[Penetration of lincomycin into suppurative lesion of maxilla of rabbits (author's transl)].
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Tested was the activity of linkomycin hydrochloride at the rate of 820 IU/mg. The LD50 of the preparation was found to exceed 12.0 g/kg body mass at intracrop application to broiler birds. When offered with the drinking water or the feed in amounts that were 3 to 5 times higher than the therapeutic ones for broilers in the course of 45 days it did not cause mortality nor induced changes in the white and red blood cell counts, in the total protein, and in the levels of urea, blood sugar, AlT, and AcT. Neither were there any structural changes in the internal organs. Upon the single intracrop treatment of broilers with linkomycin at 50 and 100 mg/kg most of the amount introduced was established in the blood serum at the second hour and up to the 6th and 8th hour, respectively. Studies on the effect of age on the serum concentrations at this route of introduction revealed that the preparation was absorbed at higher rates in the broilers than in the layers, while with the persistence of the levels there were no essential differences. At the single oral administration with broilers in amounts of 100 mg/kg linkomycin was chiefly retained in the kidneys, liver, and lungs as well in the content of the small and large intestines. At intracrop application to layers in doses of 100 mg/kg in the course of 7 days the antibiotic was excreted with the eggs at the time of treatment and in the course of 4 days later in bacteriostatic concentrations of 0.6-5.9 micrograms/cm3.
Tested was the teratogenic and embryotoxic action of linkomycin hydrochloride with both placental and nonplacental animals. It was found that when applied twice, orally, to albino rats on the 4th day of pregnancy at the rate of 250 mg/kg body mass (=5 ED50), and once to chick embryos at 50 mg per egg the antibiotic raised the percent of pre- and postimplantation loss of embryos. In a series of applications (oral) from the 3rd up to the 19th day at 50 mg/kg body mass to rats as well as in a single application to chick embryos at 10, 20, and 50 mg per egg linkomycin showed no teratogenic effects.
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Each of the preparations described here was obtained and evaluated at the request of a WHO Expert Committee on Biological Standardization. Unless otherwise stated, a standard procedure was used to distribute the material into individual ampoules. The procedure was as follows. Upon receipt by the National Institute for Medical Research (NIMR), London, materials were stored temporarily in the dark at a temperature of -10 degrees C or lower, and protected from moisture. At a convenient time they were brought back to room temperature, mixed, and distributed into individual neutral glass ampoules so that each ampoule contained 50-100 mg of powder. If it was known that the material was light-sensitive non-actinic glass ampoules were used. After exhaustive drying in vacuum over phosphorus(V) oxide, the ampoules were either constricted (up to 1963) or fitted with capillary leak plugs, dried for a further period under the same conditions, filled with dry nitrogen, and sealed by fusion of the glass. The total drying period varied from 8 to 38 days according to the nature of the material. After they had been tested for leaks, the ampoules were stored in the dark at -20 degrees C.
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