[In Vitro and in Vivo Evaluation of Total Flavones of Hippophae Rhamnoides Self-Microemulsifying Drug Delivery System].

[In vitro and in vivo evaluation of total flavones of hippophae rhamnoides self-microemulsifying drug delivery system].

Filed under: Drug and Alcohol Rehabilitation

Yao Xue Xue Bao. 2012 Aug; 47(8): 1055-62
Li GL, Fan YT, Zhang YH, Li YF, Li XR, Liu Y, Li M

The goal of the study is to evaluate the self-microemulsifying drug delivery system (SMEDDS) which enhances the oral bioavailability of the poorly water-soluble drug, total flavones of hippophae rhamnoides (TFH). It is orally administered for the protection of human cardiovascular system. Self-microemulsifying time, particle size, polydispersity index (PDI), morphological characterization, in vitro dispersity, stability, in situ intestinal absorption and relative bioavailability were investigated in detail. The TFH-SMEDDS rapidly formed fine oil-in-water microemulsions with 0.1 mol x L(-1) hydrochloride solution, with average size of which was less than 40 nm, PDI was below 0.2, and the particles of which were observed round-shaped under transmission electron microscope. Almost 90% of TFH (expressed with quercetin) was released from SMEDDS within 20 min, which was remarkably higher than that from common capsules. The stability test showed the TFH-SMEDDS maintained stable in 6 months under accelerated condition. In situ absorption study demonstrated the absorption rate constant of TFH-SMEDDS (expressed with quercetin) was significantly higher than that of TFH in ethanolic solution (P < 0.05). The absorption of TFH from SMEDDS showed a 4.18-fold increase in relative bioavailability (expressed with quercetin) compared with that of the suspension. The results suggest that SMEDDS is a promising drug delivery system to increase the oral bioavailability of TFH. HubMed – drug


[Analysis of primary metabolites of ranolazine in dog urine by LC-MS(n)].

Filed under: Drug and Alcohol Rehabilitation

Yao Xue Xue Bao. 2012 Aug; 47(8): 1031-8
Tang JY, Wang W, Li L, Zhang CG, Wang DM, Sun L

Ranolazine and metabolites in dog urine were identified by LC-MS(n). Dog urine samples were collected after ig 30 mg x kg(-1) ranolazine, then the samples were enriched and purified through solid-phase extraction cartridge. The purified samples were analyzed by LC-MS(n). The possible metabolites were discovered by comparing the full scan and SIM chromatograms of the test samples with the corresponding blanks. Seventeen phase I metabolites and fourteen phase II metabolites were identified in dog urine. Three metabolites were identified by comparing with the control article. The metabolites were formed via the following metabolic pathways: O-demethylation, O-dearylation, hydroxylation, N-dealkylation, amide hydrolysis, glucuronidation and sulfation. The LC-MS(n) method is suitable for the rapid identification of drug and its metabolites in biologic samples.
HubMed – drug


[Effects of isorhamnetin on CYP3A4 and herb-drug interaction].

Filed under: Drug and Alcohol Rehabilitation

Yao Xue Xue Bao. 2012 Aug; 47(8): 1006-10
Ding LL, Zhang JJ, Dou W

The study is to report the investigation of the effects of isorhamnetin on CYP3A4 and herb-drug interaction. A reporter gene assay is used to test pregnane X receptor transactivation action, qRT-PCR and a luminescence-based assay were applied to determine mRNA induction and enzyme activity of CYP3A4 after isorhamnetin treatment. The interaction of irinotecan and isorhamnetin was assessed by inhibition assay of cell proliferation. Isorhamnetin at 1, 10 and 25 micromol x L(-1) transactivated the CYP3A4 reporter construct and upregulated CYP3A4 mRNA as well in a dose-dependent manner. However, isorhamnetin had no effect on enzyme activity of CYP3A4 and irinotecan HepG2 cytotoxicity. In conclusion, activation of PXR by isorhamnetin played a role in the upregulation of CYP3A4 mRNA. Moreover, joint action of isorhamnetin with other drugs may not be associated with the herb-drug interaction.
HubMed – drug



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