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Karhu D.,Labopharm | Groenewoud G.,PAREXEL | Potgieter M.A.,PAREXEL | Mould D.R.,Projections Research Inc.
Journal of Clinical Pharmacology | Year: 2010

An extended-release trazodone HCl formulation, Trazodone Contramid OAD (TzCOAD), was developed as scored 150-mg and 300-mg caplets for once-daily administration. Dose proportionality of intact and bisected caplets (dose range, 75-375 mg) was evaluated in a single-dose, randomized, 5-way crossover study. Plasma trazodone and m-chlorophenylpiperazine (mCPP) levels were determined using a validated liquid chromatography-tandem mass spectroscopy method. Dose proportionality was assessed based on confidence intervals for logarithmically transformed, dose-normalized maximum plasma concentration (C max), area under the plasma concentration versus time data pairs (AUC 0-t), and area under the curve from time 0 to infinity (AUC 0-∞) in relation to the acceptance range of 80% to 125% (bioequivalence approach). The power method, combined with confidence interval criteria, was also used to assess proportionality. The conclusion of dose proportionality was generally supported using the bioequivalence approach. Based on the power model, values of the slope and corresponding 90% confidence interval for trazodone C max, AUC 0-t, and AUC 0-∞ were 0.948 (0.899-0.997), 0.920 (0.875-0.964), and 0.913 (0.867-0.958), respectively. All were within the acceptance interval (0.861-1.139). Results for mCPP also fell within the acceptance interval. TzCOAD exhibits linear pharmacokinetics over doses ranging from 75 to 375 mg and maintains its controlled-release properties when the caplets are bisected along the score line. © 2010 The Author(s).


Karhu D.,Labopharm | Gossen E.R.,Labopharm | Mostert A.,PAREXEL | Cronje T.,PAREXEL | Fradette C.,Labopharm
International Journal of Clinical Pharmacology and Therapeutics | Year: 2011

Objective: To characterize the pharmacokinetics, safety, and tolerability of an extended-release formulation of trazodone hydrochloride (HCl), Trazodone Contramid® Once-a-Day (TzCOAD) developed as scored 150-mg and 300-mg caplets for once-daily administration. Methods: Relative bioavailability studies compared the pharmacokinetics of TzCOAD and trazodone immediate-release (TzIR) tablets following single- and multiple-dose administration. In addition, the effect of food on the pharmacokinetics of TzCOAD was assessed. Results: After single-dose administration of 300 mg TzCOAD, trazodone AUC and C max were approximately 20% and 60% lower, respectively, than for TzIR 100-mg tablets administered as 3 doses, 8 h apart. After multiple-dose administration of 300 mg daily for 7 days, TzCOAD given once daily and TzIR given 3 times a day were equivalent with respect to AUC, while C max was 43% lower for TzCOAD. Trazodone AUC following single-dose administration of TzCOAD was similar to AUC at steady state, suggesting that steady-state exposure can be predicted from single-dose data. When TzCOAD was taken shortly after ingestion of a high-fat meal, C max increased 86% compared with fasting conditions. However, AUC and t maxwere not affected by food. Conclusion: Administration of TzCOAD 300 mg once daily provides equivalent steady-state exposure to, with a lower C max than, TzIR 100 mg given 3 times a day. A high-fat meal results in an increase in C max, but there is no substantial effect on AUC. ©2011 Dustri-Verlag Dr. K. Feistle.


Karhu D.,Labopharm | Fradette C.,Labopharm | Potgieter M.A.,PAREXEL | Ferreira M.M.,PAREXEL | Terblanche J.,PAREXEL
Journal of Clinical Pharmacology | Year: 2010

The pharmacokinetics of a once-daily formulation of tramadol (Tramadol Contramid OAD 200-mg tablets) following single-dose and multiple-dose administration was compared with that of an immediate-release product (tramadol IR 50-mg tablets) in 2 separate studies. In both studies, AUC parameters met bioequivalence criteria, whereas Cmax of Tramadol Contramid OAD was lower than that of tramadol IR following a 200-mg daily dosage. After single-dose administration, the mean tramadol concentration at 1 hour postdose was within the range associated with analgesic efficacy (>100 ng/mL), and the mean concentration remained above this level for the remainder of the dosing interval. Steady state was attained within 48 hours following multiple-dose administration. Tramadol Contramid OAD provides a rapid rise in plasma concentrations and an equivalent daily systemic exposure as tramadol IR, with a reduction in peak plasma concentrations. © 2010 the American College of Clinical Pharmacology© 2010 the American College of Clinical Pharmacology.


Skinner-Robertson S.,University of Montréal | Skinner-Robertson S.,Labopharm | Fradette C.,Labopharm | Bouchard S.,Labopharm | And 3 more authors.
Drugs and Aging | Year: 2015

Background: Tramadol is frequently used in geriatric patients; however, pharmacokinetic (PK) publications on tramadol and O-desmethyltramadol (ODM) in elderly patients are rare. Objective: Our objective was to characterize the PK of tramadol and ODM, including absorption processes and covariates for tramadol, in elderly and young subjects after single-dose administration of 200-mg extended-release tablets. Methods: We conducted a PK study in 15 elderly (aged ≥75 years) subjects with mild renal insufficiency and 20 young (18–40 years) subjects; blood and urine samples were collected for 48 h post-dose. Non-compartmental analysis (NCA) of each tramadol and ODM enantiomer included area under the concentration–time curve (AUC), terminal elimination rate (kel), total body clearance, volume of distribution (Varea/F), and renal clearance (Clr0–48). A one-compartment population model of total tramadol concentration was parameterized with clearance (CL/F), volume of distribution (V/F), and mixed order absorption (first-order and zero-order absorption rate constants with lag times). Results: NCA demonstrated comparable maximum plasma concentration (Cmax) and AUC between age groups for tramadol enantiomers, but significant differences in Varea/F (mean 34 % higher) and kel (mean 28 % lower) in the elderly. PK of ODM were significantly different in the elderly for AUC0–inf (mean 35 % higher), Clr0–48 (mean 29 % lower), and kel (mean 33 % lower). The population analysis identified age as a covariate of V/F (young 305 L; elderly 426 L), with a 50 % longer mean elimination half-life in the elderly. No differences in absorption processes were observed. Conclusions: Tramadol exposure was similar between the age groups; exposure to ODM was higher in elderly subjects. © 2015, Springer International Publishing Switzerland.


Trademark
Paladin Labs and Labopharm | Date: 2011-10-04

Modified starch used in the manufacture of pharmaceutical products as an agent for controlled or sustained release drug delivery for oral and parenteral administration.


Trademark
Angelini Pharma Inc. and Labopharm | Date: 2011-05-10

Pharmaceutical preparations, namely, an anti-depressant.


Trademark
Angelini Pharma Inc. and Labopharm | Date: 2011-08-02

PHARMACEUTICAL PREPARATIONS, NAMELY, AN ANTIDEPRESSANT.


There is disclosed a once daily oral pharmaceutical compositon for controlled release of tramadol or a salt thereof, wherein the composition, when ingested orally, provides a clinical effect over 24 hours which is a least as good as the clinical effect over 24 hours of two doses of a twice daily oral pharmaceutical composition for controlled release of tramadol, taken 12 hours apart.


The instant invention provides a two-step polymerization process for preparing amphiphilic poly(N-vinyl-2 pyrrolidone), (PVP)-block-polyester copolymers and other diblock and triblock copolymers consisting of PVP as one block. The block copolymers of the invention can be used as vehicles for drug delivery.


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