We have evaluated the percutaneous penetration of felbinac following application of topical patches using a microdialysis technique, and have examined correlations with pharmacological effects. A linear microdialysis probe with a 20-mm dialysis fibre was inserted into the skin of anaesthetized rats. Probe perfusion was started at 2.0 microL min(-1) with physiological saline and after a 60-min baseline sampling of dialysate, 0.1 mL croton oil was applied to the skin surface at a concentration of 8%, v/v. A felbinac patch was then applied to the same point 60 min thereafter and dialysate was sampled at 60-min intervals up to 300 min after patch application, for determination of concentrations of felbinac and prostaglandin (PG) E2. Analgesic effects of felbinac patches in an iodoacetateinduced osteoarthritis model and an incisional pain model were evaluated using the weight bearing method. After application of patches, felbinac penetration into the skin was rapid, maximum concentrations in the dialysates with 0.07, 0.5 and 3.5% w/w felbinac patches being 0.046+/-0.02, 0.104+/-0.06 and 0.244+/-0.2 microg mL(-1), respectively. Dermal administration of croton oil caused an increment in PGE2 levels, which was significantly decreased by 0.5 and 3.5% felbinac patches 2-5 h after application. In pharmacological studies, 3.5% felbinac patches suppressed pain-associated behaviour induced by iodoacetate injection and plantar incision. These results suggested that the transdermal patch containing 3.5% felbinac may become a useful formulation.

RESUME. La Microsporidie Nosema bombycis, Protozoaire parasite agent de la pébrine du ver à soie, a étéétudiée cytochimiquement à la fois en microscopie photonique et électronique. Les examens ont porté sur la détection et la localisation des acides nucléiques (ADN et ARN), des polysaccharides, de la phosphatase acide, au cours des différents stades du développement dans les cellules de I'hôte (du schizonte à la spore). Les principaux résultats concernent les observations relatives aux polysaccharides et à la phosphatase qui ne sont détectés qu'au stade de la spore et ne sont pas observés au stade du schizonte. Les polysaccharides sont présents au niveau du sac polaire, du filament polaire et sur la membrane cytoplasmique; la phosphatase acide est localisée au niveau du sac polaire, du filament polaire et dans la vacuole postérieure. SYNOPSIS. Nosema bombycis, agent of pebrine disease of silkworm, was studied cytochemically, using both light and electron microscopy. Presence of nucleic acids (DNA and RNA), polysaccharides, and acid phosphatases was demonstrated and localization of these substances was determined in various stages of the parasite (from the schizont to the spore). DNA and RNA were detected in all these stages. Polysaccharides and acid phosphatase were found in the spore but not in the schizogonic stages. Polysaccharides were detected in the polar cap, the polar filament, and the limiting membrane of the cytoplasm of the spore. Acid phosphatase was found in the polar cap, the polar filament, and the posterior vacuole.

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