title: [Stability testing of meloxicam-containing microcomposites for inhalation].
abstract: The formulation of inhalation agents is a major challenge for the pharmaceutical technologist. The innovative inhalation formulations mean a new area of indication for active pharmaceutical ingredients. Among pulmonary preparations, dry powder inhalers (DPIs) can ensure stability, a high payload and patient convenience. Our aim was to develop a carrier-based, crystalline co-spray-dried DPI product containing the low-solubility meloxicam (MX). Instead of the classical approach based on micronization to prepare drug particles followed by blending with a carrier, co-spray-drying of the MX/mannitol (M)/additives was performed in a one-step process. The product parameters were optimized with PVA, PVP, TWEEN and LEU as additives in order to improve the drug deposition in the lung. The mean particle size in the M-based systems was in the required range (2-5 microm). The particle dimensions, morphology and physical-chemical properties of the microcomposites were suitable for the pulmonary administration of DPI formulations based on the applicability of efficacy and safety. We investigated the influence of temperature and relative humidity on the physical-chemical properties with a view to optimization of the analytical methods, with the expiration date as a limiting parameter. The most important parameters of the DPI are the particle size, the particle size distribution, the morphology, the crystallinity of the drug and the dissolution rate. The DPI quality is assessed by the determination of aerodynamic properties such as the aerodynamic the particle size distribution, the mass median aerodynamic diameter (MMAD) and the fine particle fraction (FPF). Critical parameters were determined by thermoanalytical studies (TG), X-ray diffraction, electron microscopy and laser diffraction. The chemical stability of the components was tested by FT-IR spectroscopy. The in vitro aerosol performance was tested by using the multistage Andersen Cascade Impactor.
authors.forename: Anita
authors.initials: A
authors.lastname: Pomázi
authors.forename: Rita
authors.initials: R
authors.lastname: Ambrus
authors.forename: Piroska
authors.initials: P
authors.lastname: Szabóné Révész
mesh_terms: D000280:Administration, Inhalation; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers; D004355:Drug Stability; D006801:Humans; D006813:Humidity; D007834:Lasers; D008353:Mannitol / Q000008:administration & dosage / Q000737:chemistry; D000077239:Meloxicam; D046529:Microscopy, Electron, Transmission; D010316:Particle Size; D011208:Powders; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature; D013843:Thiazines / Q000008:administration & dosage* / Q000737:chemistry*; D013844:Thiazoles / Q000008:administration & dosage* / Q000737:chemistry*; D014961:X-Ray Diffraction
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D011208:Powders; D013843:Thiazines; D013844:Thiazoles; D008353:Mannitol; D000077239:Meloxicam