Biopharmaceutical Aspects of the Developmentof a Phytoecdisteroids (Pe) Ointment Composition

Abstract

Abstracts. PHYTOPHARM 2012 M 78Obzory po kliniceskoj farmacologii i lekarstvennoj terapii [Reviews of clinical pharmacology and drug therapy]ТОМ 10/2012/2 leaves, to rats and understanding of the relevant mechanisms governing the intestinal absorption and presystemic elimination. To define the ginkgo compounds to be studied, literature informatics-guided chemical profiling revealed that GbE50 extract contained 72 ginkgo constituents, including terpene lactones, flavonols, flavones, an isoflavone, biflavones, flavanols, and carboxylic acids, at levels ranging from 0.01 to 55.3 mg/g. Among the ginkgo constituent groups were the terpene lactones and the flavonols that were significantly measurable in plasma after p. o. administration of GbE50 extract to rats. The intestinal absorption of terpene lactones appeared to be dictated by their intermediate membrane permeability, while the influences of MdR-1-and MRP-2-mediated intestinal efflux and the presystemic metabolism and biliary excretion might be relatively limited. because of their deglycosylation absent in the small intestine and relatively slow presystemic elimination, many intact flavonol glycosides appeared in the rat plasma albeit with a limited extent of absorption. Colonic deglycosylation of the flavonol glycosides occurred and the glucuronides of flavonol aglycones were also measured in the plasma. Although some biflavones also had relatively high abundance in GbE50 extract, these ginkgo constituents were not measured in the rat plasma because of their poor solubility and poor permeability that hindered the intestinal absorption. The levels of the remaining ginkgo constituents in GbE50 extract were too low to be measured in the rat plasma. The current study enabled us to better understand the nature of systemic exposure to ginkgo compounds after p. o. administration of GbE50 extract and to more precisely implement multicomponent Pk study of the extract. РЕ are analogues of insect steroid hormones occurring in plants. The establishment of reparative activity of PE (1) makes it relevant to develop compositions on their base. РЕ molecules have six or more hydroxyl groups and hydrophobic core and therefore the influence of the ointment composition nature on the bioavailability of PE was trialed. in these investigations preparation Serpisten (mixture of 20-hydroxyecdisone and 25S-inocosterone obtained from the plant Serratula coronata l.) has been used. for this purpose three types of compositions have been prepared at a concentration of Serpisten 0.02 % (w/w): hydrophobic (lanolin and vaseline -C1), hydrophilic (3 % sodium carboxymethyl cellulose gel -C2), emulsive (aerosil, vaseline oil, water purified, monoglyceride purified -C3). biopharmaceutical evaluation of prepared formulations has been performed using drug releasing from the compositions by dialysis through a membrane with subsequent determination of the release profile in the UV region at λ = 240nm. The concentration of PE was determined at 30, 60 and 120 minutes of dialysis. The test revealed that...