Evaluation of the effects of lactose on the surface properties of alginate coated trandolapril particles prepared by a spray-drying method

• Published in: Carbohydrate polymers 2008-11, Vol.74 (3), p.712-716
• Main Authors: Makai, Zsolt, Bajdik, János, Erős, István, Pintye-Hódi, Klára
• Format: Article
• Language: English
• Subjects: Applied sciences; Biological and medical sciences; Exact sciences and technology; General pharmacology; Medical sciences; Natural polymers; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Physicochemistry of polymers; Polarity; Sodium alginate; Spray-drying; Starch and polysaccharides; Surface free energy; Trandolapril
• ISSN: 0144-8617; 1879-1344
• DOI: 10.1016/j.carbpol.2008.04.029

This preliminary work involved a comparison of untreated microcrystals, alginate-based spray-dried microparticles, and alginate-based lactose containing spray-dried of the antihypertensive drug, trandolapril. Physicochemical properties, such as surface free energy, the polarity and the dissolution profiles of the untreated drug and the spray-dried particles were investigated. The main objective was the separation of crystals suitable for the production of intermediates for high-speed tablet-making from materials with low melting point. The aim was to modify the surface properties of trandolapril without changing the dissolution profile of the active agent; this was achieved by the application of spray-drying technology for the production of coated particles with a hydrophilic surface in order to attain better wetting properties, and better processibility. The aggregation of the spray-dried coated particles and their subsequent coalescence is very favourable for the liquid containing lactose. The kinetics of dissolution of the active ingredient was not changed appreciably by the surface modification obtained by spray-drying, regardless of whether alginate or alginate and lactose was used. Slightly quicker dissolution was observed for the sample containing lactose. The spray-drying with alginate increased the polarity of the surface of the particles. The application of lactose caused a more marked increase in this property; and this can be a very useful way to produce a powder mixture containing polar components (e.g. lactose). Thus, the spray-drying method is a very suitable procedure for the preparation of coated crystals as intermediates for tablet-making. The evaluation of the surface properties of these particles can promote an understanding of the production process and optimization of the composition.