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PREPARATION OF PELLETS WITH TRAMADOL HYDROCHLORIDE OF MODIFIED RELEASE

Jaroslaw Mazgalski 

Medical University of Gdańsk, Department of Pharmaceutical Technology, Hallera 107, Gdańsk 80-416, Poland

Abstract

The results constitute a part of project aiming at working out method of obtaining modern multiparticulate drug in form of compressed pellets with tramadol hydrochloride (TH). That form is to ensure a more effective, slower TH release and contribute to pain treatment pharmacotherapy optimization. It was assumed that the TH contents in pellets cores will amount to at least 50%. Pellets, directly with the drug were obtained by means of extrusion and spheronization. Microcrystalline cellulose was used as a basic TH carrier. Powdered cellulose, hydroxypropylomethylocellulose, carmellose sodium, povidone and guar gum were also examined as fillers in the process of water granulation. Colloidal silica and glyceryl behenate were added to the contents of the powder mixture in order to decrease agglomeration of the granulated mass. The attempts of using hydrophilic polymer, e.g. PVP K - 30, failed due to too intensive powder mixture binding. It was found that cores having very good sphericality and smooth surface, deprived of the "shark skin" effect, may be obtained at 60% TH contents in pellets. After examining a dozen or so formulations optimum core contents (%) was selected: TH (60.0); Avicel PH 101 (35.0); Aerosil R972 (2.0); glyceryl behenate (3.0). Formulations with 70% TH contents in pellets had smooth core surface but significantly worse sphericality compared to 60%. The effect of modified slow TH release rate from cores was obtained by coating them with film Eudragit NE. Using also other copolymers of methacrylic acid, ethylcellulose and shellac is planned to this end. Evaluation of film endurance and diffusion properties according to the fact if polymers are showered on cores in the form of solution or dispersion in a water or organic solvent will also be conducted. Selected formulations of coated pellets will be directly compressed into tablets using laboratory rotation tabletting machine with the power of monitoring compression forces and the force of tablet expulsion from matrix.

 

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Presentation: Poster at V Multidyscyplinarna Konferencja Nauki o Leku, by Jaroslaw Mazgalski
See On-line Journal of V Multidyscyplinarna Konferencja Nauki o Leku

Submitted: 2006-01-30 06:53
Revised:   2009-06-07 00:44