Urinary and serum concentrations of diclofenac after topical application to horses.

The liposomal cream formulation of diclofenac, an NSAID, is an effective, safe, and convenient way to treat localized areas of inflammation in horses. The results of this study reveal urinary and serum concentrations of diclofenac following topical administration of 1% liposomal diclofenac cream for 10 days at the labeled dose and at 2X and 4X the labeled dose. These results demonstrate the slow absorption and elimination of 1% liposomal diclofenac cream and may be useful when estimating the withdrawal time needed before a competition in order to prevent an inadvertent positive drug test.

Double-blinded placebo-controlled clinical field trial to evaluate the safety and efficacy of topically applied 1% diclofenac liposomal cream for the relief of lameness in horses.

A topical 1% diclofenac liposomal cream proved to be safe, easy to use, and effective in reducing equine lameness caused by degenerative joint disease. Diclofenac liposomal cream was shown to reduce lameness as graded by owners and veterinarians, regardless of the severity or chronicity of the clinical condition. Topical application allowed for more convenient administration than oral or injectable agents, and no clinically relevant hematologic or serum biochemical changes were noted. The liposomal cream provided a delivery system for diclofenac, an NSAID, to achieve therapeutic levels locally with decreased risk for systemic toxicity and side effects and improved targeting of the painful area.

Effect of terminal sterilization by irradiation on amber Type I and Type III glass containers containing veterinary oxytetracycline suspension.

The purpose of this study is to determine the effect of terminal sterilization by gamma irradiation on 500-mL amber Type I and Type III glass containers (bottles) containing oxytetracycline (OTC) (25% W/V) suspension formulated using 20% (W/V) phospholipids syrup. The formulation was developed for veterinary parenteral administration. The results of terminal sterilization were used to assess the acceptability for this suspension product. OTC is light-sensitive and needs to be stored in amber glass containers. Amber Type I and Type III glass containers were considered for this formulation during development. Type I is a highly resistant, borosilicate glass (oxidized glass). Type III, which is soda-lime glass (reduced glass, see Materials and Methods), may also be used for parenteral products. The amber Type I and Type III glass containers, containing the suspension, were irradiated at 20-40 kGy for 150 min. In order to determine the sterility of the suspension, ampoules of the biological indicator, Bacillus pumilus, were placed in a number of bottles of the suspension. The bottles with the biological indicators were then positioned among the rest of the production bottles as per a radiation dose-mapping study conducted at the sterilization facility. Potency determination and stability evaluations for OTC were performed using high pressure liquid chromatography (HPLC). The results indicate that the gamma irradiation dose of 20-40 kGy for 150 min was able to inactivate 10(6) Bacillus pumilus spores in ampoules. After gamma sterilization, OTC concentration, pH, particle size, endotoxins, and sterility were evaluated. The assay results were comparable for the suspension in amber Type I and Type III glass containers. Sterility and pyrogenicity were measured by the USP Membrane Filtration Method and USP Bacterial Endotoxins Test, respectively. The suspension in the amber Type III glass container was also chemically (HPLC) and physically (suspension mean particle size, viscosity, density, and syringeability) stable for at least 12 months at room temperature. However, amber Type I glass darkened following irradiation, leading to a substantial reduction in glass transparency. The appearance of amber Type III glass was acceptable. Thus, the "reduced" glass, such as soda-lime, was found to be much less susceptible to darkening than the highly oxidized borosilicate amber. Due to the potential aesthetic concerns with Type I glass, the amber Type III glass container was selected for this suspension formulation.

Use of lufenuron for treatment of generalized demodicosis in dogs.

Abstract The efficacy of lufenuron for treatment of generalized demodicosis in dogs was investigated. Eleven dogs with generalized demodicosis received either low-dose lufenuron (mean 13.3 mg kg-1 once a day on the first 5 days of the month) or high-dose lufenuron (mean 15.8 mg kg-1 three times a week) orally for 2 or 3 months. None of the dogs showed a decrease in mite numbers on monthly examination of deep skin scrapings. To determine levels of orally administered lufenuron in the skin (epidermis and dermis), three adult dogs were each given lufenuron orally at a mean dose of 19.3 mg kg-1 once a day for 5 days. Lufenuron was measured in samples of blood and skin collected on days 0, 1, 6, 16, 30, 44 and 60 after administering the drug. Mean skin levels of lufenuron were 10 times the corresponding blood levels. Lufenuron was ineffective as a treatment for generalized demodicosis in these dogs despite the fact that high drug levels were achieved in the skin. Résumé- L'efficacitée du Lufénuron dans le traitement de la démodécie généralisée du chien a étéévaluée 11 chiens présentant une démodécie généralisée ont reçu soit du lufeAnuron à dose faible (en moyenne 13, 3 mg kg-1 , 1 fois par jour les 5 premiers jours de chaque mois) ou à dose élevée (en moyenne 15, 8 mg kg-1 fois par semaine) par voie orale pendant 2 à 3 mois. Aucun des chiens traités ne montre une diminution du nombre de parasites determine à partir de raclages cutanés profonds mensuels. Afin de déterminer les taux de lufénuron dans la peau (épiderme et derme), trois chiens adultes ont reçu chacun du lufénuron par voie orale à une dose moyenne de 19, 3 mg kg-1 , une fois par jour pendant 5 jours. Le lufénuron a été mesuré dans des échantillons sanguins et cutanés à JO, J1, J6, J16, J30, J44 et J60 après administration. Les taux moyens dans la peau sont 10 fois supérieurs aux taux sanguins correspondants. Le lufénuron est inefficace dans le traitement de la démodécie généralisée en dépit des concentrations élévées dans la peau. [Schwassmann, M., Kunkle, G. A., Hepler, D. I., Lewis, D. T. Use of lufénuron for treatment of generalized demodicosis in dogs. (Utilisation du Lufénuron pour le traitement de la démodécie généralisée du chien.) Veterinary Dermatology 1997; 8: 11-18.] Resumen Se investigó la eficacia de lufénuron para el tratamiento de la demodicosis generalizada en perros. Once perros con demodicosis generalizada recibieron o bien una dosis baja de lufénuron (medía 13.3 mg kg-1 una vez al día en los primeros 5 meses del mes) o una dosis alta de lufénuron (medía 15.8 mg kg-1 3 veces a la semana) oralmente durante 2 o 3 meses. Ninguno de los perros mostró dismunición en el número de ácaros en los exámenes mensuales de raspados cutáneos profundos. Para detectar en la piel (epidermis y dermis) los niveles de lufénuron administrado oralmente, a tres perros adultos se les administró a cada uno lufénuron oral a una dosis medía de 19.3 mg kg-1 una vez al día durante 5 días. Se cuantificó el lufénuron en muestras de sangre y piel tomadas a días 0, 1, 6, 16, 30, 44 y 60 después de la administración del fármaco. Los valores cutáneos medios de lufénuron fueron 10 veces los valores sanguineos correspondientes. Lufénuron no tuvo efecto como tratamiento de la demodicosis generalizada en estos perros a pesar de los altos niveles farmacológicos alcanzados a nivel cutáneo. [Schwassmann, M., Kunkle, G. A., Hepler, D. I., Lewis, D. T. Use of lufénuron for treatment of generalized demodicosis in dogs. (Uso de lufénuron para el tratamiento de la demodicosis generalizada en perros.) Veterinary Dermatology 1997; 8: 11-18.] Zusammenfassung- Die Wirksamkeit von Luferunon in der Behandlung von generalisierter Demodikose wurde untersucht. Elf Hunde mit generalisierter Demodikose erhielten entweder eine niedrige (durchschnittlich 13.3 mg kg-1 täglich an den ersten fünf Monatstagen) oder hohe Dosis Lufénuron (durchschnittlich 15.8 mg kg-1 dreimal wöchentlich) oral für 2-3 Monate. Bei keinem Hund zeigte die monatliche Untersuchung von tiefen Hautgeschabseln eine Verminderung der Milbenanzahl. Um den Hautspiegel (Epidermis und Dermis) des oral verabreichten Lufénurons zu bestimmen, erhielten drei Hunde jeweils oral Lufénuron in einer Durchschnittsdosis von 19.3 mg kg-1 täglich für 5 Tage. Lufénuron wurde in Serum-und Hautproben gemessen die vor und 1, 6, 16, 30, 44 und 60 Tage nach Beginn der Medikamenteneinnahme genommen wurden. Durchschnittliche Hautspiegel von Lufénuron waren zehn Mai so hoch wie die korrespondierenden Blutspiegel. Die Behandlung der generalisierten Demodikose mit Lufénuron war trotz der hohen Medikamentenkonzentration in der Haul unwirksam. [Schwassmann, M., Kunkle, G. A., Hepler, D. I., Lewis, D. T. Use of lufénuron for treatment of generalized demodicosis in dogs. (Die Verwendung von Lufénuron für die Behandlung der generalisierten Demodikose beim Hund.) Veterinary Dermatology 1997; 8: 11-18.].