ABSTRACT
Gliclazide is practically insoluble in water and its GI absorption is limited by its dissolution rate. Our previously published works indicated that preparing gliclazide-crosspovidone solid dispersion in the drug/ carrier ratio of 1:1 using cogrinding technique is able to enhance drug dissolution rate. The coground of gliclazide-crosspovidone was administrated to the rats and the hypoglycemic effects of pure drug, a physical mixture and the coground were considered in 3 groups of rats weighing 200-250 g (n=6). The rats were made diabetic by single intravenous administration of streptozotocin (60 mg/kg). Each of the rats received a single dose of gliclazide (equivalent to 40 mg/kg) as pure drug, physical mixture and coground in an aqueous suspension. Glucose level was assessed via glucometer after collecting the blood samples from tail vein. Gliclazide concentration in plasma was assessed applying high pressure liquid chromatography. According to 1-way ANOVA, Student-Newman-Keuls test, the coground revealed enhanced hypoglycemic effects as well as higher serum gliclazide concentration relative to pure drug and its corresponding physical mixture in the all sampling times. The area under serum glucose concentration curve vs. time for the pure gliclazide, physical mixture and coground formulations were 3 090.5±79, 3 018.8±96 and 2 374.0±73 mg.h/dl, respectively. Correspondingly, their area under serum gliclazide concentration curve vs. time were 1 171.8±156.8, 1 379.5±96.2 and 4 827.7±637.5 µg.h/ml. It follows that; formulation of gliclazide-crosspovidone coground is able to improve oral absorption of the drug.
Subject(s)
Diabetes Mellitus, Experimental/drug therapy , Gliclazide/therapeutic use , Hypoglycemic Agents/therapeutic use , Animals , Blood Glucose/analysis , Diabetes Mellitus, Experimental/blood , Drug Carriers , Gliclazide/blood , Male , Rats , Solubility , StreptozocinABSTRACT
A hydrodistillation sampling method, coupled to gas chromatography-mass spectrometry, was used in monitoring the volatile organic compounds in flowers of Astragalus sahendi. Accordingly, a total of 48 compounds were recognised, which were united by their terpenoid or aliphatic skeletons and low molecular weight. Above all, the significant presence of some insect-favoured terpenoid compounds, such as farnesol, cis- and trans-geraniol, alpha-bisabolol, nerolidol isomer, alpha-terpineol, alpha-terpinolene and thymol was significant. These findings confer a better understanding of pollination processes in the giant genus Astragalus. Furthermore, the results add to an increasing quantity of data corroborating the ecologic and evolutionary correlation between the floral bioactive compounds of plant species and their special types of pollinators.