocrystals.

Significance: For final solid dosage forms, aqueous liquid nanosuspensions need to be solidified, whereas spray drying is a large-scale cost-effective industrial process.

Methods: A nanosuspension with 18% (w/w) of hesperidin stabilized by 1% (w/w) of poloxamer 188 was produced by wet bead milling.

Oral hesperidin-Amorphization and improved dissolution properties by controlled loading onto porous silica.

The oral bioavailability of poorly soluble drugs can be improved by amorphization generated by loading into the pores of mesoporous particles (pore size 2-50nm). The main mechanisms are increased kinetic saturation solubility and dissolution velocity due to the amorphous drug state and the nano-size of the drug (=increased dissolution pressure). In this study, the maximum achievable drug loading compared to the theoretical drug loading, and the effect of drug loading degree on the dissolution properties (solubility, dissolution velocity) were investigated.

Preparation and tableting of long-term stable amorphous rutin using porous silica.

Amorphous state of drugs increases the oral bioavailability, but typically faces physical stability problems. Amorphous rutin was generated and physically stabilized by encapsulating inside mesopores of porous AEROPERL® 300 Pharma and named as rutin CapsMorph® in this study. AEROPERL® 300 Pharma was loaded with rutin dissolved in DMSO containing Tween 80, and subsequently the solvent evaporated (wetness impregnation method).

CapsMorph® technology for oral delivery--theory, preparation and characterization.

The CapsMorph(®) technology prepares amorphous drugs for oral delivery by encapsulating them into porous materials. Hesperidin as model compound was loaded onto AEROPERL(®) 300 Pharma using the wetness impregnation method. Hesperidin was dissolved in dimethyl sulfoxide (DMSO) and alternatively in DMSO with addition of Tween 80.

Preparation and in vitro/in vivo evaluation of a ketoprofen orally disintegrating/sustained release tablet.

Context: Orally disintegrating tablets (ODTs) with sustained release profiles are a new generation of ODTs called orally disintegrating/sustained release tablets (ODSRTs), which are convenient in use and able to slowly release drugs to maintain effective blood concentrations over a prolonged period of time. Ketoprofen, one of non-steroidal anti-inflammatory drugs, is an ideal model drug for ODSRTs.

Methods: We designed a simple two-step process to develop novel ketoprofen orally disintegrating/sustained release tablets (KODSRTs).