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    Inert monolithic device with a central hole for constant drug release

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    In vitro drug release from inert monolithic matrices is generally characterized by a non-linear profile. This paper examines the release of drugs from a heterogeneous insoluble matrix which was designed to obtain an in vitro constant release. This matrix system, which shows a special geometry, consists of a biconvex perforated inert core that is partially covered with a water impermeable polymeric film so that the inner hole surface is the only releasing surface. Both the tabletting of perforated cores and their partial coating can be performed under continuous operating processes. This makes the system suitable for industrial applications thus differentiating it from all previous geometry-based inert systems. The release rate from this kind of device proved to be constant, irrespective of drug solubility, at up to 80% of delivery

    Properties of tolmetin-loaded Eudragit RL100 and Eudragit RS100 microparticles prepared by different techniques

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    The feasibility of different techniques for the preparation of tolmetin-loaded microparticles of Eudragit RL100 and Eudragit RS100 was evaluated. The traditional emulsion-solvent evaporation method was compared to spray-drying and the quasi-emulsion-solvent diffusion technique. The results were analysed in terms of drug encapsulation and in vitro release (pH 1.2 and 6.8), as well as in terms of particle yield and size distribution. Preliminary physicochemical studies also indicated the possibility of a polymorphic change of the drug during the microsphere preparation using the first procedure

    Tabletted polylactide microspheres prepared by a w/o emulsion-spray drying method

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    An emulsification-spray drying technique is used to prepare poly(d,l-lactic acid) (PDLLA) microparticles loaded with a water soluble, non-steroidal anti-inflammatory drug (NSAID), sodium naproxen (NaNPX). The method involves the preparation of a w/o emulsion in which the water soluble drug is dissolved in the aqueous dispersed phase, while the polymer is dissolved in the organic continuous phase. As a comparison, microparticles were prepared by spraying a suspension of the drug into an organic solution of the polymer. The spray-dried particles were characterized using SEM, DSC, XRD and in vitro release tests. The spray-dried product was then compressed (direct compression) to obtain controlled release matrix tablets. All microparticles release NaNPX within 30 min. The matrix tablets release the drug in 8-10 h; the matrix tablets characterized by the presence of surfactant (due to the emulsion used to obtain the microparticles) have the highest release rate
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