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Selected AbstractsChiral separation of cetirizine by capillary electrophoresisELECTROPHORESIS, Issue 12 2006Ann Van Eeckhaut Abstract Chiral separation of cetirizine, a second-generation H1 -antagonist, was studied by CD-mediated CE. Several parameters, including pH, CD type, buffer concentration, type of co-ion, applied voltage and temperature, were investigated. The best conditions for chiral separation were obtained using a 75,mM triethanolamine-phosphate buffer (pH,2.5) containing 0.4,mg/mL heptakis(2,3-diacetyl-6-sulfato)-,-CD and 10%,ACN. Online UV detection was performed at 214,nm, a voltage of 20,kV was applied and the capillary was temperature controlled at 25°C by liquid cooling. Hydrodynamic injection was performed for 1,s. The method was validated for the quantification of levocetirizine in tablets and for enantiomeric purity testing of the drug substance. Selectivity, linearity, LOD and LOQ, precision and accuracy were evaluated for both methods. The amount of levocetirizine dihydrochloride in the commercially available tablets was quantified and was found to be within the specification limits of the claimed amount (5,mg). The amount of distomer in levocetirizine drug substance was found to be 0.87 ± 0.09%,w/w, which is in agreement with the certificate of analysis supplied by the company. [source] Is there variability in drug release and physical characteristics of amiodarone chloride from different commercially available tablets?INTERNATIONAL JOURNAL OF PHARMACY PRACTICE, Issue 4 2010Possible therapeutic implications Abstract Objectives, Amiodarone is a low-solubility, high-permeability drug with a narrow therapeutic index and reported bioavailability problems associated with switching formulations. The aim of this study was to identify whether there is variability in drug release and physical characteristics of different commercially available amiodarone hydrochloride formulations in Australia. Methods, Four available formulations (innovator Cordarone (COR) and generic products G1, G2 and G3) were tested for drug dissolution, content uniformity, hardness, weight variation, friability and disintegration in accordance with the US Pharmacopeia specifications. Key findings, The tested formulations exhibited variable dissolution behaviours: G1 and G3 exhibited the fastest dissolution, G2 dissolution was the slowest and Cordarone showed a medium dissolution. After 3 months' exposure to high temperature (40 ± 2°C) and relative humidity (75 ± 5%), the products exhibited a higher degree of disparity, with drug-release profiles of the generics being markedly different from that of Cordarone. This suggests possible implications on bioequivalence for patients who live in warm/tropical regional areas. Most products met the US Pharmacopeia specifications for drug-content uniformity and other test physical characteristics. Conclusions, The results suggested that variability in drug release profiles in vitro of amiodarone formulations might be a potential indicator of compromised bioavailability, causing possible interference with the therapeutic response of the drug. [source] Plasma pharmacokinetics of warfarin enantiomers in catsJOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 6 2000S.A. SMITH The purpose of this study was to determine the dispositions of S-warfarin and R-warfarin in normal cats following intravenous and oral administrations of racemic warfarin. Citrated blood samples were collected from 10 cats prior to and at times 5, 15, and 30 min, 1, 2, 3, 4, 5, 6, 12, 24, 36, 48, 72, 96, and 120 h following a single intravenous bolus of 0.5 mg/kg of racemic warfarin. After a 21-day washout period, samples were then similarly collected in three groups of four cats for 120 h following oral administration of 0.1, 0.25, and 0.5 mg/kg racemic warfarin. S-warfarin and R-warfarin were detected using a high-performance liquid chromatography assay validated for cat plasma. Drug concentration,time curves were subjected to non-compartmental analysis. Median pharmacokinetic parameters associated with the intravenous administration of 0.5 mg/kg racemic warfarin were as follows: t1/2 (S:28.2, R:18.3 h), area under the plasma concentration,time curve (AUC; S:33.0, R:24.6 h*,g/mL), area under the moment curve (AUMC; S:1889, R:527.8 h*h*,g/mL), and mean residence time (MRT; S:38.7, R:20.9 h). For each parameter, S-warfarin was significantly different from R-warfarin (P<0.05). Warfarin was absorbed rapidly after oral administration, and the dosage did not affect the time to maximum concentration (S:0.87, R:0.75 h). Oral dosage significantly influenced maximum plasma concentration (ng/mL, S:1267, R:1355 at 0.5 mg/kg; S:614.9, R:679.4 at 0.25 mg/kg; S:250.5, R:367.6 at 0.1 mg/kg), AUC (h*,g/mL, S:45.12, R:30.91 at 0.5 mg/kg; S:22.98:, R:18.99 at 0.25 mg/kg; S:3.922, R:3.570 at 0.1 mg/kg) and AUMC (h*h*,g/mL, S:2135, R:1062 at 0.5 mg/kg; S:943.1, R:599.9 at 0.25 mg/kg; S:132.2, R:59.03 at 0.1 mg/kg), but not t1/2 (S:23.5, R:11.6 h) nor MRT (S:26.3, R:13.5 h). Both warfarin enantiomers were highly (>96.5%) protein-bound. Quantitation of the warfarin content in commercially available tablets indicated an unequal distribution of the drug throughout the tablet. [source] Superior palatability of crushed lercanidipine compared with amlodipine among childrenBRITISH JOURNAL OF CLINICAL PHARMACOLOGY, Issue 2 2010Gregorio Milani WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT , Among children, medication palatability is crucial for adherence to therapeutic regimen. , Since there is a lack of appropriate formulations for children prescribed drugs originally designed for adults, parents crush available tablets and administer the medication mixed with solid food or a palatable drink. , Crushed amlodipine, a very popular calcium channel blocker, is bitter and unpalatable. WHAT THIS STUDY ADDS , From the perspective of the child with arterial hypertension, the taste of pulverized lercanidipine is superior to that of pulverized amlodipine. AIMS To compare the taste of equivalent doses of pulverized amlodipine and lercanidipine, two calcium channel blockers, among children with kidney disease. METHODS Each child received a test dose of 1 mg of amlodipine besylate and 2 mg of lercanidipine in a single-blinded fashion. Children indicated their preference by pointing to the appropriate face on a visual analogue scale (VAS) that depicts five degrees of pleasure. RESULTS The VAS palatability score assigned to lercanidipine was higher than that assigned to amlodipine both in nine children 4,7 years of age (P < 0.005) and in 10 children 8,11 years of age (P < 0.005). The preference for lercanidipine was statistically significant in both girls (P < 0.02) and boys (P < 0.001) and in both children initially presented amlodipine (P < 0.005) and children initially presented lercanidipine (P < 0.005). CONCLUSIONS There is a lack of appropriate formulations for children prescribed drugs originally designed for adults, such as calcium channel blockers. Parents therefore crush available tablets and administer the medication mixed with solid food or a palatable drink. From the perspective of the child, the taste of pulverized lercanidipine is superior to that of pulverized amlodipine. [source] | ||||||||||