Current Issue : January - March Volume : 2016 Issue Number : 1 Articles : 5 Articles
Solid dispersions are a useful approach to improve the dissolution rate and\nbioavailability of poorly water-soluble active pharmaceutical ingredients (APIs). The aim of\nthis study was to improve the physicochemical properties and bioavailability of a poorly\nwater-soluble aprepitant by preparation of solid dispersions. The solid dispersions were\ncharacterized by dissolution, FTIR, XRPD, DSC, SEM and pharmacokinetic studies in rats.\nThe dissolution rate of the aprepitant was significantly increased by solid dispersions, and\nXRD, DSC, and SEM analysis indicated that the aprepitant existed in an amorphous form\nwithin the solid dispersions. The result of dissolution study showed that the dissolution rate\nof SDs was nearly five-fold faster than aprepitant. FTIR spectrometry suggested the presence\nof intermolecular hydrogen bonds between the aprepitant and polymer. Pharmacokinetic\nstudies in rats indicated that the degree drug absorption was comparable with that of\nEmendÃ?®. Aprepitant exists in an amorphous state in solid dispersions and the solid\ndispersions can markedly improve the dissolution and oral bioavailability of the aprepitant.\nThe AUC0ââ?¬â??t of the SDs was 2.4-fold that of the aprepitant. In addition, the method and its\nassociated techniques are very easy to carry out....
This study measures the curcumin concentration in rat plasma by liquid chromatography and investigates the changes in the glucose\ntolerance and insulin sensitivity of streptozotocin-diabetic rats treated with curcumin-enriched yoghurt. The analytical method for\ncurcumin detection was linear from 10 to 500 ng/mL. The ...
Objectives. To characterize the pharmacokinetic profile of levodopa (L-dopa) and carbidopa after repeated doses of the effervescent\ntablet of melevodopa/carbidopa (V1512; Sirio) compared with standard-release L-dopa/carbidopa in patients with fluctuating\nParkinson�s disease. Few studies assessed the pharmacokinetics of carbidopa to date. Methods. This was a single-centre, randomized,\ndouble-blind, double-dummy, two-period crossover study. Patients received V1512 (melevodopa 100 mg/carbidopa 25 mg) or L dopa\n100mg/carbidopa 25mg, 7 doses over 24 hours (Cohort 1), 4 doses over 12 hours (Cohort 2), or 2 doses over 12 hours in\ncombination with entacapone 200 mg (Cohort 3). Pharmacokinetic parameters included area under the plasma-concentration\ntime curve (AUC), maximum plasma concentration (...
Our recent studies showed that schisantherin A (StA) is a promising candidate for PDtreatment, but the pharmacokinetic profile of\nStA is largely unknown. The effects of different formulations on the pharmacokinetics and bioavailability of StA were investigated\nby HPLC equipped with a vacuum degasser, a quaternary pump, a manual sampler, and an ultraviolet detector. The absolute\nbioavailability of StA in nanoemulsion formulation was significantly increased from 4.3% to 47.3%. To the best of our knowledge,\nthis is the first report of absolute bioavailability for StA in rats and successful increase of bioavailability of StA by nanoemulsion\nformulation. The pharmacokinetic profiles of StA could be significantly improved by a safe nanoemulsion formulation. This\nstudy provides a successful example of advanced delivery system for improving the bioavailability of potential central nervous\nsystem (CNS) drug candidate with poor solubility. This novel approach could be an effective alternative solution to overcome\nthe shortcomings of conventional poor drug delivery of CNS drugs. The results of present study not only indicate that StA has\npotential to be developed as a promising oral therapeutic agent for the management of PD but also shed light on novel way to\nimprove bioavailability of PD drugs....
The experiment studies the effect of baicalin and baicalein on mice U14 cervical cancer and its pharmacokinetics in mice. By using\ndifferent mouse models of cancer treatment program administered and uptake kinetics experiments, tissue distribution experiment,\nexcretion, and metabolism in experimental experiments,we found that baicalin and baicalein can improve immunity and the ability\nof antioxidation and inhibit the growth of tumor.The absorption of intestinal drug takes place in intestinal tract. Tissue distribution\nwas ideal. Because of the ideal drug distribution, the liver and kidney were protected. Drug was mainly excreted through the feces\nand bile excretion....
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