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1.
Biomed Khim ; 59(5): 585-90, 2013.
Article in Russian | MEDLINE | ID: mdl-24479349

ABSTRACT

Low bioavailability of rifampicin, one of the main antituberculous drug, stimulates searches of its new optimized formulations. The present study has showen possibility of rifampicin embedding into nanoparticles from plant phosphatidylcholine (diameter of 20-30 nm). Addition of sodium oleate to the phospholipid system caused a 2-fold increase of the percent of rifampicin incorporation. After oral administration to rats, the maximal drug observed in plasma one hour after was 0.5 and 4.2 mkg/ml for free rifampicin for rifampicin in phospholipids-oleate nanoparticles, respectively. These levels were maintained for more than two hours of the experiment. High rifampicin bioavailability in the oleate containing phospholipid nanosystem suggests prospectivity of its pharmaceutical elaboration.


Subject(s)
Antibiotics, Antitubercular , Nanoparticles/chemistry , Oleic Acid , Phospholipids , Rifampin , Animals , Antibiotics, Antitubercular/chemistry , Antibiotics, Antitubercular/pharmacokinetics , Antibiotics, Antitubercular/pharmacology , Drug Delivery Systems , Male , Nanoparticles/ultrastructure , Oleic Acid/chemistry , Oleic Acid/pharmacokinetics , Oleic Acid/pharmacology , Particle Size , Phospholipids/chemistry , Phospholipids/pharmacokinetics , Phospholipids/pharmacology , Rats , Rats, Wistar , Rifampin/chemistry , Rifampin/pharmacokinetics , Rifampin/pharmacology
2.
Biull Eksp Biol Med ; 113(1): 55-8, 1992 Jan.
Article in Russian | MEDLINE | ID: mdl-1391866

ABSTRACT

The effects of polyene phosphatidylcholine (PPC) treatment at oral and intravenous administration to rats and rabbits in hypercholesterolemic diet were studied. No aorta damage was observed in either of rat groups. But fatty liver appeared, and it was the greatest in rats, who received cholesterol and PPC. The result may be attributed to adaptive protection of peripheral tissues due to high experiment duration (18 months) in the state of active reverse cholesterol transport (RChT). No antiatherogenic effect was noted in rabbits at PPC administration (170 mg/kg), while its intravenous injection (50 mg/kg) resulted in marked reduction of plasma cholesterol level, elevation of HDL cholesterol and decrease of the extent of aorta damage. The conclusion is drawn on the ppc high antiatherogenic effect predominantly at intravenous administration, and on advisability of its use in cases of RChT deficiencies, as its activator.


Subject(s)
Phosphatidylcholines/administration & dosage , Administration, Oral , Animals , Arteriosclerosis/blood , Arteriosclerosis/drug therapy , Arteriosclerosis/metabolism , Cholesterol/blood , Cholesterol/metabolism , Diet, Atherogenic , Injections, Intravenous , Lipoproteins/blood , Phosphatidylcholines/pharmacology , Rabbits , Rats , Rats, Wistar , Species Specificity , Triglycerides/blood
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