Articles Related to Pharmacokinetics

Justificative: This trial was conducted in order to register a new generic product of Rivaroxaban. Objective: To evaluate the bioequivalence of rivaroxaban formulations manufactured by Eurofarma Laboratórios S/A and the reference drug, Xarelto (Bayer) under fasting and fed conditions. Methods: Three randomized, open label, balanced, 2 treatments, 4 periods, 2 sequences, single dose, full replicate, crossover studies in 48 healthy adult human subjects under fed and fasting conditions for rivaroxaban 10 mg and 20 mg. Rivaroxaban concentrations in plasma were determined using a validated HPLC-MS/MS method.

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This study was conducted to compare the bioavailability of two tablet formulations containing 200 mg Lacosamide (one Lacosamide 200 mg film-coated tablet marketed in Italy as Ollat®, one Vimpat® coated tablet). 20 healthy subjects were enrolled in a single-center, randomized, single-dose, laboratory-blinded, 2-period, 2-sequence, crossover study, with a minimum washout period of 7 days. All the 20 subjects completed the study. Plasma samples were collected up to 72.0 hours post-dosing. Lacosamide levels were determined using a validated high-performance liquid chromatography with tandem mass spectrometry (HPLC/MS/MS) method

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Purpose: The present bioequivalence study aimed at demonstrating the bioequivalence of a recently developed novel riluzole orodispersible film vs. a reference tablet. Methods: Healthy male and female volunteers received single oral doses of 50 mg of riluzole, as test and reference formulation, under fasting conditions, in each of 4 subsequent periods separated by wash-out intervals of at least 7 days, according to a 2-treatment, 4-period, replicate randomised cross-over design. Findings: Riluzole plasma concentrations were almost superimposable. Riluzole attained a similar peak concentration (315.62±124.95 ng/mL with the film and 278.81±123.32 ng/mL with the tablet) at a median tmax of 0.75 h after both treatments. Then, riluzole plasma concentrations showed a superimposable decline from the peak up to 36 h post-dose, with mean half-lives of 10.22±1.66 and 10.22±1.48 h with the film and the tablet. Mean AUC0-t was 1263.40±571.58 h*ng/mL with the film and 1135.98±514.98 h*ng/mL with the tablet. The 90% confidence intervals of Cmax, AUC0-t and AUC0-¥ of riluzole fell within the predefined range 80.00-125.00%. The treatments did not differ significantly either in tmax or t1/2. On average, the test orodispersible film dissolved on the tongue in a median time of about 2.5 min with a range of 0.7-5.7 min. Orodispersible film palatability was good or acceptable for most subjects.

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Donepezil is a potent, selective, noncompetitive and reversible inhibitor of acetylcholinesterase, commonly used for the treatment of Alzheimer’s disease. The form of orally disintegrating tablets (ODTs) is a good alternative dosage form for patients who have a difficulty in swallowing conventional tablets or capsules.

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Pantoprazole is a H+,K+-ATPase enzyme inhibitor for the treatment of acid-related gastrointestinal diseases. The Government Pharmaceutical Organization (GPO), Thailand had developed Pantoprazole GPO® (pantoprazole 40 mg delayed-release tablets) as a generic substitute for the corresponding innovator product, CONTROLOC® 40 mg.

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Fixed-dose combination tablet formulation of efavirenz/emtricitabine/tenofovir disoproxil fumarate 600/200/300 mg is an antiretroviral therapy comprising one non-nucleoside reverse-transcriptase inhibitor and two nucleoside reverse-transcriptase inhibitors to control human immunodeficiency virus infection.

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Tepilamide fumarate (PPC-06) is a new, patented prodrug of monomethyl fumarate (MMF), belonging to the fumaric acid esters (FAEs) class of drugs. The efficacy and safety of a 400 mg PPC-06 dose administered twice daily, achieved thus far through concomitant intake of two tablets of 200 mg, was demonstrated previously in two Phase 2 clinical trials on patients with moderate to severe chronic plaque-type psoriasis.

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A comparative randomized, single dose, two-way crossover, open label study was carried out to assess bioequivalence and tolerability of test (ZOLAN GPO®) and reference (Zyprexa Zydis®) products of olanzapine 5 mg orally disintegrating tablets for interchange ability in the same quality and safety.

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Aim of this study was to compare the bioavailability of two tablet formulations containing Rosuvastatin: Rosuvastatin tablets 40 mg manufactured by MacLeods Pharmaceuticals Ltd. (marketed in Italy with the brand name Exorta®) and CRESTOR® 40 mg tablets marketed by Astra Zeneca.

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This study was conducted to compare the bioavailability of 1000 mg levetiracetam film-coated tablet, marketed in Italy as Italept®, with Keppra® coated tablet.

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The primary objectives of this study were to investigate the in vivo pharmacokinetics and in vitro plasma protein binding of ropivacaine at the concentration range observed after intravenous administration of different doses in anesthetized rabbits.

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Migraine is a global disorder and considerably affecting people`s quality of life. Treatments include nonsteroidal anti-inflammatory drugs-containing medicinal products among whom acetylsalicylic acid-containing Aspirin® has been proven effectively to relief migraine headache. Early treatment is recommended for patients with migraine attacks.

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Pamabrom is a common over-the-counter mild diuretic that is often used in combination with acetaminophen and other drugs for the treatment of menstrual pain. It consists of a 1:1 ratio mixture of 8-bromotheophylline and 2-amino-2-methyl-1-propanol. A bioanalytical method for pamabrom, determined as 8-bromotheophylline, was developed and validated using reverse-phase HPLC coupled with UV detection.

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The objective of the study was to compare bioavailability of 1 mg rasagiline (as tartrate) immediate release tablets and Azilect® 1 mg immediate release tablets.

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In Mexico, the immediate-release formulation of omeprazole 20 mg in combination with 1100 mg of sodium bicarbonate (oral capsules) is indicated for patients over 18 years for the treatment of gastritis, reflux, heartburn and the sensation of emptiness caused by the excessive acid production.

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