ABSTRACT
OBJECTIVES: To compare the bioavailability of two meloxicam tablet formulations (MEL-OD, Zydus Cadila Healthcare Limited, India, as a test formulation and Mobic, Boehringer Ingelheim International GmbH, Germany, as a reference formulation) in healthy Thai male volunteers under fasting condition. MATERIALS AND METHODS: A randomized, 2-treatment, 2-period, 2-sequence, single dose, crossover with a washout period of 2 weeks, was conducted in 26 healthy Thai male volunteers. Blood samples were collected 0, 1, 2, 3, 3.5, 4, 4.5, 5, 5.5, 6, 7, 8, 10, 12, 24, 36, 48, 72 and 96 h post dose. Plasma concentrations of meloxicam were determined using a validated HPLC method. The pharmacokinetic parameters of meloxicam were determined using a non-compartmental model. RESULTS: The mean Cmax was 1,027.32 +/- 251.91 and 1,151.89 +/- 282.58 ng/ml while the mean AUC0-t was 34,024.31 +/- 11,811.68 and 35,137.66 +/- 11,970.47 ng x h/ml for the test and reference formulation, respectively. In addition, the mean AUC0-infinity for test formulation was 37,241.44 +/- 14,888.85 ng x h/ml and for the reference formulation was 39,541.04 +/- 16,624.64 ng x h/ml. The median tmax for the test and reference formulation was 4.50 (range 2.00 - 12.00) and 4.50 (range 3.00 - 10.00), respectively. The geometric means (90% confidence intervals) of the ratio for the log-transformed pharmacokinetic parameters, Cmax, AUC0-t and AUC0-inf were 0.8919 (82.58 - 96.32%), 0.9697 (89.46 - 105.10%) and 0.9525 (87.68 - 103.47%), respectively. CONCLUSIONS: It can be concluded that two meloxicam tablet formulations are bioequivalent both in term of rate and extent of absorption after single-dose administration under fasting condition.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Thiazines/pharmacokinetics , Thiazoles/pharmacokinetics , Adolescent , Adult , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Area Under Curve , Biological Availability , Chromatography, High Pressure Liquid , Cross-Over Studies , Humans , Male , Meloxicam , Tablets , Thailand , Therapeutic Equivalency , Thiazines/administration & dosage , Thiazoles/administration & dosage , Young AdultSubject(s)
Malaria/metabolism , Phagocytes/metabolism , Reactive Oxygen Species/metabolism , Animals , Brain/pathology , Brain Edema/etiology , Cerebral Hemorrhage/etiology , Cytoplasmic Granules/enzymology , Female , Hematocrit , Malaria/immunology , Malaria/pathology , Malaria, Cerebral/complications , Malaria, Cerebral/immunology , Malaria, Cerebral/metabolism , Malaria, Cerebral/pathology , Membrane Glycoproteins/deficiency , Membrane Glycoproteins/genetics , Membrane Glycoproteins/physiology , Mice , Mice, Inbred C57BL , Mice, Knockout , NADPH Oxidase 2 , NADPH Oxidases/blood , NADPH Oxidases/deficiency , NADPH Oxidases/physiology , Parasitemia/immunology , Parasitemia/metabolism , Phagocytes/enzymology , Phagocytosis , Plasmodium bergheiABSTRACT
Two isolectins (ALA-I and ALA-II), were isolated from seed extracts of Artocarpus lakoocha by anion exchange chromatography on Q-Sepharose fast flow columns at pH 8.5 and 8.0 ALA-I was unbound to the column at pH 8.5 and moved towards the cathode in non-denaturing polyacrylamide gel electrophoresis, whereas ALA-II possessed opposite properties. The two A. lakoocha agglutinins appeared to be composed of two dissimilar subunits (alpha and beta of M(r) 14,000 and 17,200) bound non-covalently. The isolectins possessed several similar properties including: blood type agglutination; pH optimum; pH and temp stability; as well as binding specificity towards asialomucins.