rifampin and osteum

The formulation of the antituberculosis drug rifampicin embedded into 20-30 nm nanoparticles from soy phosphatidylcholine and sodium oleate, is characterized by greater bioavailability as compared with free drug substance. In this study higher antituberculosis activity of this formulation was shown. Rifampicin in nanoparticles demonstrated more effective inhibition of M. tuberculosis H37Rv growth: minimal inhibiting concentration (MIC) was twice smaller than for free rifampicin. Administration of this preparation to mice with tuberculosis induced by M. tuberculosis Erdman revealed that after 6 weeks of oral administration the CUF value in lung was 22 times smaller for rifampicin in nanoparticles than for free drug (1.7 un. vs. 37.4 un.). The LD50 value in mice was two fold higher for rifampicin in nanoformulation.. V IBMKh ranee byla razrabotana lekarstvennaia kompozitsiia protivotuberkuleznogo preparata rifampitsina, vstroennogo v nanochastitsy s diametrom 20-30 nm iz soevogo fosfatidilkholina s dobavleniem oleata natriia. Ona proiavliala bol'shuiu biodostupnost' po sravneniiu so svobodnym lekarstvom. V dannoĭ rabote pokazana bolee vysokaia protivotuberkuleznaia aktivnost' étoĭ kompozitsii. V éksperimentakh na kletkakh M. tuberculosis H37Rv rifampitsin v nanochastitsakh bolee aktivno tormozil rost kletok po sravneniiu so svobodnym lekarstvom, chto proiavilos' vo vdvoe men'sheĭ velichine minimal'noĭ ingibiruiushcheĭ kontsentratsii – 0,5 mkg/ml po sravneniiu s 1 mkg/ml dlia svobodnogo rifampitsina. V éksperimentakh na myshakh s tuberkulezom, vyzvannym shtammom M. tuberculosis Erdman, posle 6 nedel' peroral'nogo vvedeniia rifampitsina v nanochastitsakh (po profilakticheskoĭ skheme, nachinaia s 3-go dnia posle zarazheniia) velichina KOE v legkikh byla v 22 raza nizhe, chem posle svobodnogo rifampitsina (1,7 ed. po sravneniiu s 37,4 ed.). Velichina LD50 na myshakh byla vdvoe vyshe dlia rifampitsina v nanokompozitsii – kak rezul'tat zashchitnogo deĭstviia fosfolipidov nanochastits. V sviazi s ispol'zovaniem rifampitsina, kak neot"emlemogo komponenta sovremennykh skhem protivotuberkuleznoĭ terapii, poluchennye dannye ukazyvaiut na perspektivnost' razrabotannoĭ lekarstvennoĭ kompozitsii.

Topics: Animals; Antitubercular Agents; Drug Carriers; Mice; Mycobacterium tuberculosis; Nanoparticles; Oleic Acid; Rifampin