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This article reports on the effects of a new combined wet milling technique on the physicochemical properties of meloxicam (MEL). The influence of milling time on the particle size, the crystallinity, the morphology and the dissolution rate of MEL has been studied in the presence and absence of polyvinyl alcohol (PVA) as a stabilizer agent. Micronized MEL particles were produced in aqueous medium which did not contain additive after milling for 10 min. For nanonization an additive and longer milling time were required. After particle size determination the structural and morphological characterization of the wet milled, dried products containing MEL were studied. X-ray powder diffractometry (XRPD) and differential scanning calorimetry (DSC) examinations revealed the change in the crystallinity of MEL. Scanning electron microscopy (SEM) images showed that aggregates of nanosized MEL particles were formed, regardless of the presence of PVA. The nanonized MEL crystals (D50 = 126 nm) exhibited a regular shape and a smooth surface. The increased specific surface area resulted in a high dissolution rate and concentration of free MEL. According to the results, the produced samples could be applied as a basic material (micronized MEL) and intermediate product (micronized and nanonized MEL with PVA) for the design of dosage forms. [ABSTRACT FROM AUTHOR]

Different pharmaceutical technological processes have been used for modification of the physico-chemical and biopharmaceutical properties of drugs. Changes of crystal size, distribution and morphology can open up new, alternative administration routes, e.g. intranasally and the pulmonary route, where the particle size is a determining factor. A wet grinding method based on acoustic cavitation (the collapse of bubbles or voids formed by sound waves) is a novel possibility for modification of the properties of particles. During our work this wet grinding technique was studied. The effect of this method was investigated on particle size reduction. The samples were treated with extreme sonication parameters. The effect of the concentration of the polymer was examined on the particle size reduction. Meloxicam was chosen as a model crystalline drug because of its poor aqueous solubility. The structural characterization and the morphological analysis of the dried products were carried out by DSC, XRPD and SEM. It was found that the acoustic cavitation resulted in crystalline micronized product.

The main aspect in the field of pharmaceutical technology is the preformulation of the poorly water soluble drugs. The habit of particles can effect the physico-chemical properties which are important factors by drug administration. In the past years the role of the procedures by acustic cavitation increased in the field of particle engineering. Application of high power ultrasound by integration and dezintegration can lead to particle size decreasing. Meloxicam as a nonsteroid anti-inflammatory model drug was used to study the effect of power ultrasound on the particle size decreasing. During our work technological parameters, as amplitude, temperature, time, excipients and concentration were optimized based on particle size distribution. Physico-chemical stability tests were also performed (XRPD, DSC, SEM, particle size). With optimized parameters (70% amplitude, 20 min, 47 0C) using excipients, crystalline micronized product was produced.