生物分析与生物医学杂志

Direct factor X_a inhibitors are being used clinically. Clinical trials have shown promise for these compounds as substitutes for the currently administered vitamin K antagonists or low molecular weight heparin. Those trials demonstrated efficacy and safety against warfarin for stroke prevention in atrial fibrillation and against lowmolecular- weight heparin for treatment and secondary prevention of venous thromboembolism or for initial treatment and prevention of venous thromboembolism in patients undergoing hip or knee replacement. Advantages of orally administered direct X_a inhibitors lie in the fact that they have a rapid onset and offset of action which reduces need for “bridging” with a parenteral anticoagulant, that they don’t require frequent monitoring or re-dosing whilst having few strong drug interactions and no food interactions, leading to greater convenience by patients and doctors and that they have a lower risk of intra cranial bleeding in trials. Disadvantages compared to warfarin include the currently limited prospective experience, concerns regarding patient adherence without laboratory monitoring, uncertainty about dosing in some patient populations (eg, renal dysfunction, marked extremes of body weight), their contraindication in severe renal impairment, their lack of specific antidotes and assays to measure drug levels in case of severe bleeding, their potential to overuse in low risk atrial fibrillation people, their short half live affecting efficacy and their higher drug acquisition costs. Direct factor X_a inhibitors (‘xabans’) are a class of anticoagulant drugs which act directly upon Factor X in the coagulation cascade, without using antithrombin as a mediator.

The term “phyto” means plant while “some” means cell-like. Phytosome is a novel emerging technique applied to phyto-pharmaceutical which contains phytoconstituents of herbal extract surrounds and bound by lipid. Most of bioactive constituents of phyto-medicine are water soluble compounds like flavonoids. Because of water solubility and lipophilic outer layer, phytosome shows better absorption, hence produces better bioavailability than the conventional herbal extracts. Because of their improved pharmacological and pharmacokinetic properties, phytosome are used to treat acute and chronic liver diseases and therapeutically used as dietary supplements. The current review highlights key findings of recent research work conducted on phytosomes with our own viewpoints which can give the new directions and advancements to herbal dosage forms and the technical aspects of phyto-phospholipid formulations to face the future challenges.

Research suggests that ~60% of patients prescribed cardiovascular drugs do not take their medication correctly. The analysis of dried blood samples (DBS) by liquid chromatography-high resolution mass spectrometry (LC-HRMS) for assessing medication adherence to candidate therapeutic drugs used in cardiovascular therapy was investigated. Specificity using this analytical method was based on the measurement at the accurate mass to charge ratio of the target analyte. To evaluate the method 8mm discs were punched from each DBS and extracted followed by subjecting to LC-HRMS analysis. Trials on 6 commonly UK used cardiovascular drugs are reported demonstrating the ability of the system to detect the target analytes during the 24 hour repeat prescription cycle. Samples from volunteers with confirmed adherence were used to validate the response from the system as were samples from volunteers receiving no medication. No false positives were observed and adherence assessment for bisoprolol, ramipril, amlodipine, valsartan, doxasozin and simvastatin was demonstrated using the LC-HRMS method. Furthermore examples of incorrect adherence were identified.

Forty Guinea pigs (1-2 month old) were divided into 4 equal groups to study the efficacy of treatment of facioliasis with triclabendazole (TCBZ) and mirazid. Group (Gp.1) was the control, GPs (2-4) were orally inoculated with 20 Fasciola gigantic metacercariae (FGM) for each as a single dose by using stomach tube. Gps (3 and 4) were treated orally, with TCBZ, as a single dose (36 mg/Kg Bw) and mirazid 200 mg/Kg Bw for six successive days respectively. The drugs were administered in the 8th week post-infection to evaluate their efficacy against adult stages of Fasciola gigantica. Blood samples were collected at the end of the 1st and 2nd week post treatment for hematological and serum biochemical examination. TCBZ treated groups (GP 3) showed macrocytic hypochromic anemia, which disappeared at the end of the 2nd week post treatment. Heterophilia, esinophilia and lymphopenia were encountered in non treated group (GP 2) and mirazid treated group (GP 4). The liver transaminase (ALT, AST), gamma glytamyl transferase (GGT) and alkaline phosphatase (ALP) as well as total bilirubin, urea and creatinine, were elevated while serum albumin was decreased in GP (2) and returned to the normal value in GP (3) and GP (4) after two weeks post-treatment. It could be concluded that; the triclabendazole is more effective than mirazid in the treatment of Fasciola gigantica infection. Further research should be done for more precise knowledge about the efficacy of mirazid as a fasciolicidal drug.