Single-Dose Relative Bioavailability of a New Quetiapine Fumarate Extended-Release Formulation: A Postprandial, Randomized, Open-Label, Two-Period Crossover Study in Healthy Uruguayan Volunteers

Development and biopharmaceutical evaluation of extended release formulation of tramadol hydrochloride based on osmotic technologyExtended release formulation of tramadol hydrochloride (TRH) based on osmotic technology was developed and evaluated. Target release profile was selected and different variables were optimized to achieve it. Formulation variables such as the level of swellable polymer, plasticizer and the coat thickness of semipermeable membrane (SPM) were found to markedly affect drug release. TRH release was directly proportional to the levels of plasticizer but inversely proportional to the levels of swellable polymer and coat thickness of SPM. Drug release from developed formulations was independent of pH and agitation intensity but dependent on osmotic pressure of the release media.In vivostudy was also performed on six healthy human volunteers and various pharmacokinetic parameters (cmax,tmax,AUC0-24,MRT) and relative bioavailability were calculated. Thein vitroandin vivoresults were compared with the performance of two commercial TRH tablets. The developed formulation provided more prolonged and controlled TRH release compared to the marketed formulation.In vitro-in vivocorrelation (IVIVC) was analyzed according to the Wagner-Nelson method. The optimized formulation (batch IVB) exhibited good IVIV correlation (R= 0.9750). The manufacturing procedure was found to be reproducible and formulations were stable over 6 months of accelerated stability testing.

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Relative bioavailability of two formulations of nevirapine 200-mg tablets in healthy Chinese male volunteers: A single-dose, randomized-sequence, open-label, two-way crossover study

Clinical Therapeutics ◽

10.1016/s0149-2918(10)80028-1 ◽

2010 ◽

Vol 32 (13) ◽

pp. 2258-2264 ◽

Cited By ~ 1

Author(s):

Yubing Zhu ◽

Qian Zhang ◽

Cuixia Yu ◽

Jianjun Zou ◽

Xiaohong Yang ◽

...

Keyword(s):

Single Dose ◽

Crossover Study ◽

Relative Bioavailability ◽

Open Label ◽

Male Volunteers ◽

Healthy Chinese ◽

Chinese Male

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Development of a new single dose extended release formulation of cefpodoxime proxetil

Asian Pacific Journal of Tropical Medicine ◽

10.1016/s1995-7645(10)60048-x ◽

2010 ◽

Vol 3 (2) ◽

pp. 117-120 ◽

Cited By ~ 1

Author(s):

Deepa Karthikeyan ◽

M Karthikeyan

Keyword(s):

Single Dose ◽

Extended Release ◽

Release Formulation ◽

Cefpodoxime Proxetil ◽

Extended Release Formulation

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Single- and Multiple-Dose Pharmacokinetics of an Oral Mixed Amphetamine Salts Extended-Release Formulation in Adults

CNS Spectrums ◽

10.1017/s109285290000239x ◽

2005 ◽

Vol 10 (S20) ◽

pp. 6-15 ◽

Cited By ~ 21

Author(s):

Susan B. Clausen ◽

Stephanie C. Read ◽

Simon J. Tulloch

Keyword(s):

Multiple Dose ◽

Extended Release ◽

Research Unit ◽

Dose Proportionality ◽

Open Label ◽

Release Formulation ◽

Extended Release Formulation ◽

Clinical Research Unit ◽

Multiple Dose Pharmacokinetics ◽

Oral Doses

AbstractObjectives: Assess the bioavailability of mixed amphetamine salts extended-release (MAS XR) 30-mg capsules and the dose proportionality of pharmacokinetic measures for MAS XR 20,40, and 60 mg.Methods: Study A, an open-label single-period study, and Study B, a randomized, open-label, three threeway crossover study, were conducted in healthy adults in a clinical research unit. In Study A, 20 subjects received a single MAS XR 30-mg capsule by mouth daily for 7 days. In Study B, 12 subjects received single oral doses of MAS XR 20,40, and 60 mg separated by 7-14-day washout periods.Findings: Plasma dextroamphetamine (D-amphetamine) and levoamphetamine (L-amphetamine) concentrations were measured using a validated LC-MS/MS method. In Study A, a 3:1 ratio of D-amphetamine to L-amphetamine was observed for AUC0-∞ and Cmax. Tmax was 4.2 and 4.3 hours for D-amphetamine to Lamphetamine, respectively. In Study B, for D- and Lamphetamine, statistically significant differences were observed for AUC0-t, AVC0-∞, and Cmax between all doses; there was a linear relationship between pharmacokinetic variables and dose and Tmax was similar for each isomer (range: 4.5–5.3 hours) with all given MAS XR doses.Conclusion: The extent of exposure as assessed by mean AUC0-24 and Cmax reflected the 3:1 ratio of D-amphetamine to L-amphetamine in MAS XR 30-mg capsules. The pharmacokinetic profiles of MAS XR 20, 40, and 60 mg are dose proportional for the isomers.

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